Payload ID	PAY0NLPCS
Name	MMAE
Target	Microtubule (MT)					Target Info
Structure
				2D MOL

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Objective Response Rate (ORR)	34.70%
Patients Enrolled	Advanced/metastatic HER2-low expressing breast cancer that failed standard therapies.
Administration Dosage	MRG002 was administered intravenously once every 3 weeks at the dose of 2.60 mg/kg, until disease progression or unacceptable toxicity which ever occurred first.
Related Clinical Trial
NCT Number	NCT04742153	Phase Status	Phase 2
Clinical Description	A multicenter, non-randomized, open-label phase 2 clinical study to evaluate the efficacy and safety of MRG002 in the treatment of patients with HER2-low locally advanced or metastatic breast cancer (BC).
Experiment 2 Reporting the Activity Date of This ADC					[2]
Efficacy Data	Objective Response Rate (ORR)	65%
Patients Enrolled	Histologically HER2-positive (IHC 2+ or 3+) UC pts confirmed by a central-laboratory, ECOG PS 0-1, prior received 1 standard treatment.
Administration Dosage	Receive MRG002 at a dose of 2.60 mg/kg or 2.20 mg/kg administered by intravenous infusion every 3 weeks.
Related Clinical Trial
NCT Number	NCT04839510	Phase Status	Phase 2
Clinical Description	An open-label, single-arm, multi-center, phase 2 clinical study of MRG002 in the treatment of patients with HER2-positive unresectable locally advanced or metastatic urothelium cancer.
Experiment 3 Reporting the Activity Date of This ADC					[3]
Related Clinical Trial
NCT Number	NCT05754853	Phase Status	Phase 3
Clinical Description	An open-label, randomized, multi-center, phase 3 clinical study of MRG002 versus investigator's choice of chemotherapy in the treatment of patients with HER2-positive unresectable locally advanced or metastatic urothelial cancer previously treated with platinum-based chemotherapy and PD-1/PD-L1 inhibitors.
Experiment 4 Reporting the Activity Date of This ADC					[4]
Related Clinical Trial
NCT Number	NCT04924699	Phase Status	Phase 2/3
Clinical Description	A study of MRG002 in the treatment of patients with HER2-positive unresectable locally advanced or metastatic breast cancer.
Experiment 5 Reporting the Activity Date of This ADC					[5]
Related Clinical Trial
NCT Number	NCT05141786	Phase Status	Phase 2
Clinical Description	An open-label, multi-center, non-randomized phase 2 clinical study to evaluate the efficacy and safety of MRG002 in patients With HER2-mutated unresectable/metastatic non-small cell lung cancer (NSCLC).
Experiment 6 Reporting the Activity Date of This ADC					[6]
Related Clinical Trial
NCT Number	NCT04837508	Phase Status	Phase 2
Clinical Description	An open-label, single-arm, multi-center, phase 2 clinical study of MRG002 in the treatment of patients with HER2-positive unresectable, locally advanced or metastatic biliary tract cancer.
Experiment 7 Reporting the Activity Date of This ADC					[7]
Related Clinical Trial
NCT Number	NCT05141747	Phase Status	Phase 2
Clinical Description	An open-label, multi-center, phase 2 clinical study to evaluate the safety, efficacy and pharmacokinetics of MRG002 in patients with HER2-positive/HER2-low locally advanced or metastatic gastric/ gastroesophageal junction cancer.
Experiment 8 Reporting the Activity Date of This ADC					[8]
Related Clinical Trial
NCT Number	NCT05263869	Phase Status	Phase 2
Clinical Description	An open-label, multi-center, single-arm phase 2 clinical study to evaluate the efficacy and safety of MRG002 in advanced HER-2 positive breast cancer patients previously treated with trastuzumab and TKIs (Magic-009).
Experiment 9 Reporting the Activity Date of This ADC					[9]
Related Clinical Trial
NCT Number	NCT04492488	Phase Status	Phase 1/2
Clinical Description	An open-label, multi-center phase 1/2 dose escalation and expansion study to assess the safety, efficacy and pharmacokinetics of MRG002 in patients with HER2-positive advanced solid tumors and locally advanced or metastatic gastric/gastroesophageal junction (GEJ) cancer.
Experiment 10 Reporting the Activity Date of This ADC					[10]
Related Clinical Trial
NCT Number	NCT05338957	Phase Status	Phase 1/2
Clinical Description	An open-label, multi-center, phase 1/2 dose escalation and expansion study to evaluate the safety, tolerability, pharmacokinetics and preliminary efficacy of MRG002 in combination with HX008 in patients with HER2-expressed advanced malignant solid tumors.
Experiment 11 Reporting the Activity Date of This ADC					[12]
Related Clinical Trial
NCT Number	NCT04941339	Phase Status	Phase 1
Clinical Description	A phase 1, open-label, multi-center, first in human, dose escalation and expansion study to assess the safety, tolerability, efficacy and pharmacokinetics of MRG002 in patients with HER2 positive advanced solid tumors.
Experiment 12 Reporting the Activity Date of This ADC					[14]
Efficacy Data	Progression Free Survival	5.5 months
Patients Enrolled	Eligible patients (18-75 years) must have HER2-positive (IHC 3+/2+) metastatic urothelial cancer with ≥1 measurable lesion (RECIST v1.1), ECOG 0-1, and adequate organ function, following ≥1 prior chemotherapy failure. Key exclusions include active infections, CNS metastasis, uncontrolled systemic/autoimmune diseases, recent immunotherapy (≤4 weeks), pregnancy, or investigator-deemed ineligibility. LVEF must be ≥50%, with prior treatment toxicities resolved to ≤Grade 1.    Click to Show/Hide
Administration Dosage	MRG002 will be administrated by an IV infusion of 2.6 mg/kg on Day 1 of every 3 weeks (21-day cycle).
Related Clinical Trial
NCT Number	NCT04839510	Phase Status	PHASE2
Clinical Description	An Open-label, Single-arm, Multi-center, Phase II Clinical Study of MRG002 in the Treatment of Patients With HER2-positive Unresectable Locally Advanced or Metastatic Urothelium Cancer
Primary Endpoint	The primary efficacy endpoint is the Objective Response Rate (ORR) assessed by Independent Review Committee (IRC) per RECIST v1.1 criteria, measuring complete and partial responses over 12 months from baseline.
Other Endpoint	Secondary endpoints include investigator-assessed ORR, Duration of Response (DoR), Time to Response (TTR), Disease Control Rate (DCR), Progression-Free Survival (PFS), and Overall Survival (OS), all evaluated over 12 months. Safety assessments involve adverse event monitoring (30 days post-treatment), pharmacokinetic concentration-time analysis, and anti-drug antibody (ADA) incidence among all treated patients.    Click to Show/Hide
Experiment 13 Reporting the Activity Date of This ADC					[15]
Efficacy Data	Objective Response Rate (ORR)	37.5 39.5 %
Patients Enrolled	Inclusion: HER2-low metastatic breast cancer (≥1 prior systemic therapy), ECOG 0-1, measurable disease (RECIST 1.1), LVEF≥50%, adequate organ function. Exclusion: Active CNS metastases, uncontrolled infections (HBV/HCV/HIV), severe cardiac/autoimmune diseases, recent thromboembolism (≤3 months), pregnancy/lactation, or prior grade≥3 hypersensitivity to trastuzumab components.    Click to Show/Hide
Administration Dosage	MRG002 will be administrated via intravenous infusion of 2.6 mg/kg once on Day 1 of every 3 weeks (21-day cycle).
Related Clinical Trial
NCT Number	NCT04742153	Phase Status	PHASE2
Clinical Description	A Multicenter, Non-randomized, Open-label Phase II Clinical Study to Evaluate the Efficacy and Safety of MRG002 in the Treatment of Patients With HER2-low Locally Advanced or Metastatic Breast Cancer (BC)
Primary Endpoint	Objective Response Rate (ORR) by Independent Review Committee (IRC) is defined as CR+PR per RECIST v1.1, assessed from baseline to 12 months. Safety data (AEs/SAEs by NCI-CTCAE v5.0), PK analysis (MRG002 concentration-time curve), and immunogenicity (anti-drug antibody incidence) are collected during treatment and follow-up.
Other Endpoint	Efficacy endpoints include ORR by investigator, PFS (baseline to progression/death), 6/12-month PFSR, TTR, DoR, DCR (CR+PR+SD), and OS (baseline to death), all evaluated per RECIST v1.1 over 12 months.
Experiment 14 Reporting the Activity Date of This ADC					[14]
Efficacy Data	Objective Response Rate (ORR)	65%
Patients Enrolled	Eligible patients (18-75 years) must have HER2-positive (IHC 3+/2+) metastatic urothelial cancer with ≥1 measurable lesion (RECIST v1.1), ECOG 0-1, and adequate organ function, following ≥1 prior chemotherapy failure. Key exclusions include active infections, CNS metastasis, uncontrolled systemic/autoimmune diseases, recent immunotherapy (≤4 weeks), pregnancy, or investigator-deemed ineligibility. LVEF must be ≥50%, with prior treatment toxicities resolved to ≤Grade 1.    Click to Show/Hide
Administration Dosage	MRG002 will be administrated by an IV infusion of 2.6 mg/kg on Day 1 of every 3 weeks (21-day cycle).
Related Clinical Trial
NCT Number	NCT04839510	Phase Status	PHASE2
Clinical Description	An Open-label, Single-arm, Multi-center, Phase II Clinical Study of MRG002 in the Treatment of Patients With HER2-positive Unresectable Locally Advanced or Metastatic Urothelium Cancer
Primary Endpoint	The primary efficacy endpoint is the Objective Response Rate (ORR) assessed by Independent Review Committee (IRC) per RECIST v1.1 criteria, measuring complete and partial responses over 12 months from baseline.
Other Endpoint	Secondary endpoints include investigator-assessed ORR, Duration of Response (DoR), Time to Response (TTR), Disease Control Rate (DCR), Progression-Free Survival (PFS), and Overall Survival (OS), all evaluated over 12 months. Safety assessments involve adverse event monitoring (30 days post-treatment), pharmacokinetic concentration-time analysis, and anti-drug antibody (ADA) incidence among all treated patients.    Click to Show/Hide
Experiment 15 Reporting the Activity Date of This ADC					[15]
Efficacy Data	Disease control rate (DCR)	62.5 76.3 %
Patients Enrolled	Inclusion: HER2-low metastatic breast cancer (≥1 prior systemic therapy), ECOG 0-1, measurable disease (RECIST 1.1), LVEF≥50%, adequate organ function. Exclusion: Active CNS metastases, uncontrolled infections (HBV/HCV/HIV), severe cardiac/autoimmune diseases, recent thromboembolism (≤3 months), pregnancy/lactation, or prior grade≥3 hypersensitivity to trastuzumab components.    Click to Show/Hide
Administration Dosage	MRG002 will be administrated via intravenous infusion of 2.6 mg/kg once on Day 1 of every 3 weeks (21-day cycle).
Related Clinical Trial
NCT Number	NCT04742153	Phase Status	PHASE2
Clinical Description	A Multicenter, Non-randomized, Open-label Phase II Clinical Study to Evaluate the Efficacy and Safety of MRG002 in the Treatment of Patients With HER2-low Locally Advanced or Metastatic Breast Cancer (BC)
Primary Endpoint	Objective Response Rate (ORR) by Independent Review Committee (IRC) is defined as CR+PR per RECIST v1.1, assessed from baseline to 12 months. Safety data (AEs/SAEs by NCI-CTCAE v5.0), PK analysis (MRG002 concentration-time curve), and immunogenicity (anti-drug antibody incidence) are collected during treatment and follow-up.
Other Endpoint	Efficacy endpoints include ORR by investigator, PFS (baseline to progression/death), 6/12-month PFSR, TTR, DoR, DCR (CR+PR+SD), and OS (baseline to death), all evaluated per RECIST v1.1 over 12 months.
Experiment 16 Reporting the Activity Date of This ADC					[14]
Efficacy Data	Disease control rate (DCR)	91%
Patients Enrolled	Eligible patients (18-75 years) must have HER2-positive (IHC 3+/2+) metastatic urothelial cancer with ≥1 measurable lesion (RECIST v1.1), ECOG 0-1, and adequate organ function, following ≥1 prior chemotherapy failure. Key exclusions include active infections, CNS metastasis, uncontrolled systemic/autoimmune diseases, recent immunotherapy (≤4 weeks), pregnancy, or investigator-deemed ineligibility. LVEF must be ≥50%, with prior treatment toxicities resolved to ≤Grade 1.    Click to Show/Hide
Administration Dosage	MRG002 will be administrated by an IV infusion of 2.6 mg/kg on Day 1 of every 3 weeks (21-day cycle).
Related Clinical Trial
NCT Number	NCT04839510	Phase Status	PHASE2
Clinical Description	An Open-label, Single-arm, Multi-center, Phase II Clinical Study of MRG002 in the Treatment of Patients With HER2-positive Unresectable Locally Advanced or Metastatic Urothelium Cancer
Primary Endpoint	The primary efficacy endpoint is the Objective Response Rate (ORR) assessed by Independent Review Committee (IRC) per RECIST v1.1 criteria, measuring complete and partial responses over 12 months from baseline.
Other Endpoint	Secondary endpoints include investigator-assessed ORR, Duration of Response (DoR), Time to Response (TTR), Disease Control Rate (DCR), Progression-Free Survival (PFS), and Overall Survival (OS), all evaluated over 12 months. Safety assessments involve adverse event monitoring (30 days post-treatment), pharmacokinetic concentration-time analysis, and anti-drug antibody (ADA) incidence among all treated patients.    Click to Show/Hide
Experiment 17 Reporting the Activity Date of This ADC					[14]
Efficacy Data	Complete response (CR)	9%
Patients Enrolled	Eligible patients (18-75 years) must have HER2-positive (IHC 3+/2+) metastatic urothelial cancer with ≥1 measurable lesion (RECIST v1.1), ECOG 0-1, and adequate organ function, following ≥1 prior chemotherapy failure. Key exclusions include active infections, CNS metastasis, uncontrolled systemic/autoimmune diseases, recent immunotherapy (≤4 weeks), pregnancy, or investigator-deemed ineligibility. LVEF must be ≥50%, with prior treatment toxicities resolved to ≤Grade 1.    Click to Show/Hide
Administration Dosage	MRG002 will be administrated by an IV infusion of 2.6 mg/kg on Day 1 of every 3 weeks (21-day cycle).
Related Clinical Trial
NCT Number	NCT04839510	Phase Status	PHASE2
Clinical Description	An Open-label, Single-arm, Multi-center, Phase II Clinical Study of MRG002 in the Treatment of Patients With HER2-positive Unresectable Locally Advanced or Metastatic Urothelium Cancer
Primary Endpoint	The primary efficacy endpoint is the Objective Response Rate (ORR) assessed by Independent Review Committee (IRC) per RECIST v1.1 criteria, measuring complete and partial responses over 12 months from baseline.
Other Endpoint	Secondary endpoints include investigator-assessed ORR, Duration of Response (DoR), Time to Response (TTR), Disease Control Rate (DCR), Progression-Free Survival (PFS), and Overall Survival (OS), all evaluated over 12 months. Safety assessments involve adverse event monitoring (30 days post-treatment), pharmacokinetic concentration-time analysis, and anti-drug antibody (ADA) incidence among all treated patients.    Click to Show/Hide
Experiment 18 Reporting the Activity Date of This ADC					[16]
Patients Enrolled	Inclusion: HER2-positive breast cancer (unresectable/metastatic), prior anti-HER2 therapy failure (Phase II: trastuzumab/TKI/ADC-resistant; Phase III: 1-2 prior lines excluding ADCs), measurable disease (RECIST 1.1), ECOG 0-1, adequate organ function. Exclusion: Active CNS metastases, uncontrolled infections (HBV/HCV/HIV), severe cardiac/pulmonary diseases, prior hypersensitivity to trastuzumab components, recent major surgery/radiotherapy (<4 weeks), Child-Pugh B/C cirrhosis, or >Grade 1 neuropathy. Contraception required for reproductive-age participants.    Click to Show/Hide
Administration Dosage	MRG002 will be administrated via intravenous infusion of 2.6 mg/kg once on Day 1 of every 3 weeks (21-day cycle).
Related Clinical Trial
NCT Number	NCT04924699	Phase Status	PHASE2|||PHASE3
Clinical Description	A Study of MRG002 in the Treatment of Patients With HER2-positive Unresectable Locally Advanced or Metastatic Breast Cancer
Primary Endpoint	Progression-Free Survival (PFS) as assessed by Independent Review Committee (IRC) is the primary efficacy endpoint, defined as time from treatment initiation to disease progression or death (per RECIST v1.1) over 36 months. Secondary objectives include pharmacokinetic analysis (drug concentration-time curve) and immunogenicity assessment (anti-drug antibody incidence).    Click to Show/Hide
Other Endpoint	Key secondary endpoints include Objective Response Rate (ORR=CR+PR), Duration of Response (DoR), Disease Control Rate (DCR=CR+PR+SD) per RECIST v1.1, investigator-assessed PFS, Overall Survival (OS), and safety monitoring (AEs tracked until 30 days post-treatment). All efficacy measures are evaluated over a 36-month period.
Experiment 19 Reporting the Activity Date of This ADC					[17]
Patients Enrolled	Inclusion criteria: HER2-positive breast cancer patients (18-75 years) with liver metastasis (confirmed by central lab), measurable lesions (RECIST v1.1), ECOG 0-1, life expectancy ≥12 weeks, and adequate organ function. Exclusion criteria: Prior ADC treatment, CNS metastasis, severe neuropathy (≥Grade 2), uncontrolled infections/systemic diseases (e.g., cardiac, hepatic cirrhosis with single metastasis ≥10 cm), active autoimmune disease requiring immunosuppressants, or prior hypersensitivity to trastuzumab components. Effective contraception is mandatory for participants of childbearing potential.    Click to Show/Hide
Administration Dosage	MRG002 will be administrated via intravenous infusion of 2.6 mg/kg once on Day 1 of every 3 weeks (21-day cycle).
Related Clinical Trial
NCT Number	NCT05263869	Phase Status	PHASE2
Clinical Description	An Open-label, Multi-center, Single-arm Phase II Clinical Study to Evaluate the Efficacy and Safety of MRG002 in Advanced HER-2 Positive Breast Cancer Patients Previously Treated With Trastuzumab and TKIs (Magic-009)
Primary Endpoint	The primary endpoint is Objective Response Rate (ORR) by Independent Review Committee (IRC), defined as the proportion of patients achieving complete response (CR) or partial response (PR) per RECIST v1.1 criteria, evaluated over 12 months from baseline.
Other Endpoint	Secondary efficacy endpoints include investigator-assessed ORR, Duration of Response (DoR), Clinical Benefit Rate (CBR=CR+PR+SD≥6 months), Time to Response (TTR), Disease Control Rate (DCR=CR+PR+SD), Progression-Free Survival (PFS), and Overall Survival (OS). Safety assessments (AEs) and pharmacokinetics (drug concentration-time curve) are monitored during treatment and post-treatment follow-up, with immunogenicity analyzed via anti-drug antibody (ADA) incidence.    Click to Show/Hide
Experiment 20 Reporting the Activity Date of This ADC					[18]
Patients Enrolled	Inclusion criteria: HER2-positive (IHC 2+/3+) carcinoma of unknown primary origin (squamous/adenocarcinoma) patients (≥18 years) with ≥1 prior systemic therapy line, measurable disease (RECIST 1.1), ECOG 0-1, LVEF≥50%, and adequate organ function. Exclusion criteria: Active/uncontrolled metastases (CNS/third-space effusions), severe cardiac/infectious diseases (HBV/HCV/HIV), autoimmune disorders requiring immunosuppressants, allergy to MRG002 components, pregnancy/lactation, or other investigator-assessed ineligibility. Contraception is mandatory during and 6 months post-treatment.    Click to Show/Hide
Administration Dosage	Pucotenlimab 200mg iv d1, Q3W MRG002 2.2mg/kg d1, Q3W
Related Clinical Trial
NCT Number	NCT06869174	Phase Status	PHASE2
Clinical Description	A Phase II Clinical Trial to Evaluate the Efficacy and Safety of Pucotenlimab in Combination with MRG002 in Treating HER2-positive Cancer of Unknown Primary
Primary Endpoint	The primary endpoint is overall response rate (ORR), defined as the percentage of participants achieving complete response (CR) or partial response (PR) per RECIST 1.1 criteria, as assessed by investigators, with evaluation spanning from enrollment until first documented response (up to 12 months).
Experiment 21 Reporting the Activity Date of This ADC					[19]
Patients Enrolled	Inclusion criteria: HER2-positive (IHC 3+ or 2+) biliary tract cancer patients (18-75 years) with unresectable/metastatic disease, ≥1 prior therapy failure, measurable lesions (RECIST v1.1), ECOG 0-1, LVEF≥50%, and adequate organ function. Exclusion criteria: Severe allergies to MRG002 components, active infections (HBV/HCV/HIV), CNS metastasis, uncontrolled effusions requiring drainage, autoimmune diseases, decompensated cirrhosis, or pregnancy/lactation. Contraception is mandatory during and 6 months post-treatment.    Click to Show/Hide
Administration Dosage	MRG002 will be administrated by an IV infusion of 2.6 mg/kg on Day 1 of every 3 weeks (21-day cycle).
Related Clinical Trial
NCT Number	NCT04837508	Phase Status	PHASE2
Clinical Description	An Open-label, Single-arm, Multi-center, Phase II Clinical Study of MRG002 in the Treatment of Patients With HER2-positive Unresectable, Locally Advanced or Metastatic Biliary Tract Cancer
Primary Endpoint	The primary endpoint is objective response rate (ORR) assessed by Independent Review Committee (IRC), defined as the percentage of patients achieving complete response (CR) or partial response (PR) based on RECIST v1.1 criteria, evaluated from baseline until study completion (up to 12 months).
Other Endpoint	Secondary endpoints include investigator-assessed ORR, duration of response (DOR), time to response (TTR), disease control rate (DCR), progression-free survival (PFS), and overall survival (OS). Safety is monitored via adverse events (AEs) up to 30 days post-treatment. Pharmacokinetic (PK) parameters, including concentration-time curve, and immunogenicity (anti-drug antibody, ADA) incidence are analyzed.    Click to Show/Hide
Experiment 22 Reporting the Activity Date of This ADC					[20]
Patients Enrolled	Inclusion criteria: HER2-positive (IHC 3+ or IHC 2+/ISH+) or low HER2 (IHC 1+ or IHC 2+/ISH-) gastric/GEJ cancer patients (≥18 years) with progression after platinum/fluoropyrimidine ± anti-HER2 therapy, measurable disease (RECIST v1.1), ECOG 0-1, and adequate organ function. Exclusion criteria: Prior HER2-ADC exposure, untreated CNS metastases, severe cardiac/pulmonary disease, active infections (HBV/HCV/HIV/syphilis), recent major surgery, or uncontrolled comorbidities. Contraception is required during and 180 days post-treatment.    Click to Show/Hide
Administration Dosage	MRG002 will be administrated by an IV infusion of 2.6 mg/kg on Day 1 of every 3 weeks (21-day cycle).
Related Clinical Trial
NCT Number	NCT05141747	Phase Status	PHASE2
Clinical Description	An Open-label, Multi-center, Phase II Clinical Study to Evaluate the Safety, Efficacy and Pharmacokinetics of MRG002 in Patients With HER2-positive/HER2-low Locally Advanced or Metastatic Gastric/ Gastroesophageal Junction Cancer.
Primary Endpoint	The primary endpoints are objective response rate (ORR) per RECIST v1.1 and adverse events (AEs). ORR is defined as the percentage of patients achieving complete or partial response, evaluated over 24 months, while AEs are monitored for 45 days post-treatment.
Other Endpoint	Secondary endpoints include progression-free survival (PFS), overall survival (OS), duration of response (DOR), and disease control rate (DCR), all assessed over 24 months. Pharmacokinetic (PK) analysis tracks drug concentration over time, and immunogenicity measures anti-drug antibody (ADA) incidence up to 30 days post-treatment.
Experiment 23 Reporting the Activity Date of This ADC					[21]
Patients Enrolled	Inclusion criteria: HER2-positive metastatic/unresectable cancer patients (≥18 years) with prior standard therapy failure, measurable disease (RECIST v1.1), ECOG 0-1, adequate organ function, and available tumor tissue. Exclusion criteria: Unresolved Grade >1 toxicities from prior treatments, untreated CNS metastases, recent major surgery, severe cardiac/pulmonary conditions, active infections (HBV/HCV/HIV), uncontrolled comorbidities, or hypersensitivity to MRG002 components. Pregnancy and strong CYP3A4 inhibitor use are prohibited.    Click to Show/Hide
Administration Dosage	Phase I Dose Escalation: MRG002 will be administrated by an IV infusion of escalating doses (starting dose of 2.2 mg/kg, followed by 2.6 mg/kg) on Day 1 of every 3 weeks (21-day cycle).
Related Clinical Trial
NCT Number	NCT04492488	Phase Status	PHASE1|||PHASE2
Clinical Description	An Open-Label, Multi-center Phase I/II Dose Escalation and Expansion Study to Assess the Safety, Efficacy and Pharmacokinetics of MRG002 in Patients with HER2-Positive Advanced Solid Tumors and Locally Advanced or Metastatic Gastric/Gastroesophageal Junction (GEJ) Cancer
Primary Endpoint	The primary objectives include determining the Maximum Tolerated Dose (MTD) by assessing dose-limiting toxicities (DLT) during the first 21-day cycle and establishing the Recommended Phase II Dose (RP2D) for MRG002. Key efficacy measures include Objective Response Rate (ORR) assessed by Independent Central Review (ICR) per RECIST v1.1 over 24 months, alongside comprehensive safety evaluations of adverse events (AEs) coded via MedDRA until 45 days post-treatment.    Click to Show/Hide
Other Endpoint	Secondary efficacy endpoints (Duration of Response [DoR], Disease Control Rate [DCR], Progression-Free Survival [PFS]) will undergo sensitivity analyses based on investigator assessments. Pharmacokinetic (PK) parameters (Cmax, AUClast) for MRG002, total antibody (TAb), and Monomethyl Auristatin E (MMAE) will be derived from serial blood samples, with immunogenicity monitored via anti-drug antibody (ADA) incidence throughout the study.    Click to Show/Hide
Experiment 24 Reporting the Activity Date of This ADC					[22]
Patients Enrolled	The study excludes patients with small-cell/mixed lung cancer, uncontrolled comorbidities (hypertension, bleeding disorders), autoimmune/active infections, or live vaccinations within 30 days. Other disqualifiers include interstitial lung disease, pleural effusions requiring frequent drainage, or conditions compromising safety/study integrity per investigator judgment. Strict contraception (120 days post-treatment) and avoidance of immunotherapies/systemic steroids are mandated.    Click to Show/Hide
Administration Dosage	MRG002 will be administrated via intravenous infusion of 2.6 mg/kg once on Day 1 of every 3 weeks (21-day cycle).
Related Clinical Trial
NCT Number	NCT05141786	Phase Status	PHASE2
Clinical Description	An Open-label, Multi-center, Non-randomized Phase II Clinical Study to Evaluate the Efficacy and Safety of MRG002 in Patients With HER2-mutated Unresectable/Metastatic Non-small Cell Lung Cancer (NSCLC).
Primary Endpoint	ORR assessed by Independent Review Committee (IRC) is the primary efficacy endpoint, defined as the proportion of subjects achieving CR or PR per RECIST v1.1 over 12 months. Secondary assessments include investigator-evaluated ORR, DCR (CR+PR+SD), DOR, PFS, and OS, all measured over 12 months. Safety monitoring tracks AEs until 45 days post-treatment, while PK analysis evaluates drug concentration-time curves and immunogenicity (ADA incidence) up to 30 days post-treatment.    Click to Show/Hide
Other Endpoint	NSCLC patients with HER2 mutations (aged 18-75, life expectancy ≥3 months) who failed prior SOC therapy are eligible if they have measurable disease (RECIST v1.1), ECOG 0-1, and adequate organ function. Key exclusions: prior HER2-ADC/antibody treatment, active CNS metastases, uncontrolled infections (HBV/HCV/HIV), severe cardiac/pulmonary conditions, recent major surgery/immunotherapy, or concurrent strong CYP3A4 modifiers. Pregnancy and inadequate contraception are prohibited.    Click to Show/Hide
Experiment 25 Reporting the Activity Date of This ADC					[23]
Patients Enrolled	Eligibility requires HER2-positive solid tumor patients (18-75 years, ECOG 0-1) with progressed/refractory disease, ≥1 measurable lesion (RECIST 1.1), and adequate organ function. Exclusions: recent antitumor therapy (≤3 weeks), uncontrolled comorbidities (cardiac/pulmonary/GI), active infections (HBV/HCV/HIV), major surgery (≤4 months), or corticosteroid use (≤4 weeks). Pregnancy, inadequate contraception, or investigator-deemed ineligibility also preclude participation.    Click to Show/Hide
Administration Dosage	All patients in Phase Ia (dose escalation) and Phase Ib (dose expansion) will be administrated MRG002 on Day 1 of every 3 weeks (21-day cycle).
Related Clinical Trial
NCT Number	NCT04941339	Phase Status	PHASE1
Clinical Description	A Phase I, Open-label, Multi-center, First in Human, Dose Escalation and Expansion Study to Assess the Safety, Tolerability, Efficacy and Pharmacokinetics of MRG002 in Patients With HER2 Positive Advanced Solid Tumors
Primary Endpoint	The study aims to determine the Maximum Tolerated Dose (MTD) of MRG002, defined as the highest dose where ≤1/6 patients experience dose-limiting toxicities (DLT) during the first 28-day cycle. The Recommended Phase II Dose (RP2D) will be established based on comprehensive safety, efficacy, and PK assessments over 6 months. Adverse events (AEs) will be monitored from baseline through 49 days post-treatment, capturing all treatment-related reactions.    Click to Show/Hide
Other Endpoint	Key efficacy measures include Objective Response Rate (ORR) per RECIST v1.1, Duration of Response (DoR), and Progression-Free Survival (PFS), all evaluated over 6 months. Pharmacokinetic parameters (Cmax, Tmax, t1/2, AUClast) will be analyzed from baseline to 21 days post-treatment, alongside immunogenicity assessments (ADA positivity rate).
Experiment 26 Reporting the Activity Date of This ADC					[24]
Patients Enrolled	Eligible patients (18-75 years) must have HER2-positive advanced solid tumors with measurable lesions (RECIST v1.1), ECOG 0-1, and adequate organ function. Key exclusions include prior ADC/immunotherapy (≤60 days), steroid use (≤14 days), active infections, CNS metastases, significant cardiorespiratory disease, or pregnancy. Anthracycline exposure is capped at ≤450 mg/m2 doxorubicin equivalent. Investigators may exclude patients deemed unsuitable for study participation.    Click to Show/Hide
Administration Dosage	Experimental: MRG002+HX008, MRG002 will be administrated via intravenous infusion at 1.8,,2.2, or 2.6 mg/kg , (if appropriate) once on Day 1 of every 3 weeks (21-day cycle), up to 24 months.HX008 will be administrated via intravenous infusion at 3 mg/kg once on Day 1 of every 3 weeks (21-day- cycle), up to 24 months.
Related Clinical Trial
NCT Number	NCT05338957	Phase Status	PHASE1|||PHASE2
Clinical Description	An Open-label, Multi-center, Phase I/II Dose Escalation and Expansion Study to Evaluate the Safety, Tolerability, Pharmacokinetics and Preliminary Efficacy of MRG002 in Combination With HX008 in Patients With HER2-expressed Advanced Malignant Solid Tumors.
Primary Endpoint	The study will evaluate dose-limiting toxicities (DLTs) occurring within 28 days post-first dose to establish the safety profile of MRG002. Adverse events will be monitored from consent until 90 days after treatment completion, with all potential drug-related reactions recorded. The Recommended Phase II Dose (RP2D) will be determined based on 24-month safety, efficacy, and pharmacokinetic data.    Click to Show/Hide
Other Endpoint	Efficacy outcomes include Objective Response Rate (ORR), Duration of Response (DOR), Disease Control Rate (DCR), Progression-Free Survival (PFS), Time to Response (TTR), and Overall Survival (OS), all measured over 24 months. Pharmacokinetic profiling will examine concentration-time curves, while immunogenicity will assess anti-drug antibody (ADA) incidence - both monitored up to 90 days post-treatment.    Click to Show/Hide
Experiment 27 Reporting the Activity Date of This ADC					[25]
Patients Enrolled	Eligible patients (18-75 years) must have platinum/PD- (L)1-refractory, HER2-positive (IHC 3+/2+) metastatic urothelial carcinoma with measurable lesions (RECIST v1.1), ECOG 0-1, and adequate organ function. Exclusions involve prior ADC/taxane therapy (≤4 weeks), uncontrolled effusions/CNS metastasis, active infections, severe comorbidities, autoimmune diseases requiring immunosuppression, or investigator-deemed risks. Prior treatment toxicities must resolve to ≤Grade 1 (excluding alopecia/asymptomatic lab abnormalities).    Click to Show/Hide
Administration Dosage	MRG002 will be administrated by an IV infusion of 2.2 mg/kg on Day 1 of every 3 weeks (21-day cycle).
Related Clinical Trial
NCT Number	NCT05754853	Phase Status	PHASE3
Clinical Description	An Open-label, Randomized, Multi-center, Phase III Clinical Study of MRG002 Versus Investigator's Choice of Chemotherapy in the Treatment of Patients With HER2-positive Unresectable Locally Advanced or Metastatic Urothelial Cancer Previously Treated With Platinum-based Chemotherapy and PD-1/PD-L1 Inhibitors
Primary Endpoint	The primary endpoints include Overall Survival (OS) and Independent Review Committee-assessed Progression-Free Survival (PFS), both measured from randomization to death or progression over 36 months.
Other Endpoint	Secondary efficacy measures comprise ORR, DoR, DCR, CBR (responses lasting ≥6 months), and investigator-assessed PFS, along with TTR-all evaluated for 36 months. Safety assessments track AEs (30 days post-treatment), PK concentration-time curves (7 days post-discontinuation), and immunogenicity (ADA/NAb incidence and titers).

Experiment 1 Reporting the Activity Date of This ADC					[13]
Efficacy Data	Tumor Growth Inhibition value (TGI)	0%	Moderate HER2 expression (HER2++; IHC 2+)
In Vivo Model	HER2-positive gastric cancer PDX model (PDX: STO#151)
Experiment 2 Reporting the Activity Date of This ADC					[13]
Efficacy Data	Tumor Growth Inhibition value (TGI)	10%	Low HER2 expression (HER2+; IHC 1+)
In Vivo Model	HER2-positive gastric cancer PDX model (PDX: STO#395)
Experiment 3 Reporting the Activity Date of This ADC					[13]
Efficacy Data	Tumor Growth Inhibition value (TGI)	17%	High HER2 expression (HER2+++; IHC 3+)
In Vivo Model	HER2-positive breast cancer PDX model (PDX: BC#239)
Experiment 4 Reporting the Activity Date of This ADC					[13]
Efficacy Data	Tumor Growth Inhibition value (TGI)	19%	Moderate HER2 expression (HER2++; IHC 2+)
In Vivo Model	HER2-positive gastric cancer PDX model (PDX: STO#053)
Experiment 5 Reporting the Activity Date of This ADC					[13]
Efficacy Data	Tumor Growth Inhibition value (TGI)	41%	Moderate HER2 expression (HER2++; IHC 2+)
In Vivo Model	HER2-positive gastric cancer PDX model (PDX: STO#240)
Experiment 6 Reporting the Activity Date of This ADC					[13]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 55.10%	High HER2 expression (HER2+++; IHC 3+)
In Vivo Model	HER2-positive breast cancer PDX model (PDX: BC#046)
Experiment 7 Reporting the Activity Date of This ADC					[13]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 70%	Moderate HER2 expression (HER2++; IHC 2+)
In Vivo Model	HER2-positive gastric cancer PDX model (PDX: STO#179)
Experiment 8 Reporting the Activity Date of This ADC					[13]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 70.40%	High HER2 expression (HER2+++; IHC 3+)
In Vivo Model	HER2-positive gastric cancer PDX model (PDX: STO#410)
Experiment 9 Reporting the Activity Date of This ADC					[13]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 78.90%
In Vivo Model	HER2-positive gastric cancer PDX model (PDX: STO#410)
Experiment 10 Reporting the Activity Date of This ADC					[13]
Efficacy Data	Tumor Growth Inhibition value (TGI)	84%
In Vivo Model	HER2-positive gastric cancer PDX model (PDX: STO#410)
Experiment 11 Reporting the Activity Date of This ADC					[13]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 87.90%
In Vivo Model	HER2-positive breast cancer PDX model (PDX: BC#197)
Experiment 12 Reporting the Activity Date of This ADC					[13]
Efficacy Data	Tumor Growth Inhibition value (TGI)	90%
In Vivo Model	HER2-positive gastric cancer PDX model (PDX: STO#069)
Experiment 13 Reporting the Activity Date of This ADC					[13]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 94%
In Vivo Model	HER2-positive breast cancer PDX model (PDX: BC#046)
Experiment 14 Reporting the Activity Date of This ADC					[13]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 96.10%
In Vivo Model	HER2-positive gastric cancer PDX model (PDX: STO#179)
Experiment 15 Reporting the Activity Date of This ADC					[13]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100%	Low HER2 expression (HER2+; IHC 1+)
In Vivo Model	HER2-positive gastric cancer PDX model (PDX: STO#410)
Experiment 16 Reporting the Activity Date of This ADC					[13]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100%	High HER2 expression (HER2+++; IHC 3+)
In Vivo Model	HER2-positive breast cancer PDX model (PDX: BC#197)

Experiment 1 Reporting the Activity Date of This ADC					[13]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 60.70%	Moderate HER2 expression (HER2++)
In Vivo Model	HER2-positive gastric cancer NCI-N87 CDX model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[13]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 66.20%	High HER2 expression (HER2+++)
Method Description	MRG-002 induces efficient tumor cell killing in PDX models of breast cancer or gastric cancer tissues with HER2 expression,administered with vehicle,MRG002,HX008 or MRG002 + HX008 combo intravenously.
In Vivo Model	HER2-positive breast cancer BT-474 CDX model
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 3 Reporting the Activity Date of This ADC					[13]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 90%	High HER2 expression (HER2+++)
In Vivo Model	HER2-positive gastric cancer NCI-N87 CDX model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 4 Reporting the Activity Date of This ADC					[13]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 90%	High HER2 expression (HER2+++)
In Vivo Model	HER2-positive gastric cancer NCI-N87 CDX model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 5 Reporting the Activity Date of This ADC					[13]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 90%	Moderate HER2 expression (HER2++; IHC 2+)
In Vivo Model	HER2-positive breast cancer BT-474 CDX model
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 6 Reporting the Activity Date of This ADC					[13]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 90%	Moderate HER2 expression (HER2++; IHC 2+)
In Vivo Model	HER2-positive breast cancer BT-474 CDX model
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179

Experiment 1 Reporting the Activity Date of This ADC					[13]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.01 nM
Method Description	The inhibitory activity of MRG-002 against cancer cell growth was evaluated in various human cancer cell lines in vitro. The cells were treated with MRG-002 for 96±2 hrs.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[13]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.04 nM
Method Description	The inhibitory activity of MRG-002 against cancer cell growth was evaluated in various human cancer cell lines in vitro. The cells were treated with MRG-002 for 96±2 hrs.
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 3 Reporting the Activity Date of This ADC					[13]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.15 nM
Method Description	The inhibitory activity of MRG-002 against cancer cell growth was evaluated in various human cancer cell lines in vitro. The cells were treated with MRG-002 for 96±2 hrs.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 4 Reporting the Activity Date of This ADC					[13]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.4 nM
Method Description	The inhibitory activity of MRG-002 against cancer cell growth was evaluated in various human cancer cell lines in vitro. The cells were treated with MRG-002 for 96±2 hrs.
In Vitro Model	Breast adenocarcinoma	MDA-MB-453 cells		CVCL_0418

Experiment 1 Reporting the Activity Date of This ADC					[11]
Related Clinical Trial
NCT Number	NCT05156866	Phase Status	Phase 1
Clinical Description	A phase 1, first in human, dose-escalation study of TORL-2-307-ADC in participants with advanced cancer.
Experiment 2 Reporting the Activity Date of This ADC					[26]
Patients Enrolled	Eligible patients had advanced solid tumors (RECIST v1.1 measurable), ECOG 0-1, and adequate organ function. Exclusions included: unresolved toxicities (>Grade 1); recent anticancer therapy (14 days small molecule/28 days biologic); active brain metastases; uncontrolled comorbidities; cardiac disease; MDS/AML history; secondary malignancies (except curatively treated skin/DClS/low-risk prostate cancer); pregnancy/breastfeeding.    Click to Show/Hide
Related Clinical Trial
NCT Number	NCT05156866	Phase Status	PHASE1
Clinical Description	A Phase 1, First in Human, Dose-Escalation Study of TORL-2-307-ADC in Participants With Advanced Cancer
Primary Endpoint	Safety assessments included AE/SAE incidence (NCI-CTCAE v5.0 graded) over 2 years, with MTD determined as the highest dose causing <33% DLTs among 6 evaluable participants in cycle 1 (28 days). RP2D derived from MTD, safety, and PK data.
Other Endpoint	Efficacy measures (ORR/DOR/PFS/TTR) followed RECIST 1.1 over 2 years, with 1-/2-year OS rates tracked. PK profiles (Cmax/Cmin/Tmax/t1/2/AUC/Vz/CL/Rac) for TORL-2-307-ADC were analyzed at steady state (63 days) and single-dose (21 days). ADA positivity was monitored.

Experiment 1 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Two-year Progression-Free Survival (PFS)	97.30 (BV-AVD group); 92.60 (ABVD group) %
Patients Enrolled	34 patients with previously untreated classical Hodgkin lymphoma (cHL).
Administration Dosage	After 2 cycles of Brentuximab vedotin, doxorubicin, dacarbazine combination therapy.
Related Clinical Trial
NCT Number	NCT02505269	Phase Status	Phase 2
Clinical Description	Brentuximab vedotin plus ad in non-bulky limited stage Hodgkin lymphoma.
Primary Endpoint	For patients with high total metabolic tumor volume, the 2-year PFS rate was 90.90% and 70.70% in the BV-AVD and ABVD arms, respectively. 82.30% in the BV-AVD arm were PET-negative compared with 75.40% in the ABVD arm.
Experiment 2 Reporting the Activity Date of This ADC					[30]
Efficacy Data	Objective Response Rate (ORR)	59%
Patients Enrolled	Eastern Cooperative Oncology Group performance status 2 with previously untreated CD30-positive PTCL (CD30 detected in 10% of neoplastic cells by local review.
Administration Dosage	Patients were treated with six or eight 21-day cycles of either brentuximab vedotin, cyclophosphamide, doxorubicin, prednisone (A+CHP) or cyclophosphamide, doxorubicin, vincristine, prednisone (CHOP).
Related Clinical Trial
NCT Number	NCT01777152	Phase Status	Phase 3
Clinical Description	A randomized, double-blind, placebo-controlled, phase 3 study of brentuximab vedotin and CHP (A+CHP) versus CHOP in the frontline treatment of patients with CD30-positive mature T-cell lymphomas.
Primary Endpoint	The median PFS = 62.30 months (95% CI: 42.00 months to not evaluable) for A+CHP. The median PFS = 23.80 months (95% CI: 13.60-60.80 months) for CHOP.
Other Endpoint	5-year overall survival (OS) rates = 70.10% (95% CI: 63.30% to 75.90%) with A+CHP VS 61.00% (95% CI: 54.00% to 67.30%) with CHOP (hazard ratio = 0.72; 95% CI: 0.53-0.99), The PFS HR = 0.55 (95% CI: 0.39-0.79; P = 0.0009) in the subset of patients with sALCL, and the estimated 5-year PFS = 60.60% (95% CI: 49.50% to 69.90%) for A+CHP,the estimated 5-year PFS= 48.40% (95% CI: 39.60% to 56.70%) for CHOP The ORR with first subsequent therapy on the A+CHP arm = 42.00% (27.00% CR) VS The ORR with first subsequent therapy = 42.00% (19.00% CR) in the CHOP armCR=72.57% (82/113) in the A+CHP arm were in CR at EOT, and = 30.49% (25/82) underwent consolidative SCT.    Click to Show/Hide
Experiment 3 Reporting the Activity Date of This ADC					[31]
Efficacy Data	Objective Response Rate (ORR)	60%	Positive CD30 expression (CD30+++/++)
Patients Enrolled	Relapsed or progressive Hodgkin lymphoma (HL).
Administration Dosage	1.8 mg/kg IV once every 3 weeks for up to 16 cycles.
Related Clinical Trial
NCT Number	NCT01100502	Phase Status	Phase 3
Clinical Description	A phase 3 study of brentuximab vedotin (SGN-35) in patients at high risk of residual Hodgkin lymphoma following stem cell transplant (the AETHERA trial).
Primary Endpoint	Objective response rate=60.00% (including 4 complete responses, 2 partial responses, 1 stable disease, 1 progressive disease, and 2 unknown).
Other Endpoint	5-year PFS=59.00% (95% CI 51.00-66.00).
Experiment 4 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Objective Response Rate (ORR)	60.13%
Patients Enrolled	Elapsed or refractory classical Hodgkin lymphoma with measurable disease and an Eastern Cooperative Oncology Group performance status of 0 or 1 who were ineligible for or had relapsed after autologous haematopoietic stem-cell transplantation (HSCT).
Administration Dosage	1.80 mg/kg intravenously every 3 weeks.
Related Clinical Trial
NCT Number	NCT02684292	Phase Status	Phase 3
Clinical Description	A phase 3, randomized, open-label, clinical trial to compare pembrolizumab with brentuximab vedotin in subjects with relapsed or refractory classical hodgkin lymphoma.
Primary Endpoint	Median progression-free survival = 13.20 months (95% CI 10.90-19.40) for pembrolizumab vs median progression-free survival = 8.30 months (5.70-8.80) for brentuximab vedotin (hazard ratio 0.65 [95% CI 0.48-0.88].; p=0.0027).
Other Endpoint	Objective responses (by investigator review) were recorded in 103 (68.21% [95% CI 60.1-75.5]) of 151 patients in the pembrolizumab group (40 [26.48%] complete responses and 63 [41.72%] partial responses), and in 92 (60.13% [51.9-67.9]) of 153 patients in the brentuximab vedotin group (36 [23.53%] complete responses and 56 [36.60%] partial responses).    Click to Show/Hide
Experiment 5 Reporting the Activity Date of This ADC					[34]
Efficacy Data	Objective Response Rate (ORR)	0%	Positive CD30 expression (CD30+++/++)
Patients Enrolled	Histologically confirmed diagnoses of advSM (ASM, SM-AHN, or MCL).
Administration Dosage	1.8 mg/kg IV every 3 weeks up to 8 cycles.
Related Clinical Trial
NCT Number	NCT01807598	Phase Status	Phase 2
Clinical Description	Brentuximab vedotin in treating patients with advanced systemic mastocytosis or mast cell leukemia.
Primary Endpoint	Objective response rate=0.00%.
Other Endpoint	Median progression-free survival=210 days (95% CI 77-343 days).
Experiment 6 Reporting the Activity Date of This ADC					[35]
Efficacy Data	Objective Response Rate (ORR)	8%	Positive CD30 expression (CD30+++/++)
Patients Enrolled	CD30-expressing nonlymphomatous cancer, not have been treated with chemotherapy, radiotherapy, biologics.
Administration Dosage	1.8 or 2.4 mg/kg BV once every three weeks.
Related Clinical Trial
NCT Number	NCT01461538	Phase Status	Phase 2
Clinical Description	Brentuximab vedotin in patients with CD30-positive nonlymphomatous malignancies.
Primary Endpoint	Objective response rate= 8.00% (95% CI 1.10, 28.00).
Other Endpoint	Median progression-free survival=2.10 months (95% CI 1.20- 2.80).
Experiment 7 Reporting the Activity Date of This ADC					[36]
Efficacy Data	Objective Response Rate (ORR)	13.33%	Negative Lewis Y expression (Lewis Y-); Positive CD30 expression (CD30+++/++)
Patients Enrolled	Relapsed/refractory CD30+ primary mediastinal large B-cell lymphoma (PmLBCL).
Administration Dosage	1.80 mg per kg as a single IV infusion on day 1 of each 21-day cycle.
Related Clinical Trial
NCT Number	NCT02423291	Phase Status	Phase 2
Clinical Description	A phase 2 study of SGN-35 (Brentuximab Vedotin) of patients with relapsed or refractory primary mediastinal large B-cell lymphoma (PmLBCL).
Primary Endpoint	The ORR was 13.33% (2/15): 2 patients PR, 1 patient SD, and the remaining 12 patients PD.
Experiment 8 Reporting the Activity Date of This ADC					[38]
Efficacy Data	Objective Response Rate (ORR)	36.40%	Negative Lewis Y expression (Lewis Y-); Positive CD30 expression (CD30+++/++)
Patients Enrolled	Any subtype of histologically confirmed high-CD30expressing non Hodgkin lymphoma (NHL), except anaplastic large-cell lymphoma (ALCL). High CD30 expression was defined as membranous CD30 expression in 30% of tumor cells detectable by visual assessment of routine immunohistochemistry staining using the anti-CD30 antibody on biopsy at the time of diagnosis or relapse. (2) A bidimensionally measurable lesion 1.5 cm in the greatest transverse diameter. (3) Age 20-75 years and an Eastern Cooperative Oncology Group performance status of 2. (4) Adequate bone marrow and organ function. (5) No history of another active cancer within the previous 5 years except basal cell carcinoma. Note that patients who had relapsed after autologous stem cell transplantation (SCT) were considered eligible. Exclusion criteria were: undergoing allogeneic SCT; active infection, human immunodeficiency virus infection, or hepatitis B or C; and lymphomatous involvement of the central nervous system. The 30% cutoff was established by consensus during an investigation initiation meeting of the pathologists from each of the study sites after they reviewed various cutoff values for positive and strong positive of CD30 expression across various subtypes of NHL.    Click to Show/Hide
Administration Dosage	Intravenously at 1.80 mg/kg every 3 weeks and the primary endpoint was > 40% disease control rate.
Related Clinical Trial
NCT Number	NCT02280785	Phase Status	Phase 2
Clinical Description	A phase 2 study of brentuximab vedotin for relapsed/refractory CD30-positive non-Hodgkin lymphomas other than anaplastic large cell lymphoma.
Primary Endpoint	For 1.80 mg/kg BV intravenously, the overall disease control rate was 48.48% (16/33).
Other Endpoint	For 1.80 mg/kg BV intravenously, the median PFS and OS 1.90 months and 6.10 months.
Experiment 9 Reporting the Activity Date of This ADC					[39]
Efficacy Data	Objective Response Rate (ORR)	41.18 54.00 %
Patients Enrolled	Relapsed/refractory CD30+ non-Hodgkin lymphomas; at least 1 prior systemic therapy, measurable disease, age 12 years, and Eastern Cooperative Oncology Group (ECOG) performance status of 2.
Administration Dosage	1.80 mg/kg was administered every 3 weeks until progression or unacceptable toxicity.
Related Clinical Trial
NCT Number	NCT01421667	Phase Status	Phase 2
Clinical Description	A phase 2 study of brentuximab vedotin in relapsed or refractory non-hodgkin lymphoma (NHL).
Primary Endpoint	In 34 evaluable patients, ORR was 41.18% (8 CRs, 6 PRs,and ORR was 54.00% in AITL (5 CRs, 2 PRs) with median PFS of 6.70 months thus far.
Other Endpoint	Median baseline sCD30 for patients with AITL and PTCL-NOS was 1214 ng/mL (range, 108-9473 ng/mL) and 840 ng/mL, respectively. Median duration of response for all patients was 7.60 months (range, 1.30-14.10 months), 5.50 months for AITL patients,and 7.60 months (range, 1.40-10.11 months) for PTCL-NOS patients.
Experiment 10 Reporting the Activity Date of This ADC					[41]
Efficacy Data	Objective Response Rate (ORR)	48%	Positive CD30 expression (CD30+++/++; FACS analysis = 495)
Patients Enrolled	EBV-positive and CD30- positive non-Hodgkin lymphomas with various levels of CD30 in the relapsed or refractory setting.
Administration Dosage	1.80 mg/kg brentuximab vedotin intravenously every 3 weeks for up to 16 cycles or until disease progression.
Related Clinical Trial
NCT Number	NCT02388490	Phase Status	Phase 2
Clinical Description	A phase 2 study of brentuximab vedotin in patients with relapsed or refractory EBV-and CD30-positive lymphomas.
Primary Endpoint	For 1.80 mg/kg BV intravenously, the ORR was 48.00% (90% CI: 31.00%-64.00%).
Other Endpoint	For 1.80 mg/kg BV intravenously, Median Progression-Free Survival (mPFS)= 6.20 months (95% CI: 2.90-13.60), overall survival(mOS)=15.70 months (95% CI: 6.10-not reached).
Experiment 11 Reporting the Activity Date of This ADC					[43]
Efficacy Data	Objective Response Rate (ORR)	52.94%	Positive CD30 expression (CD30+++/++; FACS analysis = 116)
Patients Enrolled	Elderly patients with relapsed/refractory Hodgkin lymphoma (R/R HL).
Administration Dosage	1.80 mg/kg administered as a single outpatient intravenous infusion on Day 1 of each 21-day treatment cycle, for a maximum of 16 cycles.
Related Clinical Trial
NCT Number	NCT02227433	Phase Status	Phase 2
Clinical Description	A phase 2 study of brentuximab vedotin (BV) in the treatment of elderly Hodgkin lymphoma (HL) patients at first relapse or with primary refractory disease.
Primary Endpoint	The efficacy of single agent BV was measured by overall objective response rate (ORR, sum of CR and partial response [PR] rates),Best response was reached at fourth cycle of BV therapy. ORR was 52.94% (9 of 17 patients) with a CR rate of 23.5% (4 of 17 patients).
Other Endpoint	Secondary endpoints were CR rate, disease free survival (DFS), 1-year PFS, 1-year OS and safety and tolerability of BV. With a median follow-up of 24.90 months, median PFS was 8.80 months and median OS was 21.70 months.
Experiment 12 Reporting the Activity Date of This ADC					[45]
Efficacy Data	Objective Response Rate (ORR)	67.86 60.00 87.50 %
Patients Enrolled	Patients who previously experienced a CR or PR with brentuximab vedotin, discontinued treatment while in remission, and subsequently experienced disease progression or relapse. Patients who received an allogeneic stem cell transplant (SCT) were eligible if they were >100 days from transplant and had no evidence of cytomegalovirus by polymerase chain reaction.    Click to Show/Hide
Administration Dosage	1.80 mg/kg intravenously approximately every 3 weeks over 30 minutes as an outpatient infusion.
Related Clinical Trial
NCT Number	NCT00947856	Phase Status	Phase 2
Clinical Description	Treatment with SGN-35 in patients with CD30-positive hematologic malignancies who have previously participated in an SGN-35 study.
Primary Endpoint	The ORR for HL and systemic ALCL retreatment patients was 67.86% (95% CI; 47.60-84.10),with a CR rate of 39.29% (95% CI; 21.50-59.40). The ORR was 60.00% (30.00% CR) for HL patients and 87.50% (62.50% CR) for systemic ALCL patients. The majority of patients (81.00%) who received brentuximab vedotin retreatment experienced reduction in measurable tumor volume.    Click to Show/Hide
Other Endpoint	The objective response rate = 60.00% (30.00% CR) in HL patients and 87.50% (62.50% CR) in systemic ALCL patients.
Experiment 13 Reporting the Activity Date of This ADC					[46]
Efficacy Data	Objective Response Rate (ORR)	71%
Patients Enrolled	Relapsed or refractory Hodgkin lymphoma (HL) after auto-stem cell transplant.
Administration Dosage	1.80 mg/kg IV once every 3 weeks over 30 minutes on an outpatient basis for up to 16 infusions.
Related Clinical Trial
NCT Number	NCT00848926	Phase Status	Phase 2
Clinical Description	A pivotal study of SGN-35 in treatment of patients with relapsed or refractory hodgkin lymphoma (HL).
Primary Endpoint	OrR = 72.00% (33.00% CR, 38.00% PR).
Other Endpoint	The estimated median DOR of PR in the 73 patients= 11.20 months (95% CI: 7.70, 18.70), The median DOR of CR in the 34 patients = not been reached (95% CI: 20.50 months, ). The estimated median OS for all patients was 40.50 months (95% CI: 28.70, ). The estimated 3-year OS for the 34 patients with a CR to brentuximab vedotin was 73.00% (95% CI: 57%, 88%). The estimated median PFS for all patients was 9.30 months (95% CI: 7.10, 12.20). Three-year PFS was estimated at 58.00% (95% CI: 41.00%, 76.00%) for the 34 CR patients.    Click to Show/Hide
Experiment 14 Reporting the Activity Date of This ADC					[47]
Efficacy Data	Objective Response Rate (ORR)	75%
Patients Enrolled	Relapsed or refractory Hodgkin lymphoma (HL) after high-dose chemotherapy and auto-stem cell transplant, histologically documented CD30-positive Hodgkin's Reed-Sternberg cells by central pathology review.
Administration Dosage	1.80 mg/kg by intravenous infusion every 3 weeks; received a maximum of 16 cycle.
Related Clinical Trial
NCT Number	NCT00848926	Phase Status	Phase 2
Clinical Description	A pivotal study of SGN-35 in treatment of patients with relapsed or refractory hodgkin lymphoma (HL).
Primary Endpoint	Tumor reductions were observed in 94% of patients. The ORR was 75.00% (95% CI, 64.90% to 82.60%); 34% of all patients achieved a CR (95% CI, 25.20% to 44.40%), and the overall disease control rate (CR + partial remission + stable disease) was 96% (95% CI, 90.30% to 98.90%). The median time to objective response was 5.70 weeks (range, 5.10 to 56 weeks),and the median time to CR was 12 weeks (range, 5.10 to 56 weeks).    Click to Show/Hide
Other Endpoint	For patients who had an objective response,the median duration of response was 6.70 months (95% CI,3.60 to 14.80 months). The median duration of response for patients who achieved a CR was 20.50 months (95% CI,10.80 months to not estimable).
Experiment 15 Reporting the Activity Date of This ADC					[48]
Efficacy Data	Objective Response Rate (ORR)	86%
Patients Enrolled	Relapsed or refractory systemic anaplastic large cell lymphoma (ALCL) after treatment failure of at least one prior therapy with curative intent, the most common being a combination of cyclophosphamide, doxorubicin, vincristine, and prednisone.
Administration Dosage	1.80 mg/kg was administered intravenously once every 3 weeks over 30 minutes on an outpatient basis for up to 16 total doses.
Related Clinical Trial
NCT Number	NCT00866047	Phase Status	Phase 2
Clinical Description	A phase 2 study of SGN-35 in treatment of patients with relapsed or refractory systemic anaplastic large cell lymphoma (ALCL).
Primary Endpoint	The ORR per independent review was 86.00% (95% CI,74.60% to 93.90%); 57% of patients achieved CR (95% CI, 43.20% to 69.80%), and 29.00% achieved partial remission. Tumor reductions were observed in 97.00% of patients.
Other Endpoint	The estimated median PFS time per independent review was 13.30 months (95% CI,6.90 months to NE); in the subset of patients who achieved a CR,the median PFS was 14.60 months. Per investigator assessment,the median PFS with brentuximab vedotin was 14.30 months (95% CI,9.10 months to NE). The median OS had not yet been reached. The estimated 12-month survival rate was 70.00%.    Click to Show/Hide
Experiment 16 Reporting the Activity Date of This ADC					[49]
Efficacy Data	Objective Response Rate (ORR)	92.31%
Patients Enrolled	Patients were aged 60 years with classical HL (ie, patients with nodular lymphocyte predominant HL [NLPHL] were excluded). Patients were treatment nave and were either ineligible for frontline conventional combination treatment of HL (eg, ABVD or bleomycin, etoposide, doxorubicin, cyclophosphamide, vincristine, procarbazine, and prednisone [BEACOPP]) in the investigators judgment or had declined the available chemotherapy options after being informed of the potential benefits and risks.    Click to Show/Hide
Administration Dosage	1.80 mg/kg of IV brentuximab vedotin every 3 weeks for up to 16 doses.
Related Clinical Trial
NCT Number	NCT01716806	Phase Status	Phase 2
Clinical Description	A phase 2 open-label study of brentuximab vedotin in front-line therapy of Hodgkin lymphoma (HL) an dCD30-expressing peripheral t-cell lymphoma (PTCL) in older patients or patients with significant comorbidities ineligible for standard chemotherapy.
Primary Endpoint	The ORR among the 26 efficacy-evaluable patients was 92.31% (n=24, 95% CI 74.90-99.10). The median duration of objective response was 9.10 months (range 2.80-20.90 months) for all responder.
Other Endpoint	The CR among the 26 efficacy-evaluable patients was 73.08% (n=19, 95% CI 52.20-88.40), The median PFS was 10.50 months (range 2.61-22.31 months) for all efficacy evaluable patients and 11.80 months (range 4.10-22.31months) for CR.
Experiment 17 Reporting the Activity Date of This ADC					[50]
Efficacy Data	Objective Response Rate (ORR)	100%	High CD30 expression (CD30+++)
Patients Enrolled	35 patients with R/R Hodgkin lymphoma (HL).
Administration Dosage	Any time before on-protocol consolidation (nivolumab + BV; BV + bendamustine).
Related Clinical Trial
NCT Number	NCT02927769	Phase Status	Phase 2
Clinical Description	Risk-based, response-adapted, phase II open-label trial of nivolumab + brentuximab vedotin (N + BV) for children, adolescents, and young adults with relapsed/refractory (R/R) CD30 + classic hodgkin lymphoma (cHL) after failure of first-line therapy, followed by brentuximab + bendamustine (BV + B) for participants with a suboptimal response (checkmate 744: checkpoint pathway and nivolumab clinical trial evaluation)    Click to Show/Hide
Experiment 18 Reporting the Activity Date of This ADC					[51]
Efficacy Data	Objective Response Rate (ORR)	100%	Positive CD30 expression (CD30 +++/++)
Patients Enrolled	Patients with previously untreated, early-stage unfavorable Hodgkin lymphoma.
Administration Dosage	Patients were randomly assigned (2:1) to four cycles of BV-AVD or standard doxorubicin, bleomycin, vincristine, and dacarbazine (ABVD), followed by 30 Gy involved node radiotherapy.
Related Clinical Trial
NCT Number	NCT02292979	Phase Status	Phase 2
Clinical Description	Brentuximab vedotin associated with chemotherapy in untreated patients with stage I/II unfavourable hodgkin lymphoma. a randomized phase ii lysa-fil-eortc intergroup study.
Primary Endpoint	CRR was 94.12% (32/34).
Other Endpoint	ORR was 100.00% (34/34).
Experiment 19 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Objective Response Rate (ORR)	100%
Patients Enrolled	Had treatment-naive classical HL (excluding nodular lymphocyte predominant HL), fluorodeoxyglucose positron emission tomography (PET)-avid disease, bidimensional measurable disease of >=1.5 cm in the greatest transverse diameter, and an ECOG performance status of <=3 and were ineligible for or declined standard frontline chemotherapies (eg, ABVD or bleomycin, etoposide, Adriamycin, cyclophosphamide, Oncovin, procarbazine, and prednisone).    Click to Show/Hide
Administration Dosage	1.80 mg/kg BV and 375 mg/m2 DTIC for up to 12 cycles, and 20 more patients received 1.80 mg/kg BV plus 90 or 70 mg/m2 bendamustine for up to 6 cycles (dose reduced due to toxicity).
Related Clinical Trial
NCT Number	NCT01716806	Phase Status	Phase 2
Clinical Description	A phase 2 open-label study of brentuximab vedotin in front-line therapy of hodgkin lymphoma (HL) an dCD30-expressing peripheral t-cell lymphoma (PTCL) in older patients or patients with significant comorbidities ineligible for standard chemotherapy.
Primary Endpoint	For efficacy-evaluable patients treated with BV plus DTIC (n = 21), the ORR was 100.00%. For efficacy-evaluable patients treated with BV plus bendamustine (n = 17), the ORR was also 100.00%.
Other Endpoint	For efficacy-evaluable patients treated with BV plus DTIC (n = 21), the CR rate was 62.00%. At the time of this analysis, the median observation time from first dose was 21.60 months (range, 14.80 to 29.00 months), and median PFS was 17.90 months (range, 4.20 to 29.00 months). For efficacy-evaluable patients treated with BV plus bendamustine (n = 17), the CR was also 88.00%. Out of 7 patients (57.00%) with B symptoms at baseline had resolution. The median observation time from first dose was 10.80 months (range, 2.90 to 18.20 months). Neither the median PFS (range, 2.90 to 18.00 months) nor the median OS (range, 2.90 to 18.20 months) was reached at the time of this analysis.    Click to Show/Hide
Experiment 20 Reporting the Activity Date of This ADC					[59]
Efficacy Data	Objective Response Rate (ORR)	60.71 78.38 %
Patients Enrolled	Relapsed/refractory CD30+ biopsy proven Hodgkin lymphoma (HL) or anaplastic large cell lymphoma (ALCL) and an ECOG Performance Status 2.
Administration Dosage	Bv was escalated from 1.20 mg/kg Day 1, and B from 70 mg/m2 Days 1 and 2 every 21 days until the MTD or recommended phase 2 dose (RP2D) was reached;Bv escalating to a dose of 1.80 mg/kg and B was escalated to 90 mg/m2.
Related Clinical Trial
NCT Number	NCT01657331	Phase Status	Phase 1/2
Clinical Description	A phase 1/2 clinical trial of the combination of brentuximab vedotin and bendamustine in patients with relapsed or refractory hodgkin lymphoma or anaplastic large cell lymphoma.
Primary Endpoint	The MTD was not reached, based on the fact there was no maximum administrable dose identified. The RP2D was Bv at 1.80 mg/kg and B at 9.00 mg/kg. Only 1 of 11 patients qualified as a DLT (Grade 4 neutropenia) at the RP2D.
Other Endpoint	17 of 28 (ORR 60.71%, 95% CI 41.00-79.00) of patients achieved a response in the Phase 1, with 5 of 28 (17.86%) being CR. In the Phase 2, 29 of 37 (ORR 78.38%, 95% CI 62.00-91.00) patients responded, with 16 of 37 (43.24%) attaining a CR.
Experiment 21 Reporting the Activity Date of This ADC					[69]
Efficacy Data	Objective Response Rate (ORR)	50%	Positive CD30 expression (CD30+++/++; FACS analysis = 102)
Patients Enrolled	Patients had relapsed or refractory, histologically confirmed CD30-positive hematologic cancers. Patients with Hodgkin's lymphoma had received systemic chemotherapy either as induction therapy for advanced-stage disease or salvage therapy after initial radiotherapy for early-stage disease and had previously undergone autologous stem cell transplant (ASCT).    Click to Show/Hide
Administration Dosage	Intravenously at doses of 0.10 to 3.60 mg per kilogram of body weight every 3 weeks (one cycle).
Related Clinical Trial
NCT Number	NCT00430846	Phase Status	Phase 1
Clinical Description	A phase 1 dose escalation study of SGN-35 in patients with relapsed/refractory CD30-positive hematologic malignancies.
Primary Endpoint	Safety profile of brentuximab vedotin =1.80 mg/kg.
Other Endpoint	Secondary objectives were to determine pharmacokinetic measures for the antibody-drug conjugate and MMAE, evaluate immunogenicity, and assess antitumor response.The median time to maximum concentration occurred immediately after infusion for the antibody-drug conjugate and approximately 2 to 3 days after infusion for MMAE. Steady-state pharmacokinetics for both the antibody-drug conjugate and MMAE occurred by approximately 21 days,consistent with the half-life estimates of 4 to 6 days and 3 to 4 days, respectively.    Click to Show/Hide
Experiment 22 Reporting the Activity Date of This ADC					[72]
Efficacy Data	Objective Response Rate (ORR)	73.00 70.00 %
Patients Enrolled	R/R PMBL; had an Eastern Cooperative Oncology Group performance status of 0 to 1, had a CD30 expression level of 1% or greater in the tumor or tumor-infiltrating lymphocytes by local immunohistochemistry, and had 1 or more measurable sites of disease according to the Lugano 2014 classification.
Administration Dosage	Received nivolumab (240 mg intravenously) and BV (1.80 mg/kg intravenously) every 3 weeks until disease progression or unacceptable toxicity.
Related Clinical Trial
NCT Number	NCT02581631	Phase Status	Phase 1
Clinical Description	A phase 1/ 2 study to evaluate the safety and preliminary efficacy of nivolumab in combination with brentuximab vedotin in subjects with relapsed refractory non hodgkin lymphomas with CD30 expression (checkmate 436: CHECK point pathway and nivolumab clinical trial evaluation 436).
Primary Endpoint	For nivolumab (240 mg intravenously) and BV (1.8 mg/kg intravenously), ORR(95% CI) was 73.00% (54.00% to 88.00%), with a 37.00% complete remission rate per investigator, and ORR of 70.00% (51.00% to 85.00%), with a 43.00% complete metabolic response rate per independent review.
Other Endpoint	For nivolumab (240 mg intravenously) and BV (1.80 mg/kg intravenously), the 6-month PFS rate was 63.50% (95% CI, 42.50 to 78.60), and the 6-month OS rate was 86.30% (95% CI, 67.50 to 94.60). Median PFS and median OS were not reached.
Experiment 23 Reporting the Activity Date of This ADC					[75]
Efficacy Data	Objective Response Rate (ORR)	81.97 83.33 %
Patients Enrolled	Refractory Hodgkin lymphoma (defined as not achieving a CR to frontline therapy or progression within 3 months of CR), or Hodgkin lymphoma that had relapsed (defined as progression 3 months after CR to frontline therapy).
Administration Dosage	Received BV (1.80 mg/kg IV, 30-minute infusion) and Nivo (3.00 mg/kg IV, 60-minute infusion) in 3-week cycles for up to 12 weeks (4 cycles). During the first cycle, BV was administered on day 1 and Nivo on day 8. During cycles 2 to 4, BV and Nivo were administered on day 1, with Nivo given at least 30 minutes after BV.
Related Clinical Trial
NCT Number	NCT02572167	Phase Status	Phase 1
Clinical Description	A phase 1/2 study evaluating brentuximab vedotin in combination with nivolumab in patients with relapsed or refractory Hodgkin lymphoma after failure of frontline therapy.
Primary Endpoint	Response rates and Deauville 5-point score for all treated patients (n = 61) and efficacy-evaluable patients (n = 60) are presented. The CR rate among all treated patients was 61.00% (95% CI,47.00%-73.00%). Among efficacy-evaluable patients,the CR rate was 62.00% (95% CI,48.00%-74.00%).
Other Endpoint	Response rates and Deauville 5-point score for all treated patients (n = 61) and efficacy-evaluable patients (n = 60) are presented. The ORR rate among all treated patients was 81.97% (95% CI, 70.00%-91.00%). Among efficacy-evaluable patients, the ORR rate was 83.33% (95% CI,72.00%-92.00%).
Experiment 24 Reporting the Activity Date of This ADC					[76]
Efficacy Data	Objective Response Rate (ORR)	85%
Patients Enrolled	Biopsy-proven primary refractory (ie, not achieving a CR or progression <3 months after CR) or relapsed Hodgkin lymphoma (HL; progression 3 months after CR).
Administration Dosage	Received up to 4 cycles of BV 1.80 mg/kg every 3 weeks IV over 30 minutes followed by Nivo 3.00 mg/kg IV over 60 minutes. In parts 1/2 (staggered dosing), BV was administered on day 1 and Nivo on day 8 of cycle 1, with both agents administered on day 1 during cycles 2 to 4. During part 2, the protocol was amended to mandate prophylactic treatment with steroids (hydrocortisone 100 mg or equivalent) and antihistamines (diphenhydramine 25-50 mg or equivalent) at day 1 of each cycle beginning at cycle 2. Patients in part 3 (same-day dosing) received both BV and Nivo on day 1 of all cycles, based on the interim efficacy and safety results in parts 1 and 2 of this study and encouraging results with same-day dosing of both agents in the Eastern Cooperative Oncology Group and the American College of Radiology Imaging Network (ECOG-ACRIN) study E4412.    Click to Show/Hide
Related Clinical Trial
NCT Number	NCT02572167	Phase Status	Phase 1
Clinical Description	A phase 1/2 study evaluating brentuximab vedotin in combination with nivolumab in patients with relapsed or refractory Hodgkin lymphoma after failure of frontline therapy.
Primary Endpoint	The objective response rate (ORR; N=91) = 85.00%, with 67.00% achieving a complete response (CR); progression-free survival (PFS) rate at 3 years = 77.00% (95% CI, 65.00% to 86.00%) and 91.00% (95% CI, 79.00% to 96.00%) for patients undergoing ASCT directly after study treatment.
Other Endpoint	OS= 93.00% (95% CI, 85.00% to 97.00%) at 3 years.
Experiment 25 Reporting the Activity Date of This ADC					[77]
Efficacy Data	Objective Response Rate (ORR)	100%	Positive CD30 expression (CD30+++/++)
Patients Enrolled	CD30 peripheral T-cell lymphoma.
Administration Dosage	1.8 mg/kg IV once every 3 weeks for 6 cycles.
Related Clinical Trial
NCT Number	NCT01309789	Phase Status	Phase 1
Clinical Description	A phase 1 study of brentuximab vedotin given sequentially and combined with multi-agent chemotherapy for CD30-positive mature T-cell and NK-cell neoplasms.
Primary Endpoint	Objective response rate=100.00%.
Other Endpoint	5-year PFS= 52.00%; OS=80.00%
Experiment 26 Reporting the Activity Date of This ADC					[78]
Efficacy Data	Objective Response Rate (ORR)	73.00 86.00 %
Patients Enrolled	Hodgkin lymphoma who had relapsed after autologous stem cell transplant (ASCT); systemic anaplastic large-cell lymphoma (sALCL) who had previously been treated with curative intent.
Administration Dosage	1.80 mg/kg, i.v., once every 21 days; a maximum of 16 cycles.
Experiment 27 Reporting the Activity Date of This ADC					[79]
Efficacy Data	Objective Response Rate (ORR)	58.54%
Patients Enrolled	Relapsed or refractory, histologically confirmed CD30-positive hematologic malignancies with bi-dimensional measurable disease of at least 1.5 cm by radiographic evaluation. Patients with Hodgkin lymphoma had received systemic chemotherapy as induction therapy for advanced-stage disease or salvage therapy after initial radiotherapy for early-stage disease and had previously undergone autologous stem cell transplantation (ASCT) unless they were ineligible for or had declined treatment. Patients with other CD30-positive malignancies had previously failed or were refractory to front-line chemotherapy. Patients who had transformed to systemic anaplastic large cell lymphoma (ALCL) were eligible.    Click to Show/Hide
Administration Dosage	Intravenously on Days 1, 8, and 15, of each 28-day cycle at doses ranging from 0.40 to 1.40 mg/kg.
Experiment 28 Reporting the Activity Date of This ADC					[80]
Efficacy Data	Complete Remission (CR)	35%
Patients Enrolled	Histologically confirmed rel/ref de novo or transformed diffuse large B-cell lymphoma (DLBCL) after at least 1 prior therapy, Eastern Cooperative Oncology Group (ECOG) performance status 2, and adequate organ function as defined in supplemental Methods.
Administration Dosage	The treatment cycle was 21 days with intravenous BV administered on day 1 and Len administered on days 1 to 21 for a maximum of 16 cycles, the maximum tolerated dose of the combination was 1.20 mg/kg BV with 20 mg/d Len.
Related Clinical Trial
NCT Number	NCT04404283	Phase Status	Phase 3
Clinical Description	A randomized, double-blind, placebo-controlled, active-comparator, multicenter, phase 3 study of brentuximab vedotin or placebo in combination with lenalidomide and rituximab in subjects with relapsed or refractory diffuse large B-cell lymphoma (DLBCL).
Primary Endpoint	The maximum tolerated dose of the combination was 1.20 mg/kg BV with 20 mg/d lenalidomide.
Other Endpoint	The overall response rate was 57.00% (95% CI, 39.60-72.50), complete response rate, 35.00% (95% CI, 20.70-52.60); median duration of response, 13.10 months; median progression-free survival, 10.20 months (95% CI, 5.50-13.70); and median overall survival, 14.30 months (95% CI, 10.20-35.60).
Experiment 29 Reporting the Activity Date of This ADC					[81]
Efficacy Data	Complete Remission (CR)	61.54%
Patients Enrolled	Previously untreated, histologically confirmed stage III/IV classical Hodgkin lymphoma (cHL).
Administration Dosage	A+AVD (brentuximab vedotin, 1.20 mg/kg of bodyweight, doxorubicin 25 mg/m2 of body surface area, vinblastine 6 mg/m2, and dacarbazine 375 mg/m2) or ABVD (doxorubicin 25 mg/m2, bleomycin 10 U/m2, vinblastine 6 mg/m2, and dacarbazine 375 mg/m2) intravenously on days 1 and 15 of each 28-day cycle for up to six cycles.    Click to Show/Hide
Related Clinical Trial
NCT Number	NCT01712490	Phase Status	Phase 3
Clinical Description	A randomized, open-label, phase 3 trial of A+AVD versus ABVD as frontline therapy in patients with advanced classical hodgkin lymphoma.
Primary Endpoint	For 1.20 mg/kg BV intravenously, the 3-year PFS rates=83.10% (95% CI, 79.90-85.90) in the A+AVD arm.
Other Endpoint	For 1.20 mg/kg BV intravenously, complete resolution(CR)=61.54% of (272/442) in the A+AVD arm.
Experiment 30 Reporting the Activity Date of This ADC					[82]
Efficacy Data	Complete Remission (CR)	71.33%
Patients Enrolled	Previously untreated patients (18 years with an Eastern Cooperative Oncology Group performance status of 2) with stage III or IV classical Hodgkin lymphoma.
Administration Dosage	A+AVD (brentuximab vedotin, 1.20 mg/kg of bodyweight, doxorubicin 25 mg/m2 of body surface area, vinblastine 6 mg/m2, and dacarbazine 375 mg/m2) or ABVD (doxorubicin 25 mg/m2, bleomycin 10 U/m2, vinblastine 6 mg/m2, and dacarbazine 375 mg/m2) intravenously on days 1 and 15 of each 28-day cycle for up to six cycles.    Click to Show/Hide
Related Clinical Trial
NCT Number	NCT01712490	Phase Status	Phase 3
Clinical Description	A randomized, open-label, phase 3 trial of A+AVD versus ABVD as frontline therapy in patients with advanced classical hodgkin lymphoma.
Primary Endpoint	For 1.20 mg/kg BV intravenously, 5-year PFS rates=82.20% (95% CI 79.00-85.00) with A+AVD.
Other Endpoint	For 1.20 mg/kg BV intravenously, complete resolution(CR)=71.33% of (31.6/44.3) of patients with peripheral neuropathy in the A+AVD arm. Peripheral neuropathy occurred in 443 (66.91%) of 662 patients in the A+AVD group.
Experiment 31 Reporting the Activity Date of This ADC					[83]
Efficacy Data	Complete Remission (CR)	12%
Patients Enrolled	Part (A) relapsed/refractory CD30-expressing mature T-cell and B-cell non-Hodgkin lymphomas (NHL), including DLBCL; Part (B) brentuximab vedotin plus rituximab in relapsed/refractory CD30-expressing DLBCL; and Part (C) single-agent brentuximab vedotin in relapsed/refractory CD30u DLBCL.
Administration Dosage	1.80 mg/kg was administered IV every 21 days.
Related Clinical Trial
NCT Number	NCT01421667	Phase Status	Phase 2
Clinical Description	A phase 2 study of brentuximab vedotin in relapsed or refractory non-hodgkin lymphoma (NHL).
Primary Endpoint	ORR=31.00%, median duration=4.70 months (range 0.50-11.60) for 16 patients enrolled on Part C.
Other Endpoint	Six patients had CR (12.00%) with a median duration of 11.60 months (range,1.40+ - 11.60) and median PFS of 15.60 months (range,3.8+ - 15.6). Overall median PFS was 1.4 months (range, 0.40- 15.60). Median overall survival (OS) was 7.50 months (range, 0.7-18.6).
Experiment 32 Reporting the Activity Date of This ADC					[84]
Efficacy Data	Complete Remission (CR)	35.41%
Patients Enrolled	A clinical and histologically confirmed diagnosis of CD30+ LyP, CD30+ pc-anaplastic large-cell lymphoma (ALCL), or myelofibrosis (MF). Eastern Cooperative Oncology Group performance status of 2 and adequate bone marrow and organ function were required.
Administration Dosage	Intravenously at 1.80 mg/kg every 21 days for a maximum of eight doses.
Related Clinical Trial
NCT Number	NCT01352520	Phase Status	Phase 2
Clinical Description	Phase 2 trial of brentuximab vedotin (SGN-35) at dose of 1.80 mg/kg IV every 3 weeks in patients with CD30-positive lymphoproliferative disorders (cutaneous anaplastic large T-cell lymphoma (ALCL), mycosis fungoides, and extensive lymphomatoid papulosis (LyP).
Primary Endpoint	Os rate=72.92% (95% CI, 60.00% to 86.00%; 35 of 48 patients), CR raate=35.41% (95% CI, 22.00% to 49.00%; 17 of 48 patients). Fifteen (53.57%; 95% CI, 31% to 59%) of 28 patients with MF responded, independent of CD30 expression.
Other Endpoint	In patients with MF/Szary syndrome, the overall response rate was 50.00% (five of 10 patients) in patients with low CD30 expression (< 10%), 58.33% (seven of 12 patients) in patients with medium expression (10% to 50%), and 50.00% (three of six patients) in patients with high expression (50%).
Experiment 33 Reporting the Activity Date of This ADC					[85]
Efficacy Data	Complete Remission (CR)	43%
Patients Enrolled	Patients over 10 years of age with biopsy-proven cHL that had relapsed or was primary refractory (lack of CR or PD within 3months of upfront therapy) after standard initial therapy were eligible.
Administration Dosage	1.80 mg/kg intravenously every 3 weeks for two cycles.
Related Clinical Trial
NCT Number	NCT01393717	Phase Status	Phase 2
Clinical Description	A phase 2 study of brentuximab vedotin as salvage therapy for hodgkin lymphoma prior to autologous hematopoietic stem cell transplantation.
Primary Endpoint	The 2-year PFS among patients in CR at the time of AHCT (n=37) was 71% compared with 54% in patients not in CR (p=0.12). The 2-year PFS in patients who proceeded to AHCT directly after receiving BV alone was 77%.
Other Endpoint	Of 56 evaluable patients treated across cohorts, the overall response rate (ORR) to second-line BV was 75.00% with 43.00% CR.
Experiment 34 Reporting the Activity Date of This ADC					[86]
Efficacy Data	Complete Remission (CR)	58%
Patients Enrolled	LyP and were also required to have scarring, more than 10 lesions, or active lesions on the face, hands, or feet.
Administration Dosage	Intravenous brentuximab vedotin 1.80 mg/kg infused over 30 minutes every 21 days.
Related Clinical Trial
NCT Number	NCT01352520	Phase Status	Phase 2
Clinical Description	Phase 2 trial of brentuximab vedotin (SGN-35) at dose of 1.80 mg/kg IV every 3 weeks in patients with CD30-positive lymphoproliferative disorders (cutaneous anaplastic large T-cell lymphoma (ALCL), mycosis fungoides, and extensive lymphomatoid papulosis (LyP).
Primary Endpoint	The overall response rate was 100% and at 4 months was 80% (8 of 10 patients).
Experiment 35 Reporting the Activity Date of This ADC					[87]
Efficacy Data	Complete Remission (CR)	14.70%
Patients Enrolled	Steroid-refractory acute graft-versus-host disease (SR-aGVHD).
Administration Dosage	The study included weekly dosing for 3 weeks followed by maintenance dosing every 3 weeks for an 4 additional doses. A standard 3+3 dose-escalation cohort (0.60 mg/kg, 0.90 mg/kg, and 1.20 mg/kg) was planned to define the maximum tolerated dose (MTD). After treating the first 6 patients, the study was revised to dosing every 2 weeks for 4 doses only for safety purposes, and to enroll cohorts of 5 patients at each dose level (0.60 mg/kg, 0.80 mg/kg, 1.00 mg/kg, and 1.20 mg/kg).    Click to Show/Hide
Related Clinical Trial
NCT Number	NCT01940796	Phase Status	Phase 1
Clinical Description	Phase 1 trial of brentuximab vedotin for refractory chronic graft-vs.-host disease (GVHD).
Primary Endpoint	The MTD was defined at 0.80 mg/kg with one DLT observed (sepsis).
Other Endpoint	At day 28, the overall response rate was 38.20% with 5 complete responses (CR, 14.70%) and 8 very good partial responses (VGPR, 23.50%).Overall survival was 41.00% (95% CI, 25.00%-57.00%) at 6 months and 38.00% (95% CI, 22.00%-54.00%) at 12 months.
Experiment 36 Reporting the Activity Date of This ADC					[88]
Efficacy Data	Complete Remission (CR)	35%
Patients Enrolled	Relapsed or refractory diffuse large B-cell lymphoma (DLBCL); have previously received at least two lines of therapy, including rituximab and an anthracycline; patients had either had a relapse after or were ineligible for autologous transplantation.
Administration Dosage	1.20 mg/kg intravenously (IV) on Day 1 of every 21 day cycle.
Related Clinical Trial
NCT Number	NCT02086604	Phase Status	Phase 1
Clinical Description	A phase 1 trial of brentuximab vedotin in combination with lenalidomide in relapsed or refractory diffuse large B-cell lymphoma.
Primary Endpoint	Most patients required granulocyte colony-stimulating factor support because of neutropenia. The overall response rate was 57.00% (95% CI, 39.60-72.50), complete response rate, 35.00% (95% CI, 20.70-52.60); median duration of response, 13.10 months; median progression-free survival, 10.20 months (95% CI, 5.50-13.70); and median overall survival, 14.30 months (95% CI, 10.20-35.60). Response rates were highest in patients with CD301 DLBCL (73.00%), but they did not differ according to cell of origin (P=5.96).    Click to Show/Hide
Experiment 37 Reporting the Activity Date of This ADC					[90]
Efficacy Data	Complete Remission (CR)	66.67%
Patients Enrolled	Primary refractory Hodgkin Lymphoma or early relapse. Eligibility criteria included age 30 years; no prior Brentuximab vedotin exposure; and relapse <1 year from completion of initial therapy.
Administration Dosage	Each 21-day cycle consisted of intravenous day 1 at 1.40 mg/kg or 1.80 mg/kg.
Related Clinical Trial
NCT Number	NCT01780662	Phase Status	Phase 1
Clinical Description	A phase 1/2 study of brentuximab vedotin (SGN35) in combination with gemcitabine for pediatric and young adult patients with relapsed or refractory Hodgkin lymphoma.
Primary Endpoint	For four of the 13 patients with stable disease or partial response,all target lesions were Deauville score 3 on central review,and would thus be considered CRs by response criteria published after AHOD1221 opened. By these criteria,the complete response rate observed on AHOD1221 was 28 of 42 patients (66.67%; 95% CI, 51.00-80.00%).
Experiment 38 Reporting the Activity Date of This ADC					[91]
Efficacy Data	Complete Remission (CR)	74%
Patients Enrolled	First relapse or primary refractory classic Hodgkin lymphoma (CHL) after one prior line of therapy.
Administration Dosage	Days 1 and 8 at either 1.20 or 1.50 mg/kg IV (capped at 150 mg) with standard dosing of ICE on days 13 for two cycles.
Related Clinical Trial
NCT Number	NCT02227199	Phase Status	Phase 1
Clinical Description	A phase 1/2 trial of brentuximab vedotin (BV), ifosfamide (I), carboplatin (C), and etoposide (E) for patients with relapsed or refractory Hodgkin lymphoma (BV-ICE).
Primary Endpoint	Rp2D=BV 1.50 mg/kg IV CR=74.00%.
Other Endpoint	ORR=91.00%.
Experiment 39 Reporting the Activity Date of This ADC					[92]
Efficacy Data	Complete Remission (CR)	86%
Patients Enrolled	CD30+ primary mediastinal large B-cell lymphoma (PMBCL), diffuse large B-cell lymphoma (DLBCL), or gray zone lymphoma (GZL). Patients with any stage, measurable disease, and an Eastern Cooperative Oncology Group Performance Status of 3 or less were eligible. The diagnostic biopsy had to demonstrate at least 1% or higher expression of CD30 on the lymphoma B cells by immunohistochemistry and was assessed independently by two pathologists. Patients with active central nervous system involvement and uncontrolled systemic infections were excluded.    Click to Show/Hide
Administration Dosage	Six cycles of BV (1.80 mg/kg, maximum dose of 180 mg) administered with the R-CHOP regimen without vincristine, including: rituximab 375 mg/m2, cyclophosphamide 750 mg/m2, and doxorubicin 50 mg/m2 on day 1 and prednisone 100 mg (or equivalent) daily on days 1 through 5 of each 21-day cycle. For cycle 1, rituximab was split into two doses (100 mg/m2 on day 1 and 275 mg/m2 on day 2) to reduce risks of an infusion reaction to rituximab.    Click to Show/Hide
Related Clinical Trial
NCT Number	NCT01994850	Phase Status	Phase 1
Clinical Description	A phase 1/2 study of brentuximab vedotin in combination with multi-agent chemotherapy as front-line treatment in patients with CD30 positive primary mediastinal large B-cell, diffuse large B-cell, and grey zone lymphomas.
Primary Endpoint	For Brentuximab vedotin dose of 1.80 mg/kg, the overall response rate was 100.00% (95%CI: 88.00-100.00) with 86.00% (95% CI: 68.00-96.00) of patients achieving complete response at the end of systemic treatment.
Other Endpoint	For Brentuximab vedotin dose of 1.80 mg/kg, the 2-year PFS and overall survival rates were 85.00% (95%CI: 66.00-94.00) and 100.00%, respectively.
Experiment 40 Reporting the Activity Date of This ADC					[93]
Efficacy Data	Complete Remission (CR)	95.45 96.00 %
Patients Enrolled	Newly diagnosed, treatment-naive, CD30-positive patients with Hodgkin's lymphoma who had histologically confirmed stage IIA bulky disease or stage IIB-IV disease and an Eastern Cooperative Oncology Group performance status of two or less.
Administration Dosage	0.60, 0.90, or 1.20 mg/kg brentuximab vedotin by intravenous infusion every 2 weeks with either ABVD (25 mg/m(2) doxorubicin, 10 units/m(2) bleomycin, 6 mg/m(2) vinblastine, and 375 mg/m(2) dacarbazine) or AVD (ABVD modified regimen without the inclusion of bleomycin) for up to six cycles.
Related Clinical Trial
NCT Number	NCT01060904	Phase Status	Phase 1
Clinical Description	A phase 1 dose-escalation safety study of brentuximab vedotin in combination with multi-agent chemotherapy as frontline therapy in patients with Hodgkin lymphoma.
Primary Endpoint	The MTD of brentuximab vedotin 1.20 mg/kg ; CR of brentuximab vedotin + ABVD = 95.45%(21/22); CR of brentuximab vedotin + AVD = 96.00%(24 /25 ).
Other Endpoint	Maximum tolerated dose was not exceeded at 1.20 mg/kg of brentuximab vedotin combined with either ABVD or AVD.
Experiment 41 Reporting the Activity Date of This ADC					[95]
Efficacy Data	Complete Remission (CR)	60%
Patients Enrolled	Had prior solid organ or hematopoietic stem cell transplantation, received immunosuppressive therapy for a nonmalignant condition, and/or had an aggressive EBV+lymphoid malignancy.
Administration Dosage	Induction therapy consisted of R 375 mg/m2 given on days 1, 8, 15, 22, and BV 1.20 mg/kg given on days 1, 8, 15, followed by restaging as assessed by CT imaging. MT consisted of BV 1.8 mg/kg every 3 weeks and R 375 mg/m2 every 6 weeks for up to one year of total therapy.
Experiment 42 Reporting the Activity Date of This ADC					[97]
Patients Enrolled	Patients aged 18 years with previously treated CD30-expressing myelofibrosis (MF) or classic anaplastic large-cell lymphoma (after at least 1 prior systemic therapy or prior radiotherapy) were enrolled; CD30 positivity was defined as 10% of target lymphoid cells exhibiting a membrane, cytoplasmic, and/or Golgi staining pattern for CD30. An Eastern Cooperative Oncology Group performance status of 0 to 2 was required.    Click to Show/Hide
Administration Dosage	Brentuximab vedotin (1.80 mg/kg IV every 3 weeks, for up to 16 cycles) or physicians choice (methotrexate, 5-50 mg orally once weekly or bexarotene 300 mg/m2 [target dose] orally once daily, for up to 48 weeks).
Related Clinical Trial
NCT Number	NCT01578499	Phase Status	Phase 3
Clinical Description	A previously treated, recurrent or metastatic cervical cancer (SGN-35) versus physician's choice (methotrexate or bexarotene) in patients with CD30-positive cutaneous T-cell lymphoma.
Primary Endpoint	For 1.80 mg/kg BV intravenously, objective responses lasting 4 months (ORR4) was 54.70%; the ORR per IRF was 65.60%.
Other Endpoint	For 1.80 mg/kg BV intravenously, the CR rate was 17.20%; median PFS 16.70 (95% CI, 0.25-0.58); 3-year estimates of OS was 64.40% (95% CI, 0.42-1.32); time to next treatment (TTNT) was 14.20 (95% CI, 0.17-0.42).
Experiment 43 Reporting the Activity Date of This ADC					[98]
Patients Enrolled	Advanced classic Hodgkins lymphoma (Ann Arbor stage III or IV, as determined on a 4-point scale, with higher stages indicating more widespread disease),17 according to the World Health Organization classification system. Patients who had not been previously treated with systemic chemotherapy or radiotherapy were eligible. Patients were required to have an Eastern Cooperative Oncology Group performance status of 0, 1, or 2 (on a scale of 0 to 5, with higher scores indicating greater disability).    Click to Show/Hide
Administration Dosage	A+AVD (1.20 mg of brentuximab vedotin per kilogram of body weight, 25 mg of doxorubicin per square meter of body-surface area, 6 mg of vinblastine per square meter, and 375 mg of dacarbazine per square meter) or ABVD (25 mg of doxorubicin per square meter, 10 units of bleomycin per square meter, 6 mg of vinblastine per square meter, and 375 mg of dacarbazine per square meter) intravenously on days 1 and 15 of each 28-day cycle for up to 6 cycles.    Click to Show/Hide
Related Clinical Trial
NCT Number	NCT01712490	Phase Status	Phase 3
Clinical Description	A randomized, open-label, phase 3 trial of A+AVD versus ABVD as frontline therapy in patients with advanced classical Hodgkin lymphoma.
Primary Endpoint	After a median follow-up of 24.90 months (range, 0 to 49.30), the rate of the primary end point of independently determined modified progression-free survival was significantly higher in the A+AVD group than in the ABVD group (2-year modified progression-free survival rate, 82.10% [95% confidence interval {CI}, 78.70 to 85.00] vs. 77.20% [95% CI, 73.70 to 80.40]; hazard ratio for progression, death, or modified progression, 0.77 [95% CI, 0.60 to 0.98]; P = 0.03), corresponding to a 23.00% risk reduction.    Click to Show/Hide
Other Endpoint	The interim 2-year overall survival rate for the A+AVD group was 96.60% (95% CI,94.80 to 97.70) and that for the ABVD group was 94.90% (95% CI,92.90 to 96.40),which corresponded to a reduction in the risk of death of 28.00% in favor of the A+AVD regimen (hazard ratio,0.72; 95% CI,0.44 to 1.17; P = 0.19).
Experiment 44 Reporting the Activity Date of This ADC					[99]
Patients Enrolled	CD30-positive mycosis fungoides or primary cutaneous anaplastic large-cell lymphoma who had been previously treated.
Administration Dosage	Interactive voice and web response system to receive intravenous brentuximab vedotin 1.80 mg/kg once every 3 weeks, for up to 16 3-week cycles.
Related Clinical Trial
NCT Number	NCT01578499	Phase Status	Phase 3
Clinical Description	A randomized, open-label, phase 3 trial of brentuximab vedotin (SGN-35) versus physician's choice (methotrexate or bexarotene) in patients with CD30-positive cutaneous T-cell lymphoma.
Primary Endpoint	At a median follow-up of 22.90 months (95% CI 18.40-26.10), the proportion of patients achieving an objective global response lasting at least 4 months was 56.25% (36 of 64 patients) with brentuximab vedotin versus 12.50% (8/64) with physicians choice, resulting in a between-group difference of 43.80% (95% CI 29.10-58.40).
Other Endpoint	Median progression-free survival per EMA criteria was 16.70 months in the brentuximab vedotin group versus 3.50 months in the physicians choice group (HR 0.270, 95% CI 0.169-0.430).
Experiment 45 Reporting the Activity Date of This ADC					[100]
Patients Enrolled	Previously untreated Hodgkins lymphoma of stage IIB with bulk tumor or stage IIIB, IVA, or IVB.
Administration Dosage	Brentuximab vedotin (at a dose of 1.80 mg per kilogram) plus doxorubicin, vincristine, etoposide, prednisone, and cyclophosphamide or the standard bleomycin-containing chemotherapy regimen was administered every 21 days.
Related Clinical Trial
NCT Number	NCT02166463	Phase Status	Phase 3
Clinical Description	A randomized phase 3 study of brentuximab vedotin (SGN-35) for newly diagnosed high-risk classical hodgkin lymphoma (cHL) in children and young adults.
Primary Endpoint	At a median follow-up of 42.10 months (range, 0.10 to 80.90), the 3-year event-free survival was 92.10% (95% confidence interval [CI],88.40 to 94.70) in the brentuximab vedotin group.
Other Endpoint	Overall survival at 3 years was 99.30% (95% CI,97.30 to 99.80) in the brentuximab vedotin group.
Experiment 46 Reporting the Activity Date of This ADC					[101]
Patients Enrolled	III or IV Hodgkins lymphoma.
Administration Dosage	1.20 mg of brentuximab vedotin per kilogram of body weight, 25 mg of doxorubicin per square meter of body-surface area, 6 mg of vinblastine per square meter, and 375 mg of dacarbazine per square meter; intravenously on days 1 and 15 of each 28-day cycle for up to six cycles.
Related Clinical Trial
NCT Number	NCT01712490	Phase Status	Phase 3
Clinical Description	A randomized, open-label, phase 3 trial of A+AVD Versus ABVD as frontline therapy in patients with advanced classical hodgkin lymphoma.
Primary Endpoint	The analysis of overall survival significantly favored A+AVD over ABVD (95% CI,0.40-0.88).The 6-year overall survival estimates were 93.90% (95% CI,91.60 to 95.50) in the A+AVD group and 89.40% (95% CI,86.60 to 91.70) in the ABVD group.
Other Endpoint	The median follow-up in the overall survival analysis was 73.00 months (95% CI,72.30 to 73.60; range,0.0 to 100.6). A total of 39 deaths occurred in the A+AVD group and 64 in the ABVD group.
Experiment 47 Reporting the Activity Date of This ADC					[103]
Patients Enrolled	46 patients with classic Hodgkin lymphoma, unsuitable for standard chemotherapy because of a cardiac ejection fraction of less than 50%, pulmonary diffusion capacity of less than 80%, or a creatinine clearance of 30 mL/min or more but less than 60 mL/minrequired to have an Eastern Cooperative Oncology Group (ECOG) performance status of 0-2.
Administration Dosage	Brentuximab vedotin (1.8 mg/kg, dose cap at 180 mg) and nivolumab (3 mg/kg) intravenously every 21 days for 8 cycles.
Related Clinical Trial
NCT Number	NCT02758717	Phase Status	Phase 2
Clinical Description	Phase II, multi-center trial of nivolumab and brentuximab vedotin in patients with untreated Hodgkin lymphoma over the age of 60 years or unable to receive standard adriamycin, bleomycin, vinblastine, and dacarbazine (ABVD) chemotherapy.
Primary Endpoint	The overall response, defined as a partial metabolic response or complete metabolic response at the end of 8 cycles of treatment
Other Endpoint	The complete metabolic response rate, safety and tolerability of the regimen in this population, duration of response, progression-free survival, and overall survival.
Experiment 48 Reporting the Activity Date of This ADC					[105]
Patients Enrolled	Metastatic non-seminomatous germ cell tumor (GCT) with the exception of pure teratoma who progressed after first-line cisplatin-based chemotherapy and after at least one salvage regimen.
Administration Dosage	1.80 mg/kg IV every 3 weeks until disease progression or intolerable toxicities.
Related Clinical Trial
NCT Number	NCT01461538	Phase Status	Phase 2
Clinical Description	A phase 2, open-label study of brentuximab vedotin in patients with CD30-positive nonlymphomatous malignancies.
Primary Endpoint	For 1.80 mg/kg BV intravenously, Median PFS in the CD30 positive cohort was 1.20 months (95% CI: 0.90-2.10) and in the CD30 negative cohort was 1.40 months (95% CI: 0.00-2.10). Median OS in the CD30 positive cohort was 2.50 months (95% CI: 1.10-12.90) and in the CD30 negative cohort was 5.90 months (95% CI: 1.60-8.20).
Experiment 49 Reporting the Activity Date of This ADC					[106]
Patients Enrolled	Histologically proven anaplastic lymphoma kinase (ALK)+ anaplastic large-cell lymphoma (ALCL) and were younger than 22 years of age at diagnosis.
Administration Dosage	Brentuximab vedotin was administered on day 1 of each of the 6 cycles for a total of 6 doses. The starting dose of brentuximab vedotin was 1.80 mg/kg (maximum dose, 180 mg) given IV over 30 minutes on day 1 of each cycle prior to all other chemotherapy. Dose reductions to 1.20 mg/kg (maximum dose, 120 mg), followed by 0.80 mg/kg (maximum dose, 80 mg), were mandated for certain toxicities.    Click to Show/Hide
Related Clinical Trial
NCT Number	NCT01979536	Phase Status	Phase 2
Clinical Description	A randomized phase 2 trial of brentuximab vedotin (SGN35, NSC# 749710), or crizotinib (NSC#749005, commercially labeled) in combination with chemotherapy for newly diagnosed patients with anaplastic large cell lymphoma (ALCL).
Primary Endpoint	For 1.80 mg/kg BV intravenously, the complete response rate (complete response + complete response, unconfirmed) was 62.12% for patients who underwent evaluation after cycle 2 (41/66 patients) and 96.88% after cycle 6 (62/64 patients).
Other Endpoint	For 1.80 mg/kg BV intravenously, The 2-year event-free survival (EFS)=79.10% (95%CI, 67.20-87.10). The 2-year overall survival (OS)=97.00% (95% CI, 88.10-99.20).
Experiment 50 Reporting the Activity Date of This ADC					[107]
Patients Enrolled	High-risk relapsed or refractory classic Hodgkin lymphoma, had an ECOG performance status of 0-2, and had adequate organ and bone marrow function.
Administration Dosage	Enrolled patients received brentuximab vedotin (1.8 mg/kg) intravenously starting 30-60 days after autologous HSCT on day 1 of each 21-day cycle for up to 8 cycles.
Related Clinical Trial
NCT Number	NCT03057795	Phase Status	Phase 2
Clinical Description	A phase 2 study of nivolumab and brentuximab vedotin consolidation after autologous stem cell transplantation in patients with high-risk classical hodgkin lymphoma.
Primary Endpoint	The 18-month progression-free survival in all 59 patients was 94% (95% CI 84-98).
Other Endpoint	The 24-month overall survival was 98.00% (95% CI 88.00-100.00). The 24-month progression-free survival according to the number of risk factors was 94.00% (95% CI 67.00-99.00) in patients with one risk factor (n=21),96.00% (73.00-99.00) in patients with two risk factors (n=24), and 85.00% (51.00-96.00) in patients with three or more risk factors (n=14). The 24-month cumulative incidence of relapse and progression was 5.70% (95% CI 1.50-14.00); the 24-month cumulative incidence of non-relapse mortality was 1.80% (0.14-8.40).    Click to Show/Hide
Experiment 51 Reporting the Activity Date of This ADC					[109]
Related Clinical Trial
NCT Number	NCT02686346	Phase Status	Phase 1/2
Clinical Description	Phase 1/2 feasibility study of brentuximab vedotin in refractory/relapsed hodgkin lymphoma patients who are treated by chemotherapy (ICE) in second line and eligible for autologous transplantation.

Experiment 1 Reporting the Activity Date of This ADC					[118]
Efficacy Data	Tumor Growth Inhibition value (TGI)	0%	Positive CD30 expression (CD30+++/++)
Method Description	3 mg conjugate/kg/inj.
In Vivo Model	L2987 cell line xenograft model
In Vitro Model	Lung adenocarcinoma	L2987 cells		CVCL_H586
Experiment 2 Reporting the Activity Date of This ADC					[120]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 28.40%	Positive CD30 expression (CD30+++/++)
Method Description	The inhibitory activity of all possible combination Brentuximab Vedotin with TGR-1202 (PI3K- inhibitor) against cancer cell growth was evaluated in the HL xenograft model. Six- to eight-week-old NOD/SCID mice (20 to 25 g) were xenografted with L-540 (2.5x106 cells/mouse) and KM-H2 (2.0x106 cells/mouse) cells by inoculation into the left flank. When the tumor volume reached approximately 100 mg, the mice were randomly assigned to receive TGR-1202 (150 mg/kg/5 day/3 wks, PO) and/or BV (0.5 mg/kg/q4d/2 weeks, IP).    Click to Show/Hide
In Vivo Model	L-540 cell line xenograft model
In Vitro Model	Hodgkin lymphoma	L-540 cells		CVCL_1362
Experiment 3 Reporting the Activity Date of This ADC					[120]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 31.50%	Positive CD30 expression (CD30+++/++)
Method Description	The inhibitory activity of all possible combination Brentuximab Vedotin with TGR-1202 (PI3K- inhibitor) against cancer cell growth was evaluated in the HL xenograft model. Six- to eight-week-old NOD/SCID mice (20 to 25 g) were xenografted with L-540 (2.5x106 cells/mouse) and KM-H2 (2.0x106 cells/mouse) cells by inoculation into the left flank. When the tumor volume reached approximately 100 mg, the mice were randomly assigned to receive TGR-1202 (150 mg/kg/5 day/3 wks, PO) and/or BV (0.5 mg/kg/q4d/2 weeks, IP).    Click to Show/Hide
In Vivo Model	KM-H2 cell line xenograft model
In Vitro Model	Hodgkin lymphoma	KM-H2 cells		CVCL_1330
Experiment 4 Reporting the Activity Date of This ADC					[120]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 51.70%	Positive CD30 expression (CD30+++/++)
Method Description	The inhibitory activity of all possible combination Brentuximab Vedotin with TGR-1202 (PI3K- inhibitor) against cancer cell growth was evaluated in the HL xenograft model. Six- to eight-week-old NOD/SCID mice (20 to 25 g) were xenografted with L-540 (2.5x106 cells/mouse) and KM-H2 (2.0x106 cells/mouse) cells by inoculation into the left flank. When the tumor volume reached approximately 100 mg, the mice were randomly assigned to receive TGR-1202 (150 mg/kg/5 day/3 wks, PO) and/or BV (0.5 mg/kg/q4d/2 weeks, IP).    Click to Show/Hide
In Vivo Model	KM-H2 cell line xenograft model
In Vitro Model	Hodgkin lymphoma	KM-H2 cells		CVCL_1330
Experiment 5 Reporting the Activity Date of This ADC					[120]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 53.40%	Positive CD30 expression (CD30+++/++)
Method Description	The inhibitory activity of all possible combination Brentuximab Vedotin with TGR-1202 (PI3K- inhibitor) against cancer cell growth was evaluated in the HL xenograft model. Six- to eight-week-old NOD/SCID mice (20 to 25 g) were xenografted with L-540 (2.5x106 cells/mouse) and KM-H2 (2.0x106 cells/mouse) cells by inoculation into the left flank. When the tumor volume reached approximately 100 mg, the mice were randomly assigned to receive TGR-1202 (150 mg/kg/5 day/3 wks, PO) and/or BV (0.5 mg/kg/q4d/2 weeks, IP).    Click to Show/Hide
In Vivo Model	KM-H2 cell line xenograft model
In Vitro Model	Hodgkin lymphoma	KM-H2 cells		CVCL_1330
Experiment 6 Reporting the Activity Date of This ADC					[120]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 65.80%	Positive CD30 expression (CD30+++/++)
Method Description	The inhibitory activity of all possible combination Brentuximab Vedotin with TGR-1202 (PI3K- inhibitor) against cancer cell growth was evaluated in the HL xenograft model. Six- to eight-week-old NOD/SCID mice (20 to 25 g) were xenografted with L-540 (2.5x106 cells/mouse) and KM-H2 (2.0x106 cells/mouse) cells by inoculation into the left flank. When the tumor volume reached approximately 100 mg, the mice were randomly assigned to receive TGR-1202 (150 mg/kg/5 day/3 wks, PO) and/or BV (0.5 mg/kg/q4d/2 weeks, IP).    Click to Show/Hide
In Vivo Model	L-540 cell line xenograft model
In Vitro Model	Hodgkin lymphoma	L-540 cells		CVCL_1362
Experiment 7 Reporting the Activity Date of This ADC					[120]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 74.70%	Positive CD30 expression (CD30+++/++)
Method Description	The inhibitory activity of all possible combination Brentuximab Vedotin with TGR-1202 (PI3K- inhibitor) against cancer cell growth was evaluated in the HL xenograft model. Six- to eight-week-old NOD/SCID mice (20 to 25 g) were xenografted with L-540 (2.5x106 cells/mouse) and KM-H2 (2.0x106 cells/mouse) cells by inoculation into the left flank. When the tumor volume reached approximately 100 mg, the mice were randomly assigned to receive TGR-1202 (150 mg/kg/5 day/3 wks, PO) and/or BV (0.5 mg/kg/q4d/2 weeks, IP).    Click to Show/Hide
In Vivo Model	KM-H2 cell line xenograft model
In Vitro Model	Hodgkin lymphoma	KM-H2 cells		CVCL_1330
Experiment 8 Reporting the Activity Date of This ADC					[121]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 78.80%	Positive CD30 expression (CD30+++/++)
Method Description	The inhibitory activity of all possible combination regimens of ruxolitinib and BV against cancer cell growth was evaluated in the HDLM-2 xenograft mouse model of human HL. Mice of the ruxolitinib group received ruxolitinib at a dose of 50 mg/kg per day by s.c. inserted osmotic minipumps for 2 wk. Mice of the BV group received BV at 4 mg/kg by i.v. injection every 4 d for three injections. Mice of the combination group received a combination of ruxolitinb with BV at the same doses and dosing schedules as those in the ruxolitinib and BV groups.    Click to Show/Hide
In Vivo Model	HDLM-2 cell line xenograft model
In Vitro Model	Hodgkin lymphoma	HDLM-2 cells		CVCL_0009
Experiment 9 Reporting the Activity Date of This ADC					[121]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 87.30%	High CD30 expression (CD30+++)
Method Description	The inhibitory activity of all possible combination regimens of ruxolitinib, Navitoclax, and BV against cancer cell growth was evaluated in the HDLM-2 xenograft mouse model of human HL. The xenograft tumor model of human HL HDLM-2 was established by s.c. injection of 2x107 HDLM-2 cells into the right flank of female, 8-wk-old, NOD/SCID mice.    Click to Show/Hide
In Vivo Model	HDLM-2 cell line xenograft model
In Vitro Model	Hodgkin lymphoma	HDLM-2 cells		CVCL_0009
Experiment 10 Reporting the Activity Date of This ADC					[121]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 92%	Moderate CD30 expression (CD30++)
Method Description	The inhibitory activity of all possible combination regimens of ruxolitinib, Navitoclax, and BV against cancer cell growth was evaluated in the HDLM-2 xenograft mouse model of human HL. The xenograft tumor model of human HL HDLM-2 was established by s.c. injection of 2x107 HDLM-2 cells into the right flank of female, 8-wk-old, NOD/SCID mice.    Click to Show/Hide
In Vivo Model	HDLM-2 cell line xenograft model
In Vitro Model	Hodgkin lymphoma	HDLM-2 cells		CVCL_0009
Experiment 11 Reporting the Activity Date of This ADC					[121]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 94.70%	Negative CD30 expression (CD30-)
Method Description	The inhibitory activity of all possible combination regimens of ruxolitinib, Navitoclax, and BV against cancer cell growth was evaluated in the HDLM-2 xenograft mouse model of human HL. The xenograft tumor model of human HL HDLM-2 was established by s.c. injection of 2x107 HDLM-2 cells into the right flank of female, 8-wk-old, NOD/SCID mice.    Click to Show/Hide
In Vivo Model	HDLM-2 cell line xenograft model
In Vitro Model	Hodgkin lymphoma	HDLM-2 cells		CVCL_0009
Experiment 12 Reporting the Activity Date of This ADC					[118]
Efficacy Data	Tumor Growth Inhibition value (TGI)	96.83%	Positive CD30 expression (CD30+++/++)
Method Description	1 mg conjugate/kg/inj.
In Vivo Model	Karpas 299 ALCL cell line xenograft model
In Vitro Model	ALK-positive anaplastic large cell lymphoma	Karpas-299 cells		CVCL_1324
Experiment 13 Reporting the Activity Date of This ADC					[118]
Efficacy Data	Tumor Growth Inhibition value (TGI)	99.20%	Positive CD30 expression (CD30+++/++)
Method Description	0.5 mg/kg/in.
In Vivo Model	Karpas 299 ALCL cell line xenograft model
In Vitro Model	ALK-positive anaplastic large cell lymphoma	Karpas-299 cells		CVCL_1324
Experiment 14 Reporting the Activity Date of This ADC					[121]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 99.80%	High CD30 expression (CD30+++)
Method Description	The inhibitory activity of all possible combination regimens of ruxolitinib and BV against cancer cell growth was evaluated in the HDLM-2 xenograft mouse model of human HL. Mice of the ruxolitinib group received ruxolitinib at a dose of 50 mg/kg per day by s.c. inserted osmotic minipumps for 2 wk. Mice of the BV group received BV at 4 mg/kg by i.v. injection every 4 d for three injections. Mice of the combination group received a combination of ruxolitinb with BV at the same doses and dosing schedules as those in the ruxolitinib and BV groups.    Click to Show/Hide
In Vivo Model	HDLM-2 cell line xenograft model
In Vitro Model	Hodgkin lymphoma	HDLM-2 cells		CVCL_0009
Experiment 15 Reporting the Activity Date of This ADC					[121]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 99.90%	High CD30 expression (CD30+++)
Method Description	The inhibitory activity of all possible combination regimens of ruxolitinib, Navitoclax, and BV against cancer cell growth was evaluated in the HDLM-2 xenograft mouse model of human HL. The xenograft tumor model of human HL HDLM-2 was established by s.c. injection of 2x107 HDLM-2 cells into the right flank of female, 8-wk-old, NOD/SCID mice.    Click to Show/Hide
In Vivo Model	HDLM-2 cell line xenograft model
In Vitro Model	Hodgkin lymphoma	HDLM-2 cells		CVCL_0009
Experiment 16 Reporting the Activity Date of This ADC					[123]
Efficacy Data	Tumor Growth Delay (TGD)	40 Day	High CD30 expression (CD30+++)
Method Description	SCID mice were implanted with L540cy HL cells in the right flank. Groups of mice (9-10/group) were untreated or received SGN-35 (1 mg/kg, q4dx3, i.p.) and/or ABVD [Adriamycin (0.75 mg/kg, q4dx3, i.v.), Bleomycin (6u/kg, q4dx3, i.p.), Vinblastine (0.01 mg/kg, q4dx3, i.p.) and Dacarbazine (15 mg/kg, q3dx4, i.p.)] when tumour size averaged approximately 300 mm3.    Click to Show/Hide
In Vivo Model	L540cy cell line xenograft model
In Vitro Model	Hodgkin's disease	L540cy cells		Homo sapiens
Experiment 17 Reporting the Activity Date of This ADC					[123]
Efficacy Data	Tumor Growth Delay (TGD)	62 Day	High CD30 expression (CD30+++/++)
Method Description	SCID mice were implanted with L540cy HL cells in the right flank. Groups of mice (9-10/group) were untreated or received SGN-35 (1 mg/kg, q4dx3, i.p.) and/or ABVD [Adriamycin (0.75 mg/kg, q4dx3, i.v.), Bleomycin (6u/kg, q4dx3, i.p.), Vinblastine (0.01 mg/kg, q4dx3, i.p.) and Dacarbazine (15 mg/kg, q3dx4, i.p.)] when tumour size averaged approximately 300 mm3.    Click to Show/Hide
In Vivo Model	L540cy cell line xenograft model
In Vitro Model	Hodgkin's disease	L540cy cells		Homo sapiens
Experiment 18 Reporting the Activity Date of This ADC					[123]
Efficacy Data	Tumor Growth Delay (TGD)	63 Day	High CD30 expression (CD30+++)
Method Description	SCID mice were implanted with L540cy HL cells in the right flank. Groups of mice (9-10/group) were untreated or received SGN-35 (1 mg/kg, q4dx3, i.p.) and/or ABVD [Adriamycin (0.75 mg/kg, q4dx3, i.v.), Bleomycin (6u/kg, q4dx3, i.p.), Vinblastine (0.01 mg/kg, q4dx3, i.p.) and Dacarbazine (15 mg/kg, q3dx4, i.p.)] when tumour size averaged approximately 100 mm3.    Click to Show/Hide
In Vivo Model	L540cy cell line xenograft model
In Vitro Model	Hodgkin's disease	L540cy cells		Homo sapiens
Experiment 19 Reporting the Activity Date of This ADC					[123]
Efficacy Data	Tumor Growth Delay (TGD)	> 80 Day	Negative Lewis Y expression (Lewis Y-); Positive CD30 expression (CD30+++/++)
Method Description	SCID mice were implanted with L540cy HL cells in the right flank. Groups of mice (9-10/group) were untreated or received SGN-35 (1 mg/kg, q4dx3, i.p.) and/or ABVD [Adriamycin (0.75 mg/kg, q4dx3, i.v.), Bleomycin (6u/kg, q4dx3, i.p.), Vinblastine (0.01 mg/kg, q4dx3, i.p.) and Dacarbazine (15 mg/kg, q3dx4, i.p.)] when tumour size averaged approximately 100 mm3.    Click to Show/Hide
In Vivo Model	L540cy cell line xenograft model
In Vitro Model	Hodgkin's disease	L540cy cells		Homo sapiens
Experiment 20 Reporting the Activity Date of This ADC					[124]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	2.5 ng/mL
Method Description	The inhibitory activity of cAC10 vcMMAE against cancer cell growth was compared with other anti-CD30 mAbs against the growth of a variety of HD and ALCL cell lines in vitro. For localized, subcutaneous disease models of ALCL and HD,5x106 Karpas 299 or 2x107 L540cy cells, respectively, were implanted into the right flanks of C.B.-17/IcrHsd-SCID mice (Harlan, Indianapolis, IN).Therapy with cAC10-vcMMAE or controls was initiated when the tumor size in each group of 5 animals averaged approximately 100 mm3.Treatment consisted of intravenous injections every fourth day for 4 injections (q4d x 4).    Click to Show/Hide
In Vitro Model	ALK-positive anaplastic large cell lymphoma	Karpas-299 cells		CVCL_1324

Experiment 1 Reporting the Activity Date of This ADC					[126]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.9 pM
Method Description	The inhibitory activity of Brentuximab vedotin against cancer cell growth was evaluated in various human cancer cell lines in vitro.
In Vitro Model	ALK-positive anaplastic large cell lymphoma	Karpas-299 cells		CVCL_1324
Experiment 2 Reporting the Activity Date of This ADC					[126]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	6.7 pM
Method Description	The inhibitory activity of Brentuximab vedotin against cancer cell growth was evaluated in various human cancer cell lines in vitro.
In Vitro Model	Hodgkin lymphoma	L-540 cells		CVCL_1362
Experiment 3 Reporting the Activity Date of This ADC					[126]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	14.2 pM
Method Description	The inhibitory activity of Brentuximab vedotin against cancer cell growth was evaluated in various human cancer cell lines in vitro.
In Vitro Model	Adult acute myeloid leukemia	HL-60 cells		CVCL_0002
Experiment 4 Reporting the Activity Date of This ADC					[126]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	14.5 pM
Method Description	The inhibitory activity of Brentuximab vedotin against cancer cell growth was evaluated in various human cancer cell lines in vitro.
In Vitro Model	Anaplastic large cell lymphoma	SU-DHL-1 cells		CVCL_0538
Experiment 5 Reporting the Activity Date of This ADC					[127]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	4.5 ng/mL
Method Description	The inhibitory activity of the mAb-Val-Cit-MMAE conjugates exhibited greater in vitrospecificity and lower in vivo toxicity was compared with corresponding hydrazone conjugatescorresponding hydrazone conjugates on H3396 cells.The cytotoxic effects of the conjugates on H3396 cells (cBR96 Ag+,cAC10 Ag-) were determined using both pulsed (2 h) and long-term(97 h) drug exposure assays.    Click to Show/Hide
In Vitro Model	ALK-positive anaplastic large cell lymphoma	Karpas-299 cells		CVCL_1324
Experiment 6 Reporting the Activity Date of This ADC					[117]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	6 ng/mL
Method Description	The inhibitory activity of the mAb-Val-Cit-MMAE conjugates exhibited greater in vitrospecificity and lower in vivo toxicity was compared with corresponding hydrazone conjugatescorresponding hydrazone conjugates on H3396 cells.The cytotoxic effects of the conjugates on H3396 cells (cBR96 Ag+,cAC10 Ag-) were determined using both pulsed (2 h) and long-term(97 h) drug exposure assays.    Click to Show/Hide
In Vitro Model	Adult acute myeloid leukemia	CESS cells		CVCL_0209
Experiment 7 Reporting the Activity Date of This ADC					[117]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	63 ng/mL
Method Description	The inhibitory activity of the mAb-Val-Cit-MMAE conjugates exhibited greater in vitrospecificity and lower in vivo toxicity was compared with corresponding hydrazone conjugatescorresponding hydrazone conjugates on H3396 cells.The cytotoxic effects of the conjugates on H3396 cells (cBR96 Ag+,cAC10 Ag-) were determined using both pulsed (2 h) and long-term(97 h) drug exposure assays.    Click to Show/Hide
In Vitro Model	Hodgkin's disease	L540cy cells		Homo sapiens
Experiment 8 Reporting the Activity Date of This ADC					[117]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	90 ng/mL
Method Description	The inhibitory activity of the mAb-Val-Cit-MMAE conjugates exhibited greater in vitrospecificity and lower in vivo toxicity was compared with corresponding hydrazone conjugatescorresponding hydrazone conjugates on H3396 cells.The cytotoxic effects of the conjugates on H3396 cells (cBR96 Ag+,cAC10 Ag-) were determined using both pulsed (2 h) and long-term(97 h) drug exposure assays.    Click to Show/Hide
In Vitro Model	Hodgkin lymphoma	KM-H2 cells		CVCL_1330
Experiment 9 Reporting the Activity Date of This ADC					[129]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	219.5 ng/mL
Method Description	The inhibitory activity of Brentuximab Vedotin against cancer cell growth was evaluated in CD30positive GCT27 cell line in vitro. The cells were treated with 250 ng/mL ADC for 96 hours.
In Vitro Model	Testicular teratoma	GCT 27 cells		CVCL_A344
Experiment 10 Reporting the Activity Date of This ADC					[129]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1013 ng/mL
Method Description	The inhibitory activity of Brentuximab Vedotin against cancer cell growth was evaluated in CD30negative JAR cell line in vitro. The cells were treated with 1000 ng/mL ADC for 96 hours.
In Vitro Model	Gestational choriocarcinoma	JAR cells		CVCL_0360
Experiment 11 Reporting the Activity Date of This ADC					[129]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1400.8 ng/mL
Method Description	The inhibitory activity of Brentuximab Vedotin against cancer cell growth was evaluated in moderate expression NCCIT cell line in vitro. The cells were treated with 500 ng/mL ADC for 96 hours.
In Vitro Model	Testicular embryonal carcinoma	NCC-IT cells		CVCL_1451
Experiment 12 Reporting the Activity Date of This ADC					[130]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	3300.00 1.30 9.90 ng/mL ng/mL ng/mL
Method Description	The antitumor activity of SGN-35 was prepared with 14C-labeled MMAE. Intracellular ADC activation on CD30+ and negative cell lines was determined using a combination of radiometric and liquid chromatograhpy/mass spectrometry-based assays. The bystander activity of SGN-35 was determined using mixed tumor cell cultures consisting of CD30+ and CD30 lines.    Click to Show/Hide
In Vitro Model	ALK-positive anaplastic large cell lymphoma	Karpas-299 cells		CVCL_1324
	Diffuse large B-cell lymphoma	WSU-NHL cells		CVCL_1793
	Hodgkin's disease	L540cy cells		Homo sapiens

Experiment 1 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Partial Response (PR)	40%	Moderate Tissue factor expression (TF++; IHC H-score=155)
Patients Enrolled	Ovary Cancer; Cervix Cancer; Endometrium Cancer; Bladder Cancer; Prostate Cancer; Esophagus Cancer; Lung Cancer, Nonsmall Cell; Squamous Cell Carcinoma of the Head and Neck.
Administration Dosage	Once every 3 weeks intravenous (IV).
Related Clinical Trial
NCT Number	NCT03245736	Phase Status	Phase 2
Clinical Description	A multi-center, open-label trial investigating the efficacy and safety of continued treatment with tisotumab vedotin in patients with solid tumors known to express tissue factor.
Primary Endpoint	Number of participants who experienced a treatment emergent adverse event (TEAE): 5/5 Participants (100%).
Other Endpoint	Partial Response Rate=2/5 (40.00%), Stable Disease Rate=2/5(40.00%), Progressive Disease Rate=1/5 (20.00%), Increased Cancer Antigen (CA 125) Levels Rate=1/2 (50.00%).
Experiment 2 Reporting the Activity Date of This ADC					[37]
Efficacy Data	Objective Response Rate (ORR)	24%	High Tissue factor expression (TF+++; IHC H-score=250)
Patients Enrolled	Recurrent or metastatic squamous cell, adenocarcinoma, or adenosquamous cervical cancer; disease progression on or after doublet chemotherapy with bevacizumab (if eligible by local standards); who had received two or fewer previous systemic regimens for recurrent or metastatic disease; had measurable disease based on Response Evaluation Criteria in Solid Tumors (RECIST; version 11); and had an Eastern Cooperative Oncology Group performance status of 0 or 1.    Click to Show/Hide
Administration Dosage	20 mg/kg (up to a maximum of 200 mg) intravenously once every 3 weeks.
Related Clinical Trial
NCT Number	NCT03438396	Phase Status	Phase 2
Clinical Description	A Single arm, multicenter, international trial of tisotumab vedotin (HuMax-TF-ADC) in previously treated, recurrent or metastatic cervical cancer.
Primary Endpoint	Objective response rate=24.00% (95% CI 16.00%-33.00%), comprising 7 (7.00%) complete responses and 17 (17.00%) partial responses, Disease Control Rate (DCR)=72.00%.
Other Endpoint	Median duration of response=8.30 months, 62.00% (95% CI 3.70-8.00) of patients > 6months,median progression-free survival = 4.20 months (95% Cl 3.00-4.40), median overall survival = 12.10 months (95% Cl, 9.60-13.90).
Experiment 3 Reporting the Activity Date of This ADC					[53]
Efficacy Data	Objective Response Rate (ORR)	38.24%	Low Tissue factor expression (TF+; <7,000 TF molecules/cell)
Patients Enrolled	Recurrent/metastatic cervical cancer (r/mCC).
Administration Dosage	20 mg/kg + pembro 200 mg IV Q3W.
Related Clinical Trial
NCT Number	NCT03786081	Phase Status	Phase 1b/2
Clinical Description	A phase 1b/2 open-label trial of tisotumab vedotin (HuMax-TF-ADC) monotherapy and in combination with other agents in subjects with recurrent or stage IVB cervical cancer.
Primary Endpoint	In the second- or third-line group,objective response rate=38.24% (95% Cl 22.00-56.00), comprising 2 (5.88%) complete responses and 11 (32.35%) partial responses.
Other Endpoint	In the second- or third-line group,median duration of response was 13.80 months, median progression-free survival was 5.60 months.
Experiment 4 Reporting the Activity Date of This ADC					[53]
Efficacy Data	Objective Response Rate (ORR)	54.55%	High Tissue factor expression (TF+++; >300,000 TF molecules/cell)
Patients Enrolled	Recurrent/metastatic cervical cancer (r/mCC).
Administration Dosage	20 mg/kg + carbo AUC 5 IV every 3 weeks (Q3W).
Related Clinical Trial
NCT Number	NCT03786081	Phase Status	Phase 1b/2
Clinical Description	A phase 1b/2 open-label trial of tisotumab vedotin (HuMax-TF-ADC) monotherapy and in combination with other agents in subjects with recurrent or stage IVB cervical cancer.
Primary Endpoint	In the first-line treatment group, objective response rate= 54.55%, comprising 4 (12.12%) complete responses and 14 (42.42%) partial responses.
Other Endpoint	In the first-line treatment group, median duration of response=83 months,median progression-free survival was 95 months.
Experiment 5 Reporting the Activity Date of This ADC					[56]
Efficacy Data	Objective Response Rate (ORR)	15.65 26.67 26.47 7.14 13.33 13.33 13.89 %	Low Tissue factor expression (TF+; <15,000 TF molecules/cell)
Patients Enrolled	Relapsed, advanced, or metastatic cancer of the ovary, cervix, endometrium, bladder, prostate, oesophagus, squamous cell carcinoma of the head and neck or non-small-cell lung cancer; an Eastern Cooperative Oncology Group performance status of 0-1; and had relapsed after or were not eligible to receive the available standard of care.
Administration Dosage	0.3 and 2.2 mg/kg intravenously once every 3 weeks in a traditional 3+3 design.
Related Clinical Trial
NCT Number	NCT02001623	Phase Status	Phase 1/2
Clinical Description	First-in-human, dose-escalating safety study of tissue factor specific antibody drug conjugate tisotumab vedotin (HuMax TF ADC) in patients with locally advanced and/or metastatic solid tumors known to express tissue factor.
Primary Endpoint	OrR of all patients=15.65% (23/147, 95% Cl 10.20-22.00), ORR of Bladder cancer=26.67% (4/15, 95% Cl 7.80-55.10), ORR of Cervical cancer=26.47% (9/34, 95% Cl 12.90-44.40), ORR of Endometrial cancer=7.14% (1/14, 95% Cl 0.20-33.90), ORR of Oesophageal cancer=13.33% (2/15, 95% Cl 1.70-40.50), ORR of NSCLC=13.33% (2/15, 95% Cl 1.70-40.50), ORR of Ovarian cancer=13.89% (5/36, 95% Cl 4.70-29.50).    Click to Show/Hide
Experiment 6 Reporting the Activity Date of This ADC					[57]
Efficacy Data	Objective Response Rate (ORR)	24%	High Tissue factor expression (TF+++; IHC H-score=250)
Patients Enrolled	Cervical cancer.
Administration Dosage	20 mg/kg every 3 weeks.
Related Clinical Trial
NCT Number	NCT02001623	Phase Status	Phase 1/2
Clinical Description	First-in-human, dose-escalating safety study of tissue factor specific antibody drug conjugate tisotumab vedotin (HuMax TF ADC) in patients with locally advanced and/or metastatic solid tumors known to express tissue factor.
Primary Endpoint	Objective response rate=24.00% (95% Cl 13.00%-37.00%).
Other Endpoint	Median duration of response was 4.20 months (range: 1.00-9.70 months), comprising four patients responding for > 8 months Six-month progression-free survival was 29.00% (95% CI 17.00-43.00).
Experiment 7 Reporting the Activity Date of This ADC					[58]
Efficacy Data	Objective Response Rate (ORR)	29.41%	Positive Tissue factor expression (TF+++/++; 380,000 TF receptor copy number)
Patients Enrolled	Recurrent/metastatic cervical cancer (r/mCC).
Administration Dosage	15 or 20 mg/kg once every 3 weeks.
Related Clinical Trial
NCT Number	NCT03913741	Phase Status	Phase 1/2
Clinical Description	Open label phase 1/2 trial of tisotumab vedotin in japanese subjects with advanced solid malignancies.
Primary Endpoint	OrR (CR+PR)=29.41% (95% Cl, 10.30-56.00), Disease Control Rate (DCR)=70.60% (95% Cl 44.00-89.70), CR=0/17 (0%), PR=5/17 (29.41%), SD=7/17 (41.17%), PD=2/17 (11.76%).
Other Endpoint	Median TTR=12 months (range, 11-27 months), median DOR=7.10 months (range, 3.10 months to not reached), median OS=11.4 months (95% Cl 6.2 -not reached) Kaplan-Meier estimates showed that the percentages of patients with an OS 6 months and 12 months were 81.60% (95% CI, 53.00-93.70) and 25.70% (95% CI, 16.00-63.90), respectively.
Experiment 8 Reporting the Activity Date of This ADC					[28]
Related Clinical Trial
NCT Number	NCT04697628	Phase Status	Phase 3
Clinical Description	A randomized, open-label, phase 3 trial of tisotumab vedotin vs investigator's choice chemotherapy in second- or third-line recurrent or metastatic cervical cancer.
Experiment 9 Reporting the Activity Date of This ADC					[28]
Related Clinical Trial
NCT Number	NCT03485209	Phase Status	Phase 2
Clinical Description	Open label phase 2 study of tisotumab vedotin for locally advanced or metastatic disease in solid tumors.
Experiment 10 Reporting the Activity Date of This ADC					[28]
Related Clinical Trial
NCT Number	NCT03657043	Phase Status	Phase 2
Clinical Description	Open label phase 2 study of tisotumab vedotin for patients with platinum-resistant ovarian cancer with a safety run-in of a dose-dense regimen.
Experiment 11 Reporting the Activity Date of This ADC					[28]
Related Clinical Trial
NCT Number	NCT02552121	Phase Status	Phase 1/2
Clinical Description	Dose-escalating and cohort expansion safety trial of tissue factor specific antibody drug conjugate tisotumab vedotin (HuMax-TF-ADC) in patients with locally advanced and/or metastatic solid tumors known to express tissue factor.

Experiment 1 Reporting the Activity Date of This ADC					[117]
Efficacy Data	Tumor Growth Inhibition value (TGI)	72%	High Tissue factor expression (TF+++; >300,000 TF molecules/cell)
Method Description	TF-positive patient-derived xenograft (PDX) models were performed in athymic nude mice to evaluate the efficacy of the ADCs in vivo. Study animals were implanted unilaterally on the left flank with tumor fragments. Animals were randomized and treated as indicated in the figures. Animals were removed from study and euthanized once tumor size reached 1,200 mm3 or skin ulceration was evident. In addition, the MTV curve for the treatment group in question was no longer shown once an animal was removed from study due to size TGI and statistical analyses were conducted in the same manner as for the CDX studies. The CR and PR response definitions were as follows for the PDX studies: a PR responder had a MTV 30% of MTV at day 1 for two consecutive measurements; a CR responder had an undetectable MTV for two consecutive measurement IHC analisys: Formalin-fixed paraffin-embedded (FFPE) tissues were sectioned at 4-m thickness and mounted onto positive-charged glass slides The tissue sections were stained with the anti-TF antibody HTF-1 ADC treatment started on day 1 after animals with a tumor size of approximately 190 mm3 The model dosed weekly at 25 mg/kg for 3 weeks.    Click to Show/Hide
In Vivo Model	Patient-derived xenograft (PDX) ovarian carcinomamodel
Experiment 2 Reporting the Activity Date of This ADC					[117]
Efficacy Data	Tumor Growth Inhibition value (TGI)	100%	Positive Tissue factor expression (TF+++/++; 570,000 TF receptor copy number)
Method Description	TF-positive patient-derived xenograft (PDX) models were performed in athymic nude mice to evaluate the efficacy of the ADCs in vivo. Study animals were implanted unilaterally on the left flank with tumor fragments. Animals were randomized and treated as indicated in the figures. Animals were removed from study and euthanized once tumor size reached 1,200 mm3 or skin ulceration was evident. In addition, the MTV curve for the treatment group in question was no longer shown once an animal was removed from study due to size TGI and statistical analyses were conducted in the same manner as for the CDX studies. The CR and PR response definitions were as follows for the PDX studies: a PR responder had a MTV 30% of MTV at day 1 for two consecutive measurements; a CR responder had an undetectable MTV for two consecutive measurement IHC analisys: Formalin-fixed paraffin-embedded (FFPE) tissues were sectioned at 4-m thickness and mounted onto positive-charged glass slides The tissue sections were stained with the anti-TF antibody HTF-1 ADC treatment started on day 1 after animals with a tumor size of approximately 140 mm3 The model dosed weekly at 4 mg/kg for 3 weeks.    Click to Show/Hide
In Vivo Model	Patient-derived gastric adenocarcinoma xenograft (PDX) model
Experiment 3 Reporting the Activity Date of This ADC					[117]
Efficacy Data	Tumor Growth Inhibition value (TGI)	100%	Low Tissue factor expression (TF+; <15,000 TF molecules/cell)
Method Description	TF-positive patient-derived xenograft (PDX) models were performed in athymic nude mice to evaluate the efficacy of the ADCs in vivo. Study animals were implanted unilaterally on the left flank with tumor fragments. Animals were randomized and treated as indicated in the figures. Animals were removed from study and euthanized once tumor size reached 1,200 mm3 or skin ulceration was evident. In addition, the MTV curve for the treatment group in question was no longer shown once an animal was removed from study due to size TGI and statistical analyses were conducted in the same manner as for the CDX studies. The CR and PR response definitions were as follows for the PDX studies: a PR responder had a MTV 30% of MTV at day 1 for two consecutive measurements; a CR responder had an undetectable MTV for two consecutive measurement IHC analisys: Formalin-fixed paraffin-embedded (FFPE) tissues were sectioned at 4-m thickness and mounted onto positive-charged glass slides The tissue sections were stained with the anti-TF antibody HTF-1 ADC treatment started on day 1 after animals with a tumor size of approximately 210 mm3 The model dosed weekly at 5 mg/kg for 2 weeks.    Click to Show/Hide
In Vivo Model	Patient-derived head and neck carcinoma xenograft (PDX) model

Experiment 1 Reporting the Activity Date of This ADC					[117]
Efficacy Data	Tumor Growth Inhibition value (TGI)	71.40%	High Tissue factor expression (TF+++; >300,000 TF molecules/cell)
Method Description	Cell line-derived xenograft models were established in female SCID mice by subcutaneous injection of 5x106 (A431) tumor cells, and treatment with 3 mg/kg TF-ADCs (four injections in 2 weeks) was initiated at day 11 after tumor inoculationDetermined tumor volume after the experiment.
In Vivo Model	A431 cell line xenograft model
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037
Experiment 2 Reporting the Activity Date of This ADC					[117]
Efficacy Data	Tumor Growth Inhibition value (TGI)	76.60%	Low FOLR1 expression (FOLR1+)
Method Description	Cell line-derived xenograft models were established in female SCID mice by subcutaneous injection of 05x106 (HCT-116) tumor cells, and treatment with 3 mg/kg TF-ADCs (four injections in 2 weeks) was initiated at day 7 after tumor inoculationDetermined tumor volume after the experiment.
In Vivo Model	HCT-116 cell line xenograft model
In Vitro Model	Colon carcinoma	HCT 116 cells		CVCL_0291
Experiment 3 Reporting the Activity Date of This ADC					[117]
Efficacy Data	Tumor Growth Inhibition value (TGI)	100%	Low FOLR1 expression (FOLR1+)
Method Description	Cell line-derived xenograft models were established in female SCID mice by subcutaneous injection of 2-10 x106 (HPAF-II) tumor cells, and treatment with 3 mg/kg TF-ADCs (four injections in 2 weeks) was initiated at day 13 after tumor inoculationDetermined tumor volume after the experiment.
In Vivo Model	HPAF-II cell line xenograft model
In Vitro Model	Pancreatic ductal adenocarcinoma	HPAF-II cells		CVCL_0313
Experiment 4 Reporting the Activity Date of This ADC					[122]
Efficacy Data	Tumor Growth Inhibition value (TGI)	100%	Low FOLR1 expression (FOLR1+)
Method Description	Cell line-derived xenograft (CDX) models The A431 epidermoid carcinoma and the HPAF-II pancreatic carcinoma cell lines were implanted subcutaneously in the flank of athymic nude mice Animals were removed from study and euthanized once tumor size reached 1200 mm3 or skin ulceration was evident ADC was dosed weekly at 5 mg/kg for 3 weeks.
In Vivo Model	HPAF-II xenograft model
In Vitro Model	Pancreatic ductal adenocarcinoma	HPAF-II cells		CVCL_0313

Experiment 1 Reporting the Activity Date of This ADC					[122]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	5 nM
Method Description	To evaluate ADC cytotoxicity, cells were plated in 384-well plates Anti-TF antibodies conjugated to MC-vc-PAB-MMAE were serially diluted as shown Plates were incubated for 3 days, followed by lysis in CTG assay reagent For each ADC, the IC50 and its associated 95% confidence interval (95% CI) were calculated Titrations of the TF-specific ADCs were added to A431 cells, with a 72-hour incubationThis treatment resulted in efficacious cell killing.    Click to Show/Hide
In Vitro Model	Erythroleukemia	HEL 92.1.7 cells (Multidrug resistance)		CVCL_2481
Experiment 2 Reporting the Activity Date of This ADC					[131]
Efficacy Data	Half Maximal Effective Concentration (EC50)	14 nM
Method Description	A431 cells were pre-incubated for 30 min without or with 50 nM of FVIIa prior to the addition of an anti-TF ADC (Tisotumab Vedotin-tftv) titration After a 4 h incubation at 37°C, the FVIIa and ADC were washed out and the cells were cultured for another 68 h before cell viability assessment.
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037
Experiment 3 Reporting the Activity Date of This ADC					[131]
Efficacy Data	Half Maximal Effective Concentration (EC50)	14 nM
Method Description	To evaluate ADC cytotoxicity, cells were plated in 384-well plates Anti-TF antibodies conjugated to MC-vc-PAB-MMAE were serially diluted as shown Plates were incubated for 3 days, followed by lysis in CTG assay reagent For each ADC, the IC50 and its associated 95% confidence interval (95% CI) were calculated Titrations of the TF-specific ADCs were added to A431 cells, with a 4-hour incubation followed by removal of excess ADC and culture for another 68 hours This treatment resulted in efficacious cell killing.    Click to Show/Hide
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037
Experiment 4 Reporting the Activity Date of This ADC					[131]
Efficacy Data	Half Maximal Effective Concentration (EC50)	14 nM
Method Description	Cytotoxicity assay in vitroCells were seeded in 96-well plates (2,500-5,000 cells/well) and incubated for 6 hours (37°C), before adding ADCs After 3 to 5 days (37°C), the viability of the culture was assessed Staurosporine ( 10 ug/mL) was used a positive control (100% cell death) and untreated cells were used as a negative control.
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037
Experiment 5 Reporting the Activity Date of This ADC					[117]
Efficacy Data	Half Maximal Effective Concentration (EC50)	411 ng/mL
Method Description	Cytotoxicity assay in vitroCells were seeded in 96-well plates (2,500-5,000 cells/well) and incubated for 6 hours (37°C), before adding ADCs After 3 to 5 days (37°C), the viability of the culture was assessed Staurosporine ( 10 ug/mL) was used a positive control (100% cell death) and untreated cells were used as a negative control.
In Vitro Model	Pancreatic ductal adenocarcinoma	HPAF-II cells		CVCL_0313
Experiment 6 Reporting the Activity Date of This ADC					[117]
Efficacy Data	Half Maximal Effective Concentration (EC50)	> 10 ug/mL
Method Description	Cytotoxicity assay in vitroCells were seeded in 96-well plates (2,500-5,000 cells/well) and incubated for 6 hours (37°C), before adding ADCs After 3 to 5 days (37°C), the viability of the culture was assessed Staurosporine ( 10 ug/mL) was used a positive control (100% cell death) and untreated cells were used as a negative control.
In Vitro Model	Colon carcinoma	HCT 116 cells		CVCL_0291
Experiment 7 Reporting the Activity Date of This ADC					[117]
Efficacy Data	Half Maximal Effective Concentration (EC50)	> 10 mg/mL
Method Description	Cytotoxicity assay in vitroCells were seeded in 96-well plates (2,500-5,000 cells/well) and incubated for 6 hours (37°C), before adding ADCs After 3 to 5 days (37°C), the viability of the culture was assessed Staurosporine ( 10 ug/mL) was used a positive control (100% cell death) and untreated cells were used as a negative control.
In Vitro Model	Ovarian clear cell adenocarcinoma	TOV-21G cells		CVCL_3613

Experiment 1 Reporting the Activity Date of This ADC					[29]
Efficacy Data	Objective Response Rate (ORR)	24.80%	High HER2 expression (HER2+++; IHC 3+)
Patients Enrolled	Locally advanced or metastatic gastric cancer with HER2-overexpression.
Administration Dosage	2.50 mg/kg IV every 2 weeks.
Related Clinical Trial
NCT Number	NCT04714190	Phase Status	Phase 3
Clinical Description	Randomized, controlled, multicenter phase 1/2 clinical study evaluating the efficacy and safety of RC48-ADC for the treatment of locally advanced or metastatic gastric cancer with HER2-overexpression.
Primary Endpoint	The ORR was 24.80% (95% confidence interval [CI]: 17.50%-33.30%).
Other Endpoint	The median PFS and OS were 4.10 months (95% CI: 3.70-4.90 months) and 7.90 months (95% CI: 6.70-9.90 months), respectively. The most frequently reported adverse events were decreased white blood cell count (53.60%), asthenia (53.60%), hair loss (53.60%), decreased neutrophil count (52.00%), anemia (49.60%), and increased aspartate aminotransferase level (43.20%). Serious adverse events (SAEs) occurred in 45 (36.00%) patients, and RC48-related SAEs were mainly decreased neutrophil count (3.20%). Seven patients had adverse events that led to death were not RC48-related.    Click to Show/Hide
Experiment 2 Reporting the Activity Date of This ADC					[29]
Efficacy Data	Objective Response Rate (ORR)	24.80%	High HER2 expression (HER2+++; IHC 3+)
Patients Enrolled	HER2overexpressing (IHC 2+ or 3+), locally advanced or metastatic gastric or gastroesophageal junction cancer who were under at least secondline therapy.
Administration Dosage	2.50 mg/kg alone by intravenous infusion during 30-90 min (60 min is recommended) every two weeks.
Related Clinical Trial
NCT Number	NCT03556345	Phase Status	Phase 2
Clinical Description	A multicenter, open label single arm, phase 2 study to evaluate the effect and safety of recombinant humanized anti-HER2 monoclonal antibody-mmae conjugate for injection in HER2 overexpressing local advanced or metastatic gastric cancer.
Primary Endpoint	The ORR was 24.80% (95% confidence interval [CI]: 17.50%-33.30%).
Experiment 3 Reporting the Activity Date of This ADC					[62]
Efficacy Data	Objective Response Rate (ORR)	21.05 35.71 20.00 13.64 15.00 %
Patients Enrolled	Patients with incurable, locally advanced or metastatic solid cancers were eligible for inclusion if their tumors showed HER2 protein overexpression by IHC (3+or 2+), regardless of whether FISH was positive or negative.
Administration Dosage	0.10 mg/kg, 0.50 mg/kg, 1.00 mg/kg, 1.50 mg/kg, 2.00 mg/kg, 2.50 mg/kg, 3.00 mg/kg, 3.50 mg/kg, and 4.00 mg/kg; Q3W; dose expansion proceeded at the dose of 2.00 mg/kg Q2W.
Related Clinical Trial
NCT Number	NCT02881190	Phase Status	Phase 1
Clinical Description	A tolerance, safety and pharmacokinetic ascending dose phase 1 study of RC48-ADC administered intravenously to subjects with HER2-positive malignant in advanced malignant solid tumors.
Primary Endpoint	The MTD was unavailable due to termination of 3.0 mg/kg cohort; 2.5 mg/kg Q2W was declared the RP2D.
Other Endpoint	ORR and DCR were 21.05% (12/57) and 49.12% (28/57). Notably, patients who were HER2 IHC2+/FISH- responded similarly to those who were IHC2+/FISH+and IHC3+, with ORRs of 35.71% (5/14), 20.00% (2/10), and 13.64% (3/22), respectively. In patients who were pretreated with HER2-targeted drugs, RC48 also showed promising efcacy, with ORR of 15.00% (3/20) and DCR of 45.00% (9/20).    Click to Show/Hide
Experiment 4 Reporting the Activity Date of This ADC					[70]
Efficacy Data	Objective Response Rate (ORR)	51.20%
Patients Enrolled	Advanced or metastatic urothelial cancer.
Related Clinical Trial
NCT Number	NCT04264936	Phase Status	Phase 1
Clinical Description	A open-label, single-arm, phase 1b/2 study of RC48-ADC and JS001 to evaluate the safety and pharmacokinetics of subjects with locally advanced or metastatic urothelial cancer.
Primary Endpoint	The overall confirmed ORR as assessed by the BIRC was 51.20% (95% CI: 35.50%, 66.70%).
Other Endpoint	For RC48-ADC at 2.00 mg/kg, The median PFS and OS were 6.90 months (95% CI: 5.60, 8.90) and 13.90 months (95% CI: 9.10, NE), respectively.
Experiment 5 Reporting the Activity Date of This ADC					[74]
Efficacy Data	Objective Response Rate (ORR)	80.00 75.00 100.00 77.80 66.70 50.00 97.10 50.00 %
Patients Enrolled	HER2-positive and even negative patients (pts) with metastatic urothelial carcinoma (mUC).
Administration Dosage	1.50 or 2.00 mg/kg RC48-ADC + 3 mg/kg toripalimab with the traditional 3+3 escalation design. In the expansion cohort, patients received the recommended dose of RC48-ADC + toripalimab every 2 weeks. The primary endpoints were safety/tolerability and recommended RC48-ADC dose.
Related Clinical Trial
NCT Number	NCT04264936	Phase Status	Phase 1
Clinical Description	A open-label, single-arm, phase 1b/2 study of RC48-ADC and JS001 to evaluate the safety and pharmacokinetics of subjects with locally advanced or metastatic urothelial cancer.
Primary Endpoint	At data cutoff, confirmed investigator-assessed ORR=75.00% (95%CI: 50.90-91.30), including 15.00% CRs; DCR=95.00% (95%CI: 75.10-99.90).
Other Endpoint	The ORR for 1L previously untreated mUC pts was 80.00%. The ORR for pts with liver mets was 75.00%. The ORR was 100.00% for pts with HER2 (3+), 77.80% for HER2 (2+), 66.70% for HER2 (1+), and 50.00% for HER2 (0) respectively. The ORR was 97.10% in pts with PD-L1 CPS1 and 50.00% in CPS < 1.

Experiment 1 Reporting the Activity Date of This ADC					[116]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 61.20%	Moderate HER2 expression (HER2++)
Method Description	The inhibitory activity of RC48 against cancer cell growth was evaluated in various human cancer cell lines in vitro. The cells were treated with RC48 for 22 days.
In Vivo Model	Gastric cancer PDX model (PDX: Model6)
Experiment 2 Reporting the Activity Date of This ADC					[116]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 64.50%	High HER2 expression (HER2+++)
Method Description	The inhibitory activity of RC48 against cancer cell growth was evaluated in various human cancer cell lines in vitro. The cells were treated with RC48 for 22 days.
In Vivo Model	Gastric cancer PDX model (PDX: Model8)
Experiment 3 Reporting the Activity Date of This ADC					[116]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 70.80%	High HER2 expression (HER2+++)
Method Description	The inhibitory activity of RC48 against cancer cell growth was evaluated in various human cancer cell lines in vitro. The cells were treated with RC48 for 22 days.
In Vivo Model	Gastric cancer PDX model (PDX: Model9)
Experiment 4 Reporting the Activity Date of This ADC					[116]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 81.80%	High HER2 expression (HER2+++)
Method Description	The inhibitory activity of RC48 against cancer cell growth was evaluated in various human cancer cell lines in vitro. The cells were treated with RC48 for 22 days.
In Vivo Model	Gastric cancer PDX model (PDX: Model3)
Experiment 5 Reporting the Activity Date of This ADC					[116]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 89.60%	High HER2 expression (HER2+++)
Method Description	The inhibitory activity of RC48 against cancer cell growth was evaluated in various human cancer cell lines in vitro. The cells were treated with RC48 for 22 days.
In Vivo Model	Gastric cancer PDX model (PDX: Model5)
Experiment 6 Reporting the Activity Date of This ADC					[116]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 94%	High HER2 expression (HER2+++; IHC 3+)
Method Description	The inhibitory activity of RC48 against cancer cell growth was evaluated in various human cancer cell lines in vitro. The cells were treated with RC48 for 22 days.
In Vivo Model	Gastric cancer PDX model (PDX: Model7)
Experiment 7 Reporting the Activity Date of This ADC					[116]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100%	Moderate HER2 expression (HER2++)
Method Description	The inhibitory activity of RC48 against cancer cell growth was evaluated in various human cancer cell lines in vitro. The cells were treated with RC48 for 22 days.
In Vivo Model	Gastric cancer PDX model (PDX: Model4)
Experiment 8 Reporting the Activity Date of This ADC					[116]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100%	High HER2 expression (HER2+++)
Method Description	The inhibitory activity of RC48 against cancer cell growth was evaluated in various human cancer cell lines in vitro. The cells were treated with RC48 for 22 days.
In Vivo Model	Gastric cancer PDX model (PDX: Model2)
Experiment 9 Reporting the Activity Date of This ADC					[116]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100%	High HER2 expression (HER2+++)
Method Description	The inhibitory activity of RC48 against cancer cell growth was evaluated in various human cancer cell lines in vitro. The cells were treated with RC48 for 22 days.
In Vivo Model	Gastric cancer PDX model (PDX: Model1)

Experiment 1 Reporting the Activity Date of This ADC					[125]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	90 ng/mL	Low HER2 expression (HER2+; IHC 1+)
Method Description	The inhibitory activity of RC48 against cancer cell growth was evaluated in various human cancer cell lines in vitro. The cells were treated with PBS, ADC (5 mg/kg), PD-1 antibody (10 mg/kg), or their combination (ADC+PD-1 antibody or ADC+PD-L1 antibody) for 10 days.
In Vivo Model	Triple-negative breast cancer cell line E0771-hHER2 xenograft model
In Vitro Model	Mammary gland malignant neoplasms	EO771 cells		CVCL_GR23
Experiment 2 Reporting the Activity Date of This ADC					[116]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.8 ug/mL	High HER2 expression (HER2+++)
Method Description	The inhibitory activity of RC48 against cancer cell growth was evaluated in various human cancer cell lines in vitro. The cells were treated with RC48 for 72 h.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[116]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.3 ug/mL	High HER2 expression (HER2+++; IHC 3+)
Method Description	The inhibitory activity of RC48 against cancer cell growth was evaluated in various human cancer cell lines in vitro. The cells were treated with RC48 for 72 h.
In Vitro Model	Gastric tubular adenocarcinoma	SNU-216 cells		CVCL_3946
Experiment 4 Reporting the Activity Date of This ADC					[116]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	3.8 ug/mL	Moderate HER2 expression (HER2++; IHC 2+)
Method Description	The inhibitory activity of RC48 against cancer cell growth was evaluated in various human cancer cell lines in vitro. The cells were treated with RC48 for 72 h.
In Vitro Model	Gastric signet ring cell adenocarcinoma	NUGC-4 cells		CVCL_3082
Experiment 5 Reporting the Activity Date of This ADC					[116]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	52.4 ug/mL	Moderate HER2 expression (HER2++; IHC 2+)
Method Description	The inhibitory activity of RC48 against cancer cell growth was evaluated in various human cancer cell lines in vitro. The cells were treated with RC48 for 72 h.
In Vitro Model	Gastric carcinoma	HGC-27 cells		CVCL_1279

Experiment 1 Reporting the Activity Date of This ADC					[128]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	4.91 ng/mL	High HER2 expression (HER2+++)
Method Description	To test the anti-tumor effect of single drug, SK-BR-3, NCI-N87 and SK-OV-3 cells were selected for viability analysis following 72 h incubation with or without RC48ADC which was dispersed in a concentration gradient.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[128]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	11.28 ng/mL	High HER2 expression (HER2+++)
Method Description	To test the anti-tumor effect of single drug, SK-BR-3, NCI-N87 and SK-OV-3 cells were selected for viability analysis following 72 h incubation with or without RC48ADC which was dispersed in a concentration gradient.
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 3 Reporting the Activity Date of This ADC					[128]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	14.54 ng/mL	High HER2 expression (HER2+++)
Method Description	To test the anti-tumor effect of single drug, SK-BR-3, NCI-N87 and SK-OV-3 cells were selected for viability analysis following 72 h incubation with or without RC48ADC which was dispersed in a concentration gradient.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[33]
Efficacy Data	Objective Response Rate (ORR)	73.30%
Patients Enrolled	Histologically documented locally advanced/metastatic urothelial carcinoma (la/mUC) (including squamous differentiation and mixed cell types), an Eastern Cooperative Oncology Group performance status score of 0 or 1 (on a 5-point scale; higher scores indicate greater disability), and an investigator-assessed life expectancy of 3 or more months.
Administration Dosage	1.25 mg/kg once daily on days 1 and 8 intravenously once daily in 3-week cycles.
Related Clinical Trial
NCT Number	NCT04223856	Phase Status	Phase 3
Clinical Description	An open-label, randomized, controlled phase 3 study of enfortumab vedotin in combination with pembrolizumab versus chemotherapy alone in previously untreated locally advanced or metastatic urothelial cancer.
Primary Endpoint	Safety: Seven patients (15.60%) experienced a serious TRAE, with no serious TRAE occurring more than once. TRAEs led to dose reductions in 14 (31.10%) patients and discontinuations in 11 (24.40%) patients and were not mutually exclusive. Peripheral sensory neuropathy was the most common TRAE leading to either dose reduction (six patients, 13.30%) or treatment discontinuation (four patients, 8.90%). No patients discontinued therapy because of a skin reaction or hyperglycemia. One patient (2.20%) died because of a TRAE (multiple organ dysfunction syndrome).    Click to Show/Hide
Other Endpoint	The confirmed objective response rate after a median of nine cycles was 73.30% with a complete response rate of 15.60%. The median DOR and median OS were 25.60 months and 26.10 months, respectively.
Experiment 2 Reporting the Activity Date of This ADC					[40]
Efficacy Data	Objective Response Rate (ORR)	44%	High Nectin-4 expression (NECTIN4+++)
Patients Enrolled	Locally advanced or metastatic urothelial carcinoma who were previously treated with platinum chemotherapy and antiPD-1/L1 therapy.
Administration Dosage	1.25 mg/kg (intravenously on days 1, 8, and 15 of every 28-day cycle).
Related Clinical Trial
NCT Number	NCT03219333	Phase Status	Phase 2
Clinical Description	A single-arm, open-label, multicenter study of enfortumab vedotin (ASG-22CE) for Treatment of patients with locally advanced or metastatic urothelial cancer who previously received immune checkpoint inhibitor (CPI) Therapy.
Primary Endpoint	Confirmed objective response rate was 44.00% (95% CI, 35.10% to 53.20%), including 12.00% complete responses.
Other Endpoint	Median duration of response was 7.60 months (range, 0.95 to 11.30 months).
Experiment 3 Reporting the Activity Date of This ADC					[42]
Efficacy Data	Objective Response Rate (ORR)	51.68%	High Nectin-4 expression (NECTIN4+++)
Patients Enrolled	Locally advanced or metastatic urothelial carcinoma previously treated with PD-1 or PD-L1 inhibitors; an Eastern Cooperative Oncology Group performance status score of 2 or less who were considered ineligible for cisplatin at enrolment and who had not received platinum-containing chemotherapy in the locally advanced or metastatic setting.
Administration Dosage	Intravenously at a dose of 1.25 mg/kg on days 1, 8, and 15 of every 28-day cycle.
Related Clinical Trial
NCT Number	NCT03219333	Phase Status	Phase 2
Clinical Description	A single-arm, open-label, multicenter study of enfortumab vedotin (ASG-22CE) for treatment of patients with locally advanced or metastatic urothelial cancer who previously received immune checkpoint inhibitor (CPI) therapy.
Primary Endpoint	The confirmed objective response rate was 51.68% (46 of 89 patients; 95% CI 41.00-62.00), with 18 (20.22%) of 89 patients achieving a complete response and 28 (31.46%) achieving a partial response.
Other Endpoint	Duration of response, progression-free survival, objective response rate, overall survival, safety, and tolerability, plasma or serum pharmacokinetic parameters of enfortumab vedotin, MMAE, and total antibody, and incidence of antitherapeutic antibody to enfortumab vedotin.
Experiment 4 Reporting the Activity Date of This ADC					[65]
Efficacy Data	Objective Response Rate (ORR)	35.30%	Moderate Nectin-4 expression (NECTIN4++)
Patients Enrolled	Histologically confirmed, locally advanced or metastatic transitional cell carcinoma of the urothelium (ie, cancer of the bladder, renal pelvis, ureter, or urethra), or UC with squamous differentiation or mixed cell types and an Eastern Cooperative Oncology Group (ECOG) performance status of 0 or 1.
Administration Dosage	1.00 mg/kg (Arm A) or 1.25 mg/kg (Arm B) on Days 1, 8, and 15 of each 28-day cycle.
Related Clinical Trial
NCT Number	NCT03070990	Phase Status	Phase 1
Clinical Description	An open-label, randomized, phase 1 safety and pharmacokinetic study of enfortumab vedotin (ASG-22CE) in Japanese patients with locally advanced or metastatic urothelial carcinoma.
Primary Endpoint	Safety/tolerability of EV, EV PK profile.
Experiment 5 Reporting the Activity Date of This ADC					[68]
Efficacy Data	Objective Response Rate (ORR)	43%	High Nectin-4 expression (NECTIN4+++)
Patients Enrolled	Nectin-4positive solid tumors, including mUC, who progressed on 1 prior chemotherapy regimen or who were ineligible for cisplatin chemotherapy.
Administration Dosage	Weight-based doses (0.50, 0.75, 1.00, and 1.25 mg/kg) through 30-minute infusion on days 1, 8, and 15 of a 28-day cycle.
Related Clinical Trial
NCT Number	NCT02091999	Phase Status	Phase 1
Clinical Description	A phase 1 study of the safety and pharmacokinetics of escalating doses of ASG-22CE given as monotherapy in subjects with metastatic urothelial cancer and other malignant solid tumors that express nectin-4.
Primary Endpoint	The determination of safety/tolerability, recommended phase II dose (RP2D), and pharmacokinetic (PK) profile of EV.
Other Endpoint	Antitumor activity,including confirmed investigator-assessed ORR (RECIST version 1.1), duration of response (DoR), progression-free survival (PFS), and overall survival (OS).
Experiment 6 Reporting the Activity Date of This ADC					[102]
Patients Enrolled	Histologically or cytologically confirmed urothelial carcinoma (including differentiation in squamous cells or in multiple cell types), radiologically documented metastatic or unresectable locally advanced disease at baseline, and an Eastern Cooperative Oncology Group (ECOG) performance-status score of 0 or 1 (scores range from 0 to 4, with higher scores indicating greater disability).    Click to Show/Hide
Administration Dosage	Intravenous infusion over 30 minutes on days 1, 8, and 15 of a 28-day cycle.
Related Clinical Trial
NCT Number	NCT03474107	Phase Status	Phase 3
Clinical Description	An open-label, randomized phase 3 study to evaluate enfortumab vedotin vs chemotherapy in subjects with previously treated locally advanced or metastatic urothelial cancer (EV-301).
Primary Endpoint	Overall survival was prolonged with enfortumab vedotin compared with chemotherapy (HR=0.70 [95% CI: 0.56-0.89];.
Other Endpoint	Median overall survival: 12.88 vs 8.97 months, respectively). Progression-free survival was also longer in the enfortumab vedotin group compared with the chemotherapy group (HR=0.62 [95% CI: 0.51-0.75]; P<0.00001; median progression-free survival: 5.55 vs 3.71 months, respectively).

Experiment 1 Reporting the Activity Date of This ADC					[115]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 30.80%	High Nectin-4 expression (NECTIN4+++)
Method Description	AGS-22M6E induces efficient tumor cell killing in PDX models of a bladder cancer cell with Nectin-4 high expression, dosed every 4 days at 0.4 mg/kg for 5 times.
In Vivo Model	Bladder cancer PDX model (PDX: AG-B1)
Experiment 2 Reporting the Activity Date of This ADC					[115]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 33.90%	Moderate Nectin-4 expression (NECTIN4++)
Method Description	AGS-22M6E induces efficient tumor cell killing in PDX models of a pancreatic cancer cell with Nectin-4 moderate expression, dosed every 4 days at 1 mg/kg for 6 times.
In Vivo Model	Pancreatic cancer PDX model (PDX: AG-Panc4)
Experiment 3 Reporting the Activity Date of This ADC					[115]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 45%	High Nectin-4 expression (NECTIN4+++)
Method Description	AGS-22M6E induces efficient tumor cell killing in PDX models of a breast cancer cell with Nectin-4 high expression, dosed every 4 days at 1 mg/kg for 6 times.
In Vivo Model	Breast cancer PDX model (PDX: AG-Br7)
Experiment 4 Reporting the Activity Date of This ADC					[115]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 68.80%	Moderate Nectin-4 expression (NECTIN4++)
Method Description	AGS-22M6E induces efficient tumor cell killing in PDX models of a pancreatic cancer cell with Nectin-4 moderate expression, dosed every 4 days at 3 mg/kg for 6 times.
In Vivo Model	Pancreatic cancer PDX model (PDX: AG-Panc4)
Experiment 5 Reporting the Activity Date of This ADC					[115]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 80.70%	High Nectin-4 expression (NECTIN4+++)
Method Description	AGS-22M6E induces efficient tumor cell killing in PDX models of a bladder cancer cell with Nectin-4 high expression, dosed every 4 days at 0.8 mg/kg for 5 times.
In Vivo Model	Bladder cancer PDX model (PDX: AG-B1)
Experiment 6 Reporting the Activity Date of This ADC					[115]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 93.80%	High Nectin-4 expression (NECTIN4+++)
Method Description	AGS-22M6E induces efficient tumor cell killing in PDX models of a breast cancer cell with Nectin-4 high expression, dosed every 4 days at 3 mg/kg for 6 times.
In Vivo Model	Breast cancer PDX model (PDX: AG-Br7)
Experiment 7 Reporting the Activity Date of This ADC					[115]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 97.60%	High Nectin-4 expression (NECTIN4+++)
Method Description	AGS-22M6E induces efficient tumor cell killing in orthotopic PDX models of a breast cancer cell with Nectin-4 high expression, established in mammary fat pads of SCID mice, dosed single 10 mg/kg.
In Vivo Model	Breast cancer orthotopic PDX model (PDX: AG-Br7)
Experiment 8 Reporting the Activity Date of This ADC					[115]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 97.70%	High Nectin-4 expression (NECTIN4+++)
Method Description	AGS-22M6E induces efficient tumor cell killing in orthotopic PDX models of a breast cancer cell with Nectin-4 high expression, established in mammary fat pads of SCID mice, dosed twice 5 mg/kg.
In Vivo Model	Breast cancer orthotopic PDX model (PDX: AG-Br7)
Experiment 9 Reporting the Activity Date of This ADC					[115]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 98.70%	High Nectin-4 expression (NECTIN4+++)
Method Description	AGS-22M6E induces efficient tumor cell killing in PDX models of a bladder cancer cell with Nectin-4 high expression, single 4 mg/kg dose.
In Vivo Model	Bladder cancer PDX model (PDX: AG-B1)

Experiment 1 Reporting the Activity Date of This ADC					[115]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 26%	High Nectin-4 expression (NECTIN4+++)
Method Description	AGS-22M6E induces efficient tumor cell killing in PDX models of a lung adenocarcinoma cell with Nectin-4 high expression, dosed every 4 days at 1 mg/kg for 5 times.
In Vivo Model	NCI-H322M CDX model
In Vitro Model	Minimally invasive lung adenocarcinoma	NCI-H322M cells		CVCL_1557
Experiment 2 Reporting the Activity Date of This ADC					[115]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 83.60%	High Nectin-4 expression (NECTIN4+++)
Method Description	AGS-22M6E induces efficient tumor cell killing in PDX models of a lung adenocarcinoma cell with Nectin-4 high expression, dosed every 4 days at 3 mg/kg for 5 times.
In Vivo Model	NCI-H322M CDX model
In Vitro Model	Minimally invasive lung adenocarcinoma	NCI-H322M cells		CVCL_1557

Experiment 1 Reporting the Activity Date of This ADC					[115]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.2 ng/mL
Method Description	The inhibitory activity of AGS-22M6, AGS-22M6E ADC, and an isotype control ADC were added to various cancer cell lines in vitro and cell viability was measured after 5 days.
In Vitro Model	Prostate carcinoma	PC-3 cells		CVCL_0035
Experiment 2 Reporting the Activity Date of This ADC					[115]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	3.4 ng/mL
Method Description	The inhibitory activity of AGS-22M6, AGS-22M6E ADC, and an isotype control ADC were added to various cancer cell lines in vitro and cell viability was measured after 5 days.
In Vitro Model	Prostate carcinoma	PC-3 cells		CVCL_0035
Experiment 3 Reporting the Activity Date of This ADC					[115]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	4.7 ng/mL
Method Description	The inhibitory activity of AGS-22M6, AGS-22M6E ADC, and an isotype control ADC were added to various cancer cell lines in vitro and cell viability was measured after 5 days.
In Vitro Model	Prostate carcinoma	PC-3 cells		CVCL_0035
Experiment 4 Reporting the Activity Date of This ADC					[115]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	37.8 ng/mL
Method Description	The inhibitory activity of AGS-22M6, AGS-22M6E ADC, and an isotype control ADC were added to various cancer cell lines in vitro and cell viability was measured after 5 days.
In Vitro Model	Invasive breast carcinoma	T-47D cells		CVCL_0553

Experiment 1 Reporting the Activity Date of This ADC					[44]
Efficacy Data	Objective Response Rate (ORR)	54%
Patients Enrolled	Relapsed or refractory diffuse large B-cell lymphoma or relapsed or refractory grade 13a follicular lymphoma.
Administration Dosage	Either rituximab (375 mg/m2) followed by pina (2.4 mg/kg) every 21 days, or rituximab (375 mg/m2) followed by pola (2.4 mg/kg) every 21 days until disease progression or unacceptable toxicity up to 1 year.
Related Clinical Trial
NCT Number	NCT01691898	Phase Status	Phase 2
Clinical Description	A randomized, open-label, multicenter, phase 2 trial evaluating the safety and activity of pinatuzumab vedotin (DCDT2980S) in combination with rituximab or polatuzumab vedotin (DCDS4501A) in combination with rituximab and a non-randomized phase 1b/2 evaluation of polatuzumab vedotin in combination with obinutuzumab in patients with relapsed or refractory B-cell non-Hodgkin's lymphoma.    Click to Show/Hide
Primary Endpoint	Among patients with refractory diffuse large B-cell lymphoma, complete responses and median overall survival compares favourably with immunochemotherapy regimens reported in the SCHOLAR-1 study, in which 7.00% of patients achieved a complete response and a median overall survival of 6.30 months was observed.
Experiment 2 Reporting the Activity Date of This ADC					[54]
Efficacy Data	Objective Response Rate (ORR)	41.50%
Patients Enrolled	Patients aged 18 years were eligible if they had histologically confirmed R/R DLBCL (excluding transformed follicular lymphoma), received 1 prior line of therapy, had an Eastern Cooperative Oncology Group performance status of 0 to 2, and were considered transplant ineligible by the treating physician or experienced treatment failure with prior autologous SCT.    Click to Show/Hide
Administration Dosage	Bendamustine 90 mg/m2 intravenously (IV) on days 2 and 3 of cycle 1, and days 1 and 2 of subsequent cycles, plus rituximab IV (375 mg/m2 on day 1 of each cycle); polatuzumab vedotin received 1.80 mg/kg IV on day 2 of cycle 1, and day 1 of subsequent cycles; up to six 21-day cycles.
Related Clinical Trial
NCT Number	NCT02257567	Phase Status	Phase 1b/2
Clinical Description	A phase 1b/2 study evaluating the safety, tolerability and anti-tumor activity of polatuzumab vedotin in combination with rituximab (R) or obinutuzumab (G) plus bendamustine (B) in relapsed or refractory follicular or diffuse large B-cell lymphoma.
Primary Endpoint	With an additional 27 months of follow-up in the randomized pola + BR arm was 62.50% vs 25.00%; best CR rate was 52.50% vs 22.50%.
Other Endpoint	The median IRC-assessed PFS (95% CI) was 9.20 months (6.00-13.90) with pola + BR vs 3.70 months (2.10-4.50) with BR (HR, 0.39; 95% CI, 0.23-0.66); median investigator-assessed PFS was 7.50 vs 2.00 months (HR, 0.33; 95% CI, 0.20-0.56) with pola + BR and BR, respectively. Median OS (95% CI) was 12.40 months (9.00-32.00) vs 4.70 months (3.70-8.30) with pola + BR vs BR (HR, 0.42; 95% CI, 0.24-0.72). The 24-month OS probability was 38% (95% CI, 22.50-53.90) with pola + BR vs 17.0% (3.60-30.40) with BR. The 24-month PFS probability was 28.40% (95% CI, 13.9-43.0) with pola + BR vs 9.10% (95% CI, 0.00-18.90) with BR.The median DOR was 9.50 months (95% CI, 7.90-12.10) by IRC assessment and 8.70 months (95% CI, 5.90-12.10) by investigator assessment. The median IRC-assessed PFS was 6.6 months (95% CI, 5.10-9.20). Median OS was 12.50 months (95% CI, 8.20-23.10); the 12-month OS probability was 50.20% (95% CI, 40.40-60.10).    Click to Show/Hide
Experiment 3 Reporting the Activity Date of This ADC					[55]
Efficacy Data	Objective Response Rate (ORR)	76.09%
Patients Enrolled	CD20-positive relapsed or refractory follicular lymphoma (excluding grade 3b) and Eastern Cooperative Oncology Group performance status of 2 or less who had previously received anti-CD20-containing chemotherapy were eligible for inclusion.
Administration Dosage	Six 28-day cycles of induction treatment with intravenous obinutuzumab 1000 mg (all cohorts), and intravenous polatuzumab vedotin and oral lenalidomide (Celgene, Summit, NJ, USA) in the following doses: 14 mg/kg polatuzumab vedotin and 10 mg lenalidomide (cohort 1); 18 mg/kg polatuzumab vedotin and 10 mg lenalidomide (cohort 2); 14 mg/kg polatuzumab vedotin and 15 mg lenalidomide (cohort 3); 18 mg/kg polatuzumab vedotin and 15 mg lenalidomide (cohort 4); 14 mg/kg polatuzumab vedotin and 20 mg lenalidomide (cohort 5); and 18 mg/kg polatuzumab vedotin and 20 mg lenalidomide (cohort 6). Polatuzumab vedotin was administered on day 1, lenalidomide on days 1-21, and obinutuzumab on days 1, 8, and 15 of cycle one and day 1 of cycles two to six of each 28-day cycle.    Click to Show/Hide
Related Clinical Trial
NCT Number	NCT02600897	Phase Status	Phase 1b/2
Clinical Description	A phase 1b/2 study evaluating the safety and efficacy of obinutuzumab in combination with polatuzumab vedotin and lenalidomide in patients with relapsed or refractory follicular lymphoma and rituximab in combination with polatuzumab vedotin and lenalidomide in patients with relapsed or refractory diffuse large B-cell lymphoma.
Primary Endpoint	According to the Independent Review Committeeassessment, 29 (63.04%) of 46 patients (90% CI 50.00-75.00) had acomplete response and 35 (76.09%) patients (90% CI 64.00-86.00) had an objective response, per Modified Lugano 2014 criteria. Independent Review Committee assessment showed that 33 (71.74%) patients (90% CI59.00-82.00) had a complete metabolic response at the end ofinduction per Modified Lugano 2014 criteria.    Click to Show/Hide
Other Endpoint	At data cut-off (median follow-up 26.70 months [IQR 22.20-31.30]),median progression-free survival had not been reached. As determined by the investigator, theprogression-free survival was 86.00% (95% CI 75.00-96.00) at 12 months and 67.00% (95% CI 51.00-83.00) at 24 months, and 11 (23.91%) of 46 patients had an event reported at the time of this analysis.    Click to Show/Hide
Experiment 4 Reporting the Activity Date of This ADC					[60]
Efficacy Data	Objective Response Rate (ORR)	33.00 57.00 25.00 %
Patients Enrolled	R/R follicular lymphoma (FL); R/R diffuse large B-cell lymphoma (DLBCL).
Administration Dosage	FL patients received up to six 21-day cycles of obinutuzumab (1000 mg intravenously [IV], Day [D]1, D8, D15 of Cycle [C]1, and D1 of C26) and atezolizumab (1200 mg IV, D1 of C26) plus pola (1.40 or 1.80 mg/kg IV, D1 of C16). Subsequently, patients entered an expansion phase and received obinutuzumab and atezolizumab (same doses) plus pola at the RP2D (1.8 mg/kg). Patients who achieved at least stable disease at the end of induction (EOI; 68 weeks after D1C6) proceeded to obinutuzumab maintenance (1000 mg every 2 months) and atezolizumab (840 mg, D1 and D2 every month) for up to 2 years, or until progressive disease (PD). Unlike the FL cohort, the first seven DLBCL patients entered a safety run-in; once safety criteria were met, the cohort was expanded. All DLBCL patients received up to six 21-day cycles of rituximab (375 mg/m2 IV, D1 of C16), atezolizumab (1200 mg, D1 of C26), and pola (1.80 mg/kg, D1 of C16). Patients with at least a partial response (PR) at EOI (68 weeks after D1 of C6) received rituximab consolidation (375 mg/m2, D1 every 2 months) and atezolizumab (840 mg, D1 and D2 every month) for up to 8 months, or until PD.    Click to Show/Hide
Related Clinical Trial
NCT Number	NCT02729896	Phase Status	Phase 1b
Clinical Description	A phase 1b/2 study evaluating the safety and efficacy of obinutuzumab in combination with atezolizumab plus polatuzumab vedotin in patients with relapsed or refractory follicular lymphoma and rituximab in combination with atezolizumab plus polatuzumab vedotin in patients with relapsed or refractory diffuse large B-cell lymphoma.
Primary Endpoint	At EOI, CR rates in FL patients treated with G-atezo-pola at pola doses of 1.40 mg/kg (N=3) and 1.80 mg/kg (N=7) were 33.00% and 14.00% , respectively. In DLBCL patients who received R-atezo-pola, the CR rate at EOI was 13.00%.
Other Endpoint	At EOI, ORR rates in FL patients treated with G-atezo-pola at pola doses of 1.40 mg/kg (N=3) and 1.80 mg/kg (N=7) were 33.00% and 57.00% , respectively. In DLBCL patients who received R-atezo-pola, the ORR rate at EOI was 25.00%.
Experiment 5 Reporting the Activity Date of This ADC					[67]
Efficacy Data	Objective Response Rate (ORR)	42.86%
Patients Enrolled	Elapsed/refractory (R/R) diffuse large B-cell lymphoma (DLBCL) who received 1 prior line of therapy and were ineligible for autologous stem cell transplantation (ASCT) or experienced treatment failure with prior ASCT.
Administration Dosage	Pola 1.80 mg/kg intravenously (IV) on day 2 of cycle 1 and day 1 of subsequent cycles; bendamustine 90 mg/m2IV on days 2 and 3 of cycle 1 and then days 1 and 2 of subsequent cycles; rituximab 375 mg/m2IV on day 1 of each cycle. Three weeks of treatment was regarded as one cycle, and patients received up to six cycles of treatment.    Click to Show/Hide
Related Clinical Trial
NCT Number	NCT02257567	Phase Status	Phase 1
Clinical Description	A phase 1b/2 study evaluating the safety, tolerability and anti-tumor activity of polatuzumab vedotin in combination with rituximab (R) or obinutuzumab (G) plus bendamustine (B) in relapsed or refractory follicular or diffuse large B-cell lymphoma.
Primary Endpoint	2 patients (34.30%, 95% CI 19.1-52.2) achieved CR.
Other Endpoint	Seven of 12 patients who achieved CR completed six cycles of treatment. Fifteen patients (42.86%, 95% CI 26.30-60.70) achieved an overall response (12 patients CR; 3 patients PR). At a median followup of 5.40 months, median DOR, PFS, and EFS were 6.60 months, 5.20 months, and 5.10 months, respectively. Twentythree patients (65.71%) were alive, and median OS was not reached (95% CI 8.40-not evaluable [NE]).    Click to Show/Hide
Experiment 6 Reporting the Activity Date of This ADC					[89]
Efficacy Data	Complete Remission (CR)	57.60 23.50 %
Patients Enrolled	R/R follicular lymphoma (FL) and R/R diffuse large B-cell lymphoma (DLBCL); the majority had an Eastern Cooperative Oncology Group performance score of 0 or 1.
Administration Dosage	Dose escalation FL cohorts (3 + 3 design); Dose escalation DLBCL cohorts (3 + 3 design); polatuzumab vedotin 1.80 mg/kg and venetoclax 800 mg.
Related Clinical Trial
NCT Number	NCT02611323	Phase Status	Phase 1
Clinical Description	A phase 1b/2 study evaluating the safety and efficacy of obinutuzumab in combination with polatuzumab vedotin and venetoclax in patients with relapsed or refractory follicular lymphoma and rituximab in combination with polatuzumab vedotin and venetoclax in patients with relapsed or refractory diffuse large B-cell lymphoma.
Primary Endpoint	The overall response rate (ORR) for patients with FL was 75.80%, with 57.60% of patients achieving a complete response (CR). All patients in FL cohort 6 treated at the identified RP2D dose combination achieved CR at EOI. The ORR observed for patients with DLBCL was 29.40%; 23.50% achieved CR. Similar trends were seen in the DLBCL cohorts, with higher response rates in patients treated at the RP2D (37.5% vs. 22.2%).    Click to Show/Hide
Experiment 7 Reporting the Activity Date of This ADC					[94]
Efficacy Data	Complete Remission (CR)	50.00 40.00 17.50 %
Patients Enrolled	Patients aged 18 years were eligible if they had biopsy-confirmed R/R DLBCL (excluding transformed lymphoma) after 1 prior line of therapy, an Eastern Cooperative Oncology Group (ECOG) performance status of 0-2, grade 1 peripheral neuropathy (PN), and were considered transplantation ineligible by the treating physician or experienced treatment failure with prior ASCT. Double- and triple-hit lymphomas were not excluded.    Click to Show/Hide
Administration Dosage	1.80 mg/kg IV on day 2 of cycle 1 and day 1 of subsequent cycles. Patients were treated for up to six 21-day cycles.
Related Clinical Trial
NCT Number	NCT01287741	Phase Status	Phase Ib/II
Clinical Description	A phase Ib/II, multicenter, open-label randomized trial comparing the efficacy of GA101 (RO5072759) in combination with CHOP (G-CHOP) versus rituximab and CHOP (R-CHOP) in previously untreated patients with CD20-positive diffuse large B-cell lymphoma (DLBCL).
Primary Endpoint	In the phase Ib pola-BR arm, EOT IRC-assessed CR rate was 50.00% (3/6), with all 3 patients remaining in remission at a median follow-up of 37.60 months (DOR, > 28.90 to 38.20 months).
Other Endpoint	After a median follow-up of 22.3 months, PFS, OS, and DOR were significantly improved with pola-BR versus BR. Consistent benefit in risk reduction was seen for IRC- and INV-assessed PFS (IRC: HR, 0.36; 95% CI, 0.21-0.63; INV: HR, 0.34; 95% CI 0.20-0.57) and for DOR (IRC: HR, 0.47; 95% CI, 0.19-1.14; INV: HR,0.44, 95% CI 0.20-0.95).
Experiment 8 Reporting the Activity Date of This ADC					[96]
Patients Enrolled	CD20-positive diffuse large B-cell lymphoma (DLBCL), had not received previous treatment for lymphoma, had an Eastern Cooperative Oncology Group performance status score of 0 to 2 (on a 5-point scale, with higher numbers indicating greater disability), had a baseline International Prognostic Index (IPI) score between 2 and 5 (on a 5-level prognostic scale, with higher numbers indicating a poorer prognosis), and had adequate hematologic, renal, hepatic, and cardiac function, regardless of the cell of origin or the presence of rearrangements in MYC, BCL2, BCL6, or a combination of these.    Click to Show/Hide
Administration Dosage	Eight 21-day cycles of treatment were planned. During the first six cycles, patients received either pola-R-CHP or R-CHOP. On day 1 of each cycle, patients received either intravenous polatuzumab vedotin at a dose of 1.80 mg per kilogram of body weight and a placebo matching intravenous vincristine (pola-R-CHP group) or a placebo matching polatuzumab vedotin and intravenous vincristine at a dose of 1.40 mg per square meter of body-surface area (maximum of 2 mg) (R-CHOP group), plus intravenous doses of rituximab (375 mg per square meter), cyclophosphamide (750 mg per square meter), and doxorubicin (50 mg per square meter). All the patients also received oral prednisone at a dose of 100 mg once daily on days 1 through 5 of each of the first six cycles. During cycles 7 and 8, patients in both groups received rituximab monotherapy at a dose of 375 mg per square meter.    Click to Show/Hide
Related Clinical Trial
NCT Number	NCT03274492	Phase Status	Phase 3
Clinical Description	A phase 3, multicenter, randomized, double-blind, placebo-controlled trial comparing the efficacy and safety of polatuzumab vedotin in combination with rituximab and CHP (R-CHP) versus rituximab and CHOP (R-CHOP) in previously untreated patients with diffuse large B-cell lymphoma.
Primary Endpoint	For the pola-R-CHP group, 2 years FPS=76.70% (95% CI, 72.70-80.80). For the R-CHOP group, 2 years FPS=70.20% (95% CI, 65.80-74.60).
Other Endpoint	The relative risk of events was lower in the pola-R-CHP group than in the R-CHOP group (2-year event-free survival, 75.60% [95% CI, 71.50 to 79.70] and 69.40% [95% CI, 65.00 to 73.80%], respectively.
Experiment 9 Reporting the Activity Date of This ADC					[114]
Patients Enrolled	Non Hodgkin lymphoma (NHL) or chronic lymphocytic leukemia (CLL) expected to express CD79B (confirmation of CD79B expression was not required) and for whom no suitable therapy of curative intent or higher priority existed from 13 centres.
Administration Dosage	0.124 mg/kg every 21 days.
Related Clinical Trial
NCT Number	NCT01290549	Phase Status	Phase 1
Clinical Description	An open-label, multicenter, phase 1 trial of the safety and pharmacokinetics of escalating doses of DCDS4501A in patients with relapsed or refractory B-cell non-Hodgkins lymphoma and chronic lymphocytic leukemia and DCDS4501A in combination with rituximab in patients with relapsed or refractory B-cell non-Hodgkins lymphoma.
Primary Endpoint	Polatuzumab vedotin has an acceptable safety and tolerability profile in patients with NHL but not in those with CLL. Among 45 patients with NHL treated at the recommended phase 2 dose of single-agent polatuzumab vedotin, median progressionfree survival was 5.70 months (95% CI 3.00-7.90) and median duration of response was 6.2 months (95% CI 3.3-14.1). In patients with diffuse large B-cell lymphoma treated at the recommended phase 2 dose of single-agent polatuzumab, median progression-free survival was 5.00 months (95% CI 2.30-6.80) and median duration of response was 5.20 months (95% CI 2.40-13.10).    Click to Show/Hide

Experiment 1 Reporting the Activity Date of This ADC					[119]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 1.60%	High CD22 expression (CD22+++)
Method Description	Cells were inoculated subcutaneously into the flanks of female CB17 ICR severe combined immunodeficient (SCID) mice. When mean tumor size reached desired volume,the mice were divided into groups of 7 to 9 mice with the same mean tumor size and dosed intravenously via the tail vein with ADCs or antibodies. Rituximab was dosed at 30 mg/kg intraperitoneally (i.p.). Polatuzumab vedotin was administered as a single injection at 1 mg/kg.    Click to Show/Hide
In Vivo Model	B-cell lymphoma CDX model
In Vitro Model	Diffuse large B-cell lymphoma	WSU-DLCL2 cells		CVCL_1902
Experiment 2 Reporting the Activity Date of This ADC					[119]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 5.40%	High CD22 expression (CD22+++)
Method Description	Cells were inoculated subcutaneously into the flanks of female CB17 ICR severe combined immunodeficient (SCID) mice. When mean tumor size reached desired volume,the mice were divided into groups of 7 to 9 mice with the same mean tumor size and dosed intravenously via the tail vein with ADCs or antibodies. Rituximab was dosed at 30 mg/kg intraperitoneally (i.p.). Polatuzumab vedotin was administered as a single injection at 2 mg/kg.    Click to Show/Hide
In Vivo Model	B-cell lymphoma CDX model
In Vitro Model	Diffuse large B-cell lymphoma	WSU-DLCL2 cells		CVCL_1902
Experiment 3 Reporting the Activity Date of This ADC					[119]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 6.60%	Moderate CD22 expression (CD22++)
Method Description	Cells were inoculated subcutaneously into the flanks of female CB17 ICR severe combined immunodeficient (SCID) mice. When mean tumor size reached desired volume,the mice were divided into groups of 7 to 9 mice with the same mean tumor size and dosed intravenously via the tail vein with ADCs or antibodies. Rituximab was dosed at 30 mg/kg intraperitoneally (i.p.). Polatuzumab vedotin was administered as a single injection at 0.1 mg/kg.    Click to Show/Hide
In Vivo Model	B-cell lymphoma CDX model
In Vitro Model	Burkitt lymphoma	BJAB cells		CVCL_5711
Experiment 4 Reporting the Activity Date of This ADC					[119]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 37.10%	High CD22 expression (CD22+++)
Method Description	Cells were inoculated subcutaneously into the flanks of female CB17 ICR severe combined immunodeficient (SCID) mice. When mean tumor size reached desired volume,the mice were divided into groups of 7 to 9 mice with the same mean tumor size and dosed intravenously via the tail vein with ADCs or antibodies. Rituximab was dosed at 30 mg/kg intraperitoneally (i.p.). Polatuzumab vedotin was administered as a single injection at 4 mg/kg.    Click to Show/Hide
In Vivo Model	B-cell lymphoma CDX model
In Vitro Model	Diffuse large B-cell lymphoma	WSU-DLCL2 cells		CVCL_1902
Experiment 5 Reporting the Activity Date of This ADC					[119]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 61.20%	Moderate CD22 expression (CD22++)
Method Description	Cells were inoculated subcutaneously into the flanks of female CB17 ICR severe combined immunodeficient (SCID) mice. When mean tumor size reached desired volume,the mice were divided into groups of 7 to 9 mice with the same mean tumor size and dosed intravenously via the tail vein with ADCs or antibodies. Rituximab was dosed at 30 mg/kg intraperitoneally (i.p.). Polatuzumab vedotin was administered as a single injection at 0.5 mg/kg.    Click to Show/Hide
In Vivo Model	B-cell lymphoma CDX model
In Vitro Model	Burkitt lymphoma	BJAB cells		CVCL_5711
Experiment 6 Reporting the Activity Date of This ADC					[119]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 82.90%	High CD22 expression (CD22+++)
Method Description	Cells were inoculated subcutaneously into the flanks of female CB17 ICR severe combined immunodeficient (SCID) mice. When mean tumor size reached desired volume,the mice were divided into groups of 7 to 9 mice with the same mean tumor size and dosed intravenously via the tail vein with ADCs or antibodies. Rituximab was dosed at 30 mg/kg intraperitoneally (i.p.). Polatuzumab vedotin was administered as a single injection at 8 mg/kg.    Click to Show/Hide
In Vivo Model	B-cell lymphoma CDX model
In Vitro Model	Diffuse large B-cell lymphoma	WSU-DLCL2 cells		CVCL_1902
Experiment 7 Reporting the Activity Date of This ADC					[119]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 86.30%	Moderate CD22 expression (CD22++)
Method Description	Cells were inoculated subcutaneously into the flanks of female CB17 ICR severe combined immunodeficient (SCID) mice. When mean tumor size reached desired volume,the mice were divided into groups of 7 to 9 mice with the same mean tumor size and dosed intravenously via the tail vein with ADCs or antibodies. Rituximab was dosed at 30 mg/kg intraperitoneally (i.p.). Polatuzumab vedotin was administered as a single injection at 1 mg/kg.    Click to Show/Hide
In Vivo Model	B-cell lymphoma CDX model
In Vitro Model	Burkitt lymphoma	BJAB cells		CVCL_5711
Experiment 8 Reporting the Activity Date of This ADC					[119]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 94.90%	High CD22 expression (CD22+++)
Method Description	Cells were inoculated subcutaneously into the flanks of female CB17 ICR severe combined immunodeficient (SCID) mice. When mean tumor size reached desired volume,the mice were divided into groups of 7 to 9 mice with the same mean tumor size and dosed intravenously via the tail vein with ADCs or antibodies. Rituximab was dosed at 30 mg/kg intraperitoneally (i.p.). Polatuzumab vedotin was administered as a single injection at 12 mg/kg.    Click to Show/Hide
In Vivo Model	B-cell lymphoma CDX model
In Vitro Model	Diffuse large B-cell lymphoma	WSU-DLCL2 cells		CVCL_1902
Experiment 9 Reporting the Activity Date of This ADC					[119]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 97.10%	Moderate CD22 expression (CD22++)
Method Description	Cells were inoculated subcutaneously into the flanks of female CB17 ICR severe combined immunodeficient (SCID) mice. When mean tumor size reached desired volume,the mice were divided into groups of 7 to 9 mice with the same mean tumor size and dosed intravenously via the tail vein with ADCs or antibodies. Rituximab was dosed at 30 mg/kg intraperitoneally (i.p.). Polatuzumab vedotin was administered as a single injection at 1.5 mg/kg.    Click to Show/Hide
In Vivo Model	B-cell lymphoma CDX model
In Vitro Model	Burkitt lymphoma	BJAB cells		CVCL_5711
Experiment 10 Reporting the Activity Date of This ADC					[119]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 97.90%	High CD22 expression (CD22+++)
Method Description	Cells were inoculated subcutaneously into the flanks of female CB17 ICR severe combined immunodeficient (SCID) mice. When mean tumor size reached desired volume,the mice were divided into groups of 7 to 9 mice with the same mean tumor size and dosed intravenously via the tail vein with ADCs or antibodies. Rituximab was dosed at 30 mg/kg intraperitoneally (i.p.). Polatuzumab vedotin was administered as a single injection at 16 mg/kg.    Click to Show/Hide
In Vivo Model	B-cell lymphoma CDX model
In Vitro Model	Diffuse large B-cell lymphoma	WSU-DLCL2 cells		CVCL_1902
Experiment 11 Reporting the Activity Date of This ADC					[119]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100%	Moderate CD22 expression (CD22++)
Method Description	Cells were inoculated subcutaneously into the flanks of female CB17 ICR severe combined immunodeficient (SCID) mice. When mean tumor size reached desired volume,the mice were divided into groups of 7 to 9 mice with the same mean tumor size and dosed intravenously via the tail vein with ADCs or antibodies. Rituximab was dosed at 30 mg/kg intraperitoneally (i.p.). Polatuzumab vedotin was administered as a single injection at 4 mg/kg.    Click to Show/Hide
In Vivo Model	B-cell lymphoma CDX model
In Vitro Model	Burkitt lymphoma	BJAB cells		CVCL_5711
Experiment 12 Reporting the Activity Date of This ADC					[119]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100%	Moderate CD22 expression (CD22++)
Method Description	Cells were inoculated subcutaneously into the flanks of female CB17 ICR severe combined immunodeficient (SCID) mice. When mean tumor size reached desired volume,the mice were divided into groups of 7 to 9 mice with the same mean tumor size and dosed intravenously via the tail vein with ADCs or antibodies. Rituximab was dosed at 30 mg/kg intraperitoneally (i.p.). Polatuzumab vedotin was administered as a single injection at 2 mg/kg.    Click to Show/Hide
In Vivo Model	B-cell lymphoma CDX model
In Vitro Model	Burkitt lymphoma	BJAB cells		CVCL_5711

Experiment 1 Reporting the Activity Date of This ADC					[61]
Efficacy Data	Objective Response Rate (ORR)	7.40%
Patients Enrolled	Advanced non-small cell lung cancer (NSCLC).
Administration Dosage	Teliso-V Q2W (1.60, 1.90, or 2.20 mg/kg, intravenous) with nivolumab (3 mg/kg, or 240 mg, or per locally approved label, intravenously).
Related Clinical Trial
NCT Number	NCT02099058	Phase Status	Phase 1
Clinical Description	A multicenter, phase 1/1b, open-label, dose-escalation study of ABBV-399, an antibody drug conjugate, in subjects with advanced solid tumors.
Primary Endpoint	Most patients (97.30%, n=36) experienced one or more TEAE, with 23 (62.16%) reporting TEAEs grades 3 or higher. TEAEs considered possibly related to Teliso-V were reported in 78.38% (n=29) of patients; 32.43% (n=12) were grade greater than or equal to 3.
Other Endpoint	Combination therapy with Teliso-V plus nivolumab was well tolerated in patients with c-Met-+NSCLC with limited antitumor activity. The ORR was 7.40% (95% CI: 0.90-24.30), with two patients (PD-L1+, n =1; PD-L1-, n=1) having a confirmed PR.Overall, 66.67% of patients (16 of 24) had evidence of tumor size reduction; three (12.5%) reported a greater than 30% reduction in target lesion. The overall median PFS (95% CI) was 7.20 months (3.30-8.90); 7.20 months(1.50-not reached [NR]) for PD-L1 patients, 4.50 months(1.50-NR) for PD-L1- patients, and NR (2.00-NR) for PD-L1-unk patients. The objective response rate was 7.40%, with two patients having a confirmed partial response. Overall median progression-free survival was 7.20 months.    Click to Show/Hide
Experiment 2 Reporting the Activity Date of This ADC					[63]
Efficacy Data	Objective Response Rate (ORR)	23.00 28.00 18.00 18.00 31.00 6.00 43.00 %
Patients Enrolled	Non-small cell lung cancer (NSCLC) and c-Met H-score 150 (c-Met+) or MET amplification/exon 14 skipping mutations.
Administration Dosage	Intravenously once every 3 weeks (0.15-3.30 mg/kg) or once every 2 weeks (1.60-2.20 mg/kg).
Related Clinical Trial
NCT Number	NCT02099058	Phase Status	Phase 1
Clinical Description	A multicenter, phase 1/1b, open-label, dose-escalation study of ABBV-399, an antibody drug conjugate, in subjects with advanced solid tumors.
Primary Endpoint	Four objective responses (ORR = 26.70%; 95% CI, 7.80-55.10) were observed in this subgroup, 3 in once every 2 weeks (ORR = 43.00%; 95% CI, 9.90-81.60), and 1 in once every 3 weeks (ORR = 13.00%; 95% CI, 0.30-52.70).
Other Endpoint	The median PFS in once every 2 weeks cohorts was 8.00 months (range, 1.20-9.10) and the median treatment duration was 19.60 weeks (range, 0.10-60.10).
Experiment 3 Reporting the Activity Date of This ADC					[64]
Efficacy Data	Objective Response Rate (ORR)	30.55 32.10 52.60 %
Patients Enrolled	Advanced non-small cell lung cancer (measurable per Response Evaluation Criteria in Solid Tumors v1.1) not amenable to resection or other approved therapies until disease progression, death, or withdrawal of consent.
Administration Dosage	Teliso-V (2.70 mg/kg once every 21 days) plus erlotinib (150 mg once daily) until disease progression, death, or withdrawal of consent.
Related Clinical Trial
NCT Number	NCT02099058	Phase Status	Phase 1
Clinical Description	A multicenter, phase 1/1b, open-label, dose-escalation study of ABBV-399, an antibody drug conjugate, in subjects with advanced solid tumors.
Primary Endpoint	OrR for all efficacy-evaluable patients was 30.55% (11/36; 95% CI, 16.30 to 48.10), and DCR was 86.11% (31/36; 95% CI, 70.5 to 95.3). Median PFS for all efficacy-evaluable patients was 5.90 months (95% CI, 2.80 to not reached [NR]).
Other Endpoint	For EGFR-M+ patients (n = 28), ORR was 32.14% (9/28; 95% CI, 15.90 to 52.40), with one CR (3.57%) and eight PR (28.57%). DCR was 85.71% (24/28; 95% CI, 67.30 to 96.00) and median PFS was 5.90 months (95% CI, 2.80 to NR). Median PFS was 3.70 months (95% CI, 1.40 to NR) for T790M+ patients, compared with 6.80 months (95% CI, 4.30 to NR) for non-T790M+ patients. Of EGFR-M+ patients, those who were c-Met high (n = 15) had an ORR of 52.60%. Median PFS was 6.80 months for non-T790M+ and for those whose T790M status was unknown, versus 3.70 months for T790M+.    Click to Show/Hide
Experiment 4 Reporting the Activity Date of This ADC					[64]
Efficacy Data	Objective Response Rate (ORR)	30.60 32.18 52.60 %
Patients Enrolled	Advanced non-small cell lung cancer (measurable per Response Evaluation Criteria in Solid Tumors v1.1) not amenable to resection or other approved therapies until disease progression, death, or withdrawal of consent.
Administration Dosage	Teliso-V (2.70 mg/kg once every 21 days) plus erlotinib (150 mg once daily) until disease progression, death, or withdrawal of consent.
Related Clinical Trial
NCT Number	NCT02099058	Phase Status	Phase 1
Clinical Description	A multicenter, phase 1/1b, open-label, dose-escalation study of ABBV-399, an antibody drug conjugate, in subjects with advanced solid tumors.
Primary Endpoint	Median PFS=5.90 months (95% CI, 2.80 to not reached). ORR for EGFR-M+ patients = 32.18% (n=28). EGFR-M+ patients ORR = 52.60%.
Other Endpoint	Median PFS=6.80 months for non-T790M+.
Experiment 5 Reporting the Activity Date of This ADC					[71]
Efficacy Data	Objective Response Rate (ORR)	71.70 70.60 %
Patients Enrolled	Relapsed or refractory multiple myeloma, and ECOG performance status or Zubrod score of 2 or below, received indatuximab ravtansine with lenalidomide and dexamethasone (indatuximab ravtansine plus lenalidomide) had failure of at least one previous therapy.
Administration Dosage	Intravenously on days 1, 8, and 15 of each 28-day cycle in dose of 100 mg/m2 plus lenalidomide or pomalidomide and dexamethasone.
Related Clinical Trial
NCT Number	NCT01638936	Phase Status	Phase 1
Clinical Description	A phase 1/2a multi-dose escalation study of BT062 in combination with lenalidomide or pomalidomide and dexamethasone in subjects with relapsed or relapsed/refractory multiple myeloma.
Experiment 6 Reporting the Activity Date of This ADC					[73]
Efficacy Data	Objective Response Rate (ORR)	75%
Patients Enrolled	MA advanced GEC.
Administration Dosage	15 mg/kg IV, once every 3 weeks.
Related Clinical Trial
NCT Number	NCT01472016	Phase Status	Phase 1
Clinical Description	A multi-center, phase 1/1b, open-label, dose escalation study of ABT-700, a monoclonal antibody in subjects with advanced solid tumors.
Primary Endpoint	Among these patients, three achieved a partial response and one had progressive disease as best response (ORR=75.00%). The duration of disease control in responders ranged from 18-27 weeks and the median duration of response was 16.10 weeks. The median progression- free survival in MET-amplified patients was 17.90 weeks.
Experiment 7 Reporting the Activity Date of This ADC					[104]
Related Clinical Trial
NCT Number	NCT01915472	Phase Status	Phase 2
Clinical Description	A phase 2 study of IMMU 130 (hmn-14-SN38 antibody drug conjugate) in patients with metastatic colorectal cancer.
Experiment 8 Reporting the Activity Date of This ADC					[108]
Related Clinical Trial
NCT Number	NCT01001442	Phase Status	Phase 1/2
Clinical Description	A phase 1/2a multi-dose escalation study to evaluate maximum tolerated dose (MTD), pharmacokinetics (PK), safety and efficacy of BT062 in subjects with relapsed or relapsed/refractory multiple myeloma.
Experiment 9 Reporting the Activity Date of This ADC					[110]
Related Clinical Trial
NCT Number	NCT01270698	Phase Status	Phase 1
Clinical Description	A phase 1 study of IMMU-130 (hmn-14-SN38 antibody drug conjugate) in patients with colorectal cancer.
Experiment 10 Reporting the Activity Date of This ADC					[111]
Related Clinical Trial
NCT Number	NCT01605318	Phase Status	Phase 1
Clinical Description	A phase 1/2 study of once or twice weekly IMMU-130 (hMN-14-SN38, antibody-drug conjugate) in patients with colorectal cancer.
Experiment 11 Reporting the Activity Date of This ADC					[112]
Related Clinical Trial
NCT Number	NCT00723359	Phase Status	Phase 1
Clinical Description	A phase 1 dose escalation study to evaluate maximum tolerated dose (MTD), pharmacokinetics (PK), and safety of BT062 in subjects with relapsed or relapsed/refractory multiple myeloma.
Experiment 12 Reporting the Activity Date of This ADC					[113]
Patients Enrolled	Nonsmall-cell lung cancer (NSCLC) with c-Metoverexpressing tumors (c-Met positive; immunohistochemistry membrane H-score 150).
Administration Dosage	Teliso-V was administered by intravenous (IV) infusion to groups of three to six patients who were enrolled in eight-dose cohorts for dosing at 0.15 to 3.30 mg/kg on day 1, once every 21 days, or until disease progression or unacceptable toxicity.
Related Clinical Trial
NCT Number	NCT02099058	Phase Status	Phase 1
Clinical Description	A multicenter, phase 1/1b, open-label, dose-escalation study of ABBV-399, an antibody drug conjugate, in subjects with advanced solid tumors.
Primary Endpoint	No formal MTD was identified.
Experiment 13 Reporting the Activity Date of This ADC					[133]
Efficacy Data	Progression Free Survival	5.9 months
Patients Enrolled	Eligibility requires c-Met+ SCCA with no prior immune checkpoint inhibitor (anti-PD-1/PD-L1/CTLA-4) or autoimmune disease (exceptions: vitiligo, stable endocrine disorders). Exclusions: active HBV/HIV, chronic HCV, interstitial lung disease, NYHA Class III/IV cardiac conditions, recent corticosteroids (>10mg prednisone/day), or allergies to nivolumab/ipilimumab. Cardiac dysfunction (CHF/MI within 6 months) mandates cardiology evaluation. PRO questionnaires (English) are mandatory pre-registration.    Click to Show/Hide
Administration Dosage	ABBV-399 (Process II), 2.7 mg/kg IV over 30 minutes, Day 1, Every 21 days
Related Clinical Trial
NCT Number	NCT03574753	Phase Status	PHASE2
Clinical Description	A Phase II Study of ABBV-399 in Patients With C-Met Positive Stage IV or Recurrent Squamous Cell Lung Cancer (LUNG-MAP SUB-STUDY)
Primary Endpoint	Primary efficacy outcomes include overall response rate (ORR; confirmed/unconfirmed CR/PR per RECIST 1.1) in c-Met+ lung squamous cell carcinoma (SCCA) patients. Safety metrics focus on Grade 3-5 drug-related adverse events (CTCAE v4.0/5.0) during treatment and 3-year follow-up.
Other Endpoint	Secondary endpoints evaluate immunotherapy-exposed/relapsed c-Met+ SCCA: investigator-assessed progression-free survival (IA-PFS; time to progression/symptomatic deterioration/death), overall survival (OS; time to death), and ORR per RECIST 1.1 over 3 years. Duration of response (DoR; time from initial response to progression/death) is also measured.    Click to Show/Hide
Experiment 14 Reporting the Activity Date of This ADC					[133]
Efficacy Data	Objective Response Rate (ORR)	32.1 52.6 %
Patients Enrolled	Eligibility requires c-Met+ SCCA with no prior immune checkpoint inhibitor (anti-PD-1/PD-L1/CTLA-4) or autoimmune disease (exceptions: vitiligo, stable endocrine disorders). Exclusions: active HBV/HIV, chronic HCV, interstitial lung disease, NYHA Class III/IV cardiac conditions, recent corticosteroids (>10mg prednisone/day), or allergies to nivolumab/ipilimumab. Cardiac dysfunction (CHF/MI within 6 months) mandates cardiology evaluation. PRO questionnaires (English) are mandatory pre-registration.    Click to Show/Hide
Administration Dosage	ABBV-399 (Process II), 2.7 mg/kg IV over 30 minutes, Day 1, Every 21 days
Related Clinical Trial
NCT Number	NCT03574753	Phase Status	PHASE2
Clinical Description	A Phase II Study of ABBV-399 in Patients With C-Met Positive Stage IV or Recurrent Squamous Cell Lung Cancer (LUNG-MAP SUB-STUDY)
Primary Endpoint	Primary efficacy outcomes include overall response rate (ORR; confirmed/unconfirmed CR/PR per RECIST 1.1) in c-Met+ lung squamous cell carcinoma (SCCA) patients. Safety metrics focus on Grade 3-5 drug-related adverse events (CTCAE v4.0/5.0) during treatment and 3-year follow-up.
Other Endpoint	Secondary endpoints evaluate immunotherapy-exposed/relapsed c-Met+ SCCA: investigator-assessed progression-free survival (IA-PFS; time to progression/symptomatic deterioration/death), overall survival (OS; time to death), and ORR per RECIST 1.1 over 3 years. Duration of response (DoR; time from initial response to progression/death) is also measured.    Click to Show/Hide
Experiment 15 Reporting the Activity Date of This ADC					[136]
Efficacy Data	Objective Response Rate (ORR)	36.50%
Patients Enrolled	Eligible participants must have c-Met+ locally advanced/metastatic non-squamous EGFR-wildtype NSCLC (≤2 prior systemic therapies including ≤1 cytotoxic chemotherapy line) with ECOG 0-1. Exclusions include recent lung radiation (<6 months), adenosquamous histology, ILD/pneumonitis history (no evidence on screening imaging for Ireland sites), active infections (HIV/HBV/HCV - specific to France/CZ sites), and unresolved Grade≥2 toxicities (except alopecia/anemia). Stable CNS metastases post-definitive therapy are permitted.    Click to Show/Hide
Administration Dosage	Telisotuzumab vedotin administered via intravenous (IV) infusion every 14 days.
Related Clinical Trial
NCT Number	NCT03539536	Phase Status	PHASE2
Clinical Description	Phase 2, Open-Label Safety and Efficacy Study of Telisotuzumab Vedotin (ABBV-399) in Subjects With Previously Treated c-Met+ Non-Small Cell Lung Cancer
Primary Endpoint	Key efficacy endpoints include overall response rate (ORR; confirmed CR/PR per RECIST v1.1) and adverse events assessment in the alternate dose cohort over approximately 3 years.
Other Endpoint	Additional efficacy measures comprise duration of response (DoR; time from initial response to progression/death), disease control rate (DCR; CR+PR+SD≥12 weeks), progression-free survival (PFS; time from first dose to progression/death), and overall survival (OS; time from first dose to death) - all assessed over approximately 3 years.
Experiment 16 Reporting the Activity Date of This ADC					[138]
Efficacy Data	Disease control rate (DCR)	76.90%
Patients Enrolled	Eligible patients have advanced NSCLC (ECOG 0-2) with measurable disease and adequate organ function. Exclusions: recent lung radiation (<6 months), uncontrolled CNS metastases, ILD/pneumonitis history, unresolved Grade≥2 toxicities, major surgery within 21 days, or active COVID-19. Combination-specific exclusions apply (e.g., QTc>470ms for osimertinib arm; autoimmune disease/immunosuppressants for nivolumab arm).    Click to Show/Hide
Related Clinical Trial
NCT Number	NCT02099058	Phase Status	PHASE1
Clinical Description	A Multicenter, Phase 1/1b, Open-Label, Dose-Escalation Study of ABBV-399, an Antibody Drug Conjugate, in Subjects With Advanced Solid Tumors
Primary Endpoint	Primary outcomes assess safety (adverse events over 24 months) and pharmacokinetics of ABBV-399 (monotherapy/combination with osimertinib/erlotinib/nivolumab) including recommended Phase 2 dose (RPTD), AUC (0-t), Cmax, Tmax, and terminal half-life.
Other Endpoint	Efficacy endpoints include objective response rate (ORR; CR/PR per RECIST 1.1), progression-free survival (PFS; time from first dose to progression/death), and duration of response (DoR; time from initial response to progression) over 24 months.
Experiment 17 Reporting the Activity Date of This ADC					[139]
Patients Enrolled	Eligible participants must have c-Met-overexpressing non-squamous NSCLC (confirmed by AbbVie's IHC assay), actionable gene alterations (if applicable), measurable disease (RECIST v1.1), ECOG 0-1, and ≤1 prior cytotoxic chemotherapy line in advanced/metastatic setting. Exclusions include untreated CNS metastases, prior c-Met/EGFR-targeted therapy, docetaxel exposure, idiopathic pulmonary fibrosis, unresolved Grade ≥2 toxicities (except alopecia/anemia), major surgery within 21 days, or protocol-specified comorbidities. Stable brain metastases post-treatment are allowed if asymptomatic and off steroids (≤10mg prednisone/day).    Click to Show/Hide
Administration Dosage	Participants will receive telisotuzumab vedotin every 2 weeks until meeting study drug discontinuation criteria.
Related Clinical Trial
NCT Number	NCT04928846	Phase Status	PHASE3
Clinical Description	A Phase 3 Open-Label, Randomized, Controlled, Global Study of Telisotuzumab Vedotin (ABBV-399) Versus Docetaxel in Subjects With Previously Treated c-Met Overexpressing, EGFR Wildtype, Locally Advanced/Metastatic Non-Squamous Non-Small Cell Lung Cancer
Primary Endpoint	Efficacy evaluation includes progression-free survival (PFS) and overall survival (OS) assessed up to 39 months via Blinded Independent Central Review (BICR) and investigator assessment, with PFS defined as time from randomization to radiographic progression (RECIST v1.1) or death, and OS as time to death from any cause.
Other Endpoint	Additional efficacy measures comprise objective response rate (ORR) and duration of response (DoR) per BICR (up to 58.25 months), alongside quality-of-life changes (EORTC QLQ-C30) over 12 weeks, assessing physical function and global health status on a 0-100 scale where higher scores indicate better functioning/quality of life or worse symptom burden.    Click to Show/Hide
Experiment 18 Reporting the Activity Date of This ADC					[140]
Patients Enrolled	Eligible participants must have MET-amplified non-squamous NSCLC (central lab-confirmed), measurable disease (RECIST v1.1), ECOG 0-1, and prior adjuvant/neoadjuvant therapy completed ≥6 months pre-enrollment. Exclusions include actionable EGFR/ALK/ROS1/BRAF alterations, prior metastatic NSCLC systemic therapy (except ≤1 chemotherapy cycle), unresolved Grade ≥2 toxicities (excluding alopecia/anemia), major surgery within 21 days, or protocol-specified comorbidities (e.g., active pneumonitis). Stable CNS metastases post-treatment are permitted.    Click to Show/Hide
Administration Dosage	Participants will receive telisotuzumab vedotin every 2 weeks until meeting study drug discontinuation criteria.
Related Clinical Trial
NCT Number	NCT05513703	Phase Status	PHASE2
Clinical Description	Phase 2, Open-Label Study in Subjects With Previously Untreated MET Amplified Locally Advanced/Metastatic Non-Squamous Non-Small Cell Lung Cancer (NSCLC)
Primary Endpoint	Efficacy outcomes include objective response rate (ORR) per Independent Central Review (ICR) up to 1 year, defined as confirmed complete (CR) or partial response (PR) by RECIST v1.1, alongside duration of response (DoR), disease control rate (DCR), progression-free survival (PFS), and overall survival (OS) up to 2 years.
Other Endpoint	Patient-reported outcomes assess time to deterioration in cough, pain, dyspnea, and physical function (EORTC QLQ-LC13/QLQ-C30) and quality-of-life changes (EORTC QLQ-C30 Global Health Status) over 1 year, scored 0-100 (higher scores indicate better function/QoL or worse symptoms).
Experiment 19 Reporting the Activity Date of This ADC					[141]
Patients Enrolled	Eligible participants must have EGFR-mutated (del19/L858R ±T790M), c-Met-overexpressing non-squamous NSCLC (IHC-confirmed), ECOG 0-1, measurable disease (RECIST v1.1), and progression on prior third-generation EGFR TKI (e.g., osimertinib). Exclusions include actionable ALK/ROS1/BRAF alterations, prior metastatic chemotherapy (except limited platinum pre-TKI), unresolved Grade ≥2 toxicities (excluding alopecia/anemia), major surgery within 21 days, active pneumonitis, or protocol-specified comorbidities (e.g., uncontrolled infections, ≥Grade 2 edema/neuropathy). Stable CNS metastases post-definitive therapy are permitted if asymptomatic for ≥4 weeks.    Click to Show/Hide
Administration Dosage	Participants will receive telisotuzumab vedotin every 2 weeks in combination with osimertinib, until disease progression or unacceptable toxicity.
Related Clinical Trial
NCT Number	NCT06093503	Phase Status	PHASE3
Clinical Description	Phase 3, Open-Label, Randomized, Controlled, Global Study of Telisotuzumab Vedotin (ABBV-399) Combined With Osimertinib vs Platinum-Based Chemotherapy in Subjects With c-Met Overexpressing (OE) EGFR Mutant, Locally Advanced/Metastatic Non-Squamous NSCLC After a First Progression on Prior Third Generation EGFR TKi Treatment
Primary Endpoint	The study evaluates progression-free survival (PFS) both in participants without CNS metastases and in the overall population, defined as time from randomization to radiographic progression (RECIST v1.1) or death. Overall response (OR) and duration of response (DoR) are similarly assessed, with OR defined as confirmed complete (CR) or partial response (PR), and DoR measuring time from response to progression or death.    Click to Show/Hide
Other Endpoint	Secondary outcomes include overall survival (OS) and changes in physical functioning/quality of life using EORTC QLQ-C30 and QLQ-LC13 scales (0-100), where higher scores indicate better function/QoL or worse symptoms. Adverse events (AEs) are monitored up to 41 months, with causality assessed by investigators.
Experiment 20 Reporting the Activity Date of This ADC					[142]
Patients Enrolled	Eligible participants must have c-Met-overexpressing NSCLC (IHC-confirmed), ECOG 0-1, measurable disease (RECIST v1.1), and ≤1 prior cytotoxic chemotherapy line. Exclusions include actionable EGFR mutations, prior c-Met-targeted ADCs/docetaxel, active pneumonitis, unresolved Grade≥2 toxicities (excluding alopecia/anemia), major surgery within 21 days, or protocol-specified comorbidities (e.g., ≥Grade 2 edema/neuropathy, uncontrolled infections). Stable CNS metastases post-therapy are permitted if asymptomatic.    Click to Show/Hide
Administration Dosage	Participants will receive telisotuzumab vedotin dose A/B, as part of the 3 year study duration.
Related Clinical Trial
NCT Number	NCT06568939	Phase Status	PHASE2
Clinical Description	A Phase 2, Open-Label, Randomized, Global Study of Two Telisotuzumab Vedotin Regimens in Subjects With Previously Treated c-Met Overexpressing, EGFR Wildtype, Locally Advanced/Metastatic Non-Squamous Non-Small Cell Lung Cancer
Primary Endpoint	Safety endpoints include treatment-emergent adverse events (AEs) (any-grade/Grade≥2), specifically interstitial lung disease (ILD), peripheral neuropathy, and ocular surface disorders (corneal epitheliopathy) over 3 years, along with AEs leading to treatment discontinuation or Grade 5 (fatal) events. Efficacy measures include objective response (OR: CR/PR per RECIST v1.1) and duration of response (DoR) assessed by blinded independent central review (BICR).    Click to Show/Hide
Other Endpoint	Pharmacokinetic analyses measure telisotuzumab vedotin conjugate (serum) and MMAE payload (plasma) concentrations over 26 weeks, alongside antidrug antibody (ADA/nADA) incidence. Patient-reported outcomes assess treatment tolerability via PRO-CTCAE (0-4 scale) and FACT-G GP5 item. Secondary endpoints include PFS (time to progression/death) and OS (time to death) over 3 years.    Click to Show/Hide
Experiment 21 Reporting the Activity Date of This ADC					[143]
Patients Enrolled	The participant must not be eligible for a telisotuzumab vedotin clinical trial.
Related Clinical Trial
NCT Number	NCT04830202	Phase Status	N.A.
Clinical Description	Expanded Access to Telisotuzumab Vedotin
Experiment 22 Reporting the Activity Date of This ADC					[144]
Patients Enrolled	Eligible participants must have histologically confirmed advanced solid tumors (ECOG 0-2) with measurable disease, archived tumor tissue, and adequate organ function. Exclusions: prior anticancer therapy within 21 days (7 days for herbal), uncontrolled brain metastases (eligible post-definitive therapy if asymptomatic without steroids/anticonvulsants for ≥2 weeks), unresolved Grade≥2 toxicities (except alopecia/anemia), or major surgery within 21 days.    Click to Show/Hide
Administration Dosage	ABBV-399 via intravenous administration at escalating dose levels.
Related Clinical Trial
NCT Number	NCT03311477	Phase Status	PHASE1
Clinical Description	A Phase I Study to Evaluate the Safety and Pharmacokinetics of ABBV-399 in Japanese Subjects With Advanced Solid Tumors
Primary Endpoint	Pharmacokinetic parameters include AUC (0-t), Cmax, Tmax, and terminal elimination half-life (t1/2), measured over 24 months. Dose determination evaluates Maximum Tolerated Dose (MTD) or Maximum Administered Dose (MAD) as the highest dose with <33% dose-limiting toxicities in the first 21 days.
Other Endpoint	Efficacy outcomes measured over 24 months are Progression-Free Survival (PFS; time from first dose to progression/death), Objective Response Rate (ORR; confirmed CR/PR by RECIST 1.1), and Duration of Response (DOR; initial response to progression/death).
Experiment 23 Reporting the Activity Date of This ADC					[145]
Patients Enrolled	Eligible participants must have confirmed advanced/metastatic NSQ NSCLC, available FFPE tissue collected since 2019, and prior consent for biomarker research. Exclusions: pre-2019 specimens, inadequate tissue volume/quality (e.g., <4-5um thickness), and adenosquamous/sarcomatous histologies.
Related Clinical Trial
NCT Number	NCT06068842	Phase Status	N.A.
Clinical Description	International Real-World Study of MET Overexpression in Patients With Non-Small Cell Lung Cancer
Primary Endpoint	MET protein overexpression status (either positive [≥25% tumor cells with 3+ staining] or high-positive [≥50% tumor cells with 3+ staining]) will be assessed via local IHC testing over 15 months.

Experiment 1 Reporting the Activity Date of This ADC					[66]
Efficacy Data	Objective Response Rate (ORR)	40.00 44.00 0.00 %
Patients Enrolled	Patients with advanced or metastatic solid tumors who had failed outcomes from or were not able to receive standard treatment were enrolled in phase 1a without EGFR prescreening. Phase 1b recruited EGFR-positive patients with refractory advanced squamous cell carcinomas of the head and neck (SCCHN), nasopharyngeal carcinoma (NPC), and colorectal cancer (CRC).    Click to Show/Hide
Administration Dosage	An intravenous dose of 0.10 to 2.50 mg/kg of MRG003 was administered every 3 weeks during phase 1a. During phase 1b, patients were administered the recommended dose identified in phase 1a.
Related Clinical Trial
NCT Number	NCT04868344	Phase Status	Phase 1
Clinical Description	An open-label, dose-finding, phase 1 study in solid tumors.
Primary Endpoint	The MRG003 recommended dose was 2.50 mg/kg.
Other Endpoint	The objective response rates for SCCHN, NPC, and CRC were 40.00%, 44.00%, and 0.00%, and the disease control rates were 100.00%, 89.00%, and 25.00%, respectively. The median DOR of all patients was 5.60 months (SCCHN: DOR, 5.60 months; 95% CI,2.80-5.60; NPC: not estimable). The median PFS of all patients was 2.80 months (95% CI,1.20-4.10 months), and the PFS of SCCHN, NPC, and CRC was 2.80 (95% CI,0.60-6.80) months, 4.00 (95% CI, 1.20-not reached) months, and 1.20 (95% CI, 0.50-2.80) months, respectively. SCCHN cohort reached the median OS as of the data cutoff date, which was 11.80 (95% CI, 3.40-11.80) months.    Click to Show/Hide
Experiment 2 Reporting the Activity Date of This ADC					[132]
Efficacy Data	Progression Free Survival	4.2 months
Patients Enrolled	Eligible patients (≥18 years) have platinum/anti-PD-1-refractory recurrent/metastatic head and neck squamous cell carcinoma with measurable lesions (RECIST v1.1), ECOG 0-1, and adequate organ function (LVEF≥50%). Excluded are those with ≥4 prior systemic therapies, active CNS metastasis, uncontrolled cardiovascular/bleeding disorders, HBV/HCV/HIV, interstitial lung disease, or recent live vaccines (30 days). Prior anti-tumor therapies within specified washout periods (chemotherapy 3 weeks, targeted therapy 2 weeks, immunotherapy 4 weeks) are prohibited. Strict contraception and negative pregnancy tests are required. The study prioritizes patient safety with rigorous exclusion criteria for comorbidities.    Click to Show/Hide
Administration Dosage	On the first day of every 3 weeks, MRG003 will be administered via intravenous infusion at 2.0 mg/kg calculated based on the actual body weight
Related Clinical Trial
NCT Number	NCT04868162	Phase Status	PHASE2
Clinical Description	An Open-Label, Single Arm, Multi-Center Phase II Clinical Study to Evaluate the Efficacy and Safety of MRG003 in Patients With Recurrent or Metastatic Squamous Cell Carcinoma of Head and Neck.
Primary Endpoint	The primary endpoint is IRC-assessed ORR (complete/partial responses per RECIST v1.1) evaluated over 24 months, with safety monitoring through AEs (45 days post-treatment) regardless of causality.
Other Endpoint	Secondary endpoints include investigator-assessed ORR, PFS/PFSR, DoR, DCR, and OS (24 months), alongside PK parameters (Cmax/AUClast for MRG003, total antibody, and MMAE over 30 days) and ADA immunogenicity incidence. Comprehensive efficacy and pharmacokinetic profiles are evaluated.
Experiment 3 Reporting the Activity Date of This ADC					[134]
Efficacy Data	Progression Free Survival	7.3 months
Patients Enrolled	Eligible patients (18-75 years) have platinum/PD- (L)1-refractory metastatic nasopharyngeal carcinoma (Part A: ≥1 prior line; Part B: ≥2 prior lines including platinum, gemcitabine/taxanes) with measurable lesions (RECIST v1.1), ECOG 0-1, and adequate organ function (LVEF≥50%). Exclusions: grade≥2 neuropathy, active CNS metastases, recent anti-tumor therapy (chemotherapy/targeted therapy within 3 weeks; immunotherapy/radiotherapy within 4 weeks), uncontrolled comorbidities (cardiac, hypertension, diabetes, HBV/HCV/HIV), ILD, or strong CYP3A4 modulators. Strict contraception and negative pregnancy tests (72 hours) are required.    Click to Show/Hide
Administration Dosage	Part A: On the first day of every 3 weeks, MRG003 will be administered via intravenous infusion at 2.0 mg/kg or 2.3 mg/kg calculated based on the actual body weight.Part B: On the first day of every 3 weeks, MRG003 will be administered via intravenous infusion at 2.3 mg/kg calculated based on the actual body weight.
Related Clinical Trial
NCT Number	NCT05126719	Phase Status	PHASE2
Clinical Description	An Open-Label, Multi-Center Phase II Clinical Study to Evaluate the Efficacy and Safety of MRG003 in Patients With Recurrent Metastatic Nasopharyngeal Carcinoma
Primary Endpoint	The primary endpoint is IRC-assessed ORR (complete/partial responses per RECIST v1.1), evaluated from baseline until disease progression, intolerable toxicity, withdrawal, or study discontinuation (up to 24 months), with comprehensive efficacy assessment.
Other Endpoint	Secondary endpoints include investigator-assessed ORR, PFS (time to progression/death), DoR (response duration), DCR (CR/PR/SD rates), and OS (time to death), along with PK parameters (Cmax/AUClast for MRG003, total antibody, and MMAE over 30 days) and ADA immunogenicity incidence, all tracked until progression/discontinuation (24 months). Safety monitoring covers AEs (30 days post-treatment) and SAEs (45 days).    Click to Show/Hide
Experiment 4 Reporting the Activity Date of This ADC					[135]
Efficacy Data	Partial Response (PR)	5 21 %
Patients Enrolled	Eligible patients (18-75 years, ECOG 0-1) include Phase Ia (advanced solid tumors) and Phase Ib (EGFR+ colorectal, HNSCC, or nasopharyngeal cancer) with measurable lesions (RECIST v1.1) and adequate organ function. Exclusions: CNS metastasis, prior malignancies (exceptions apply), uncontrolled systemic/hepatic/cardiac diseases, active HIV, recent anti-tumor therapies/surgeries, high-risk ophthalmic/skin conditions, or pregnancy/breastfeeding. Contraception is mandatory for participants of childbearing potential.    Click to Show/Hide
Administration Dosage	Phase Ia: MRG003 will be administrated by an IV infusion of escalating doses (0.1, 0.3, 0.6, 1.0, 2.0, 2.5, 3.0 mg/kg) on Day 1 of every 3 weeks (Q3W); Phase Ib: MRG003 will be administrated by an IV infusion of MTD/RP2D.
Related Clinical Trial
NCT Number	NCT04868344	Phase Status	PHASE1
Clinical Description	An Open-Label, Dose-Finding, Phase I Study in Solid Tumors.
Primary Endpoint	Phase Ia assesses Dose-Limiting Toxicity (DLT) during the first 21-day cycle, while Phase Ib evaluates Objective Response Rate (ORR) per RECIST v1.1 (CR+PR) over 24 weeks.
Other Endpoint	Pharmacokinetic parameters (Cmax, AUClast) for MRG003, total antibody, and MMAE are analyzed through blood samples with descriptive statistics. Immunogenicity is monitored via anti-drug antibody (ADA) assessments. Phase Ib additionally tracks PFS, DoR, and OS over 24 weeks. Safety includes AE/SAE incidence per NCI-CTCAE v5.0 until 30 days post-treatment.    Click to Show/Hide
Experiment 5 Reporting the Activity Date of This ADC					[135]
Efficacy Data	Partial Response (PR)	23 31 %
Patients Enrolled	Eligible patients (18-75 years, ECOG 0-1) include Phase Ia (advanced solid tumors) and Phase Ib (EGFR+ colorectal, HNSCC, or nasopharyngeal cancer) with measurable lesions (RECIST v1.1) and adequate organ function. Exclusions: CNS metastasis, prior malignancies (exceptions apply), uncontrolled systemic/hepatic/cardiac diseases, active HIV, recent anti-tumor therapies/surgeries, high-risk ophthalmic/skin conditions, or pregnancy/breastfeeding. Contraception is mandatory for participants of childbearing potential.    Click to Show/Hide
Administration Dosage	Phase Ia: MRG003 will be administrated by an IV infusion of escalating doses (0.1, 0.3, 0.6, 1.0, 2.0, 2.5, 3.0 mg/kg) on Day 1 of every 3 weeks (Q3W); Phase Ib: MRG003 will be administrated by an IV infusion of MTD/RP2D.
Related Clinical Trial
NCT Number	NCT04868344	Phase Status	PHASE1
Clinical Description	An Open-Label, Dose-Finding, Phase I Study in Solid Tumors.
Primary Endpoint	Phase Ia assesses Dose-Limiting Toxicity (DLT) during the first 21-day cycle, while Phase Ib evaluates Objective Response Rate (ORR) per RECIST v1.1 (CR+PR) over 24 weeks.
Other Endpoint	Pharmacokinetic parameters (Cmax, AUClast) for MRG003, total antibody, and MMAE are analyzed through blood samples with descriptive statistics. Immunogenicity is monitored via anti-drug antibody (ADA) assessments. Phase Ib additionally tracks PFS, DoR, and OS over 24 weeks. Safety includes AE/SAE incidence per NCI-CTCAE v5.0 until 30 days post-treatment.    Click to Show/Hide
Experiment 6 Reporting the Activity Date of This ADC					[132]
Efficacy Data	Objective Response Rate (ORR)	30.60%
Patients Enrolled	Eligible patients (≥18 years) have platinum/anti-PD-1-refractory recurrent/metastatic head and neck squamous cell carcinoma with measurable lesions (RECIST v1.1), ECOG 0-1, and adequate organ function (LVEF≥50%). Excluded are those with ≥4 prior systemic therapies, active CNS metastasis, uncontrolled cardiovascular/bleeding disorders, HBV/HCV/HIV, interstitial lung disease, or recent live vaccines (30 days). Prior anti-tumor therapies within specified washout periods (chemotherapy 3 weeks, targeted therapy 2 weeks, immunotherapy 4 weeks) are prohibited. Strict contraception and negative pregnancy tests are required. The study prioritizes patient safety with rigorous exclusion criteria for comorbidities.    Click to Show/Hide
Administration Dosage	On the first day of every 3 weeks, MRG003 will be administered via intravenous infusion at 2.0 mg/kg calculated based on the actual body weight
Related Clinical Trial
NCT Number	NCT04868162	Phase Status	PHASE2
Clinical Description	An Open-Label, Single Arm, Multi-Center Phase II Clinical Study to Evaluate the Efficacy and Safety of MRG003 in Patients With Recurrent or Metastatic Squamous Cell Carcinoma of Head and Neck.
Primary Endpoint	The primary endpoint is IRC-assessed ORR (complete/partial responses per RECIST v1.1) evaluated over 24 months, with safety monitoring through AEs (45 days post-treatment) regardless of causality.
Other Endpoint	Secondary endpoints include investigator-assessed ORR, PFS/PFSR, DoR, DCR, and OS (24 months), alongside PK parameters (Cmax/AUClast for MRG003, total antibody, and MMAE over 30 days) and ADA immunogenicity incidence. Comprehensive efficacy and pharmacokinetic profiles are evaluated.
Experiment 7 Reporting the Activity Date of This ADC					[134]
Efficacy Data	Objective Response Rate (ORR)	39.3. 55.2 %
Patients Enrolled	Eligible patients (18-75 years) have platinum/PD- (L)1-refractory metastatic nasopharyngeal carcinoma (Part A: ≥1 prior line; Part B: ≥2 prior lines including platinum, gemcitabine/taxanes) with measurable lesions (RECIST v1.1), ECOG 0-1, and adequate organ function (LVEF≥50%). Exclusions: grade≥2 neuropathy, active CNS metastases, recent anti-tumor therapy (chemotherapy/targeted therapy within 3 weeks; immunotherapy/radiotherapy within 4 weeks), uncontrolled comorbidities (cardiac, hypertension, diabetes, HBV/HCV/HIV), ILD, or strong CYP3A4 modulators. Strict contraception and negative pregnancy tests (72 hours) are required.    Click to Show/Hide
Administration Dosage	Part A: On the first day of every 3 weeks, MRG003 will be administered via intravenous infusion at 2.0 mg/kg or 2.3 mg/kg calculated based on the actual body weight.Part B: On the first day of every 3 weeks, MRG003 will be administered via intravenous infusion at 2.3 mg/kg calculated based on the actual body weight.
Related Clinical Trial
NCT Number	NCT05126719	Phase Status	PHASE2
Clinical Description	An Open-Label, Multi-Center Phase II Clinical Study to Evaluate the Efficacy and Safety of MRG003 in Patients With Recurrent Metastatic Nasopharyngeal Carcinoma
Primary Endpoint	The primary endpoint is IRC-assessed ORR (complete/partial responses per RECIST v1.1), evaluated from baseline until disease progression, intolerable toxicity, withdrawal, or study discontinuation (up to 24 months), with comprehensive efficacy assessment.
Other Endpoint	Secondary endpoints include investigator-assessed ORR, PFS (time to progression/death), DoR (response duration), DCR (CR/PR/SD rates), and OS (time to death), along with PK parameters (Cmax/AUClast for MRG003, total antibody, and MMAE over 30 days) and ADA immunogenicity incidence, all tracked until progression/discontinuation (24 months). Safety monitoring covers AEs (30 days post-treatment) and SAEs (45 days).    Click to Show/Hide
Experiment 8 Reporting the Activity Date of This ADC					[135]
Efficacy Data	Objective Response Rate (ORR)	40 44 0 %
Patients Enrolled	Eligible patients (18-75 years, ECOG 0-1) include Phase Ia (advanced solid tumors) and Phase Ib (EGFR+ colorectal, HNSCC, or nasopharyngeal cancer) with measurable lesions (RECIST v1.1) and adequate organ function. Exclusions: CNS metastasis, prior malignancies (exceptions apply), uncontrolled systemic/hepatic/cardiac diseases, active HIV, recent anti-tumor therapies/surgeries, high-risk ophthalmic/skin conditions, or pregnancy/breastfeeding. Contraception is mandatory for participants of childbearing potential.    Click to Show/Hide
Administration Dosage	Phase Ia: MRG003 will be administrated by an IV infusion of escalating doses (0.1, 0.3, 0.6, 1.0, 2.0, 2.5, 3.0 mg/kg) on Day 1 of every 3 weeks (Q3W); Phase Ib: MRG003 will be administrated by an IV infusion of MTD/RP2D.
Related Clinical Trial
NCT Number	NCT04868344	Phase Status	PHASE1
Clinical Description	An Open-Label, Dose-Finding, Phase I Study in Solid Tumors.
Primary Endpoint	Phase Ia assesses Dose-Limiting Toxicity (DLT) during the first 21-day cycle, while Phase Ib evaluates Objective Response Rate (ORR) per RECIST v1.1 (CR+PR) over 24 weeks.
Other Endpoint	Pharmacokinetic parameters (Cmax, AUClast) for MRG003, total antibody, and MMAE are analyzed through blood samples with descriptive statistics. Immunogenicity is monitored via anti-drug antibody (ADA) assessments. Phase Ib additionally tracks PFS, DoR, and OS over 24 weeks. Safety includes AE/SAE incidence per NCI-CTCAE v5.0 until 30 days post-treatment.    Click to Show/Hide
Experiment 9 Reporting the Activity Date of This ADC					[137]
Efficacy Data	Objective Response Rate (ORR)	63%
Patients Enrolled	Eligible patients (18-75 years, BMI≥17, ECOG 0-1) must have EGFR+ advanced solid tumors (NSCLC, SCCHN, NPC) with measurable lesions (RECIST v1.1), adequate organ function, and life expectancy ≥12 weeks. Exclusions: CNS metastasis, prior MMAE/MMAF ADC treatment, Grade ≥2 neuropathy, uncontrolled systemic/liver/cardiac diseases, active infections (HBV/HCV/HIV), interstitial lung disease, recent major surgery/transplants, pregnancy/breastfeeding, or investigator-assessed ineligibility. Contraception is mandatory for participants of childbearing potential.    Click to Show/Hide
Administration Dosage	Experimental: MRG003+HX008, MRG003 will be administrated via intravenous infusion at 1.5, 2.0 mg/kg (MTD=2.5 mg/kg) once on Day 1 of every 3 weeks (21-day cycle). HX008 will be administrated via intravenous infusion at 3 mg/kg once on Day 1 of every 3 weeks (21-day cycle).
Related Clinical Trial
NCT Number	NCT05688605	Phase Status	PHASE1|||PHASE2
Clinical Description	An Open-label, Multi-center, Phase I/II Dose Escalation and Expansion Study to Evaluate the Safety, Tolerability, Pharmacokinetics and Efficacy of MRG003 in Combination With HX008 in Patients With EGFR-positive Advanced Solid Tumors
Primary Endpoint	The study identifies Maximum Tolerated Dose (MTD) within 21 days of the last patient's first dose in the MTD group, defined as the highest dose with <33% DLT occurrence. The Recommended Phase II Dose (RP2D) is determined based on safety, efficacy, and PK data over 12 months. Objective Response Rate (ORR) is evaluated per RECIST v1.1, measuring the proportion of patients achieving complete response (CR) or partial response (PR).    Click to Show/Hide
Other Endpoint	Secondary outcomes include Duration of Response (DOR), Disease Control Rate (DCR), Progression-Free Survival (PFS), and Overall Survival (OS), all tracked over 12 months. Immunogenicity is assessed via anti-drug antibody (ADA) incidence up to 90 days post-treatment. Safety monitoring covers Adverse Events (AEs) until 30 days and Serious Adverse Events (SAEs) until 90 days post-treatment. PK analysis includes drug concentration-time profiles.    Click to Show/Hide
Experiment 10 Reporting the Activity Date of This ADC					[134]
Efficacy Data	Disease control rate (DCR)	71.4 86.2 %
Patients Enrolled	Eligible patients (18-75 years) have platinum/PD- (L)1-refractory metastatic nasopharyngeal carcinoma (Part A: ≥1 prior line; Part B: ≥2 prior lines including platinum, gemcitabine/taxanes) with measurable lesions (RECIST v1.1), ECOG 0-1, and adequate organ function (LVEF≥50%). Exclusions: grade≥2 neuropathy, active CNS metastases, recent anti-tumor therapy (chemotherapy/targeted therapy within 3 weeks; immunotherapy/radiotherapy within 4 weeks), uncontrolled comorbidities (cardiac, hypertension, diabetes, HBV/HCV/HIV), ILD, or strong CYP3A4 modulators. Strict contraception and negative pregnancy tests (72 hours) are required.    Click to Show/Hide
Administration Dosage	Part A: On the first day of every 3 weeks, MRG003 will be administered via intravenous infusion at 2.0 mg/kg or 2.3 mg/kg calculated based on the actual body weight.Part B: On the first day of every 3 weeks, MRG003 will be administered via intravenous infusion at 2.3 mg/kg calculated based on the actual body weight.
Related Clinical Trial
NCT Number	NCT05126719	Phase Status	PHASE2
Clinical Description	An Open-Label, Multi-Center Phase II Clinical Study to Evaluate the Efficacy and Safety of MRG003 in Patients With Recurrent Metastatic Nasopharyngeal Carcinoma
Primary Endpoint	The primary endpoint is IRC-assessed ORR (complete/partial responses per RECIST v1.1), evaluated from baseline until disease progression, intolerable toxicity, withdrawal, or study discontinuation (up to 24 months), with comprehensive efficacy assessment.
Other Endpoint	Secondary endpoints include investigator-assessed ORR, PFS (time to progression/death), DoR (response duration), DCR (CR/PR/SD rates), and OS (time to death), along with PK parameters (Cmax/AUClast for MRG003, total antibody, and MMAE over 30 days) and ADA immunogenicity incidence, all tracked until progression/discontinuation (24 months). Safety monitoring covers AEs (30 days post-treatment) and SAEs (45 days).    Click to Show/Hide
Experiment 11 Reporting the Activity Date of This ADC					[137]
Efficacy Data	Disease control rate (DCR)	88.90%
Patients Enrolled	Eligible patients (18-75 years, BMI≥17, ECOG 0-1) must have EGFR+ advanced solid tumors (NSCLC, SCCHN, NPC) with measurable lesions (RECIST v1.1), adequate organ function, and life expectancy ≥12 weeks. Exclusions: CNS metastasis, prior MMAE/MMAF ADC treatment, Grade ≥2 neuropathy, uncontrolled systemic/liver/cardiac diseases, active infections (HBV/HCV/HIV), interstitial lung disease, recent major surgery/transplants, pregnancy/breastfeeding, or investigator-assessed ineligibility. Contraception is mandatory for participants of childbearing potential.    Click to Show/Hide
Administration Dosage	Experimental: MRG003+HX008, MRG003 will be administrated via intravenous infusion at 1.5, 2.0 mg/kg (MTD=2.5 mg/kg) once on Day 1 of every 3 weeks (21-day cycle). HX008 will be administrated via intravenous infusion at 3 mg/kg once on Day 1 of every 3 weeks (21-day cycle).
Related Clinical Trial
NCT Number	NCT05688605	Phase Status	PHASE1|||PHASE2
Clinical Description	An Open-label, Multi-center, Phase I/II Dose Escalation and Expansion Study to Evaluate the Safety, Tolerability, Pharmacokinetics and Efficacy of MRG003 in Combination With HX008 in Patients With EGFR-positive Advanced Solid Tumors
Primary Endpoint	The study identifies Maximum Tolerated Dose (MTD) within 21 days of the last patient's first dose in the MTD group, defined as the highest dose with <33% DLT occurrence. The Recommended Phase II Dose (RP2D) is determined based on safety, efficacy, and PK data over 12 months. Objective Response Rate (ORR) is evaluated per RECIST v1.1, measuring the proportion of patients achieving complete response (CR) or partial response (PR).    Click to Show/Hide
Other Endpoint	Secondary outcomes include Duration of Response (DOR), Disease Control Rate (DCR), Progression-Free Survival (PFS), and Overall Survival (OS), all tracked over 12 months. Immunogenicity is assessed via anti-drug antibody (ADA) incidence up to 90 days post-treatment. Safety monitoring covers Adverse Events (AEs) until 30 days and Serious Adverse Events (SAEs) until 90 days post-treatment. PK analysis includes drug concentration-time profiles.    Click to Show/Hide
Experiment 12 Reporting the Activity Date of This ADC					[135]
Efficacy Data	Disease control rate (DCR)	100 89 25 %
Patients Enrolled	Eligible patients (18-75 years, ECOG 0-1) include Phase Ia (advanced solid tumors) and Phase Ib (EGFR+ colorectal, HNSCC, or nasopharyngeal cancer) with measurable lesions (RECIST v1.1) and adequate organ function. Exclusions: CNS metastasis, prior malignancies (exceptions apply), uncontrolled systemic/hepatic/cardiac diseases, active HIV, recent anti-tumor therapies/surgeries, high-risk ophthalmic/skin conditions, or pregnancy/breastfeeding. Contraception is mandatory for participants of childbearing potential.    Click to Show/Hide
Administration Dosage	Phase Ia: MRG003 will be administrated by an IV infusion of escalating doses (0.1, 0.3, 0.6, 1.0, 2.0, 2.5, 3.0 mg/kg) on Day 1 of every 3 weeks (Q3W); Phase Ib: MRG003 will be administrated by an IV infusion of MTD/RP2D.
Related Clinical Trial
NCT Number	NCT04868344	Phase Status	PHASE1
Clinical Description	An Open-Label, Dose-Finding, Phase I Study in Solid Tumors.
Primary Endpoint	Phase Ia assesses Dose-Limiting Toxicity (DLT) during the first 21-day cycle, while Phase Ib evaluates Objective Response Rate (ORR) per RECIST v1.1 (CR+PR) over 24 weeks.
Other Endpoint	Pharmacokinetic parameters (Cmax, AUClast) for MRG003, total antibody, and MMAE are analyzed through blood samples with descriptive statistics. Immunogenicity is monitored via anti-drug antibody (ADA) assessments. Phase Ib additionally tracks PFS, DoR, and OS over 24 weeks. Safety includes AE/SAE incidence per NCI-CTCAE v5.0 until 30 days post-treatment.    Click to Show/Hide
Experiment 13 Reporting the Activity Date of This ADC					[146]
Patients Enrolled	Eligible patients (18-75 years) had EGFR-positive, unresectable/metastatic biliary tract cancer refractory to ≥1 prior therapy, with measurable lesions (RECIST v1.1), ECOG 0-1, and adequate organ function. Key exclusions included biliary obstruction, uncontrolled effusions/CNS metastasis, active infections, severe ocular/skin/pulmonary diseases, autoimmune disorders requiring immunosuppression, or prior anti-tumor therapy within 4 weeks. Treatment-related toxicities (except alopecia/asymptomatic labs) had to resolve to ≤Grade 1 (CTCAE v5.0). Pregnancy and decompensated cirrhosis (Child-Pugh B/C) were exclusionary.    Click to Show/Hide
Administration Dosage	MRG003 will be administrated via IV infusion at 2.0 mg/kg on Day 1 of every 3 weeks (21-day cycle).
Related Clinical Trial
NCT Number	NCT04838964	Phase Status	PHASE2
Clinical Description	An Open-label, Single-arm, Multi-center, Phase II Clinical Study of MRG003 in the Treatment of Patients With EGFR-positive Unresectable, Locally Advanced or Metastatic Biliary Tract Cancer
Primary Endpoint	The primary endpoint was IRC-assessed Objective Response Rate (ORR) per RECIST v1.1, evaluating complete and partial responses over 12 months from baseline.
Other Endpoint	Secondary efficacy endpoints included investigator-assessed ORR, Duration of Response (DoR), Time to Response (TTR), Disease Control Rate (DCR), Progression-Free Survival (PFS), and Overall Survival (OS). Safety assessments covered adverse events (30 days post-treatment), pharmacokinetic analysis of MRG003 (concentration-time curves), and incidence of anti-drug antibodies (ADA) in treated patients.    Click to Show/Hide
Experiment 14 Reporting the Activity Date of This ADC					[147]
Patients Enrolled	Eligible patients (18-75 years) have EGFR+/HER2- locally advanced/metastatic gastric adenocarcinoma with measurable lesions (RECIST v1.1), ECOG 0-1, adequate organ function (LVEF≥50%), and negative pregnancy tests. Exclusions: prior EGFR-targeted therapy hypersensitivity (4 weeks), active CNS metastasis, uncontrolled effusions/hemorrhage, severe infections (HBV/HCV/HIV), interstitial lung disease, Child-Pugh B/C cirrhosis, live vaccines (30 days), or grade≥2 peripheral neuropathy (CTCAE v5.0). Systemic anti-tumor therapy within 4 weeks or CYP3A4 modifiers prohibited.    Click to Show/Hide
Administration Dosage	On the first day of every 3 weeks, MRG003 will be administered via intravenous infusion at 2.0 mg/kg calculated based on the actual body weight
Related Clinical Trial
NCT Number	NCT05188209	Phase Status	PHASE2
Clinical Description	A Phase II Clinical Study to Evaluate the Efficacy and Safety of MRG003 in EGFR-Positive, HER2-Negative Advanced Gastric Cancer.
Primary Endpoint	The primary endpoints are IRC-assessed ORR (complete/partial responses per RECIST v1.1) over 24 months and adverse events monitoring (30 days for AEs, 45 days for SAEs post-treatment) regardless of causality.
Other Endpoint	Key secondary endpoints include investigator-assessed ORR, PFS, DoR, DCR, and OS over 24 months. Pharmacokinetic analysis evaluates Cmax/AUClast for MRG003, total antibody, and MMAE (30 days post-treatment), alongside ADA immunogenicity rates.
Experiment 15 Reporting the Activity Date of This ADC					[148]
Patients Enrolled	Eligible patients (18-75 years) must have PD-1/platinum-refractory metastatic head and neck squamous cell carcinoma (≤2 prior lines), measurable lesions (RECIST v1.1), ECOG 0-1, and adequate organ function (LVEF≥50%). Exclusions: grade≥2 neuropathy, active CNS metastases, recent anti-tumor therapy (chemotherapy within 3 weeks; immunotherapy within 4 weeks), uncontrolled comorbidities (cardiac, hypertension, diabetes, HBV/HCV/HIV), recent major surgery, or effusions requiring monthly drainage. Strict contraception and pregnancy testing are mandatory.    Click to Show/Hide
Administration Dosage	MRG003 will be administrated via intravenous infusion at 2.3 mg/kg once on Day 1 of every 3 weeks (21-day cycle).
Related Clinical Trial
NCT Number	NCT05751512	Phase Status	PHASE3
Clinical Description	A Randomized, Open-Label, Multicenter, Phase III Study to Evaluate MRG003 vs Cetuximab/Methotrexate as Second/Third Line of Treatment in Patient With Recurrent or Metastatic Squamous Cell Carcinoma of the Head and Neck (RM-SCCHN)
Primary Endpoint	The primary endpoint is Overall Survival (OS), defined as the time from treatment initiation to death from any cause, measured over 24 months.
Other Endpoint	Secondary endpoints include Progression-Free Survival (PFS), Objective Response Rate (ORR), Disease Control Rate (DCR), Duration of Response (DOR), Treatment-Related Adverse Events (TRAEs), general Adverse Events (AEs), Serious Adverse Events (SAEs) with 30-90-day monitoring, and Quality of Life (QOL) assessments per RECIST v1.1, all tracked over 24 months.    Click to Show/Hide
Experiment 16 Reporting the Activity Date of This ADC					[149]
Patients Enrolled	Eligible patients (18-75 years) must have CDKN2A-deficient, PD-1/platinum-refractory recurrent/metastatic HNSCC (≤2 prior lines), measurable lesions by RECIST v1.1, ECOG 0-1, and adequate organ function. Key exclusions: active CNS metastases, recent anti-cancer therapies (chemotherapy <3 weeks, immunotherapy <4 weeks), uncontrolled comorbidities (cardiac, HBV/HCV, HIV), uncontrolled effusions, or grade≥2 neuropathy. Pregnancy testing and contraception are mandatory.    Click to Show/Hide
Administration Dosage	MRG003, intravenous infusion, D1, once every 3 weeks; Dalpicicilip, taking orally, D1-21, once every 4 weeks, maintain use until progression or emergence of intolerable toxicity.
Related Clinical Trial
NCT Number	NCT06509997	Phase Status	PHASE2
Clinical Description	MRG003 Combined With Dalpicicilip Posterior Line in the Treatment of Recurrent/Metastatic CDKN2A Gene Variant Head and Neck Squamous Cell Carcinoma: A Phase II Clinical Trial
Primary Endpoint	The co-primary endpoints are Objective Response Rate (ORR) assessed by RECIST v1.1 and Safety/Tolerability measured by treatment-related adverse events (CTCAE v5.0), both evaluated approximately 9-10 weeks after treatment initiation.
Other Endpoint	Secondary endpoints include Overall Survival (OS) over 2 years, Progression-Free Survival (PFS) and Duration of Response (DOR) monitored for 1-2 years, and Disease Control Rate (DCR) assessed at 2 years.
Experiment 17 Reporting the Activity Date of This ADC					[150]
Patients Enrolled	Eligible patients (18-70 years, ECOG 0-1) must have untreated, surgically resectable EGFR+ HNSCC (Stage III-IVB non-oropharyngeal or Stage II-III HPV+ oropharyngeal cancer). Key exclusions: prior HNSCC treatment, active infections (HBV/HCV/HIV), grade≥2 neuropathy, recent major surgery/immunotherapy, uncontrolled cardiovascular disease, autoimmune disorders requiring immunosuppressants, or history of interstitial lung disease/allogeneic transplants. Adequate organ function and contraception are required.    Click to Show/Hide
Related Clinical Trial
NCT Number	NCT06530914	Phase Status	PHASE2
Clinical Description	A Phase II Study of MRG003 Injection Combined With Pucotenlimab Injection &plusmn; Cisplatin Injection in the Neoadjuvant Treatment Locally Advanced EGFR-positive Head and Neck Squamous Cell Carcinoma
Primary Endpoint	The primary endpoint is pathological complete response (pCR) rate, evaluated post-surgery at approximately 9-10 weeks after treatment initiation.
Other Endpoint	Secondary endpoints include 1-year Event-Free Survival (EFS), Objective Response Rate (ORR) at 9-10 weeks, 2-year Overall Survival (OS), safety profiles (AE/SAE/irAE incidence per CTCAE v5.0), surgical outcomes (90-day AE/SAE rates, delays), and proportion of patients achieving clinical stage reduction after neoadjuvant therapy.
Experiment 18 Reporting the Activity Date of This ADC					[151]
Patients Enrolled	Eligible patients (≥18 years, ECOG 0-1) must have EGFR+ advanced NSCLC (post ≥2 prior therapies) with measurable lesions (RECIST v1.1), adequate organ function, and controlled AEs (≤Grade 1 per CTCAE v5.0). Key exclusions: untreated CNS metastasis, active infections (HBV/HCV/HIV), severe cardiac/pulmonary disease (ILD, COPD), unresolved effusions, ongoing immunosuppressive therapy, prior EGFR-related eye/skin toxicities, or allogeneic transplants. Contraception is mandatory for patients of childbearing potential. Investigators may exclude patients with conditions compromising safety or compliance.    Click to Show/Hide
Administration Dosage	On the first day of every 3 weeks, MRG003 will be administered via intravenous infusion at 2.0 mg/kg calculated based on the actual body weight
Related Clinical Trial
NCT Number	NCT04838548	Phase Status	PHASE2
Clinical Description	An Open-Label, Multi-Cohort, Multi-center, Non-Randomized, Phase II Clinical Study to Evaluate the Efficacy and Safety of MRG003 in Patients With EGFR-Positive Advanced Non-Small Cell Lung Cancer
Primary Endpoint	The primary endpoint is Objective Response Rate (ORR) assessed per RECIST v1.1, defined as the proportion of patients achieving complete response (CR) or partial response (PR), evaluated from baseline to study completion (up to 12 months).
Other Endpoint	Secondary endpoints include Progression-Free Survival (PFS), Duration of Response (DoR), Time to Response (TTR), Disease Control Rate (DCR) (CR+PR+SD), and Overall Survival (OS), all measured over 12 months. Safety assessments involve monitoring Adverse Events (AEs) from baseline until 60 days post-treatment, including reactions, side effects, or any clinical trial events, regardless of drug-related causality.    Click to Show/Hide

Experiment 1 Reporting the Activity Date of This ADC					[152]
Efficacy Data	Objective Response Rate (ORR)	75%
Patients Enrolled	Patients with advanced malignant tumors.
Administration Dosage	Day 1 in 3-week (Q3W) cycle 3.40 mg/kg.
Related Clinical Trial
NCT Number	NCT04805307	Phase Status	Phase 1
Clinical Description	An open-label, phase 1, dose escalation and dose expansion study to evaluate the safety, tolerability, pharmacokinetics and antitumor activities of CMG901 in subjects with advanced unresectable or metastatic solid tumor.
Experiment 2 Reporting the Activity Date of This ADC					[165]
Efficacy Data	Objective Response Rate (ORR)	29%
Patients Enrolled	Eligibility requires ECOG 0-1, advanced solid tumors (Part A: measurable/evaluable; Part B: confirmed Claudin 18.2+ lesions). Key exclusions: recent anticancer therapies (<28 days), active infections/CNS metastases, neuropathy ≥Grade 2, uncontrolled effusions, HBV/HCV viremia, or QTc >480msec. Contraception is mandated for reproductive-age participants.    Click to Show/Hide
Administration Dosage	CMG901 will be administered intravenously (IV) on Day 1 of every 21-day cycle. Individual subjects may continue study treatment until confirmed Progressive Disease (PD), unacceptable toxicity, initiation of new anti-tumor therapy, withdrawal from the study, or death, whichever occurs first.
Related Clinical Trial
NCT Number	NCT04805307	Phase Status	PHASE1
Clinical Description	An Open-Label, Phase 1, Dose Escalation and Dose Expansion Study to Evaluate the Safety, Tolerability, Pharmacokinetics and Antitumor Activities of CMG901 in Subjects With Advanced Unresectable or Metastatic Solid Tumor
Primary Endpoint	Part A evaluates safety endpoints including AE incidence, lab abnormalities (30 days post-treatment), and MTD determination (21-day DLT window). Part B focuses on preliminary efficacy (ORR per RECIST v1.1) and RP2D establishment for Claudin 18.2+ advanced solid tumors over 24 months.
Other Endpoint	Comprehensive PK analysis covers AUC (0-last/tau/inf), Cmax, Tmax, clearance, and volume parameters through 24 months, alongside immunogenicity (anti-CMG901 antibodies). Secondary endpoints include DCR, DoR, PFS, OS, and Claudin 18.2 expression correlation, with Part B adding NCI CTCAE v5.0 safety monitoring.
Experiment 3 Reporting the Activity Date of This ADC					[181]
Patients Enrolled	Eligible participants (≥18yo, ECOG 0-1) required CLDN18.2+ lesions (RECIST v1.1), adequate organ function (>35kg). Substudies targeted specific cancers: GC/GEJC (≤2 prior lines), PDAC (treatment-naïve metastatic), biliary tract (1-2 prior lines). Key exclusions: active GI bleeding, ascites, ILD history, CNS metastases, prior MMAE-ADC/CLDN18.2 therapy (except antibodies), QTc risks (Substudy 1), UGT1A1/CYP3A4 interactions (Substudy 2), or biliary obstruction (Substudy 3).    Click to Show/Hide
Administration Dosage	Substudy 1 is recruiting patients with human epidermal growth factor receptor 2 (HER2)-negative, CLDN18.2-expressing G/GEJ cancer with ≤2 prior lines of therapy for unresectable or metastatic disease, who are randomized 1:1 to receive AZD0901 1.8 or 2.2 mg/kg intravenous (IV) every 3 weeks (Q3W).
Related Clinical Trial
NCT Number	NCT06219941	Phase Status	PHASE2
Clinical Description	A Phase II, Open-label, Multi-centre Study to Evaluate Safety, Tolerability, Efficacy, PK, and Immunogenicity of AZD0901 as Monotherapy and in Combination With Anti-cancer Agents in Participants With Advanced Solid Tumours Expressing Claudin 18.2 (CLARITY-PanTumour01)
Primary Endpoint	Safety monitoring included AEs/SAEs, lab/vital sign changes, DLTs (30 days post-treatment; AE follow-up for 90 days). Primary objective assessed AZD0901's safety (monotherapy/combination) in CLDN18.2+ advanced/metastatic solid tumors, analyzing discontinuation rates and tolerability.
Other Endpoint	Efficacy measures included ORR (RECIST v1.1), OS, PFS (both ~2 years), DoR, DCR (11-week landmark), and tumor shrinkage percentage. PK analysis covered serum concentrations (AZD0901/MMAE) and parameters (AUC/Cmax/tmax) until 90 days post-treatment, alongside immunogenicity (ADA) and biomarker correlations (tissue-based RNA/DNA/proteins) during early treatment.    Click to Show/Hide

Experiment 1 Reporting the Activity Date of This ADC					[153]
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NCT Number	NCT04826107	Phase Status	Phase 2
Clinical Description	An open-label, multicentre, phase 2 study of DP303c injection in patients with unresectable locally advanced, recurrent or metastatic gastric cancer with HER2 expression.
Experiment 2 Reporting the Activity Date of This ADC					[154]
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NCT Number	NCT04828616	Phase Status	Phase 2
Clinical Description	An open-label, multicentre, phase 2 study of DP303c injection in patients with HER2-expressing advanced ovarian cancer.
Experiment 3 Reporting the Activity Date of This ADC					[155]
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NCT Number	NCT05334810	Phase Status	Phase 2
Clinical Description	A multi-center, open-lable, single-arm phase 2 study to evaluate the efficacy and safety of DP303c in patients with HER2-positive unresectable locally advanced, relapsed, or metastatic breast cancer.
Experiment 4 Reporting the Activity Date of This ADC					[158]
Related Clinical Trial
NCT Number	NCT04146610	Phase Status	Phase 1
Clinical Description	A phase 1a, multicenter, open and dose-increasing study of DP303c to evaluate the safety , pharmacokinetics, immunogenicity and antitumor activity of subjects with HER2-positive advanced solid tumors.
Experiment 5 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Tumor-associated calcium signal transducer 2 (TACSTD2)	. . .
Patients Enrolled	Eligibility requires age ≥18 with ECOG 0-1, HER2+ advanced solid tumors, prior anti-HER2 therapy, and adequate organ function. Key exclusions: LVEF<40%, grade ≥3 neuropathy, active hepatitis/HIV, recent CYP3A modulators (14 days), anthracycline overexposure, or uncontrolled CNS metastases. Contraception mandated for 6 months post-treatment.
Administration Dosage	DP303c injection, 3.0 mg/kg, every 3 weeks.
Related Clinical Trial
NCT Number	NCT05810103	Phase Status	PHASE1
Clinical Description	A Multi-center, Single-arm, Phase I Study of DP303c in Patients With HER2-positive Advanced Solid Tumors
Primary Endpoint	Primary pharmacokinetic endpoints include Cmax, AUC0-last, AUC0-inf, and Tmax of the investigational drug measured during multiple dosing cycles (21-day cycles) in patients with HER2-positive advanced solid tumors.
Other Endpoint	Secondary endpoints assess safety (AE incidence over 12 months), efficacy (ORR, DCR, DoR over 12 months), and immunogenicity (ADA/Nab incidence measured during treatment cycles) in this phase I clinical trial.
Experiment 6 Reporting the Activity Date of This ADC					[161]
Efficacy Data	Progression Free Survival	4.44 months
Patients Enrolled	Inclusion: HER2+ (IHC2+/ISH+ or IHC3+) advanced solid tumor patients aged 18-75 with ECOG 0-1, adequate organ function, measurable disease. Exclusion: Active CNS metastases, LVEF<40%, ≥Grade 2 neuropathy, uncontrolled cardiac/electrolyte disorders, active hepatitis/HIV, recent CYP3A modulators (14 days), or anthracycline exposure ≥360mg/m2 doxorubicin equivalent. Contraception required for 12 weeks post-treatment.    Click to Show/Hide
Related Clinical Trial
NCT Number	NCT04146610	Phase Status	PHASE1
Clinical Description	A Phase Ia, Multicenter, Open and Dose-increasing Study of DP303c to Evaluate the Safety , Pharmacokinetics, Immunogenicity and Antitumor Activity of Subjects With HER2-Positive Advanced Solid Tumors
Primary Endpoint	Primary endpoint is MTD determination of DP303c during the first 21-day cycle, defined as the highest dose where <2/6 patients experience DLT in advanced HER2+ solid tumors.
Other Endpoint	Secondary endpoints include PK parameters (Cmax, Tmax, AUC over 2 years), preliminary efficacy (ORR, DoR), and immunogenicity (ADA incidence) in this Phase I study.
Experiment 7 Reporting the Activity Date of This ADC					[161]
Efficacy Data	Objective Response Rate (ORR)	42.90%
Patients Enrolled	Inclusion: HER2+ (IHC2+/ISH+ or IHC3+) advanced solid tumor patients aged 18-75 with ECOG 0-1, adequate organ function, measurable disease. Exclusion: Active CNS metastases, LVEF<40%, ≥Grade 2 neuropathy, uncontrolled cardiac/electrolyte disorders, active hepatitis/HIV, recent CYP3A modulators (14 days), or anthracycline exposure ≥360mg/m2 doxorubicin equivalent. Contraception required for 12 weeks post-treatment.    Click to Show/Hide
Related Clinical Trial
NCT Number	NCT04146610	Phase Status	PHASE1
Clinical Description	A Phase Ia, Multicenter, Open and Dose-increasing Study of DP303c to Evaluate the Safety , Pharmacokinetics, Immunogenicity and Antitumor Activity of Subjects With HER2-Positive Advanced Solid Tumors
Primary Endpoint	Primary endpoint is MTD determination of DP303c during the first 21-day cycle, defined as the highest dose where <2/6 patients experience DLT in advanced HER2+ solid tumors.
Other Endpoint	Secondary endpoints include PK parameters (Cmax, Tmax, AUC over 2 years), preliminary efficacy (ORR, DoR), and immunogenicity (ADA incidence) in this Phase I study.
Experiment 8 Reporting the Activity Date of This ADC					[161]
Efficacy Data	Disease control rate (DCR)	68.10%
Patients Enrolled	Inclusion: HER2+ (IHC2+/ISH+ or IHC3+) advanced solid tumor patients aged 18-75 with ECOG 0-1, adequate organ function, measurable disease. Exclusion: Active CNS metastases, LVEF<40%, ≥Grade 2 neuropathy, uncontrolled cardiac/electrolyte disorders, active hepatitis/HIV, recent CYP3A modulators (14 days), or anthracycline exposure ≥360mg/m2 doxorubicin equivalent. Contraception required for 12 weeks post-treatment.    Click to Show/Hide
Related Clinical Trial
NCT Number	NCT04146610	Phase Status	PHASE1
Clinical Description	A Phase Ia, Multicenter, Open and Dose-increasing Study of DP303c to Evaluate the Safety , Pharmacokinetics, Immunogenicity and Antitumor Activity of Subjects With HER2-Positive Advanced Solid Tumors
Primary Endpoint	Primary endpoint is MTD determination of DP303c during the first 21-day cycle, defined as the highest dose where <2/6 patients experience DLT in advanced HER2+ solid tumors.
Other Endpoint	Secondary endpoints include PK parameters (Cmax, Tmax, AUC over 2 years), preliminary efficacy (ORR, DoR), and immunogenicity (ADA incidence) in this Phase I study.
Experiment 9 Reporting the Activity Date of This ADC					[173]
Patients Enrolled	Inclusion: HER2+ breast cancer patients (IHC 3+ or IHC 2+/ISH+) aged 18-75 with ≥2 prior anti-HER2 lines (including trastuzumab), measurable disease, ECOG 0-1, LVEF≥50%, and adequate organ function. Exclusion: Prior DP303c treatment, active CNS metastases, LVEF<40% history, uncontrolled comorbidities, recent anticancer therapies (4w chemo/2w endocrine), active infections (HBV/HCV), or CYP3A modulator use within 14 days. Contraception required for 6 months post-treatment.    Click to Show/Hide
Administration Dosage	DP303c injection, 3.0 mg/kg, every 3 weeks.
Related Clinical Trial
NCT Number	NCT05334810	Phase Status	PHASE2
Clinical Description	A Multi-center, Open-lable, Single-arm Phase II Study to Evaluate the Efficacy and Safety of DP303c in Patients With HER2-positive Unresectable Locally Advanced, Relapsed, or Metastatic Breast Cancer
Primary Endpoint	Primary endpoint is ORR assessed by IRC per RECIST v1.1 with tumor evaluations every 6 weeks from baseline.
Other Endpoint	Secondary endpoints include DOR and PFS measured at 6-week intervals from baseline until progression.
Experiment 10 Reporting the Activity Date of This ADC					[174]
Patients Enrolled	Inclusion: HER2+ breast cancer patients (IHC 3+/ISH+) aged ≥18 with ≥2 prior systemic therapies, measurable disease, ECOG 0-1, adequate organ function. Exclusion: Pregnancy, recent anticancer treatments (28d systemic/14d TCM therapy), active CNS metastases, LVEF<40%, severe comorbidities (cardiopulmonary/neuropathic/ocular), active infections (HBV/HCV/HIV), or CYP3A modulator use. Contraception required during study participation.    Click to Show/Hide
Administration Dosage	Eligible patients will be treated with trastuzumab IV on day 1 and oral capecitabine twice daily on days 1-14 every 3 weeks, or patients will be treated with trastuzumab IV on day 1 and vinorelbine IV over on days 1 and 8 every 3 weeks.
Related Clinical Trial
NCT Number	NCT05901935	Phase Status	PHASE3
Clinical Description	A Multicentre, Randomized, Open-label, Controlled Phase III Clinical Study to Evaluate the Efficacy and Safety of DP303cversus Trastuzumab Combined With Vinorelbine/Capecitabine in of HER2-positive Advanced Breast Cancer
Primary Endpoint	Primary endpoint is PFS assessed by BIRC per RECIST v1.1 with follow-up up to 5 years.
Other Endpoint	Secondary endpoints include investigator-assessed PFS, OS, ORR, DoR (all evaluated per RECIST v1.1 over 5 years), and AE incidence/severity monitoring throughout the study period.
Experiment 11 Reporting the Activity Date of This ADC					[175]
Patients Enrolled	Inclusion: HER2+ (IHC3+/ISH+) breast cancer patients ≥18 years with prior trastuzumab/taxane treatment, ECOG 0-2, adequate organ function. Exclusion: Prior HER2-ADC therapy, active CNS metastases, uncontrolled effusions, Grade≥2 neuropathy, recent anticancer therapies (4w immunotherapy/2w chemotherapy), ocular/cardiopulmonary comorbidities, or active infections requiring IV treatment.    Click to Show/Hide
Administration Dosage	DP303c injection, 3.0 mg/kg, Q3W.
Related Clinical Trial
NCT Number	NCT06313086	Phase Status	PHASE3
Clinical Description	A Multicentre, Randomized, Open-label, Controlled Phase III Clinical Study to Evaluate the Efficacy and Safety of DP303c Versus Trastuzumab Emtansine in Patients With HER2-positive Advanced Breast Cancer
Primary Endpoint	Primary endpoint is BIRC-assessed PFS per RECIST v1.1 with 4-year follow-up in HER2+ advanced/metastatic breast cancer patients.
Other Endpoint	Secondary endpoints include investigator-assessed PFS, OS, ORR, DoR (all per RECIST v1.1) and AE monitoring over 4 years, evaluating both efficacy and safety outcomes.
Experiment 12 Reporting the Activity Date of This ADC					[176]
Patients Enrolled	Eligibility requires age 18-75 with progressed gastric cancer after 1-2 prior therapies (including platinum/fluorouracil), measurable lesions, and organ function adequacy. Key exclusions: trastuzumab intolerance, uncontrolled effusions, active CNS metastases, ≥Grade 2 neuropathy, recent CYP3A4/UGT1A1 modulator use, or significant ocular/cardiovascular comorbidities.    Click to Show/Hide
Administration Dosage	DP303c injection, dose level 1, intravenous drip, Q3W + simmitinib tablets, dose level 1, oral, QD, taken for 3 weeks, discontinued for 1 week, Q4W
Related Clinical Trial
NCT Number	NCT06577376	Phase Status	PHASE1|||PHASE2
Clinical Description	A Multicenter, Open-label Phase I/II Clinical Study to Evaluate the Safety and Efficacy of Simmitinib or Irinotecan Liposomes Combined With DP303c Injection in the Treatment of HER2 Expressing Gastric Adenocarcinoma or Gastroesophageal Junction Adenocarcinoma
Primary Endpoint	Primary endpoints include DLT occurrence/incidence, AE/SAE monitoring, and ORR per RECIST 1.1 assessed over 36 months in HER2-positive (IHC 1+/2+/3+) gastric/GEJ adenocarcinoma patients.
Other Endpoint	Secondary outcomes comprise efficacy measures (DCR, DoR, PFS, OS) and pharmacokinetic evaluations (DP303c/simmitinib concentrations, ADA incidence, HER2 expression) tracked for 36 months.
Experiment 13 Reporting the Activity Date of This ADC					[177]
Patients Enrolled	Inclusion: Age 18-75 with histologically confirmed advanced gastric cancer, ECOG 0-1, adequate organ function, measurable lesions (RECIST v1.1), and progression after platinum/taxane-based therapy (HER2-positive cohorts require prior trastuzumab). Exclusion: Active CNS metastases, uncontrolled effusions, ≥Grade 2 neuropathy, cardiac dysfunction (LVEF<50%), recent CYP3A4 modulators, or prior HER2-ADC therapy. Contraception required for 6 months post-treatment.    Click to Show/Hide
Administration Dosage	Patients with HER2-positive advanced or metastatic gastric cancer after receiving 1st-line treatment will be treated with DP303c injection at 2.0 mg/kg,2.5 mg/kg or 3.0 mg/kg every 3 weeks to determine the recommended dose.
Related Clinical Trial
NCT Number	NCT04826107	Phase Status	PHASE2
Clinical Description	An Open-label, Multicentre, Phase II Study of DP303c Injection in Patients With Unresectable Locally Advanced, Recurrent or Metastatic Gastric Cancer With HER2 Expression
Primary Endpoint	Primary endpoint is ORR (CR+PR rate) assessed over 2.5 years in HER2-positive/low-expression gastric/GEJ adenocarcinoma patients with progression after ≥1 prior therapy.
Other Endpoint	Secondary endpoints include PFS, OS, DCR, DoR (all measured over 2.5 years) and AE/SAE monitoring, evaluating both efficacy and safety outcomes in this multicenter trial.
Experiment 14 Reporting the Activity Date of This ADC					[178]
Patients Enrolled	Inclusion: Women aged 18-75 with ECOG 0-2, measurable lesions (RECIST v1.1), adequate organ function, and HER2 IHC 1+/2+/3+ status. Exclusion: Active CNS metastases, ≥Grade 2 neuropathy, LVEF<50%, uncontrolled effusions, recent CYP3A4 modulators (28 days), prior HER2-ADC therapy, or anthracycline exposure >500mg/m2 doxorubicin equivalent. Contraception required for 6 months post-treatment.    Click to Show/Hide
Administration Dosage	Part1:Patients with HER2-expressing advanced ovarian cancer will be treated with DP303c injection at 2.0 mg/kg or 3.0 mg/kg every 3 weeks (Q3W) to determine the recommended phase 2 dose (RP2D).Part2a:Patients with HER2-overexpressing advanced ovarian cancer will be treated with DP303c injection at RP2D.Part2b:Patients with HER2-lowexpressing advanced ovarian cancer will be treated with DP303c injection at RP2D.    Click to Show/Hide
Related Clinical Trial
NCT Number	NCT04828616	Phase Status	PHASE2
Clinical Description	An Open-label, Multicentre, Phase II Study of DP303c Injection in Patients With HER2-expressing Advanced Ovarian Cancer
Primary Endpoint	Primary endpoint is ORR (CR+PR rate) assessed over 3 years in HER2-positive/low-expressing ovarian/tubal/peritoneal cancer patients with prior platinum therapy.
Other Endpoint	Secondary endpoints include PFS, OS, DoR (3-year follow-up), AE/SAE monitoring (NCI-CTCAE v5.0), PK parameters (Cmax/Tmax/AUC of DP303c), and ADA incidence in this phase I/II study.

Experiment 1 Reporting the Activity Date of This ADC					[159]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 7.60%	Moderate HER2 expression (HER2++)
Method Description	DP001 (10 mg/kg).
In Vivo Model	JIMT -1 cell line xenograft model
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 2 Reporting the Activity Date of This ADC					[159]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 16.20%	Moderate HER2 expression (HER2++)
Method Description	T-DM1 (10 mg/kg).
In Vivo Model	JIMT -1 cell line xenograft model
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[159]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 28.47%	High HER2 expression (HER2+++/++)
Method Description	DP001 (10 mg/kg).
In Vivo Model	SK-OV-3 cell line xenograft model
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 4 Reporting the Activity Date of This ADC					[159]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 33.60%	High HER2 expression (HER2+++/++)
Method Description	DP001 (10 mg/kg).
In Vivo Model	NCI-N87 xenograft model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 5 Reporting the Activity Date of This ADC					[159]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 39%	Moderate HER2 expression (HER2++)
Method Description	DP303c (0.3 mg/kg).
In Vivo Model	JIMT -1 cell line xenograft model
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 6 Reporting the Activity Date of This ADC					[159]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 45.26%	High HER2 expression (HER2+++/++)
Method Description	DP303c (1 mg/kg).
In Vivo Model	SK-OV-3 cell line xenograft model
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 7 Reporting the Activity Date of This ADC					[159]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 54.40%	Moderate HER2 expression (HER2++)
Method Description	Pathogen-free female nude mice were injected subcutaneously with each cell suspension. According to tumor volumes,the mice were randomly divided in two groups: treatment and control groups. Each drug was given to the animals intravenously. The dosing frequency was once a week (qw), qw 2 or qw 3.DP303c induced obvious tumor growth inhibition at a single dose of 0.1 mg/kg.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 8 Reporting the Activity Date of This ADC					[159]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 82.10%	High HER2 expression (HER2+++)
Method Description	Pathogen-free female nude mice were injected subcutaneously with each cell suspension. According to tumor volumes,the mice were randomly divided in two groups: treatment and control groups. Each drug was given to the animals intravenously. The dosing frequency was once a week (qw), qw 2 or qw 3.DP303c induced obvious tumor growth inhibition at a single dose of 1 mg/kg.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 9 Reporting the Activity Date of This ADC					[159]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 83.94%	High HER2 expression (HER2+++/++)
Method Description	DP303c (3 mg/kg).
In Vivo Model	SK-OV-3 cell line xenograft model
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 10 Reporting the Activity Date of This ADC					[159]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 90.48%	High HER2 expression (HER2+++/++)
Method Description	DP001 (15 mg/kg).
In Vivo Model	HCC1954 cell line xenograft model
In Vitro Model	Breast ductal carcinoma	HCC1954 cells		CVCL_1259
Experiment 11 Reporting the Activity Date of This ADC					[159]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 91.60%	High HER2 expression (HER2+++/++)
Method Description	T-DM1 (10 mg/kg).
In Vivo Model	NCI-N87 xenograft model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 12 Reporting the Activity Date of This ADC					[159]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 94%	High HER2 expression (HER2+++/++)
Method Description	DP303c (10 mg/kg).
In Vivo Model	NCI-N87 xenograft model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 13 Reporting the Activity Date of This ADC					[159]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 94%	High HER2 expression (HER2+++/++)
Method Description	DP303c (5 mg/kg).
In Vivo Model	NCI-N87 xenograft model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 14 Reporting the Activity Date of This ADC					[159]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 94%	High HER2 expression (HER2+++/++)
Method Description	DP303c (2.5 mg/kg).
In Vivo Model	NCI-N87 xenograft model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 15 Reporting the Activity Date of This ADC					[159]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 94.10%	High HER2 expression (HER2+++)
Method Description	Pathogen-free female nude mice were injected subcutaneously with each cell suspension. According to tumor volumes,the mice were randomly divided in two groups: treatment and control groups. Each drug was given to the animals intravenously. The dosing frequency was once a week (qw), qw 2 or qw 3.DP303c induced obvious tumor growth inhibition at a single dose of 3 mg/kg.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 16 Reporting the Activity Date of This ADC					[159]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 94.16%	High HER2 expression (HER2+++/++)
Method Description	T-DM1 (10 mg/kg).
In Vivo Model	SK-OV-3 cell line xenograft model
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 17 Reporting the Activity Date of This ADC					[159]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 94.30%	High HER2 expression (HER2+++/++)
Method Description	T-DM1 (15 mg/kg).
In Vivo Model	HCC1954 cell line xenograft model
In Vitro Model	Breast ductal carcinoma	HCC1954 cells		CVCL_1259
Experiment 18 Reporting the Activity Date of This ADC					[159]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 97%	High HER2 expression (HER2+++/++)
Method Description	DP303c (3 mg/kg).
In Vivo Model	HCC1954 cell line xenograft model
In Vitro Model	Breast ductal carcinoma	HCC1954 cells		CVCL_1259
Experiment 19 Reporting the Activity Date of This ADC					[159]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 97%	High HER2 expression (HER2+++/++)
Method Description	DP303c (10 mg/kg).
In Vivo Model	HCC1954 cell line xenograft model
In Vitro Model	Breast ductal carcinoma	HCC1954 cells		CVCL_1259
Experiment 20 Reporting the Activity Date of This ADC					[159]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 97%	High HER2 expression (HER2+++/++)
Method Description	DP303c (15 mg/kg).
In Vivo Model	HCC1954 cell line xenograft model
In Vitro Model	Breast ductal carcinoma	HCC1954 cells		CVCL_1259
Experiment 21 Reporting the Activity Date of This ADC					[159]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 97.10%	High HER2 expression (HER2+++)
Method Description	Pathogen-free female nude mice were injected subcutaneously with each cell suspension. According to tumor volumes,the mice were randomly divided in two groups: treatment and control groups. Each drug was given to the animals intravenously. The dosing frequency was once a week (qw), qw 2 or qw 3.DP303c induced obvious tumor growth inhibition at a single dose of 3 mg/kg.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	HCC1954 cells		CVCL_1259
Experiment 22 Reporting the Activity Date of This ADC					[159]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 97.50%	High HER2 expression (HER2+++)
Method Description	Pathogen-free female nude mice were injected subcutaneously with each cell suspension. According to tumor volumes,the mice were randomly divided in two groups: treatment and control groups. Each drug was given to the animals intravenously. The dosing frequency was once a week (qw), qw 2 or qw 3.DP303c induced obvious tumor growth inhibition at a single dose of 10 mg/kg.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	HCC1954 cells		CVCL_1259
Experiment 23 Reporting the Activity Date of This ADC					[159]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 97.50%	High HER2 expression (HER2+++)
Method Description	Pathogen-free female nude mice were injected subcutaneously with each cell suspension. According to tumor volumes,the mice were randomly divided in two groups: treatment and control groups. Each drug was given to the animals intravenously. The dosing frequency was once a week (qw), qw 2 or qw 3.DP303c induced obvious tumor growth inhibition at a single dose of 2.5 mg/kg.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 24 Reporting the Activity Date of This ADC					[159]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 97.80%	Moderate HER2 expression (HER2++)
Method Description	Pathogen-free female nude mice were injected subcutaneously with each cell suspension. According to tumor volumes,the mice were randomly divided in two groups: treatment and control groups. Each drug was given to the animals intravenously. The dosing frequency was once a week (qw), qw 2 or qw 3.DP303c induced obvious tumor growth inhibition at a single dose of 1 mg/kg.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 25 Reporting the Activity Date of This ADC					[159]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 97.80%	High HER2 expression (HER2+++)
Method Description	Pathogen-free female nude mice were injected subcutaneously with each cell suspension. According to tumor volumes,the mice were randomly divided in two groups: treatment and control groups. Each drug was given to the animals intravenously. The dosing frequency was once a week (qw), qw 2 or qw 3.DP303c induced obvious tumor growth inhibition at a single dose of 10 mg/kg.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 26 Reporting the Activity Date of This ADC					[159]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 97.80%	High HER2 expression (HER2+++)
Method Description	Pathogen-free female nude mice were injected subcutaneously with each cell suspension. According to tumor volumes,the mice were randomly divided in two groups: treatment and control groups. Each drug was given to the animals intravenously. The dosing frequency was once a week (qw), qw 2 or qw 3.DP303c induced obvious tumor growth inhibition at a single dose of 5 mg/kg.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 27 Reporting the Activity Date of This ADC					[159]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 98.50%	High HER2 expression (HER2+++)
Method Description	Pathogen-free female nude mice were injected subcutaneously with each cell suspension. According to tumor volumes,the mice were randomly divided in two groups: treatment and control groups. Each drug was given to the animals intravenously. The dosing frequency was once a week (qw), qw 2 or qw 3.DP303c induced obvious tumor growth inhibition at a single dose of 10 mg/kg.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 28 Reporting the Activity Date of This ADC					[159]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 98.54%	High HER2 expression (HER2+++/++)
Method Description	DP303c (10 mg/kg).
In Vivo Model	SK-OV-3 cell line xenograft model
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 29 Reporting the Activity Date of This ADC					[159]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 98.80%	Moderate HER2 expression (HER2++)
Method Description	Pathogen-free female nude mice were injected subcutaneously with each cell suspension. According to tumor volumes,the mice were randomly divided in two groups: treatment and control groups. Each drug was given to the animals intravenously. The dosing frequency was once a week (qw), qw 2 or qw 3.DP303c induced obvious tumor growth inhibition at a single dose of 3 mg/kg.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 30 Reporting the Activity Date of This ADC					[159]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 99.10%	High HER2 expression (HER2+++)
Method Description	Pathogen-free female nude mice were injected subcutaneously with each cell suspension. According to tumor volumes,the mice were randomly divided in two groups: treatment and control groups. Each drug was given to the animals intravenously. The dosing frequency was once a week (qw), qw 2 or qw 3.DP303c induced obvious tumor growth inhibition at a single dose of 15 mg/kg.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	HCC1954 cells		CVCL_1259
Experiment 31 Reporting the Activity Date of This ADC					[159]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 99.90%	Moderate HER2 expression (HER2++)
Method Description	Pathogen-free female nude mice were injected subcutaneously with each cell suspension. According to tumor volumes,the mice were randomly divided in two groups: treatment and control groups. Each drug was given to the animals intravenously. The dosing frequency was once a week (qw), qw 2 or qw 3.DP303c induced obvious tumor growth inhibition at a single dose of 10 mg/kg.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 32 Reporting the Activity Date of This ADC					[159]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100%	Moderate HER2 expression (HER2++)
Method Description	DP303c (10 mg/kg).
In Vivo Model	JIMT -1 cell line xenograft model
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 33 Reporting the Activity Date of This ADC					[159]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100%	Moderate HER2 expression (HER2++)
Method Description	DP303c (3 mg/kg).
In Vivo Model	JIMT -1 cell line xenograft model
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 34 Reporting the Activity Date of This ADC					[159]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100%	Moderate HER2 expression (HER2++)
Method Description	DP303c (1 mg/kg).
In Vivo Model	JIMT -1 cell line xenograft model
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077

Experiment 1 Reporting the Activity Date of This ADC					[159]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.07 nM	Moderate HER2 expression (HER2++; HER2 MFI=157,231)
Method Description	Comparison of in vitro Activity Between DP303c and T -DM1 in Variable HER2 Cell Lines.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[159]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.07 nM	High HER2 expression (HER2+++)
Method Description	To obtain a single-cell suspension, the cells were harvested and resuspended. The cell density was adjusted to 1 x105 cells/mL and seeded in a 96-well cell culture plate at 100 uL/well (1 x104 cells/well). DP303c labeled with DyLight 488 was added into the 96-well plate with a final concentration of 2 ug/mL.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC					[159]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.08 nM	High HER2 expression (HER2+++; HER2 MFI=987,353)
Method Description	Comparison of in vitro Activity Between DP303c and T -DM1 in Variable HER2 Cell Lines.
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 4 Reporting the Activity Date of This ADC					[159]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.08 nM	Negative HER2 expression (HER2-; HER2 MFI=256)
Method Description	To obtain a single-cell suspension, the cells were harvested and resuspended. The cell density was adjusted to 1x105 cells/mL and seeded in a 96-well cell culture plate at 100 uL/well (1 x104 cells/well). DP303c labeled with DyLight 488 was added into the 96-well plate with a final concentration of 2 ug/mL.
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 5 Reporting the Activity Date of This ADC					[159]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.15 nM	High HER2 expression (HER2+++)
Method Description	Comparison of in vitro Activity Between DP303c and T -DM1 in Variable HER2 Cell Lines.
In Vitro Model	Breast ductal carcinoma	HCC1954 cells		CVCL_1259
Experiment 6 Reporting the Activity Date of This ADC					[159]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.15 nM	High HER2 expression (HER2+++)
Method Description	To obtain a single-cell suspension, the cells were harvested and resuspended. The cell density was adjusted to 1 x105 cells/mL and seeded in a 96-well cell culture plate at 100 uL/well (1 x104 cells/well). DP303c labeled with DyLight 488 was added into the 96-well plate with a final concentration of 2 ug/mL.
In Vitro Model	Breast ductal carcinoma	HCC1954 cells		CVCL_1259
Experiment 7 Reporting the Activity Date of This ADC					[159]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.22 nM	Negative HER2 expression (HER2-)
Method Description	Comparison of in vitro Activity Between DP303c and T -DM1 in Variable HER2 Cell Lines.
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 8 Reporting the Activity Date of This ADC					[159]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.22 nM	High HER2 expression (HER2+++)
Method Description	To obtain a single-cell suspension, the cells were harvested and resuspended. The cell density was adjusted to 1 x105 cells/mL and seeded in a 96-well cell culture plate at 100 uL/well (1 x104 cells/well). DP303c labeled with DyLight 488 was added into the 96-well plate with a final concentration of 2 ug/mL.
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 9 Reporting the Activity Date of This ADC					[159]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.23 nM	High HER2 expression (HER2+++; HER2 MFI=804,573)
Method Description	Comparison of in vitro Activity Between DP303c and T -DM1 in Variable HER2 Cell Lines.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 10 Reporting the Activity Date of This ADC					[159]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.23 nM	High HER2 expression (HER2+++; HER2 MFI=892,333)
Method Description	To obtain a single-cell suspension, the cells were harvested and resuspended. The cell density was adjusted to 1 x105 cells/mL and seeded in a 96-well cell culture plate at 100 uL/well (1 x104 cells/well). DP303c labeled with DyLight 488 was added into the 96-well plate with a final concentration of 2 ug/mL.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 11 Reporting the Activity Date of This ADC					[159]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	3.39 nM	High HER2 expression (HER2+++)
Method Description	Comparison of in vitro Activity Between DP303c and T -DM1 in Variable HER2 Cell Lines.
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 12 Reporting the Activity Date of This ADC					[159]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	3.39 nM	Moderate HER2 expression (HER2++)
Method Description	To obtain a single-cell suspension, the cells were harvested and resuspended. The cell density was adjusted to 1x105 cells/mL and seeded in a 96-well cell culture plate at 100 uL/well (1x104 cells/well). DP303c labeled with DyLight 488 was added into the 96-well plate with a final concentration of 2 ug/mL.
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 13 Reporting the Activity Date of This ADC					[159]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 50 nM	High HER2 expression (HER2+++; HER2 MFI=1,106,494)
Method Description	To obtain a single-cell suspension, the cells were harvested and resuspended. The cell density was adjusted to 1x105 cells/mL and seeded in a 96-well cell culture plate at 100 uL/well (1x104 cells/well). DP303c labeled with DyLight 488 was added into the 96-well plate with a final concentration of 2 ug/mL.
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 14 Reporting the Activity Date of This ADC					[159]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1000 nM	High HER2 expression (HER2+++; HER2 MFI=765,629)
Method Description	Comparison of in vitro Activity Between DP303c and T -DM1 in Variable HER2 Cell Lines.
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419

Experiment 1 Reporting the Activity Date of This ADC					[156]
Patients Enrolled	Patients with metastatic or unresectable solid tumors.
Administration Dosage	30 patients in Q1W (0.80, 1.00, and 1.20 mg/kg); 18 patients in 2Q3W (1.20 or 1.25 mg/kg).
Related Clinical Trial
NCT Number	NCT04389632	Phase Status	Phase 1/2
Clinical Description	A phase 1 study of SGN-B6A in advanced solid tumors.
Experiment 2 Reporting the Activity Date of This ADC					[163]
Efficacy Data	Objective Response Rate (ORR)	19.5 32.5 %
Patients Enrolled	Eligible participants must have metastatic/unresectable solid tumors (e.g., NSCLC, HNSCC, HER2-negative breast cancer) and meet cohort-specific requirements: Part A (refractory to standard therapies), Part B (prior platinum/PD-1 therapy), Part C/D (treatment-naïve for advanced disease where applicable). Key exclusions: active CNS metastases (exceptions for stable, treated cases), prior MMAE/integrin beta-6 therapy, Grade ≥2 neuropathy (Grade ≥1 for cisplatin/carboplatin cohorts), unresolved ILD/pneumonitis, or DLCO <50%.    Click to Show/Hide
Administration Dosage	Eligible pts had no therapeutic options (Part A) or had received platinum-based and anti-PD- (L)1 therapy unless contraindicated (Part B) and were dosed with the SV expansion regimens on D1 and D8 in a 21-day cycle (2Q3W; 1.2/1.25 mg/kg total body weight [TBW]) or D1 and D15 in a 28-day cycle (2Q4W; 1.5 mg/kg TBW, 1.8 mg/kg adjusted ideal body weight [AiBW]).    Click to Show/Hide
Related Clinical Trial
NCT Number	NCT04389632	Phase Status	PHASE1
Clinical Description	A Phase 1 Study of SGN-B6A in Advanced Solid Tumors
Primary Endpoint	Safety endpoints include the number of participants experiencing adverse events (AEs), laboratory abnormalities, and dose-limiting toxicities (DLTs), assessed up to 3 years, with AE monitoring extended to 90 days post-pembrolizumab for relevant cohorts.
Other Endpoint	Efficacy measures consist of confirmed objective response rate (ORR), duration of response (DOR), progression-free survival (PFS), and overall survival (OS), all per RECIST v1.1. Pharmacokinetic (PK) parameters-AUC, Cmax, Tmax, Ctrough, and t1/2-as well as antidrug antibodies (ADAs), will be evaluated up to 3 years post-treatment.
Experiment 3 Reporting the Activity Date of This ADC					[179]
Patients Enrolled	Eligible patients must have specific advanced solid tumors (NSCLC, HNSCC, ESCC, GAC/EAC/GEJ) refractory to standard therapies, adequate organ function, and ECOG 0-1. Key exclusions include recent malignancies, pulmonary complications ≥Grade 3, active CNS metastases, prior MMAE treatment, and recent anticancer therapies/herbals with defined washout periods.    Click to Show/Hide
Administration Dosage	sigvotatug vedotin monotherapy 1.8 mg/kg adjusted ideal body weight intravenous administration on Days 1 and 15 of a 28-day cycle.
Related Clinical Trial
NCT Number	NCT06549816	Phase Status	PHASE1
Clinical Description	An Open-label, Phase 1 Study to Investigate the Safety and Pharmacokinetics of SGN-B6A in Chinese Subjects With Advanced Solid Tumors
Primary Endpoint	Primary endpoints include AE assessment over 3 years, lab abnormalities tracking within 30-37 days post-treatment, and DLT monitoring during the initial 28-day period following sigvotatug vedotin administration.
Other Endpoint	Pharmacokinetic parameters (AUC, Cmax, Tmax, t1/2, Ctrough) for both ac-MMAE and MMAE will be evaluated following single and multiple doses of SGN-B6A across two treatment cycles (28 days each), along with antidrug antibody detection up to 37 days post-treatment.
Experiment 4 Reporting the Activity Date of This ADC					[180]
Patients Enrolled	Eligible patients must have unresectable/metastatic non-squamous NSCLC (Stage IIIB-IV per AJCC v8), measurable disease (RECIST v1.1), and progression after platinum/PD- (L)1 therapy (or AGA-targeted therapy if applicable). Key exclusions include life expectancy <3 months, prior taxanes/MMAE exposure in metastatic setting, unresolved Grade ≥2 neuropathy, uncontrolled ILD (steroid-dependent or DLCO <50%), active CNS metastases (unless stable for ≥4 weeks post-treatment with steroids ≤10mg/day), and recent anticancer therapy (<21 days before C1D1).    Click to Show/Hide
Administration Dosage	Given into the vein (IV; intravenously) on Day 1 and 15 of a 28-day cycle
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NCT Number	NCT06012435	Phase Status	PHASE3
Clinical Description	A Randomized, Phase 3, Open-label Study to Evaluate Sigvotatug Vedotin Compared With Docetaxel in Adult Participants With Previously Treated Non-small Cell Lung Cancer (Be6A Lung-01)
Primary Endpoint	The primary efficacy endpoints include OS (time from randomization to death) and PFS per RECIST v1.1 (time to disease progression or death) comparing sigvotatug vedotin versus docetaxel in both the overall population and IB6-high subgroup over 5 years.
Other Endpoint	Secondary endpoints include ORR per RECIST v1.1 (confirmed CR/PR rates by BICR and investigator assessment), DOR (time from response to progression/death), AEs within 30 days post-treatment, and quality-of-life metrics (EORTC QLQ-C30 and QLQ-LC13) assessing global health status, physical/role functioning, and symptom scales (dyspnea, cough, chest pain), along with TTD for key PROs over 5 years of follow-up.    Click to Show/Hide

Experiment 1 Reporting the Activity Date of This ADC					[157]
Related Clinical Trial
NCT Number	NCT05208762	Phase Status	Phase 1
Clinical Description	A phase 1 study of SGN-PDL1V in advanced solid tumors.
Experiment 2 Reporting the Activity Date of This ADC					[164]
Efficacy Data	Objective Response Rate (ORR)	27.30%
Patients Enrolled	Key exclusions were active CNS metastases (except stable treated ones 4 weeks prior), prior anti-PD-L1 within 5 half-lives, MMAE-containing agent exposure, or ≥Grade 2 neuropathy per NCI CTCAE v5.0. Stratification occurred by tumor type (Parts A-E) and PD-L1 status.
Administration Dosage	In dose escalation, pts received doses of SGN-PDL1V from 0.5-1.75 mg/kg on days 1, and 8 of every 21-day cycle using adjusted ideal body weight. The primary objectives of this study are safety/tolerability and pharmacokinetics with antitumor activity as a secondary objective.
Related Clinical Trial
NCT Number	NCT05208762	Phase Status	PHASE1
Clinical Description	A Phase 1 Study of SGN-PDL1V in Advanced Solid Tumors
Primary Endpoint	Safety evaluations included AE monitoring for up to 3 years, with specific focus on DLTs during the first treatment cycle, laboratory abnormalities, and immunogenicity (ADA incidence). PK parameters (AUC, Cmax, Ctrough) were assessed until last treatment plus 30-37 days.
Other Endpoint	Efficacy outcomes measured confirmed ORR, DOR, PFS, and OS per RECIST v1.1 over ~3 years across multiple solid tumors (NSCLC, HNSCC, TNBC, etc.), requiring PD-L1 expression (TPS/CPS ≥1 or <1) and prior therapy failure/refusal.

Experiment 1 Reporting the Activity Date of This ADC					[162]
Efficacy Data	Progression Free Survival	7.16 months
Patients Enrolled	Key inclusion criteria: fully informed consent; age 18-80; ECOG 0-1; life expectancy ≥3 months; histologically/cytologically confirmed CLDN18.2-positive advanced solid tumors (IHC by central lab) refractory to standard therapy; ≥1 evaluable (Phase I) or measurable (Phase II) lesion per RECIST v1.1; adequate organ/marrow function; ability to comply with study requirements.    Click to Show/Hide
Administration Dosage	LM-302 Dose Escalation. 6 dose levels were pre-defined, and the initial accelerated titration followed by the i3+3 design was adopted during phase I.
Related Clinical Trial
NCT Number	NCT05161390	Phase Status	PHASE1|||PHASE2
Clinical Description	A Phase I/II , Open, Multicentre, Dose-escalation and Expansion Clinical Study to Evaluate the Safety, Tolerability, Pharmacokinetics, Immunogenicity and Antitumour Activity of LM-302 in Patients With CLDN18.2 Positive Advanced Solid Tumours
Primary Endpoint	Primary safety endpoints include dose-limiting toxicity (DLT) assessment during Cycle 1 (21-day cycle), adverse events/serious adverse events monitoring per NCI CTCAE v5.0 from ICF signing until 28 days post-EOT, with determination of both recommended Phase II dose (RP2D) and maximum tolerated dose (MTD) within 21 days post-first dose.
Other Endpoint	Pharmacokinetic analysis focuses on area under plasma concentration curve (AUC) for LM-302 through completion of cycle 5 (each cycle lasting 21 days) to evaluate drug exposure changes over time.
Experiment 2 Reporting the Activity Date of This ADC					[162]
Efficacy Data	Objective Response Rate (ORR)	30.60%
Patients Enrolled	Key inclusion criteria: fully informed consent; age 18-80; ECOG 0-1; life expectancy ≥3 months; histologically/cytologically confirmed CLDN18.2-positive advanced solid tumors (IHC by central lab) refractory to standard therapy; ≥1 evaluable (Phase I) or measurable (Phase II) lesion per RECIST v1.1; adequate organ/marrow function; ability to comply with study requirements.    Click to Show/Hide
Administration Dosage	LM-302 Dose Escalation. 6 dose levels were pre-defined, and the initial accelerated titration followed by the i3+3 design was adopted during phase I.
Related Clinical Trial
NCT Number	NCT05161390	Phase Status	PHASE1|||PHASE2
Clinical Description	A Phase I/II , Open, Multicentre, Dose-escalation and Expansion Clinical Study to Evaluate the Safety, Tolerability, Pharmacokinetics, Immunogenicity and Antitumour Activity of LM-302 in Patients With CLDN18.2 Positive Advanced Solid Tumours
Primary Endpoint	Primary safety endpoints include dose-limiting toxicity (DLT) assessment during Cycle 1 (21-day cycle), adverse events/serious adverse events monitoring per NCI CTCAE v5.0 from ICF signing until 28 days post-EOT, with determination of both recommended Phase II dose (RP2D) and maximum tolerated dose (MTD) within 21 days post-first dose.
Other Endpoint	Pharmacokinetic analysis focuses on area under plasma concentration curve (AUC) for LM-302 through completion of cycle 5 (each cycle lasting 21 days) to evaluate drug exposure changes over time.
Experiment 3 Reporting the Activity Date of This ADC					[162]
Efficacy Data	Disease control rate (DCR)	75%
Patients Enrolled	Key inclusion criteria: fully informed consent; age 18-80; ECOG 0-1; life expectancy ≥3 months; histologically/cytologically confirmed CLDN18.2-positive advanced solid tumors (IHC by central lab) refractory to standard therapy; ≥1 evaluable (Phase I) or measurable (Phase II) lesion per RECIST v1.1; adequate organ/marrow function; ability to comply with study requirements.    Click to Show/Hide
Administration Dosage	LM-302 Dose Escalation. 6 dose levels were pre-defined, and the initial accelerated titration followed by the i3+3 design was adopted during phase I.
Related Clinical Trial
NCT Number	NCT05161390	Phase Status	PHASE1|||PHASE2
Clinical Description	A Phase I/II , Open, Multicentre, Dose-escalation and Expansion Clinical Study to Evaluate the Safety, Tolerability, Pharmacokinetics, Immunogenicity and Antitumour Activity of LM-302 in Patients With CLDN18.2 Positive Advanced Solid Tumours
Primary Endpoint	Primary safety endpoints include dose-limiting toxicity (DLT) assessment during Cycle 1 (21-day cycle), adverse events/serious adverse events monitoring per NCI CTCAE v5.0 from ICF signing until 28 days post-EOT, with determination of both recommended Phase II dose (RP2D) and maximum tolerated dose (MTD) within 21 days post-first dose.
Other Endpoint	Pharmacokinetic analysis focuses on area under plasma concentration curve (AUC) for LM-302 through completion of cycle 5 (each cycle lasting 21 days) to evaluate drug exposure changes over time.
Experiment 4 Reporting the Activity Date of This ADC					[166]
Patients Enrolled	Eligible subjects must be CLDN18.2-positive GI cancer patients (18-80yo, ECOG 0-1, life expectancy ≥3 months) with ≥1 measurable lesion (RECIST v1.1) and adequate organ function, having provided informed consent prior to study procedures.
Administration Dosage	LM-302 (recombinant humanized anti-CLDN18.2 monoclonal antibody, MMAE conjugate), Toripalimab (recombinant humanized anti-PD1 monoclonal antibody)
Related Clinical Trial
NCT Number	NCT05934331	Phase Status	PHASE2
Clinical Description	A Phase II, Open-Label, Multicenter Study Evaluating the Efficacy, Safety, and Tolerability of LM-302 Combined With Toripalimab in CLDN18.2 Positive Patients Advanced Gastro-Intestinal Cancer
Primary Endpoint	Primary endpoint evaluates PFS per RECIST v1.1 criteria within 6 weeks post-first dose.
Other Endpoint	Secondary endpoints assess ORR, DOR, DCR (CR+PR+SD), and OS during the same 6-week evaluation period.
Experiment 5 Reporting the Activity Date of This ADC					[167]
Patients Enrolled	Eligible patients must have unresectable/metastatic BTC (histologically confirmed) with prior treatment failure (chemotherapy+PD1/PD-L1), measurable lesions (outside prior local therapy areas if applicable), ECOG≤2, life expectancy>3 months, and adequate organ function (Cr≤1.5×ULN/GFR≥60mL/min, bilirubin≤1.5×ULN, ALT/AST≤2.5×ULN, ANC>1500/mcl, Plts>75,000/mcl). Phase II requires Claudin18.2-positivity (≥40% IHC by dual-pathologist confirmation). HBV/HCV patients eligible with viral control (HBV<2000 IU/ml with antiviral therapy; HCV treated/completed therapy with stable LFTs).    Click to Show/Hide
Administration Dosage	Each cycle of the first phase was defined as cardonilizumab (6mg/kg,Q2W) combined with different concentrations of 1.6mg/kg or 1.8mg/kg LM-302 (Q2W), 14 days as a course of treatment, and the combined dose (RP2D) of LM-302 during combination therapy was determined according to the 3+3 design.
Related Clinical Trial
NCT Number	NCT05994001	Phase Status	PHASE1|||PHASE2
Clinical Description	Two Stage, Multi-center Trial of Candonilimab in Combination With LM-302 for Treatment of Patients With Claudin 18.2 Positive-advanced Biliary Tract Cancer After Failure of Standard of Chemotherapy and PD1/PD-L1 Antibody
Primary Endpoint	Primary endpoints include ORR (RECIST 1.1) in Claudin18.2-positive patients receiving cardonilizumab+LM302 (Phase II) and treatment-emergent AE incidence in advanced BTC patients across LM-302 dose levels (Phase I), both evaluated over 24 months. Secondary efficacy endpoints assess DOR, DCR, and OS during the 24-month study period.
Other Endpoint	Secondary efficacy endpoints assess DOR, DCR, and OS during the 24-month study period.
Experiment 6 Reporting the Activity Date of This ADC					[168]
Patients Enrolled	Eligible patients are CLDN18.2-positive, HER2-negative G/GEJ adenocarcinoma patients (18-80yo, ECOG 0-1) with ≥1 measurable lesion (RECIST 1.1) who failed ≥2 systemic therapies (including adjuvant therapy relapsed within 6 months). Required: adequate organ function (hematologic/hepatic/renal/coagulation), life expectancy ≥12 weeks, and informed consent.    Click to Show/Hide
Administration Dosage	LM-302 intravenous-injection every 2 weeks on Day 1 of each 14-day cycle
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NCT Number	NCT06351020	Phase Status	PHASE3
Clinical Description	A Phase III, Open-Label, Multi Center, Randomized Study of LM-302 Versus Treatment of Physician's Choice (TPC) in Patients With CLDN18.2-Positive, Locally Advanced or Metastatic Gastric (GC) and Gastroesophageal Junction (GEJ) Adenocarcinoma.
Primary Endpoint	Primary endpoints assess OS (time from randomization to death) and PFS (time to radiographic progression/death) over 42 months, both based on investigator assessment.
Other Endpoint	Secondary endpoints include ORR (CR+PR per RECIST 1.1), DoR (response duration to progression/death), DCR (CR+PR+SD≥6 weeks), AEs/SAEs (NCI-CTCAE v5.0), immunogenicity (ADA detection), and PK evaluations (Cmax/AUC/trough for LM-302, total antibody, and MMAE using PopPK modeling) across the 42-month study period.
Experiment 7 Reporting the Activity Date of This ADC					[169]
Patients Enrolled	Eligible participants are CLDN18.2-positive (IHC≥10%) gastric/GEJ adenocarcinoma patients (≥18yo, ECOG≤1) with unresectable/metastatic disease, ≥1 measurable lesion (RECIST 1.1), and life expectancy >3 months. Key requirements: prior adjuvant therapy completed ≥6 months pre-progression (oxaliplatin toxicity resolved to CTCAE v5.0 grade 1), adequate organ function (Cr≤1.5×ULN/GFR≥60mL/min, bilirubin≤1.5×ULN, AST/ALT≤2.5×ULN [≤5×ULN if liver mets], ANC≥1.5×109/L, PLT≥100×109/L), and signed informed consent    Click to Show/Hide
Administration Dosage	1.8mg/kg ivgtt d1, q2w; Canonilimab: 6mg/kg ivgtt d1, q2w; Capecitabine: 1000mg/m^2 po bid d1-10, q2w.
Related Clinical Trial
NCT Number	NCT06587425	Phase Status	PHASE2
Clinical Description	A Phase II Study Evaluating the Efficacy and Safety of LM-302 in Combination With Candonilimab and Capecitabine for First-Line Treatment in Patients With Unresectable Advanced, Recurrent, or Metastatic CLDN18.2-Positive Gastric or Gastroesophageal Junction Adenocarcinoma
Primary Endpoint	Primary endpoints evaluate DLTs (Cycle 1 toxicities related to LM302) and PFS (time from randomization to progression/death) over a 42-month period, with investigator-assessed radiographic confirmation.
Other Endpoint	Secondary endpoints include OS (time to death from any cause), ORR (CR+PR per RECIST 1.1), DoR (response duration until progression/death), DCR (CR+PR+SD≥6 weeks), and AE/SAE monitoring (NCI-CTCAE v5.0) through treatment completion plus 40 days follow-up.
Experiment 8 Reporting the Activity Date of This ADC					[170]
Patients Enrolled	Eligible patients must have histologically confirmed HER2-negative gastric adenocarcinoma with intact primary/metastatic lesions, laparoscopy-confirmed peritoneal metastases without obstruction, Claudin 18.2 positivity (≥25% expression in ≥50% tumor cells in ≥70% cases), age ≥18 years, ECOG ≤1, life expectancy >3 months, adequate bone marrow/hepatic/renal function, and provided written informed consent.    Click to Show/Hide
Administration Dosage	LM-302 2.0mg/kg intravenous (IV) infusion on day 1, paclitaxel 20 mg/m2 intraperitoneal infusion on Days 1 and 8 plus oral S-1 80 mg/m2 for 14 consecutive days every 3 weeks.
Related Clinical Trial
NCT Number	NCT06519591	Phase Status	PHASE2
Clinical Description	Systemic Application of Cadonilimab, LM-302, and S-1 Combined With Intraperitoneal Infusion of Paclitaxel for the Treatment of Claudin 18.2-positive Gastric Cancer With Peritoneal Metastasis
Primary Endpoint	Primary endpoint evaluates 1-year survival rate at 12 months post-treatment.
Other Endpoint	Secondary endpoints assess treatment-related adverse events over 24 months, 3-year overall survival (OS) at 36 months, and 3-year progression-free survival (PFS) at 36 months.
Experiment 9 Reporting the Activity Date of This ADC					[171]
Patients Enrolled	Eligibility requires signed informed consent, age ≥18, ECOG 0-1, life expectancy ≥3 months; Phase Ia accepts advanced solid tumors (gastric/GEJ, pancreatic, biliary, colorectal, ovarian, esophageal) regardless of CLDN18.2 status, while Phase Ib requires CLDN18.2+ tumors (IHC 1±3+ in ≥10% tumor cells, with ≥3 subjects having 2±3+ in ≥40% cells); All subjects need adequate organ function (PLT≥90×109/L, ANC≥1.5×109/L, Hb≥9g/dL, bilirubin≤1.5×ULN, AST/ALT≤2.5×ULN, Cr≤1.5×ULN or CrCl≥50mL/min, LVEF≥50%, QTcF≤480ms) and measurable disease (RECIST v1.1).    Click to Show/Hide
Administration Dosage	Arm1:LM302 0.2 mg/kg i.v., QW×3 weeks group; Arm2:LM302 0.4 mg/kg i.v., QW×3 weeks group; Arm3:LM302 0.8 mg/kg i.v., QW×3 weeks group; Arm4:LM302 1.6 mg/kg i.v., QW×3 weeks group; Arm5:LM302 2.4 mg/kg i.v., QW×3 weeks group; Arm6:LM302 2.8 mg/kg i.v., QW×3 weeks group;
Related Clinical Trial
NCT Number	NCT05001516	Phase Status	PHASE1
Clinical Description	A Phase I, First-in-Human, Open-Label, Dose Escalation and Expansion Study of TPX4589 in Patients With Claudin (CLDN)18.2-Positive Advanced Solid Tumors
Primary Endpoint	Primary endpoints include dose-limiting toxicity (DLT) assessment during Cycle 1 (21-day cycle) and comprehensive safety evaluation through AE/SAE monitoring (NCI CTCAE v5.0) for 1 year post-dose, with vital signs (temperature, pulse, blood pressure), physical exams (weight), lab tests (hematology, biochemistry, urinalysis, coagulation), and ECG parameters (RR, QT, QRS intervals) being systematically tracked.    Click to Show/Hide
Other Endpoint	Pharmacokinetic analysis includes AUCtau, Vss, Cmax, Cmin, Tmax, CL, T1/2 and dose proportionality assessments through intensive blood sampling over 1 year, along with efficacy evaluations (ORR, DOR, DCR, PFS per RECIST v1.1) and immunogenicity testing (ADA) at specified cycles.
Experiment 10 Reporting the Activity Date of This ADC					[172]
Patients Enrolled	Key inclusion criteria: signed ICF; age ≥18; ECOG 0-1; life expectancy ≥3 months; histologically confirmed advanced solid tumors refractory to standard therapy.
Administration Dosage	LM-302 monotherapy dose escalation (part Ia). Accelerated titration combined with traditional 3+3 design will be used for monotherapy dose escalation (part Ia).
Related Clinical Trial
NCT Number	NCT05188664	Phase Status	PHASE1|||PHASE2
Clinical Description	A Phase I/II, Open-Label, Multiple Centre Clinical Study to Evaluate the Safety, Tolerability, Pharmacokinetics, Immunogenicity and Preliminary Efficacy of LM- 302 in Combination With Toripalimab in Patients With Advanced Solid Tumors
Primary Endpoint	Primary objectives include DLT assessment during Cycle 1 (21-day cycle) to evaluate safety of LM-302 combined with toripalimab in advanced solid tumors, along with determination of RP2D and OBD within 6 months, and MTD within 21 days post-dose. (No secondary endpoints specified).

Experiment 1 Reporting the Activity Date of This ADC					[182]
Efficacy Data	Partial Response (PR)	22.20%
Patients Enrolled	Metastatic castration-resistant prostate cancer (CRPC).
Administration Dosage	Intravenous FOR46 on day 1 of every 21-day cycle. Dose levels ranged from 0.10 mg/kg. the starting dose level, to 3.00 mg/kg. The trial established 2.70 mg/kg to be the maximum tolerated dose (MTD) and the recommended phase 2 dose (RP2D) of the agent.
Related Clinical Trial
NCT Number	NCT03575819	Phase Status	Phase 1
Clinical Description	A phase 1 study of FOR46 administered every 21 days in patients with metastatic castration-resistant prostate cancer (mCRPC).
Primary Endpoint	MtD and phase 1b dose=2.70 mg/kg.
Other Endpoint	18 pts had measurable lesions; 8 of 18 (44.44%) had tumor regression, with 4 (22.22%) confirmed partial responses (PR). The median duration of response is > 14 wks (range 9 -31+ weeks).
Experiment 2 Reporting the Activity Date of This ADC					[194]
Related Clinical Trial
NCT Number	NCT05011188	Phase Status	Phase 1/2
Clinical Description	A phase 1b/2 study of FOR46 in combination with enzalutamide in patients with metastatic castration resistant prostate cancer.
Experiment 3 Reporting the Activity Date of This ADC					[196]
Related Clinical Trial
NCT Number	NCT03650491	Phase Status	Phase 1
Clinical Description	A phase 1 study of FOR46 administered every 21 days in patients with relapsed or refractory multiple myeloma (RRMM).
Experiment 4 Reporting the Activity Date of This ADC					[200]
Efficacy Data	Objective Response Rate (ORR)	20%
Patients Enrolled	Inclusion: Men ≥18 with histologically confirmed mCRPC (progressing post-ARSI therapy), castrate testosterone (<50 ng/dL), ECOG 0-1, adequate organ function, and willingness for biopsy (dose expansion). Exclusion: Persistent toxicity (Grade≥2 neuropathy), prior mCRPC chemotherapy (hormone-sensitive >6 months prior allowed), recent therapy/surgery (≤28 days), uncontrolled comorbidities (cardio/pulmonary/CNS metastases), active HIV/HepB/C, or CYP3A4 modulators. Dose escalation excludes episodic atrial fibrillation history.    Click to Show/Hide
Administration Dosage	FOR46 is an intravenously (IV) administered antibody-drug conjugate (ADC) directed against CD46
Related Clinical Trial
NCT Number	NCT03575819	Phase Status	PHASE1
Clinical Description	A Phase 1 Study of FOR46 Administered Every 21 Days in Patients With Metastatic Castration-Resistant Prostate Cancer (mCRPC)
Primary Endpoint	Safety assessments include toxicity evaluation (type, incidence, severity, relatedness) and dose-limiting toxicities (DLTs) through 1-month post-treatment, along with disease response (≥50% PSA decline and objective response per RECIST criteria) assessed over 12 months.
Other Endpoint	Pharmacokinetics focus on FOR46 plasma concentration (Cmax, AUC, half-life), antidrug antibody levels, and median radiographic progression-free survival (rPFS) at 12 months per PCWG3 criteria, monitored for 1 month post-dosing.
Experiment 5 Reporting the Activity Date of This ADC					[204]
Patients Enrolled	Inclusion: RRMM patients (≥18 years) refractory/intolerant to PI, IMiD, and CD38 therapy; ECOG 0-1; adequate organ function; contraception compliance. Exclusion: Persistent toxicity (Grade≥2 neuropathy), recent therapy/transplant/surgery (12-28 days), uncontrolled comorbidities (cardio/pulmonary/infectious), CYP3A4 modulators, warfarin use, atrial fibrillation history, or prior MMAE/MMAF ADC exposure. Breastfeeding excluded.    Click to Show/Hide
Administration Dosage	FOR46 is an intravenously (IV) administered antibody-drug conjugate (ADC) directed against CD46
Related Clinical Trial
NCT Number	NCT03650491	Phase Status	PHASE1
Clinical Description	A Phase I Study of FOR46 Administered Every 21 Days in Patients With Relapsed or Refractory Multiple Myeloma (RRMM)
Primary Endpoint	Safety evaluation includes monitoring treatment-related adverse events by NCI CTCAE v5.0 and dose-limiting toxicities through 1-month post-treatment. Efficacy is measured by overall response rate (≥PR/CR/stringent CR/MRD negativity) at 6 months.
Other Endpoint	Pharmacokinetic analysis assesses FOR46 plasma concentration (Cmax, AUC, elimination half-life), antidrug antibody levels up to 1 month post-treatment, and treatment response (duration, progression-free survival, time to progression) via IMWG criteria over 6 months.
Experiment 6 Reporting the Activity Date of This ADC					[205]
Patients Enrolled	Inclusion: Histologically confirmed prostate adenocarcinoma (excluding small cell/neuroendocrine) with mCRPC progression post-ARSI (abiraterone/enzalutamide/apalutamide/darolutamide); castrate testosterone (<50 ng/dL); ≥1 measurable metastasis; adequate organ function. Biopsy (fresh/archival ≤1 year) required for CD46 IHC. Exclusion: Prior CD46-targeted therapy, non-adenocarcinoma histology, >1 prior ARSI, recent anticancer therapy/radiation (≤28 days), actionable mutations (unless treated/progressed), prior chemotherapy (except 1 taxane in castration-sensitive setting >12 months prior), hypersensitivity to FG-3246/antibodies, malignancy (≤5 years, excluding treated skin cancers), or strong CYP3A4 modulators.    Click to Show/Hide
Administration Dosage	FG-3246 will be administered per schedule specified in the arm description.
Related Clinical Trial
NCT Number	NCT06842498	Phase Status	PHASE2
Clinical Description	A Phase 2 Dose Optimization Trial Evaluating a CD46-Targeted Antibody-Drug Conjugate (FG-3246) in Patients With Metastatic Castration-Resistant Prostate Cancer
Primary Endpoint	The study evaluates radiographic progression-free survival (rPFS) per RECIST v1.1 and PCWG3 criteria until progression (up to ~31 months), along with treatment-emergent adverse events (TEAEs) and pharmacokinetic parameters (Cmax of FG-3246, CD46 antibody, and free MMAE) across 21-day cycles. Safety monitoring continues until 28 days after the last dose.    Click to Show/Hide
Other Endpoint	Efficacy assessments include 6- and 12-month rPFS rates, confirmed ORR, duration of response (DoR), PSA50/90 response rates, composite response (CRR), PSA-PFS, disease control (DCR), clinical benefit (CBR), time to symptomatic skeletal events (SSRE), and overall survival (OS) up to ~31 months. Immunogenicity (ADA/NAb development) is also tracked throughout treatment and post-dosing.    Click to Show/Hide
Experiment 7 Reporting the Activity Date of This ADC					[206]
Patients Enrolled	Inclusion: Men ≥18 with mCRPC (progressed post-ARSIs, no prior mCRPC taxane, PSA≥2 ng/mL or measurable disease), castrate testosterone (<50 ng/dL), ECOG≤1, adequate organ function, and biopsy/PET imaging (expansion phase). Exclusion: Prior CD46 therapy, recent radiation/systemic therapy (<14 days), small-cell histology, uncontrolled cardiac/pulmonary/CNS conditions, CYP3A4 inhibitors, or active infections.    Click to Show/Hide
Administration Dosage	A 3+3 dose escalation design was utilized with a starting dose of FOR46 of 1.8 mg/kg adjusted body weight (ABW) in combination with enza 160 mg/day. Dose escalation was explored with and without prophylactic granulocyte colony-stimulating factor (G-CSF) support.
Related Clinical Trial
NCT Number	NCT05011188	Phase Status	PHASE1|||PHASE2
Clinical Description	A Phase 1b/2 Study of FOR46 in Combination With Enzalutamide in Patients With Metastatic Castration Resistant Prostate Cancer
Primary Endpoint	The Phase 1b trial evaluates the maximum tolerated dose (MTD) of FOR46 over 3 weeks by dose-escalation with cohorts of 3+3/6 patients-dose-limiting toxicities (DLTs, per CTCAE v5.0) determine escalation (stopped if ≥2/3-6 patients experience DLTs). Phase 2 assesses composite response rate (CRR; ≥50% PSA decline + RECIST 1.1 response) over 2 years with 95% CIs.    Click to Show/Hide
Other Endpoint	Efficacy endpoints include PSA50 (≥50% PSA decline), ORR (RECIST 1.1), duration of response, time to PSA progression, rPFS (PCWG3), and median overall survival (Kaplan-Meier, 2-year follow-up). Safety tracks AE frequency/severity (CTCAE v5.0).

Experiment 1 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Objective Response Rate (ORR)	30%
Patients Enrolled	Patients with diffuse large B-cell lymphoma (DLBCL), PET-positive disease, and ECOG PS of 0-2. Pts must have received 2 prior lines of therapy.
Administration Dosage	2.50 mg/kg IV Q3W.
Related Clinical Trial
NCT Number	NCT05144841	Phase Status	Phase 2
Clinical Description	A phase 2 open-label clinical study to evaluate the efficacy and safety of zilovertamab vedotin (MK-2140) in participants with relapsed or refractory diffuse large B-cell lymphoma (waveline-004).
Experiment 2 Reporting the Activity Date of This ADC					[187]
Efficacy Data	Objective Response Rate (ORR)	47.00 60.00 %
Patients Enrolled	Patients with tumor histologies of mantle cell lymphoma (MCL), chronic lymphocytic leukemia, diffuse large B-cell lymphoma (DLBCL). Patients had received a median of four previous drug and/or cellular therapies.
Administration Dosage	2.50 mg/kg every 3 week.
Related Clinical Trial
NCT Number	NCT03833180	Phase Status	Phase 1
Clinical Description	A phase 1 dose-escalation and cohort-expansion study of VLS-101 in subjects with hematological malignancies (waveline-001).
Experiment 3 Reporting the Activity Date of This ADC					[188]
Patients Enrolled	Patients with diffuse large B-cell lymphoma (DLBCL) after 1 line of prior therapy (cohort A) or 2 lines of prior therapy (cohort B).
Administration Dosage	ZV (1.50, 1.75, 2.00, 2.25, and 2.50 mg/kg) with gemcitabine-oxaliplatin + rituximab (R-GemOx).
Related Clinical Trial
NCT Number	NCT05139017	Phase Status	Phase 2/3
Clinical Description	A phase 2/3 multicenter, open-label, randomized, active-control study of zilovertamab vedotin (MK-2140) in combination with standard of care in participants with relapsed or refractory diffuse large B-cell lymphoma (waveline-003).
Experiment 4 Reporting the Activity Date of This ADC					[190]
Patients Enrolled	Patients with mantle cell lymphoma (MCL), Richter's transformation (RT), chronic lymphocytic leukemia (CLL), or follicular lymphoma (FL), relapsed or refractory (R/R) disease, ECOG performance status of 0 to 2.
Administration Dosage	ZV 2.0 to 2.50 mg/kg IV Q3W.
Related Clinical Trial
NCT Number	NCT05458297	Phase Status	Phase 2
Clinical Description	A multicenter, open-label, phase 2 basket study to evaluate the safety and efficacy of MK-2140 as a monotherapy and in combination in participants with aggressive and indolent B-cell malignancies.
Experiment 5 Reporting the Activity Date of This ADC					[191]
Patients Enrolled	Patients with previously untreated histologically confirmed diffuse large B-cell lymphoma (DLBCL), PET-positive and ECOG PS of 0 or 1.
Administration Dosage	ZV was 1.75 mg/kg (modified to 1.50, 2.00, 2.25, or 2.50 mg/kg) administered as an intravenous infusion every 3 weeks (Q3W) in combination with R-CHP.
Related Clinical Trial
NCT Number	NCT05406401	Phase Status	Phase 2
Clinical Description	A multicenter, open-label, phase 2 dose escalation and confirmation, and efficacy expansion study of zilovertamab vedotin (MK-2140) in combination with r-chp in participants with DLBCL (waveline).
Experiment 6 Reporting the Activity Date of This ADC					[193]
Patients Enrolled	Patients with locally advanced or metastatic urothelial carcinoma (mUC) whose disease is resistant to treatment with programmed cell death-1/ligand 1 (PD-1/L1) inhibitors.
Related Clinical Trial
NCT Number	NCT05562830	Phase Status	Phase 1/2
Clinical Description	A phase 1/2 open-label rolling-arm umbrella platform study of investigational agents with or without pembrolizumab in participants with PD-1/L1 refractory locally advanced or metastatic urothelial carcinoma (keymaker-u04): substudy 04a.
Experiment 7 Reporting the Activity Date of This ADC					[195]
Related Clinical Trial
NCT Number	NCT04504916	Phase Status	Phase 1
Clinical Description	A phase 2 study of VLS-101 in patients with solid tumors.
Experiment 8 Reporting the Activity Date of This ADC					[199]
Efficacy Data	Partial Response (PR)	32%
Patients Enrolled	Key eligibility requires relapsed/refractory B-cell malignancies (MCL post ≥2 therapies including BTKi+CAR-T; FL/CLL post ≥2 lines) with histologic confirmation (WHO 2016). Exclusions encompass active CVD, Grade >1 neuropathy, prior solid organ transplant, uncontrolled infections (HBV/HCV/HIV), recent anticancer therapy (within 2-4 weeks), CNS lymphoma, or corticosteroid use >30mg prednisone equivalent. HBV+ candidates require antiviral therapy with undetectable viral load.    Click to Show/Hide
Administration Dosage	Participants will receive either zilovertamab vedotin IV infusion Dose 1/2 every 3 weeks (Q3W) until disease progression or discontinuation.
Related Clinical Trial
NCT Number	NCT05458297	Phase Status	PHASE2
Clinical Description	A Multicenter, Open-label, Phase 2 Basket Study to Evaluate the Safety and Efficacy of MK-2140 as a Monotherapy and in Combination in Participants With Aggressive and Indolent B-cell Malignancies (waveLINE-006)
Primary Endpoint	Safety outcomes include AE rates (up to 57 months) across cohorts (MCL-C, FL-D, CLL), treatment discontinuations due to AEs, and DLTs in MCL-C (per CTCAE v5.0). Efficacy measures feature ORR by disease type - MCL-A/RT/FL-D&E via Lugano criteria (BICR), MCL-C via Lugano (investigator), and CLL via iwCLL criteria.
Other Endpoint	Secondary endpoints assess DOR by Lugano criteria (BICR for MCL-A/RT/FL-D&E; investigator for MCL-C) and iwCLL (CLL), tracking time from response to progression/death. Additional safety data includes AE incidence and treatment discontinuations in MCL-A/RT/FL-E cohorts over ~57 months.
Experiment 9 Reporting the Activity Date of This ADC					[202]
Efficacy Data	Objective Response Rate (ORR)	30%
Patients Enrolled	Eligible patients must have rrDLBCL failing ≥2 prior therapies (including alkylator/anthracycline/anti-CD20) and be post-CAR-T failure or ineligible, with ECOG 0-2 and adequate organ function. Exclusions: PMBCL, solid organ transplants, active cardiovascular/liver disease, neuropathy (>Grade 1), transformed DLBCL, GVHD, recent anticancer therapies/vaccines, uncontrolled infections, HIV/HBV/HCV, or CNS involvement. Prednisone >30mg/day or live vaccines within 30 days are prohibited.    Click to Show/Hide
Administration Dosage	Participants will receive treatment with zilovertamab vedotin 2.5 mg/kg via intravenous (IV) infusion on Day 1 of each 21-day cycle (every 3 weeks (Q3W)) until documented disease progression or any other discontinuation criterion is met.
Related Clinical Trial
NCT Number	NCT05144841	Phase Status	PHASE2
Clinical Description	A Phase 2 Open-label Clinical Study to Evaluate the Efficacy and Safety of Zilovertamab Vedotin (MK-2140) in Participants With Relapsed or Refractory Diffuse Large B-Cell Lymphoma (waveLINE-004)
Primary Endpoint	The objective response rate (ORR) is defined as the percentage of participants achieving complete response (CR) or partial response (PR) per Lugano 2014 criteria, assessed by blinded independent central review (BICR), in relapsed/refractory DLBCL patients treated with zilovertamab vedotin Q3W. CR requires full radiologic resolution, while PR necessitates ≥50% reduction in tumor burden across target lesions.    Click to Show/Hide
Other Endpoint	Duration of response (DOR) measures time from first CR/PR to disease progression/death. Safety evaluations include adverse event (AE) incidence and treatment discontinuations due to AEs over 50 months, with AEs defined as any treatment-associated medical occurrences regardless of causality.
Experiment 10 Reporting the Activity Date of This ADC					[199]
Efficacy Data	Objective Response Rate (ORR)	64%
Patients Enrolled	Key eligibility requires relapsed/refractory B-cell malignancies (MCL post ≥2 therapies including BTKi+CAR-T; FL/CLL post ≥2 lines) with histologic confirmation (WHO 2016). Exclusions encompass active CVD, Grade >1 neuropathy, prior solid organ transplant, uncontrolled infections (HBV/HCV/HIV), recent anticancer therapy (within 2-4 weeks), CNS lymphoma, or corticosteroid use >30mg prednisone equivalent. HBV+ candidates require antiviral therapy with undetectable viral load.    Click to Show/Hide
Administration Dosage	Participants will receive either zilovertamab vedotin IV infusion Dose 1/2 every 3 weeks (Q3W) until disease progression or discontinuation.
Related Clinical Trial
NCT Number	NCT05458297	Phase Status	PHASE2
Clinical Description	A Multicenter, Open-label, Phase 2 Basket Study to Evaluate the Safety and Efficacy of MK-2140 as a Monotherapy and in Combination in Participants With Aggressive and Indolent B-cell Malignancies (waveLINE-006)
Primary Endpoint	Safety outcomes include AE rates (up to 57 months) across cohorts (MCL-C, FL-D, CLL), treatment discontinuations due to AEs, and DLTs in MCL-C (per CTCAE v5.0). Efficacy measures feature ORR by disease type - MCL-A/RT/FL-D&E via Lugano criteria (BICR), MCL-C via Lugano (investigator), and CLL via iwCLL criteria.
Other Endpoint	Secondary endpoints assess DOR by Lugano criteria (BICR for MCL-A/RT/FL-D&E; investigator for MCL-C) and iwCLL (CLL), tracking time from response to progression/death. Additional safety data includes AE incidence and treatment discontinuations in MCL-A/RT/FL-E cohorts over ~57 months.
Experiment 11 Reporting the Activity Date of This ADC					[199]
Efficacy Data	Complete response (CR)	32%
Patients Enrolled	Key eligibility requires relapsed/refractory B-cell malignancies (MCL post ≥2 therapies including BTKi+CAR-T; FL/CLL post ≥2 lines) with histologic confirmation (WHO 2016). Exclusions encompass active CVD, Grade >1 neuropathy, prior solid organ transplant, uncontrolled infections (HBV/HCV/HIV), recent anticancer therapy (within 2-4 weeks), CNS lymphoma, or corticosteroid use >30mg prednisone equivalent. HBV+ candidates require antiviral therapy with undetectable viral load.    Click to Show/Hide
Administration Dosage	Participants will receive either zilovertamab vedotin IV infusion Dose 1/2 every 3 weeks (Q3W) until disease progression or discontinuation.
Related Clinical Trial
NCT Number	NCT05458297	Phase Status	PHASE2
Clinical Description	A Multicenter, Open-label, Phase 2 Basket Study to Evaluate the Safety and Efficacy of MK-2140 as a Monotherapy and in Combination in Participants With Aggressive and Indolent B-cell Malignancies (waveLINE-006)
Primary Endpoint	Safety outcomes include AE rates (up to 57 months) across cohorts (MCL-C, FL-D, CLL), treatment discontinuations due to AEs, and DLTs in MCL-C (per CTCAE v5.0). Efficacy measures feature ORR by disease type - MCL-A/RT/FL-D&E via Lugano criteria (BICR), MCL-C via Lugano (investigator), and CLL via iwCLL criteria.
Other Endpoint	Secondary endpoints assess DOR by Lugano criteria (BICR for MCL-A/RT/FL-D&E; investigator for MCL-C) and iwCLL (CLL), tracking time from response to progression/death. Additional safety data includes AE incidence and treatment discontinuations in MCL-A/RT/FL-E cohorts over ~57 months.
Experiment 12 Reporting the Activity Date of This ADC					[221]
Patients Enrolled	Eligible patients (≥18 years, ECOG 0-2) must have relapsed/refractory CLL/SLL, NHL (MCL/FL/DLBCL/etc.), ALL, or AML with measurable disease and adequate organ function. Key exclusions include CNS malignancy, uncontrolled infections, Grade >1 neuropathy, recent major surgery, strong CYP3A4 modulators, HSCT/CAR-T candidates, prior ROR1-targeted therapy, or concurrent corticosteroids >30mg prednisone equivalent. Baseline tumor tissue and resolution of prior therapy toxicities (≤Grade 1) are required.    Click to Show/Hide
Administration Dosage	Participants will be administered escalating doses of zilovertamab vedotin at 0.50, 1.00, 1.50, 2.25, 2.50, 2.75, and 3.00 mg/kg IV on Day 1 of repeated 21-day cycles (Q1/3W); Participants will be administered escalating doses of zilovertamab vedotin at 0.75, 1.00, 1.25, 1.50, 1.75, 2.00, and 2.25 mg/kg IV on Day 1 and 8 of repeated 21-day cycles (Q2/3W); Participants will be administered escalating doses of zilovertamab vedotin at 0.75, 1.00, 1.25, 1.50, 1.75, 2.00, and 2.25 mg/kg IV on Day 1, 8, and 15 of repeated 21-day cycles (Q3/4W).    Click to Show/Hide
Related Clinical Trial
NCT Number	NCT03833180	Phase Status	PHASE1
Clinical Description	A Phase 1 Dose-Escalation and Cohort-Expansion Study of VLS-101 in Subjects With Hematological Malignancies (waveLINE-001)
Primary Endpoint	The primary objectives focus on determining the MTD of zilovertamab vedotin (highest dose with ≤17% DLT rate in Cycle 1) and establishing the RDR considering safety, PK/PD, and efficacy data during the initial 21-day cycle.
Other Endpoint	Key safety assessments include TEAEs, SAEs, AESIs (Grade ≥3 infusion reactions, TLS, peripheral neuropathy), treatment discontinuations, and DLTs over ~3.5 years. Pharmacokinetic parameters (Cmax, Tmax, AUC, Vd, CL, t½) for zilovertamab vedotin, UC-961 antibody, and MMAE will be evaluated across treatment cycles (up to ~3.5 years), alongside immunogenicity (anti-drug antibodies) and efficacy measures (OR, CRMRD-, tumor dimension changes, TTR, DOR, PFS, TTF, OS) in hematologic malignancies.    Click to Show/Hide
Experiment 13 Reporting the Activity Date of This ADC					[222]
Patients Enrolled	Eligibility requires untreated, PET-positive DLBCL (Lugano 4-5) confirmed by BICR, ECOG 0-1. Exclusions encompass transformed lymphoma, organ transplant history, active CVD (recent MI/stroke, NYHA ≥II), Grade >1 neuropathy, prior radiotherapy (<28 days), corticosteroids >30mg prednisone daily, strong CYP3A4 modulators (<7 days), active infections (HBV/HCV/HIV), CNS involvement, or second malignancies (<2 years remission except certain skin cancers).    Click to Show/Hide
Administration Dosage	Approximately 60 patients will be enrolled (part 1, n = 45; part 2, n = 15). Part 1 will use a modified toxicity probability interval design to establish the RP2D of ZV when administered with R-CHP. The starting dose of ZV will be 1.75 mg/kg (modified to 1.5, 2.0, 2.25, or 2.5 mg/kg) administered as an intravenous infusion every 3 weeks (Q3W) in combination with R-CHP.    Click to Show/Hide
Related Clinical Trial
NCT Number	NCT05406401	Phase Status	PHASE2
Clinical Description	A Multicenter, Open-label, Phase 2 Dose Escalation and Confirmation, and Efficacy Expansion Study of Zilovertamab Vedotin (MK-2140) in Combination With R-CHP in Participants With DLBCL (waveLINE)
Primary Endpoint	Safety assessments focus on DLTs per CTCAE v5.0 during Cycle 1 (21 days), overall AE incidence (up to 8 months), and treatment discontinuations due to AEs (up to 5.5 months). Efficacy measures include CRR and ORR per Lugano criteria (investigator-assessed via CT/MRI/PET imaging and clinical findings) with reporting through ~60 months.
Other Endpoint	Key efficacy analysis evaluates DOR (time from first CR/PR to progression/death) per Lugano criteria (investigator-assessed via imaging/clinical evaluation) over ~60 months, alongside ORR reporting (CR+PR rates) for the same period.
Experiment 14 Reporting the Activity Date of This ADC					[223]
Patients Enrolled	Eligibility requires histologically confirmed DLBCL (Lugano-measurable, ECOG 0-2) with relapsed/refractory status post ≥1 prior therapy (including ASCT/CAR-T failure). Exclusions: transformed DLBCL, organ transplant history, active CVD/GVHD, Grade >1 neuropathy, second malignancy (<2 years remission), recent anticancer therapy/radiotherapy (4 weeks), CNS involvement, active infections (HIV/HCV), or uncontrolled psychiatric/substance disorders. Prior CNS disease requires confirmed remission.    Click to Show/Hide
Administration Dosage	Approximately 420 patients will be enrolled in the study (cohort A, n = 230; cohort B, n = 190). In the part 1 dose confirmation phase, 30 patients from cohort A will receive ZV (at increasing doses: 1.5, 1.75, 2.0, 2.25, and 2.5 mg/kg; starting at 1.75 mg/kg) plus gemcitabine-oxaliplatin + rituximab (R-GemOx) to establish the recommended phase 2 dose using the mTPI design.    Click to Show/Hide
Related Clinical Trial
NCT Number	NCT05139017	Phase Status	PHASE2|||PHASE3
Clinical Description	A Phase 2/3 Multicenter, Open-label, Randomized, Active-Control Study of Zilovertamab Vedotin (MK-2140) in Combination With Standard of Care in Participants With Relapsed or Refractory Diffuse Large B-Cell Lymphoma (waveLINE-003)
Primary Endpoint	Safety analysis includes dose-limiting toxicities (DLTs) in Part 1 (6 weeks, per CTCAE v5.0), overall AE incidence (68 months), and treatment discontinuations due to AEs (68 months). Key efficacy endpoints are overall survival (OS, 35 months) and progression-free survival (PFS, 26 months) - both assessed from randomization to disease progression (Lugano/BICR) or death.    Click to Show/Hide
Other Endpoint	Response evaluation comprises objective response rate (ORR, 26 months) measuring CR+PR rates per Lugano criteria (BICR-assessed) and duration of response (DOR, 26 months) tracking time from initial response to progression/death.
Experiment 15 Reporting the Activity Date of This ADC					[224]
Patients Enrolled	Eligible patients have untreated PET-positive DLBCL (Lugano 4-5), ECOG 0-2, and adequate cardiac/organ function; HIV/HBV/HCV control is required if applicable. Exclusions: transformed DLBCL, PMBCL, Stage I disease, active CVD/neuropathy (>Grade 1), CNS involvement, uncontrolled infections/autoimmunity, or concurrent malignancies within 2 years. Live vaccines and allogeneic transplants are prohibited.    Click to Show/Hide
Related Clinical Trial
NCT Number	NCT06717347	Phase Status	PHASE3
Clinical Description	A Randomized, Open-Label, Multicenter, Phase 3 Study of Zilovertamab Vedotin (MK-2140) in Combination With R-CHP Versus R-CHOP in Participants With Previously Untreated Diffuse Large B-Cell Lymphoma (DLBCL) (waveLINE-010)
Primary Endpoint	Primary endpoints include PFS (50 months, time from randomization to progression/death per Lugano/BICR) and CR at EOT (32 months, BICR-assessed complete response excluding early discontinuations). Secondary efficacy measures comprise OS (74 months), EFS (74 months, covering progression/recurrence/second malignancy/death), and DurCR (74 months, sustained CR until progression/death).    Click to Show/Hide
Other Endpoint	Safety assessments track AE incidence (9 months) and treatment discontinuations due to AEs (6 months). HRQoL is evaluated via FACT-Lym (Week 25 vs. baseline), measuring physical, emotional, functional, and lymphoma-specific domains (0-168 scale, higher=better), alongside neurotoxicity using FACT/GOG-NTX (0-44 scale for sensory/motor symptoms).
Experiment 16 Reporting the Activity Date of This ADC					[225]
Patients Enrolled	Eligible patients must have confirmed B-ALL, DLBCL/Burkitt lymphoma, neuroblastoma, or Ewing sarcoma per WHO/histologic criteria. Exclusions: solid organ transplants, active cardiovascular disease (e.g., arrhythmias, cirrhosis), neuropathy (>Grade 1), Down syndrome, GVHD, HIV/HBV/HCV, or recent cytotoxic/CYP3A4-modulating therapies. Prohibited: live vaccines (30 days prior), chronic steroids (>10mg prednisone/day), unresolved post-surgical complications, or concurrent malignancies requiring treatment. Prior radiotherapy/systemic therapy requires washout (4 weeks).    Click to Show/Hide
Administration Dosage	Participants receive escalating doses of zilovertamab vedotin via intravenous (IV) infusion on Day 1 of each 21-day cycle (every 3 weeks).
Related Clinical Trial
NCT Number	NCT06395103	Phase Status	PHASE1|||PHASE2
Clinical Description	LIGHTBEAM-U01 Substudy 01A: A Phase 1/2 Substudy to Evaluate the Safety and Efficacy of Zilovertamab Vedotin in Pediatric and Young Adult Participants With Hematologic Malignancies or Solid Tumors
Primary Endpoint	The primary objectives assess safety and efficacy in pediatric patients (aged 1-18 years). Part 1 evaluates dose-limiting toxicities (DLTs) within 42 days and tracks adverse events (AEs), treatment discontinuations, and dose modifications over 60 months. Efficacy endpoints include objective response rates (ORR) per disease-specific criteria: CR/CRi for B-ALL (Ponte-di-Legno) and CR/PR for DLBCL/Burkitt lymphoma (IPNHL), neuroblastoma (INRC), and Ewing sarcoma (RECIST 1.1). Key secondary measures include duration of response (DOR) and rates of subsequent SCT or CAR-T therapy.    Click to Show/Hide
Other Endpoint	Pharmacokinetic analyses measure exposure (AUC), peak/trough concentrations (Cmax/Ctrough), and half-life (t1/2) for total antibody, ADC, and MMAE across cycles (21-day intervals) over 60 months. Immunogenicity is assessed via antidrug antibody (ADA) incidence. Part 2 monitors AE-related outcomes (incidence, discontinuations, dose modifications) alongside efficacy metrics. Treatment impact is further characterized by post-therapy SCT/CAR-T utilization rates.    Click to Show/Hide
Experiment 17 Reporting the Activity Date of This ADC					[226]
Patients Enrolled	Participants were required to provide tumor tissue, demonstrate negative or controlled HIV/hepatitis status, complete prior therapies, and adhere to contraception protocols, with stringent monitoring of pharmacokinetic profiles across specified timepoints in 21-day cycles.
Administration Dosage	Participants will receive intravenous (IV) zilovertamab vedotin 2.5 mg/kg on Day 1 of each repeated 21-day cycle (Q1/3W) or 1.75 mg/kg on Day 1 and Day 8 of each 21-day cycle (Q2/3W). Treatment will continue until progressive disease or discontinuation
Related Clinical Trial
NCT Number	NCT04504916	Phase Status	PHASE2
Clinical Description	A Phase 2 Study of VLS-101 in Patients With Solid Tumors
Primary Endpoint	Efficacy endpoints included Objective Response Rate (ORR) assessed by both Blinded Independent Central Review (BICR) and investigators per RECIST v1.1, with key measures like Time to Response (TTR), Duration of Response (DOR), Progression-Free Survival (PFS), Time to Treatment Failure (TTF), and Overall Survival (OS) tracked over ~30 months. Safety assessments involved monitoring Adverse Events (AEs), treatment discontinuations due to AEs, and pharmacokinetic parameters (Cmax, AUC) for zilovertamab vedotin, total antibody, and MMAE under Q1/3W and Q2/3W dosing schedules.    Click to Show/Hide
Other Endpoint	The study enrolled patients with metastatic solid tumors (TNBC, HER2-negative breast cancer, NSCLC, gastric, pancreatic, or platinum-resistant ovarian cancer) who progressed after prior therapy, had measurable disease, and adequate organ function. Key exclusions included Grade >1 neuropathy, CNS malignancies, other major cancers, uncontrolled infections, cardiovascular disease, liver cirrhosis, pregnancy, recent major surgery, MMAE intolerance, or concurrent trial participation.    Click to Show/Hide
Experiment 18 Reporting the Activity Date of This ADC					[226]
Patients Enrolled	Eligible participants had histologically confirmed locally advanced/unresectable or metastatic urothelial cancer (mUC), refractory to PD-1/L1 therapy, with available tumor biopsy for biomarker analysis. Key exclusions included other active malignancies, recent systemic therapy (within 4 weeks), active infections requiring treatment, recent live vaccines (within 30 days), and HIV/hepatitis B/C infections.    Click to Show/Hide
Administration Dosage	Participants will receive zilovertamab vedotin 2mg/kg administered on Day 1 and Day 8 of each 3 week cycle (Q3W) until documented disease progression or any other discontinuation criterion is met.
Related Clinical Trial
NCT Number	NCT05562830	Phase Status	PHASE1|||PHASE2
Clinical Description	A Phase 1/2 Open-Label Rolling-Arm Umbrella Platform Study of Investigational Agents With or Without Pembrolizumab in Participants With PD-1/L1 Refractory Locally Advanced or Metastatic Urothelial Carcinoma (KEYMAKER-U04): Substudy 04A
Primary Endpoint	The safety and efficacy endpoints involved tracking adverse events (AEs) over ~5 years, including discontinuation rates due to AEs, while efficacy was assessed via Objective Response Rate (ORR) using RECIST 1.1 criteria (CR: disappearance of all target lesions; PR: ≥30% decrease in sum of lesion diameters) over ~2 years, with results reviewed by Blinded Independent Central Review (BICR).    Click to Show/Hide
Other Endpoint	Duration of Response (DOR) was evaluated over ~2 years, measuring the time from first confirmed CR/PR (per RECIST 1.1) until progressive disease (PD: ≥20% increase in lesion diameters with ≥5 mm absolute growth or new lesions) or death, with assessments confirmed by BICR.

Experiment 1 Reporting the Activity Date of This ADC					[197]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 0%	Negative ROR1 expression (ROR1-)
Method Description	VLS-101 induces efficient tumor cell killing in cell line-derived models of IP867/17 and RS1316 cells with UC-961 expression with high expression. After palpable tumors were evident (tumor volume of 0.2 cm3),animals were randomly assigned to vehicle,VLS 101 5 mg/kg.
In Vivo Model	Richter syndrome PDX model (PDX: RS9737)
Experiment 2 Reporting the Activity Date of This ADC					[197]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 0%	Negative ROR1 expression (ROR1-)
Method Description	VLS-101 induces efficient tumor cell killing in cell line-derived models of IP867/17 and RS1316 cells with UC-961 expression with high expression. After palpable tumors were evident (tumor volume of 0.2 cm3),animals were randomly assigned to vehicle,VLS 101 2.5 mg/kg.
In Vivo Model	Richter syndrome PDX model (PDX: RS9737)
Experiment 3 Reporting the Activity Date of This ADC					[197]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 88.80%	High ROR1 expression (ROR1+++)
Method Description	VLS-101 induces efficient tumor cell killing in cell line-derived models of IP867/17 and RS1316 cells with UC-961 expression with high expression. After palpable tumors were evident (tumor volume of 0.2 cm3),animals were randomly assigned to vehicle,VLS 101 2.5 mg/kg.
In Vivo Model	Richter syndrome PDX model (PDX: IP867/17)
Experiment 4 Reporting the Activity Date of This ADC					[197]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 90.90%	Moderate ROR1 expression (ROR1++)
Method Description	VLS-101 induces efficient tumor cell killing in cell line-derived models of IP867/17 and RS1316 cells with UC-961 expression with high expression. After palpable tumors were evident (tumor volume of 0.2 cm3),animals were randomly assigned to vehicle,VLS 101 2.5 mg/kg.
In Vivo Model	Richter syndrome PDX model (PDX: RS9737)
Experiment 5 Reporting the Activity Date of This ADC					[197]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100%	Moderate ROR1 expression (ROR1++)
Method Description	VLS-101 induces efficient tumor cell killing in cell line-derived models of IP867/17 and RS1316 cells with UC-961 expression with high expression. After palpable tumors were evident (tumor volume of 0.2 cm3),animals were randomly assigned to vehicle,VLS 101 5 mg/kg.
In Vivo Model	Richter syndrome PDX model (PDX: RS9737)
Experiment 6 Reporting the Activity Date of This ADC					[197]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100%	High ROR1 expression (ROR1+++)
Method Description	VLS-101 induces efficient tumor cell killing in cell line-derived models of IP867/17 and RS1316 cells with UC-961 expression with high expression. After palpable tumors were evident (tumor volume of 0.2 cm3),animals were randomly assigned to vehicle,VLS 101 5 mg/kg.
In Vivo Model	Richter syndrome PDX model (PDX: RS9737)
Experiment 7 Reporting the Activity Date of This ADC					[197]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100%	High ROR1 expression (ROR1+++)
Method Description	VLS-101 induces efficient tumor cell killing in cell line-derived models of IP867/17 and RS1316 cells with UC-961 expression with high expression. After palpable tumors were evident (tumor volume of 0.2 cm3),animals were randomly assigned to vehicle,VLS 101 2.5 mg/kg.
In Vivo Model	Richter syndrome PDX model (PDX: RS9737)
Experiment 8 Reporting the Activity Date of This ADC					[197]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100%	High ROR1 expression (ROR1+++)
Method Description	VLS-101 induces efficient tumor cell killing in cell line-derived models of IP867/17 and RS1316 cells with UC-961 expression with high expression. After palpable tumors were evident (tumor volume of 0.2 cm3),animals were randomly assigned to vehicle,VLS 101 5 mg/kg.
In Vivo Model	Richter syndrome PDX model (PDX: IP867/17)

Experiment 1 Reporting the Activity Date of This ADC					[184]
Efficacy Data	Objective Response Rate (ORR)	35%
Patients Enrolled	Unresectable locally advanced or metastatic triple-negative breast cancer (mTNBC). Patients must have measureable disease per RECIST v1.1, an ECOG score of 0 or 1, and no prior cytotoxic or anti-PD-L1 treatment for advanced disease.
Administration Dosage	LV 2.50 mg/kg + pembrolizumab 200 mg intravenously every three weeks.
Related Clinical Trial
NCT Number	NCT03310957	Phase Status	Phase 1/2
Clinical Description	Single arm, open label phase 1b/2 study of SGN-LIV1A in combination with pembrolizumab for first-line treatment of patients with unresectable locally-advanced or metastatic triple-negative breast cancer.
Experiment 2 Reporting the Activity Date of This ADC					[186]
Efficacy Data	Objective Response Rate (ORR)	32%
Patients Enrolled	Women with LIV-1-positive, unresectable, locally advanced or metastatic breast cancer (LA/MBC).
Administration Dosage	Received a median of 3 cycles (range, 112) of SGN-LIV1A at doses of 0.50-2.80 mg/kg.
Related Clinical Trial
NCT Number	NCT01969643	Phase Status	Phase 1
Clinical Description	A phase 1, open-label, dose-escalation study to evaluate the safety and tolerability of SGN-LIV1A in patients with metastatic breast cancer.
Experiment 3 Reporting the Activity Date of This ADC					[192]
Related Clinical Trial
NCT Number	NCT04032704	Phase Status	Phase 2
Clinical Description	Open-label phase 2 study of ladiratuzumab vedotin (LV) for unresectable locally advanced or metastatic solid tumors.
Experiment 4 Reporting the Activity Date of This ADC					[201]
Efficacy Data	Objective Response Rate (ORR)	28%
Patients Enrolled	Eligible patients require pathologically confirmed, incurable LA/MBC (subtype-specific criteria for Parts A-F), measurable disease, ECOG 0-1, and adequate organ function; exclusions encompass severe neuropathy (≥Grade 2), untreated CNS metastases, prior LV/MMAE therapy, and trastuzumab hypersensitivity (combination arm). Tumor PD-L1/CPS and LIV-1 expression are mandated for specific cohorts.    Click to Show/Hide
Administration Dosage	SGNLVA-001 (NCT01969643) is an ongoing, multi-part, open label study investigating the safety and efficacy of LV in patients with metastatic breast cancer (mBC). Part E evaluated LV q1w in escalation and expansion starting at LV 1.0 mg/kg q1w. Patients with first (1L) or second line (2L) endocrine therapy refractory hormone receptor-positive (HR+)/HER2-negative (HER2-) mBC or 2L mTNBC were enrolled. Tumor assessments occurred every 6 weeks per RECIST v1.1.    Click to Show/Hide
Related Clinical Trial
NCT Number	NCT01969643	Phase Status	PHASE1
Clinical Description	A Phase 1, Open-Label, Dose-Escalation Study to Evaluate the Safety and Tolerability of SGN-LIV1A in Patients With Metastatic Breast Cancer
Primary Endpoint	Safety assessments include monitoring adverse events (AEs), laboratory abnormalities, and dose-limiting toxicities (DLTs) throughout treatment and up to 1 month post-treatment (approx. 2 years) using descriptive statistics to evaluate tolerability.
Other Endpoint	Pharmacodynamic measures (blood concentrations of LV/metabolites, anti-drug antibodies) and efficacy endpoints (ORR per RECIST v1.1, DOR, PFS, OS, PFS ratio to prior therapy) will be tracked for up to 3-8 years to assess pharmacokinetics, immunogenicity, and clinical response durability.
Experiment 5 Reporting the Activity Date of This ADC					[217]
Patients Enrolled	Eligible patients must have untreated metastatic/locally-advanced TNBC (PD-L1 CPS<10 for Part D), measurable lesions (≥10mm tumor/≥15mm lymph node), ECOG 0-1, and adequate organ function. Key exclusions: prior immuno-oncology therapy, Grade≥2 neuropathy, active CNS metastases (unless treated/stable for ≥4 weeks without steroids), recent radiotherapy (<2 weeks), active autoimmune disease/interstitial lung disease, or steroid-requiring pneumonitis.    Click to Show/Hide
Administration Dosage	Patients will receive LV at 1.5 mg/kg on Days 1 and 8 plus pembrolizumab 200 mg on Day 1 Q3W.
Related Clinical Trial
NCT Number	NCT03310957	Phase Status	PHASE1|||PHASE2
Clinical Description	Single Arm, Open Label Phase 1b/2 Study of SGN-LIV1A in Combination With Pembrolizumab for First-Line Treatment of Patients With Unresectable Locally-Advanced or Metastatic Triple-Negative Breast Cancer
Primary Endpoint	The primary efficacy and safety assessments include confirmed objective response rate (ORR) per RECIST v1.1 evaluated up to 18 weeks post-treatment (~1 year), alongside monitoring of adverse events, laboratory abnormalities, and dose-limiting toxicities throughout treatment and up to 1 month post-treatment (~10 months).
Other Endpoint	Secondary endpoints assessing long-term clinical outcomes include duration of response (DOR), disease control rate (DCR), progression-free survival (PFS), and overall survival (OS), all evaluated per RECIST v1.1 and tracked for up to 2.5 years post-treatment to determine therapeutic durability and survival benefits.
Experiment 6 Reporting the Activity Date of This ADC					[218]
Patients Enrolled	Eligible patients must have metastatic/inoperable locally advanced breast cancer (RECIST v1.1 measurable disease), ECOG 0-1, life expectancy ≥3 months, and adequate organ function. Key exclusions: prior immune checkpoint therapies (anti-PD-1/PD-L1/CTLA-4), active/uncontrolled CNS metastases, autoimmune/immunodeficiency disorders, severe infections, significant cardiovascular disease, recent immunosuppressants, or pregnancy/breastfeeding. Tumor biopsy/biomarker testing is mandatory.    Click to Show/Hide
Related Clinical Trial
NCT Number	NCT03424005	Phase Status	PHASE1|||PHASE2
Clinical Description	A Phase Ib/II, Open-Label, Multicenter, Randomized Umbrella Study Evaluating The Efficacy And Safety Of Multiple Treatment Combinations In Patients With Metastatic Breast Cancer (Morpheus-panBC)
Primary Endpoint	Primary efficacy is assessed via Objective Response Rate (ORR) evaluated from baseline until disease progression or loss of clinical benefit (up to ~10 years), alongside long-term monitoring of adverse events throughout the study duration.
Other Endpoint	Secondary endpoints include Progression-Free Survival (PFS), Disease Control Rate (DCR), Overall Survival (OS) at 12/18 months and overall study duration (up to ~10 years), Duration of Response (DOR), and safety profiles-all per RECIST v1.1-to evaluate treatment durability, disease stabilization, and survival outcomes.
Experiment 7 Reporting the Activity Date of This ADC					[219]
Patients Enrolled	Eligible patients must have newly diagnosed invasive breast cancer (Stage II-III or T4/Nany/M0; tumor ≥2.5cm) without prior chemo/radiation. Key requirements: ECOG 0-1, adequate organ function, MRI compatibility, and biomarker-evaluable tumor (MammaPrint High or ER-/HER2+). Exclusions: metastatic disease, severe cardiac conditions, active infections, or prior investigational drug use within 30 days. Baseline biopsies and serial imaging are mandatory.    Click to Show/Hide
Related Clinical Trial
NCT Number	NCT01042379	Phase Status	PHASE2
Clinical Description	I-SPY Trial (Investigation of Serial Studies to Predict Your Therapeutic Response With Imaging And moLecular Analysis 2)
Primary Endpoint	The primary objective is to evaluate if adding experimental agents to standard neoadjuvant chemotherapy improves pathologic complete response (pCR) rates, stratified by biomarker signatures, with assessments conducted post-surgery following up to 36 weeks of treatment.
Other Endpoint	Secondary goals include developing predictive/prognostic models using biomarkers (from blood/tissue collected at baseline, mid-treatment, and pre/post-surgery) for pCR and residual cancer burden (RCB), while also analyzing 3/5-year relapse-free and overall survival rates. Safety profiles (AEs/SAEs) and treatment response via MRI volumetric changes (at 4 timepoints) will be monitored throughout the study.    Click to Show/Hide
Experiment 8 Reporting the Activity Date of This ADC					[220]
Patients Enrolled	Eligible participants had measurable disease (RECIST v1.1), ECOG 0-1, and progression after prior therapy. Cohort-specific requirements: SCLC (1 prior platinum-based chemo), NSCLC (squamous/nonsquamous; EGFR/ALK/ROS wild-type; 1 prior chemo + anti-PD (L)1), HNSCC (platinum-refractory), esophageal/gastric (HER2-treated if applicable), CRPC (no prior chemo in mCRPC), and melanoma (anti-PD (L)1-refractory, BRAF-treated if mutated). Key exclusions: active CNS metastases, Grade ≥2 neuropathy, interstitial lung disease, or concurrent malignancy within 3 years.    Click to Show/Hide
Administration Dosage	SGNLVA-005 (NCT04032704) is an open-label, phase 2 study evaluating LV monotherapy in patients with 8 different advanced solid tumors in two parts (administered as a 30 minute intravenous infusion [IV]: Part A LV 2.5 mg/kg IV every 3 weeks [up to n = 72 total]; Part B LV 1.0 or 1.25 mg/kg every 1 week [up to n = 252 total]).
Related Clinical Trial
NCT Number	NCT04032704	Phase Status	PHASE2
Clinical Description	Open-Label Phase 2 Study of Ladiratuzumab Vedotin (LV) for Unresectable Locally Advanced or Metastatic Solid Tumors
Primary Endpoint	The primary efficacy endpoint was Objective Response Rate (ORR) per RECIST v1.1, defined as confirmed complete (disappearance of all target lesions) or partial response (≥30% decrease in lesion diameters) in Part A (up to 8.3 months follow-up) and Part B (up to 34.7 months). For prostate cancer (Cohort 7), PSA response (≥50% reduction confirmed ≥3 weeks apart) was additionally assessed per PCWG3 criteria with a maximum follow-up of 13.5 months.    Click to Show/Hide
Other Endpoint	Safety profiles-including treatment-emergent adverse events (TEAEs), serious AEs (≥Grade 3), and treatment-related AEs-were monitored up to 37.5 months. Secondary endpoints included Disease Control Rate (DCR: CR/PR/SD), Duration of Response (DOR), Progression-Free Survival (PFS), and Overall Survival (OS), all evaluated per RECIST v1.1. Pharmacokinetics (AUC21/AUC7, Cmax) for ladiratuzumab vedotin (ADC, TAB, MMAE) and antidrug antibody (ATA) incidence were also analyzed.    Click to Show/Hide

Experiment 1 Reporting the Activity Date of This ADC					[198]
Efficacy Data	Half Maximal Effective Concentration (EC50)	6.3 ng/mL
Method Description	The inhibitory activity of SGN-LIV1A against cancer cell growth was evaluated in various human cancer cell lines in vitro. The cells were treated 5 days.
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[185]
Efficacy Data	Objective Response Rate (ORR)	23.81 33.33 66.70 %
Patients Enrolled	CD20-positive relapsed or refractory (R/R) B-cell non Hodgkin lymphoma (NHL).
Administration Dosage	Six dose levels ranging from 0.15 to 2.50 mg/kg, intravenously once every 3 weeks (Q3W) for a maximum of 6 treatment cycles.
Related Clinical Trial
NCT Number	NCT05155839	Phase Status	Phase 1
Clinical Description	An open-label, multicenter, first-in-human, phase 1 dose-escalation and expansion clinical study to assess the safety, tolerability, pharmacokinetics and preliminary efficacy of MRG001 in patients with CD20-positive relapsed or refractory B-cell non-Hodgkin lymphoma (NHL).
Primary Endpoint	Rp2D=1.80 mg/kg.
Other Endpoint	Among 21 pts who had at least one tumor assessment, ORR=23.81% , PR rate=19.05% (N=4),CR rate=4.76% (N=1).
Experiment 2 Reporting the Activity Date of This ADC					[189]
Related Clinical Trial
NCT Number	NCT05844527	Phase Status	Phase 2
Clinical Description	Safety and efficacy of MRG-001 in wound healing in pre-abdominoplasty surgical excisions and scar appearance in subjects undergoing abdominoplasty.
Experiment 3 Reporting the Activity Date of This ADC					[211]
Patients Enrolled	Eligible patients (18-80 years) had relapsed/refractory B-cell NHL post-anti-CD20 therapy, ≥1 measurable lesion (Lugano 2014), ECOG 0-1, adequate organ function, and resolved prior toxicities (≤Grade 1). Exclusions: active HBV/HCV/HIV infection, uncontrolled infections/cardiovascular/pulmonary diseases, recent CAR-T/transplant/vaccines, concomitant CYP3A4 modulators, pregnancy/lactation, or conditions increasing study risk per investigator judgment. Phase Ia/Ib had specific hepatitis criteria.    Click to Show/Hide
Administration Dosage	All patients in Phase Ia (dose escalation) and Phase Ib (dose expansion) will be administrated MRG001 on Day 1 of every 3 weeks (21-day cycle).
Related Clinical Trial
NCT Number	NCT05155839	Phase Status	PHASE1
Clinical Description	An Open-label, Multicenter, First-in-human, Phase I Dose-escalation and Expansion Clinical Study to Assess the Safety, Tolerability, Pharmacokinetics and Preliminary Efficacy of MRG001 in Patients With CD20-positive Relapsed or Refractory B-cell Non-Hodgkin Lymphoma (NHL)
Primary Endpoint	This study evaluates safety and dosing through adverse events (AEs) recorded from baseline to 90 days post-treatment, maximum tolerated dose (MTD) defined by ≤1/6 patients experiencing dose-limiting toxicities (DLTs) in Cycle 1, and the establishment of a recommended Phase II dose (RP2D) for MRG001.
Other Endpoint	Secondary assessments include pharmacokinetics (concentration-time curves), immunogenicity (ADA positivity), and efficacy measures: objective response rate (ORR), duration of response (DoR), disease control rate (DCR), progression-free survival (PFS), and overall survival (OS)-tracked for up to 15 months from baseline.
Experiment 4 Reporting the Activity Date of This ADC					[212]
Patients Enrolled	Eligible adults (≥21 years) with recent-onset jaundice and heavy alcohol use (≥40g/day females, ≥60g/day males) must meet AH biochemical criteria (bilirubin >3mg/dL, AST 50-400 IU/L, MELD 21-30). Exclusions: concurrent liver diseases (viral/autoimmune), active infections, uncontrolled GI bleeding, severe organ dysfunction (EF <20%, platelets <30K/mm 3, hepatic encephalopathy ≥3), malignancies (<5 years), HIV/TB co-infection, transplant recipients, or hypersensitivity to MRG-001 components. Women must use contraception.    Click to Show/Hide
Related Clinical Trial
NCT Number	NCT06307522	Phase Status	PHASE2
Clinical Description	An Open-Label, Dose-Escalation Study to Assess the Safety, Pharmacokinetics and Pharmacodynamics of MRG-001 in Patients With Alcoholic Hepatitis
Primary Endpoint	The study evaluates MRG-001's safety and tolerability in alcoholic hepatitis (AH) patients by monitoring treatment-emergent adverse events (TEAEs) over 28 days, with SUSAR reporting as a key safety measure.
Other Endpoint	Pharmacokinetic analysis focuses on MRG-001's PK profile (trough levels of plerixafor/tacrolimus), while pharmacodynamic effects are assessed via flow cytometry to track CD34+ stem cell mobilization vs. baseline during the 28-day period.
Experiment 5 Reporting the Activity Date of This ADC					[213]
Patients Enrolled	Eligible patients (18-75 years) must have ALS (El Escorial criteria, symptom onset ≤48 months), ≥50% predicted vital capacity, and stable/no use of riluzole/edaravone/Relyvrio. Exclusions: organ dysfunction (e.g., EF <20%, platelets <30K/mm 3, CrCl <50 mL/min), active cancer (exceptions apply), psychiatric/cognitive impairment, prior ALS gene therapy, HIV, transplants, immunosuppressants (except steroids), pregnancy, or MRG-001 hypersensitivity.    Click to Show/Hide
Administration Dosage	MRG-001 will be subcutaneously administered at 0.01 mL/kg 3 times per week every other day for two weeks per month (Day 0, 2, 4, 7, 9, 11). This cycle will be repeated 3 months in total.
Related Clinical Trial
NCT Number	NCT06315608	Phase Status	PHASE2
Clinical Description	An Open-Label, Proof of Concept Study to Assess the Safety, Pharmacokinetics and Pharmacodynamics of MRG-001 in Patients With Amyotrophic Lateral Sclerosis
Primary Endpoint	The study evaluates the safety of MRG-001 in ALS patients over a 3-month period by monitoring treatment-emergent adverse events, with absence of serious adverse events (SAEs) as the primary safety endpoint.
Other Endpoint	Key secondary endpoints include stem cell mobilization (CD34+ count change at 24h), regulatory T-cell response (FOXP3+ count change at 24h), and disease progression (ALSFRS-R score at 0/1/2/3 months-higher scores indicate better function; positive/negative changes reflect reversal/worsening of ALS).
Experiment 6 Reporting the Activity Date of This ADC					[214]
Patients Enrolled	Eligible participants (18-55 years) are healthy non-smokers (BMI 25-35) undergoing elective abdominoplasty. Exclusions: recent investigational drug use, diabetes (HbA1C >5.7%), prior abdominal procedures, poor wound healing, collagen disorders, immunomodulatory therapy, pregnancy/breastfeeding, substance abuse, MRG-001 hypersensitivity, or situations compromising protocol adherence. Female participants must use contraception.    Click to Show/Hide
Administration Dosage	MRG-001 will be administered subcutaneously at 0.01 mL/kg bodyweight 3 times per week for 3 weeks.
Related Clinical Trial
NCT Number	NCT05844527	Phase Status	PHASE2
Clinical Description	Safety and Efficacy of MRG-001 in Wound Healing and Scar Appearance in Pre-Abdominoplasty Surgical Excisions
Primary Endpoint	The study assesses the preliminary effectiveness of MRG-001 on scar tensile strength, comparing Newton force measurements between MRG-001 and saline treatments during Weeks -6 to 0.
Other Endpoint	Safety, pharmacokinetics (Cmax, trough levels, clearance, t½), and pharmacodynamics (stem/immune cell presence in blood/tissue) of MRG-001 are evaluated versus placebo. Additional endpoints include time to wound re-epithelization (photographic assessment), scar appearance (modified POSAS), VAS pain scores, infection rates, and histological analysis of CD133+/CD34+/FOXP3+/macrophage cell populations in scars (Weeks -6 to 0).    Click to Show/Hide

Experiment 1 Reporting the Activity Date of This ADC					[203]
Efficacy Data	Objective Response Rate (ORR)	32%
Patients Enrolled	Eligibility covers stage III-IV SCCHN (oropharynx/larynx, excluding nasopharynx) in neoadjuvant/recurrent/metastatic settings; requires ECOG 0-1, measurable disease, and adequate organ function. Exclusions: prior PD-1/L1/CTLA-4 therapy (unless second-line), Grade≥3 mAb allergies, active HIV/HBV/HCV, or pregnancy.
Related Clinical Trial
NCT Number	NCT05271604	Phase Status	PHASE2
Clinical Description	A Phase 2 Open-Label Study of Ozuriftamab Vedotin (BA3021) in Patients with Recurrent or Metastatic Squamous Cell Carcinoma of the Head and Neck
Primary Endpoint	The efficacy endpoint includes confirmed ORR per RECIST v1.1 over 24 months, alongside AE/SAE incidence graded by CTCAE v5.
Other Endpoint	Additional efficacy measures assess DOR, PFS, BOR, DCR (CR/PR/SD≥12w), TTR, OS, and CR rate-all evaluated for up to 24 months.
Experiment 2 Reporting the Activity Date of This ADC					[215]
Patients Enrolled	Eligible patients have advanced/metastatic solid tumors (NSCLC/TNBC/STS preferred) refractory to SOC, measurable disease, ECOG 0-1, and adequate organ function; exclusions include active CNS metastases, prior auristatin therapy, Grade≥3 mAb allergies, HIV/HBV/HCV, or pregnancy within 4 weeks of surgery.
Related Clinical Trial
NCT Number	NCT03504488	Phase Status	PHASE1|||PHASE2
Clinical Description	A Phase 1/2 Safety and Efficacy Dose Escalation / Dose Expansion Study of a CAB-ROR2-ADC, Alone and in Combination With a PD-1 Inhibitor, in Patients With Advanced Solid Tumors (Ph1) and Melanoma and NSCLC Patients (Ph2)
Primary Endpoint	Phase 1 assesses DLTs, MTD, and AE/SAE frequency/severity over 24 months; Phase 2 evaluates confirmed ORR (CR/PR rate).
Other Endpoint	Phase 1 tracks PK profiles (ADC/MMAE plasma levels, Cmax, AUC), immunogenicity (ADA development), and efficacy (ORR, DOR, PFS, BOR, DCR, TTR, OS, tumor size change) across 24 months; Phase 2 expands efficacy endpoints.
Experiment 3 Reporting the Activity Date of This ADC					[216]
Patients Enrolled	Eligible participants are women aged ≥18 with platinum-resistant high-grade serous ovarian, fallopian tube, or peritoneal cancer, confirmed histologically, with measurable disease per RECIST 1.1, amenable to biopsies, and adequate organ function. Exclusion criteria include uncontrolled comorbidities, prior malignancies affecting safety assessment, active infections, severe autoimmune disorders, CNS metastases requiring steroids, pregnancy, and recent live vaccines.    Click to Show/Hide
Related Clinical Trial
NCT Number	NCT04918186	Phase Status	PHASE2
Clinical Description	An Immunotherapy Platform Study in Platinum Resistant High Grade Serous Ovarian Cancer
Primary Endpoint	The primary objective is to assess the objective response rate (ORR) by investigator evaluation using RECIST 1.1 criteria over 36 months, aiming to identify effective immunotherapy combinations for high-grade serous ovarian cancer for future randomized trials.
Other Endpoint	Key secondary endpoints include evaluating ORR via RECIST 1.1, progression-free survival (PFS) and overall survival (OS) by RECIST 1.1 and iRECIST, as well as monitoring adverse event frequency and severity over 36 months.

Experiment 1 Reporting the Activity Date of This ADC					[207]
Patients Enrolled	The study emphasizes rigorous safety (QTc monitoring, pregnancy prevention) and biomarker-driven enrollment (c-Met positivity), targeting refractory digestive cancers with comprehensive efficacy-safety profiling over 24 months (OS up to 5 years).
Related Clinical Trial
NCT Number	NCT05628857	Phase Status	PHASE2
Clinical Description	A Study to Evaluate the Efficacy, Safety and Pharmacokinetics of RC108 for Injection in the Treatment of Patients With c-Met-positiveAdvanced Digestive System Malignant Tumor
Primary Endpoint	Efficacy endpoints include ORR (CR+PR) and DOR per RECIST 1.1 along with disease control metrics (DCR, TTP, PFS) over 24 months. Safety assessments track AEs, while pharmacokinetics (AUC, Cmax, Tmax, half-life) are monitored throughout the treatment period.
Other Endpoint	Eligible participants (18-75 years) require c-Met-positive advanced/metastatic digestive system malignancies, ECOG 0-1, adequate organ function, and measurable lesions per RECIST 1.1. Key exclusions involve uncontrolled effusions, unresolved Grade ≥2 toxicities, recent oncology treatments/surgeries, active infections (HIV/HBV/HCV), or CNS metastases.    Click to Show/Hide
Experiment 2 Reporting the Activity Date of This ADC					[208]
Patients Enrolled	Exclusions: uncontrolled effusions, active infections (HBV/HCV/HIV), recent oncology treatments (≤4 weeks), untreated brain metastases (treated/stable≥3 months allowed), prior HGF/MET/PD-1/L1 inhibitors (Cohort-specific), QTc>450ms, ILD, or other malignancies within 5 years.
Related Clinical Trial
NCT Number	NCT05821933	Phase Status	PHASE1|||PHASE2
Clinical Description	An Open Single-arm Study to Evaluate the Safety, Tolerability, Efficacy of RC108 in Combination With Furmonertinib and Toripalimab in Patients With Advanced EGFR-mutated NSCLC Ib/II Study
Primary Endpoint	This study evaluates RC108 combined with Furmonertinib ± Toripalimab in advanced NSCLC patients with EGFR mutations (exon 19 del/L858R/T790M/etc.) and MET overexpression (IHC 1+/2+/3+), measuring efficacy (ORR, DCR, PFS, DOR up to 24 months), safety (DLTs/MTD in 21-day cycles), and PK parameters.
Other Endpoint	Key inclusion: Age 18-75, ECOG 0-1, adequate organ function (ANC≥1.5×109/L, platelets≥100×109/L, LVEF≥50%), EGFR-TKI progression history, measurable lesions (RECIST 1.1), and MET/PD-L1 testing. Pregnancy prevention required.
Experiment 3 Reporting the Activity Date of This ADC					[209]
Patients Enrolled	Eligible participants (18-70 years) must have c-Met-positive advanced solid tumors, ECOG 0-1, measurable lesions, and adequate organ function (ANC≥1.5×109/L, platelets≥100×109/L, LVEF≥50%). Exclusions: uncontrolled effusions, active infections (HBV/HCV/HIV), CNS metastases, prior anticancer therapy within 4 weeks, or unresolved CTCAE Grade ≥2 toxicity (excluding alopecia). Contraception is mandated.    Click to Show/Hide
Administration Dosage	Participants will be allocated to one of the following dose groups: 0.1, 0.3, 0.9, 1.5, 2.0, 2.5, and 3.0mg/kg, and receive a treatment of RC108-ADC followed by 21 days of dose limited toxicity (DLT) observation period.
Related Clinical Trial
NCT Number	NCT04617314	Phase Status	PHASE1
Clinical Description	A Phase I Study to Evaluate the Safety, Pharmacokinetics, and Effect of RC108-ADC for Injection in Subjects with C-Met Positive Advanced Malignant Solid Tumors
Primary Endpoint	The study monitors safety through AE reporting per NCI-CTCAE v4.03 until 28 days post-treatment and establishes MTD (≥2/6 patients experiencing DLTs within 21 days of first RC108 dose). Pharmacokinetics of RC108 (TAb/ADC/MMAE) are analyzed via serial blood sampling across doses to determine Cmax, Tmax, AUC, Ctrough, t1/2, and CL, alongside immunogenicity (anti-RC108 antibodies).    Click to Show/Hide
Other Endpoint	Efficacy endpoints include ORR (CR+PR) and median PFS per RECIST 1.1 over 24 months, with tumor assessments tracking progression (≥20% target lesion growth or new lesions). PK blood draws occur pre-dose and up to 504h post-infusion for comprehensive exposure analysis.
Experiment 4 Reporting the Activity Date of This ADC					[210]
Patients Enrolled	Eligible patients (18-81 years) must have PV diagnosed ≤5 years, meet WHO criteria, and be on hydroxyurea, with normal organ function (bilirubin/ALT/AST ≤2×ULN, creatinine ≤1.5×ULN). Exclusions: clopidogrel/aspirin intolerance, anticoagulant use, pregnancy, major bleeding history, NYHA ≥II CHF, MELD ≥8, or CYP3A4 inhibitors. Women of childbearing potential require contraception.    Click to Show/Hide
Related Clinical Trial
NCT Number	NCT00940784	Phase Status	PHASE2
Clinical Description	MPD-RC 108: Phase II, Randomized, Double-Blind, Placebo Controlled International Study of Clopidogrel and Aspirin for the Treatment of Polycythemia Vera
Primary Endpoint	This study evaluates the safety and efficacy of clopidogrel plus aspirin in polycythemia vera patients over 2 years, focusing on high-risk individuals with prior thrombotic events (stroke, MI, or VTE) and WHO-confirmed PV (Hb >18.5 g/dL [men]/16.5 g/dL [women], JAK2V617F mutation, and trilineage hyperplasia).

Experiment 1 Reporting the Activity Date of This ADC					[227]
Efficacy Data	Partial Response (PR)	7.84 45.83 25.00 6.67 %
Patients Enrolled	Incurable, locally advanced, or metastatic disease (non-squamous NSCLC or non-mucinous PROC) that had progressed on or following prior chemotherapy and for which no standard therapy existed, Eastern Cooperative Oncology Group (ECOG) performance status of 0 or 1.
Administration Dosage	The starting dose for LIFA was 0.20 mg/kg administered by intravenous infusion (IV) every 3 weeks (Q3W), in this 3+3 dose-escalation design, followed by cohort expansion at the recommended phase II dose (RP2D).
Related Clinical Trial
NCT Number	NCT01911598	Phase Status	Phase 1a
Clinical Description	A phase 1b open-label study of the safety and pharmacokinetics of MEHD7945A in combination with either cisplatin and 5-fu or paclitaxel and carboplatin in patients with recurrent/metastatic squamous cell carcinoma of the head and neck.
Primary Endpoint	The MTD was not reached on this study and the maximum administered dose (MAD) was 2.80 mg/kg. Upon evaluation of the safety data of the 6 patients treated at the MAD, the dose of 2.40 mg/kg was established as the RP2D.
Other Endpoint	At active doses 1.80 mg/kg, partial responses were observed in four of 51 (7.84%) patients with NSCLC and 11 of 24 (45.83%) patients. In the NSCLC cohorts, PRs were seen in 1 of 4 (25.00%) at 1.80 mg/kg and in 3 of 45 (6.67%) patients at 2.40 mg/kg, mDoR=161 days. In PROC, PRs were seen at 1.80 mg/kg in one of two (50.00%), at 2.40 mg/kg in seven of 18 (38.89%), and at 2.80 mg/kg in three of four (75.00%) patients; mDoR=342 days.    Click to Show/Hide
Experiment 2 Reporting the Activity Date of This ADC					[233]
Efficacy Data	Objective Response Rate (ORR)	34.00 36.00 %
Patients Enrolled	Platinum-resistant patients with histologically documented advanced epithelial ovarian, primary peritoneal, or fallopian tube cancer.
Administration Dosage	2.40 mg/kg, intravenously, every 3 weeks (Q3W).
Related Clinical Trial
NCT Number	NCT01991210	Phase Status	Phase 2
Clinical Description	A randomized, open-label, multicenter, phase 2 trial evaluating the safety and activity of DNIB0600A compared to pegylated liposomal doxorubicin administered intravenously to patients with platinum-resistant ovarian cancer.
Experiment 3 Reporting the Activity Date of This ADC					[234]
Efficacy Data	Objective Response Rate (ORR)	34.00 36.00 %
Patients Enrolled	Advanced epithelial ovarian, primary peritoneal, or fallopian tube cancer that had progressed or relapsed within 6months of the most recent treatment with a platinum-containing chemotherapy regimen and for whom PLD was considered an appropriate therapy.
Administration Dosage	2.40 mg/kg, intravenously, every 3 weeks (Q3W).
Related Clinical Trial
NCT Number	NCT01991210	Phase Status	Phase 2
Clinical Description	A randomized, open-label, multicenter, phase 2 trial evaluating the safety and activity of DNIB0600A compared to pegylated liposomal doxorubicin administered intravenously to patients with platinum-resistant ovarian cancer.
Primary Endpoint	The stratified PFS hazard ratio was 0.78 (95% CI,0.46-1.31; p=0.34) with a median PFS of 5.30 vs. 3.10 months (LIFA vs. PLD arm,respectively) in the ITT population, and 0.71 (95% CI,0.40-1.26; p=0.24) with a median PFS of 5.30 vs. 3.40 months (LIFA vs. PLD arm,respectively) in NaPi2bxhigh patients. The objective response rate (ORR) was 34.00% (95% CI,22.00-49.00%,LIFA) vs. 15.00% (95% CI, 7.00-28.00%,PLD) in the ITT population (p=0.03), and 36.00% (95% CI, 22.00-52.00%,LIFA) vs.14.00% (95% CI,6.00-27.00%,PLD) in NaPi2bxhigh patients (p=0.02).    Click to Show/Hide
Experiment 4 Reporting the Activity Date of This ADC					[236]
Efficacy Data	Objective Response Rate (ORR)	25.00 7.00 50.00 39.00 75.00 %
Patients Enrolled	Patients with nonsmall cell lung cancer (NSCLC) and platinum-resistant ovarian cancer (PROC).
Administration Dosage	Dose-escalation: 0.20-2.80 mg/kg once every 3 weeks, dose-expansion: 4 mg/kg once every 3 weeks.
Related Clinical Trial
NCT Number	NCT01363947	Phase Status	Phase 1
Clinical Description	A phase 1, open-label study of the safety and pharmacokinetics of escalating doses of DNIB0600A in patients with non-small cell lung cancer and platinum-resistant ovarian cancer.
Experiment 5 Reporting the Activity Date of This ADC					[238]
Efficacy Data	Complete Remission (CR)	58.54%
Patients Enrolled	Polycystic ovary syndrome (PSOC) patients (epithelial ovarian cancer, primary peritoneal cancer, or fallopian tube cancer) with documented radiographic progression or relapse according to RECIST v1.1.
Administration Dosage	The starting dose of LIFA was 1.20 mg/kg, once every 3 weeks (Q3W) on the first day of 21-day cycles, traditional 3 + 3 study design.
Related Clinical Trial
NCT Number	NCT01995188	Phase Status	Phase 1b
Clinical Description	A phase 1b, open-label, dose-escalation study of the safety and pharmacology of DNIB0600A in combination with carboplatin (with or without bevacizumab) in patients with platinum-sensitive ovarian cancer or non-squamous non-small cell lung cancer.
Primary Endpoint	The median duration of progression-free survival was 10.71 months (95% CI: 8.54,13.86) with confirmed complete/partial responses in 24 (58.54%) patients.
Other Endpoint	The maximum tolerated dose was not reached. The recommended phase 2 dose (RP2D) was LIFA 2.40 mg/kg + carboplatin AUC6 (cycles 16), with or without bevacizumab 15 mg/kg.
Experiment 6 Reporting the Activity Date of This ADC					[242]
Related Clinical Trial
NCT Number	NCT01995188	Phase Status	Phase 1
Clinical Description	A phase 1b, open-label, dose-escalation study of the safety and pharmacology of DNIB0600A in combination with carboplatin (with or without bevacizumab) in patients with platinum-sensitive ovarian cancer or non-squamous non-small cell lung cancer.
Experiment 7 Reporting the Activity Date of This ADC					[249]
Efficacy Data	Progression Free Survival	10.7 months
Patients Enrolled	Inclusion criteria: ECOG 0-1; histologically confirmed platinum-sensitive ovarian, peritoneal, or fallopian tube cancer or NSCLC with ≤2 prior regimens (additional targeted therapy permitted for EGFR/ALK mutations). NSCLC requires NaPi2b IHC 2+/3+. Exclusions: recent anti-tumor therapy/surgery, active infections, untreated CNS metastases, prior NaPi2b therapy, or specific contraindications for bevacizumab (e.g., uncontrolled hypertension, recent thrombosis).    Click to Show/Hide
Administration Dosage	Patients received LIFA at 1.2, 1.8, and 2.4 mg (n = 4, 5, and 20, respectively) with carboplatin.
Related Clinical Trial
NCT Number	NCT01995188	Phase Status	PHASE1
Clinical Description	A Phase Ib, Open-Label, Dose-Escalation Study of the Safety and Pharmacology of DNIB0600A in Combination With Carboplatin (With or Without Bevacizumab) in Patients With Platinum-Sensitive Ovarian Cancer or Non-Squamous Non-small Cell Lung Cancer
Primary Endpoint	The study evaluates dose-limiting toxicities (DLTs) in participants over 21 days, tracks adverse events (AEs) and serious adverse events (SAEs) from Day 1 until 30 days post-last infusion (up to ~3 years), and monitors anti-DNIB0600A antibodies at pre-infusion, specific cycles, and 30 days post-last infusion.
Other Endpoint	Pharmacokinetic parameters include AUC (0-inf), Cmax, Cmin, CL, Vss, and t1/2, measured at pre-infusion, post-infusion time points, and follow-up (up to ~3 years). Efficacy is assessed via RECIST v1.1, measuring objective response rate, duration of response, and progression-free survival (PFS) from screening until disease progression or death.
Experiment 8 Reporting the Activity Date of This ADC					[253]
Efficacy Data	Objective Response Rate (ORR)	34 15 36 14 %
Patients Enrolled	Eligible patients must have ECOG 0-1, histologically confirmed advanced ovarian, peritoneal, or fallopian tube cancer refractory to platinum therapy, ≤2 prior regimens, adequate organ function, and contraception compliance. Exclusions include prior anthracycline/NaPi2b therapy, major surgery within 4 weeks, uncontrolled comorbidities, active infections, hepatitis/HIV, CNS metastases, pregnancy, NaPi2b deficiency, or severe hypersensitivity to monoclonal antibodies.    Click to Show/Hide
Administration Dosage	DNIB0600A will be administered at a dose of 2.4 mg/kg IV every 3 weeks.
Related Clinical Trial
NCT Number	NCT01991210	Phase Status	PHASE2
Clinical Description	A Randomized, Open-Label, Multicenter, Phase II Trial Evaluating the Safety and Activity of DNIB0600A Compared to Pegylated Liposomal Doxorubicin Administered Intravenously to Patients With Platinum-Resistant Ovarian Cancer
Primary Endpoint	The primary endpoint is progression-free survival (PFS) based on RECIST v1.1, measured from baseline until disease progression or death within 30 days of last study drug administration, with an overall timeframe of approximately 2.5 years.
Other Endpoint	Secondary endpoints include objective response rate (ORR) and duration of response per RECIST v1.1, overall survival (OS), incidence of adverse events (AEs), and pharmacokinetic parameters such as AUC, Cmax, CL, t½, and Vss of DNIB0600A, along with anti-therapeutic antibody (ATA) formation. Assessments span from baseline up to 30 days post-treatment or longer, with detailed time points for PK analysis.    Click to Show/Hide
Experiment 9 Reporting the Activity Date of This ADC					[249]
Efficacy Data	Objective Response Rate (ORR)	59%
Patients Enrolled	Inclusion criteria: ECOG 0-1; histologically confirmed platinum-sensitive ovarian, peritoneal, or fallopian tube cancer or NSCLC with ≤2 prior regimens (additional targeted therapy permitted for EGFR/ALK mutations). NSCLC requires NaPi2b IHC 2+/3+. Exclusions: recent anti-tumor therapy/surgery, active infections, untreated CNS metastases, prior NaPi2b therapy, or specific contraindications for bevacizumab (e.g., uncontrolled hypertension, recent thrombosis).    Click to Show/Hide
Administration Dosage	Patients received LIFA at 1.2, 1.8, and 2.4 mg (n = 4, 5, and 20, respectively) with carboplatin.
Related Clinical Trial
NCT Number	NCT01995188	Phase Status	PHASE1
Clinical Description	A Phase Ib, Open-Label, Dose-Escalation Study of the Safety and Pharmacology of DNIB0600A in Combination With Carboplatin (With or Without Bevacizumab) in Patients With Platinum-Sensitive Ovarian Cancer or Non-Squamous Non-small Cell Lung Cancer
Primary Endpoint	The study evaluates dose-limiting toxicities (DLTs) in participants over 21 days, tracks adverse events (AEs) and serious adverse events (SAEs) from Day 1 until 30 days post-last infusion (up to ~3 years), and monitors anti-DNIB0600A antibodies at pre-infusion, specific cycles, and 30 days post-last infusion.
Other Endpoint	Pharmacokinetic parameters include AUC (0-inf), Cmax, Cmin, CL, Vss, and t1/2, measured at pre-infusion, post-infusion time points, and follow-up (up to ~3 years). Efficacy is assessed via RECIST v1.1, measuring objective response rate, duration of response, and progression-free survival (PFS) from screening until disease progression or death.
Experiment 10 Reporting the Activity Date of This ADC					[268]
Patients Enrolled	Outcomes included safety (AE incidence), pharmacokinetics (Cmax of DNIB0600A components), immunogenicity (ADA development), and efficacy (OR and DOR per RECIST v1.1). Key endpoints spanned up to 84 weeks, assessing tumor response dynamics-complete or partial shrinkage (≥30% reduction), stable disease, or progression (≥20% increase or new lesions)-while monitoring drug-related toxicities and immunologic reactions. Rigorous eligibility criteria balanced participant safety with disease relevance, excluding high-risk conditions or recent therapies to isolate investigational drug effects.    Click to Show/Hide
Administration Dosage	Several dose levels will be evaluated for DNIB0600A administered via IV infusion on Day 1 of each 21-day cycle until disease progression.
Related Clinical Trial
NCT Number	NCT01363947	Phase Status	PHASE1
Clinical Description	A Phase I, Open-Label Study of the Safety and Pharmacokinetics of Escalating Doses of DNIB0600A in Patients With Non-Small Cell Lung Cancer and Platinum-Resistant Ovarian Cancer
Primary Endpoint	The study assessed adverse events (AEs) over approximately 2 years, defined as any unfavorable or unintended sign, symptom, or disease temporally linked to investigational medicinal product (IMP) use, irrespective of causality. Peak concentrations (Cmax) of DNIB0600A components-acMMAE, total antibody, and unconjugated MMAE-were evaluated on Day 21, alongside the percentage of participants developing anti-drug antibodies (ADAs) over 84 weeks, measuring baseline prevalence and post-baseline incidence. Objective response (OR) per RECIST v1.1 criteria, including complete response (disappearance of target lesions) and partial response (≥30% decrease in lesion diameters), was tracked for 84 weeks, along with duration of response (DOR), stable disease, and progression criteria (≥20% increase in lesion diameters or new lesions).    Click to Show/Hide
Other Endpoint	Inclusion criteria required an ECOG performance status of 0 or 1, histologic evidence of incurable locally advanced/metastatic disease (e.g., non-squamous NSCLC or platinum-resistant ovarian cancer), measurable disease, access to archival tumor samples, and contraception use for fertile participants. Exclusion criteria encompassed recent anti-tumor therapy, major surgery within 4 weeks, active infections, significant liver disease, untreated CNS metastases, oxygen dependency, uncontrolled comorbidities, and prior treatments (≤2 regimens for NSCLC expansion cohort). Pregnancy or breastfeeding also disqualified participation.    Click to Show/Hide

Experiment 1 Reporting the Activity Date of This ADC					[243]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 19.60%	Moderate SLC34A2 expression (SLC34A2++)
Method Description	Animals were randomized into treatment groups (n = 10) when the tumor target volume reached 100-150 mm3. Test articles were administered intravenously via tail vein injection. Mice received a single dose of either saline vehicle; XMT-1535 at 3 mg/kg; XMT-1536 (DAR 12.4) at 3 mg/kg; IgG1-Dolaflexin (DAR 18.1) at 3 mg/kg,or lifastuzumab vedotin (DAR 4.1) at 3 mg/kg. Tumors were measured twice per week. XMT-1536 and lifastuzumab vedotin were administered at a single dose of 3 mg/kg qwk x 3.    Click to Show/Hide
In Vivo Model	Non-small cell lung cancer PDX model (PDX: CTG-0860)
Experiment 2 Reporting the Activity Date of This ADC					[243]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 25.40%	Moderate SLC34A2 expression (SLC34A2++)
Method Description	Animals were randomized into treatment groups (n = 10) when the tumor target volume reached 100-150 mm3. Test articles were administered intravenously via tail vein injection. Mice received a single dose of either saline vehicle; XMT-1535 at 3 mg/kg; XMT-1536 (DAR 12.4) at 3 mg/kg; IgG1-Dolaflexin (DAR 18.1) at 3 mg/kg,or lifastuzumab vedotin (DAR 4.1) at 3 mg/kg. Tumors were measured twice per week. XMT-1536 and lifastuzumab vedotin were administered at a single dose of 3 mg/kg qwk x 3.    Click to Show/Hide
In Vivo Model	Lung cancer PDX model (PDX: CTG-0178)
Experiment 3 Reporting the Activity Date of This ADC					[243]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 27.60%	Moderate SLC34A2 expression (SLC34A2++)
Method Description	Animals were randomized into treatment groups (n = 10) when the tumor target volume reached 100-150 mm3. Test articles were administered intravenously via tail vein injection. Mice received a single dose of either saline vehicle; XMT-1535 at 3 mg/kg; XMT-1536 (DAR 12.4) at 3 mg/kg; IgG1-Dolaflexin (DAR 18.1) at 3 mg/kg,or lifastuzumab vedotin (DAR 4.1) at 3 mg/kg. Tumors were measured twice per week. XMT-1536 and lifastuzumab vedotin were administered at a single dose of 3 mg/kg qwk x 3.    Click to Show/Hide
In Vivo Model	Lung cancer PDX model (PDX: CTG-0178)
Experiment 4 Reporting the Activity Date of This ADC					[243]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 59.30%	High SLC34A2 expression (SLC34A2+++)
Method Description	Animals were randomized into treatment groups (n = 10) when the tumor target volume reached 100-150 mm3. Test articles were administered intravenously via tail vein injection. Mice received a single dose of either saline vehicle; XMT-1535 at 3 mg/kg; XMT-1536 (DAR 12.4) at 3 mg/kg; IgG1-Dolaflexin (DAR 18.1) at 3 mg/kg,or lifastuzumab vedotin (DAR 4.1) at 3 mg/kg. Tumors were measured twice per week. XMT-1536 and lifastuzumab vedotin were administered at a single dose of 3 mg/kg qwk x 3.    Click to Show/Hide
In Vivo Model	Lung cancer PDX model (PDX: CTG-0852)
Experiment 5 Reporting the Activity Date of This ADC					[243]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 62.70%	High SLC34A2 expression (SLC34A2+++)
Method Description	Animals were randomized into treatment groups (n = 10) when the tumor target volume reached 100-150 mm3. Test articles were administered intravenously via tail vein injection. Mice received a single dose of either saline vehicle; XMT-1535 at 3 mg/kg; XMT-1536 (DAR 12.4) at 3 mg/kg; IgG1-Dolaflexin (DAR 18.1) at 3 mg/kg,or lifastuzumab vedotin (DAR 4.1) at 3 mg/kg. Tumors were measured twice per week. XMT-1536 and lifastuzumab vedotin were administered at a single dose of 3 mg/kg qwk x 3.    Click to Show/Hide
In Vivo Model	Lung cancer PDX model (PDX: CTG-0852)
Experiment 6 Reporting the Activity Date of This ADC					[243]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 62.80%	High SLC34A2 expression (SLC34A2+++)
Method Description	Animals were randomized into treatment groups (n = 10) when the tumor target volume reached 100-150 mm3. Test articles were administered intravenously via tail vein injection. Mice received a single dose of either saline vehicle; XMT-1535 at 3 mg/kg; XMT-1536 (DAR 12.4) at 3 mg/kg; IgG1-Dolaflexin (DAR 18.1) at 3 mg/kg,or lifastuzumab vedotin (DAR 4.1) at 3 mg/kg. Tumors were measured twice per week. XMT-1536 and lifastuzumab vedotin were administered at a single dose of 3 mg/kg qwk x 3.    Click to Show/Hide
In Vivo Model	Lung cancer PDX model (PDX: CTG-0852)

Experiment 1 Reporting the Activity Date of This ADC					[243]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 41.20%	High SLC34A2 expression (SLC34A2+++)
Method Description	Animals were randomized into treatment groups (n = 10) when the tumor target volume reached 100-150 mm3. Test articles were administered intravenously via tail vein injection. Mice received a single dose of either saline vehicle; XMT-1535 at 3 mg/kg; XMT-1536 (DAR 12.4) at 3 mg/kg; IgG1-Dolaflexin (DAR 18.1) at 3 mg/kg,or lifastuzumab vedotin (DAR 4.1) at 3 mg/kg. Tumors were measured twice per week. XMT-1536 and lifastuzumab vedotin were administered at a single dose of 3 mg/kg.    Click to Show/Hide
In Vivo Model	Ovarian adenocarcinoma CDX model
In Vitro Model	Ovarian serous adenocarcinoma	OVCAR-3 cells		CVCL_0465

Experiment 1 Reporting the Activity Date of This ADC					[228]
Efficacy Data	Partial Response (PR)	7.69%
Patients Enrolled	Stage IIIB or IV squamous (or mixed adenosquamous) lung cancer measurable by Response Evaluation Criteria in Solid Tumors (RECIST 1.1).
Administration Dosage	A dose of 1.90 mg/kg as a 90-minute intravenous infusion for the escalation phase, on the basis of previous clinical trial results using glembatumumab vedotin at 1.3 mg/kg one-dose level; every 3 weeks.
Related Clinical Trial
NCT Number	NCT02713828	Phase Status	Phase 1
Clinical Description	A phase 1/2 study of glembatumumab vedotin in patients with gpNMB-expressing, advanced or metastatic squamous cell carcinoma of the lung.
Primary Endpoint	To further characterize the safety of this drug, the protocol was modified and additional three patients were added to cohort 1 for a total of nine patients at 1.90 mg/kg dose. A second DLT was observed in cohort 1. The patient experienced grade 3 treatment-related pruritus requiring hospital admission. The dose was de-escalated to dose level 1. No DLT was observed at dose level 1 of 1.30 mg/kg.    Click to Show/Hide
Other Endpoint	The best objective response per RECIST 1.1 was of one patient who achieved a partial response (1 of 13 [7.69%], 90% CI: 0.40%-31.60%).The median OS in this heavily pretreated population was 5.70 months (90% CI: 2.50-16.80). All patients had disease progression or died. The median PFS was 2.50 months (90% CI: 1.60-5.30).
Experiment 2 Reporting the Activity Date of This ADC					[232]
Efficacy Data	Objective Response Rate (ORR)	11.00 21.00 7.00 %
Patients Enrolled	Stage III or IV, histologically confirmed melanoma. Patients must had previously received no more than one prior chemotherapy-containing treatment regimen for advanced disease, at least one checkpoint inhibitor (ie, antiCTLA-4, PD-1, PD-L1targeted immunotherapy), and at least one BRAF-targeted and/or MEK-targeted therapy if melanoma harbored a BRAFV600 mutation, unless it was not clinically indicated or was refused by the patient.    Click to Show/Hide
Administration Dosage	As a 90-minute intravenous infusion every 3 weeks at a starting dose of 1.90 mg/kg. Dose reductions to 1.30 and 1.00 mg/kg were allowed for toxicity.
Related Clinical Trial
NCT Number	NCT02302339	Phase Status	Phase 2
Clinical Description	A phase 2 study of glembatumumab vedotin, an anti-gpNMB antibody-drug conjugate, as monotherapy or in combination with immunotherapies in patients with advanced melanoma.
Primary Endpoint	The ORR was 11.00% and the median response duration was 6.00 months (95% confidence interval [CI],4.10 months to not reached). The median PFS was 4.40 months (95% CI,2.60-5.50 months),and the median OS was 9.00 months (95% CI,6.10-11.70 months).
Other Endpoint	For patients who developed rash during the first cycle versus those who did not,the ORR was 21.00% versus 7.00%, respectively, and there was an overall improvement in PFS (hazard ratio,0.43; P = 0.013) and OS (hazard ratio,0.43; P = 0.017).
Experiment 3 Reporting the Activity Date of This ADC					[237]
Efficacy Data	Objective Response Rate (ORR)	12.00 18.00 %
Patients Enrolled	Locally advanced or metastatic carcinoma of the breast, progressive within 6 months of last therapy; received at least two prior chemotherapeutic regimens for breast cancer, with at least one given in the locally advanced or metastatic setting.
Administration Dosage	Glembatumumab vedotin was administered as a 90 minute intravenous infusion, once every 3 weeks (day 1 of repeated 21 day cycles). Delays of up to 3 weeks and up to two dose reductions (to dose levels of 1.34, 1.00, and 0.75 mg/kg, as applicable) were permitted for toxicity. Dosing continued until unmanageable treatment-related toxicities, disease progression, or death.    Click to Show/Hide
Experiment 4 Reporting the Activity Date of This ADC					[239]
Related Clinical Trial
NCT Number	NCT01156753	Phase Status	Phase 2
Clinical Description	A phase 2, randomized, multicenter study of CDX-011 (CR011-vcMMAE) in patients with advanced GPNMB-expressing breast cancer.
Experiment 5 Reporting the Activity Date of This ADC					[247]
Efficacy Data	Progression Free Survival	3.1 months
Patients Enrolled	Patients must have histologically or cytologically confirmed metastatic or locally recurrent uveal melanoma; because histologic or cytologic confirmation of primary uveal melanoma is not always possible, confirmation of the clinical diagnosis of uveal melanoma by the treating investigator is allowed; clinical diagnosis of uveal melanoma is often made by an ophthalmologist, not by tissue diagnosis; if an ophthalmologist diagnosed and treated a patient for uveal melanoma in the past, it is sufficient for a clinical diagnosis    Click to Show/Hide
Administration Dosage	Patients receive glembatumumab vedotin IV over 90 minutes every 3 weeks in the absence of disease progression or unacceptable toxicity.
Related Clinical Trial
NCT Number	NCT02363283	Phase Status	PHASE2
Clinical Description	A Phase 2 Study of CDX-011 (Glembatumumab Vedotin) for Metastatic Uveal Melanoma
Primary Endpoint	Overall Response Rate Using Response Evaluation Criteria in Solid Tumors Version 1.1.
Other Endpoint	The Number of Participants With Change in Glycoprotein NMB Expression on Tumor Tissue Via Immunohistochemistry, Progression-free Survival, Number of Participants With Grade 3-4 Adverse Events According to the National Cancer Institute Common Toxicity Criteria Version 4.0, Overall Survival.
Experiment 6 Reporting the Activity Date of This ADC					[248]
Efficacy Data	Progression Free Survival	9.1 weeks
Patients Enrolled	Females with confirmed breast cancer, Age ≥ 18 years, Eastern Cooperative Oncology Group (ECOG) Performance Status 0 to 2.
Administration Dosage	administered as an intravenous infusion on Day 1 of a 21 day cycle.
Related Clinical Trial
NCT Number	NCT00704158	Phase Status	PHASE1|||PHASE2
Clinical Description	A Phase I/II Study of CR011-vcMMAE in Patients With Locally Advanced or Metastatic Breast Cancer
Primary Endpoint	To evaluate the safety and tolerability of CR011-vcMMAE in breast cancer patients [Time Frame: throughout the study];To determine the MTD of CR011-vcMMAE in breast cancer patients [Time Frame: throughout the study].
Other Endpoint	Evaluation of efficacy (progression-free survival rate at 12 weeks, objective response rate, time to response, duration of response and time to progression) [Time Frame: throughout the study].
Experiment 7 Reporting the Activity Date of This ADC					[250]
Efficacy Data	Partial Response (PR)	7.69%
Patients Enrolled	Male or female patients with metastatic, histologically- or cytologically-confirmed unresectable Stage IIIB or IV non-small cell lung cancer (NSCLC) of squamous histology (Staging per American Joint Committee on Cancer [AJCC], Edition 7). Mixed histology adenosquamous NSCLC will also be permitted.
Administration Dosage	Glembatumumab vedotin once every three weeks (q3w) by 90-minute intravenous (IV) infusion, until disease progression or intolerance. The Dose-Limiting Toxicity (DLT) evaluation period for determination of the appropriateness of dose-escalation will be through the end of the second treatment cycle.
Related Clinical Trial
NCT Number	NCT02713828	Phase Status	PHASE1|||PHASE2
Clinical Description	A Phase I/II Study of Glembatumumab Vedotin in Patients With gpNMB-Expressing, Advanced or Metastatic Squamous Cell Carcinoma of the Lung
Primary Endpoint	Phase I: Determine Maximum Tolerated Dose (MTD) [Time Frame: 42 (±3) days];Phase II: Objective Response Rate (ORR) [Time Frame: 40 months].
Other Endpoint	Number of Participants With Treatment-related Adverse Events as Assessed by CTCAE v4.0., Duration of Objective Response (DOR) [Time Frame: 23 months], Progression-Free Survival (PFS) [Time Frame: 23 months], Overall Survival (OS) [Time Frame: 23 months].
Experiment 8 Reporting the Activity Date of This ADC					[247]
Efficacy Data	Overall suvival (OS)	11.9 months
Patients Enrolled	Patients must have histologically or cytologically confirmed metastatic or locally recurrent uveal melanoma; because histologic or cytologic confirmation of primary uveal melanoma is not always possible, confirmation of the clinical diagnosis of uveal melanoma by the treating investigator is allowed; clinical diagnosis of uveal melanoma is often made by an ophthalmologist, not by tissue diagnosis; if an ophthalmologist diagnosed and treated a patient for uveal melanoma in the past, it is sufficient for a clinical diagnosis    Click to Show/Hide
Administration Dosage	Patients receive glembatumumab vedotin IV over 90 minutes every 3 weeks in the absence of disease progression or unacceptable toxicity.
Related Clinical Trial
NCT Number	NCT02363283	Phase Status	PHASE2
Clinical Description	A Phase 2 Study of CDX-011 (Glembatumumab Vedotin) for Metastatic Uveal Melanoma
Primary Endpoint	Overall Response Rate Using Response Evaluation Criteria in Solid Tumors Version 1.1.
Other Endpoint	The Number of Participants With Change in Glycoprotein NMB Expression on Tumor Tissue Via Immunohistochemistry, Progression-free Survival, Number of Participants With Grade 3-4 Adverse Events According to the National Cancer Institute Common Toxicity Criteria Version 4.0, Overall Survival.
Experiment 9 Reporting the Activity Date of This ADC					[251]
Efficacy Data	Objective Response Rate (ORR)	6%
Patients Enrolled	18 years of age or older.Locally advanced or metastatic breast cancer.Previous treatment with at least two but no more than seven prior chemotherapy treatments for progressive, recurrent or metastatic breast cancer.Unless not a candidate for these agents, prior therapies must have included a taxane, an anthracycline, and capecitabine, as well as trastuzumab and lapatinib for patients whose tumors are positive for the human epidermal growth factor receptor 2 (HER2). (Patients who received incomplete courses of therapy with these agents due to intolerance will be eligible.)Breast cancer tumor confirmed to express GPNMB. This will be determined by submitting a tissue sample (obtained during a diagnostic biopsy or surgery) to a central laboratory for analysis.    Click to Show/Hide
Administration Dosage	CDX-011 (1.88 mg/kg) administered as an intravenous infusion on Day 1 of each 21 day cycle.
Related Clinical Trial
NCT Number	NCT01156753	Phase Status	PHASE2
Clinical Description	The main purpose of this study is to see whether CDX-011 is effective in treating patients who have advanced breast cancer that makes a protein called glycoprotein NMB (GPNMB), and who have already received (or were not candidates for) all available approved therapies for their breast cancer. This study will also further characterize the safety of CDX-011 treatment in this patient population.    Click to Show/Hide
Primary Endpoint	Glembatumumab vedotin was well tolerated as compared with IC chemotherapy (less hematologic toxicity; more rash, pruritus, neuropathy, and alopecia). ORR was 6% (five of 83) for glembatumumab vedotin versus 7% (three of 41) for IC, without significant intertreatment differences for predefined strata. Secondary end point revealed ORR of 12% (10 of 83) versus 12% (five of 41) overall, and 30% (seven of 23) versus 9% (one of 11) for gpNMB overexpression (≥ 25% of tumor cells). Unplanned analysis showed ORR of 18% (five of 28) versus 0% (0 of 11) in patients with triple-negative breast cancer (TNBC), and 40% (four of 10) versus 0% (zero of six) in gpNMB-overexpressing TNBC.    Click to Show/Hide
Other Endpoint	In the breast cancer study, this dose resulted in an ORR of 12% (four of 33) and median progression-free survival (PFS) of 2.1 months. In the subset of patients with triple-negative breast cancer (TNBC), defined by the lack of overexpression of estrogen, progesterone, and human epidermal growth factor receptor 2 (HER2), ORR was 20% (two of 10), and median PFS was 4.1 months. For the small subset of patients with TNBC who also had gpNMB-expressing tumors (≥ 5% of epithelial or stromal cells were positive), ORR was 25% (one of four), and median PFS was 5.1 months..    Click to Show/Hide
Experiment 10 Reporting the Activity Date of This ADC					[252]
Efficacy Data	Objective Response Rate (ORR)	11.00 21.00 7.00 %
Patients Enrolled	Unresectable, histologically-confirmed advanced (Stage III or Stage IV) melanoma.Disease progression during or after the last anticancer therapy received. For Cohort 3, progression must have occurred during the PD-1 targeted CPI (checkpoint inhibitor) treatment and the investigator has deemed it appropriate to continue treatment with the PD-1 targeted CPI beyond confirmed disease progression. No more than one prior chemotherapy-containing regimen for advanced disease. Prior treatments received must include at least one CPI inhibitor (e.g., anti-CTLA-4, PD-1-, PD-L1-targeted immunotherapy) and for patients with a BRAF mutation at least one BRAF- or MEK-targeted therapy, unless patients are not candidates for, or refused, these therapies. For cohort 3, prior treatment received must include a PD-1 targeted CPI administered during the most recent disease progression and for patients with BRAF mutation at least one BRAF- or MEK-targeted therapy when appropriate. The study site will submit paraffin-embedded tumor tissue obtained from the patient for gpNMB analysis. Patients may require a biopsy if recent tumor tissue is not available. Patients in cohort 2 and 3 must submit a recently obtained biopsy of the skin fold for gpNMB analysis. Patients in Cohort 4 will submit a tumor tissue sample while on study. Eastern Cooperative Oncology Group (ECOG) Performance Status 0 to 1. Adequate bone marrow, liver and renal function.    Click to Show/Hide
Administration Dosage	glembatumumab vedotin administered as an intravenous infusion on Day 1 of each 21 day cycle.
Related Clinical Trial
NCT Number	NCT02302339	Phase Status	PHASE2
Clinical Description	A Phase 2 Study of Glembatumumab Vedotin, an Anti-gpNMB Antibody-drug Conjugate, as Monotherapy or in Combination With Immunotherapies in Patients With Advanced Melanoma
Primary Endpoint	The ORR was 11.00% and the median response duration was 6.00 months (95% confidence interval [CI],4.10 months to not reached). The median PFS was 4.40 months (95% CI,2.60-5.50 months),and the median OS was 9.00 months (95% CI,6.10-11.70 months).
Other Endpoint	For patients who developed rash during the first cycle versus those who did not,the ORR was 21.00% versus 7.00%, respectively, and there was an overall improvement in PFS (hazard ratio,0.43; P = 0.013) and OS (hazard ratio,0.43; P = 0.017).
Experiment 11 Reporting the Activity Date of This ADC					[248]
Efficacy Data	Objective Response Rate (ORR)	12%
Patients Enrolled	Females with confirmed breast cancer, Age ≥ 18 years, Eastern Cooperative Oncology Group (ECOG) Performance Status 0 to 2.
Administration Dosage	administered as an intravenous infusion on Day 1 of a 21 day cycle.
Related Clinical Trial
NCT Number	NCT00704158	Phase Status	PHASE1|||PHASE2
Clinical Description	A Phase I/II Study of CR011-vcMMAE in Patients With Locally Advanced or Metastatic Breast Cancer
Primary Endpoint	To evaluate the safety and tolerability of CR011-vcMMAE in breast cancer patients [Time Frame: throughout the study];To determine the MTD of CR011-vcMMAE in breast cancer patients [Time Frame: throughout the study].
Other Endpoint	Evaluation of efficacy (progression-free survival rate at 12 weeks, objective response rate, time to response, duration of response and time to progression) [Time Frame: throughout the study].
Experiment 12 Reporting the Activity Date of This ADC					[247]
Efficacy Data	Objective Response Rate (ORR)	51.40%
Patients Enrolled	Patients must have histologically or cytologically confirmed metastatic or locally recurrent uveal melanoma; because histologic or cytologic confirmation of primary uveal melanoma is not always possible, confirmation of the clinical diagnosis of uveal melanoma by the treating investigator is allowed; clinical diagnosis of uveal melanoma is often made by an ophthalmologist, not by tissue diagnosis; if an ophthalmologist diagnosed and treated a patient for uveal melanoma in the past, it is sufficient for a clinical diagnosis    Click to Show/Hide
Administration Dosage	Patients receive glembatumumab vedotin IV over 90 minutes every 3 weeks in the absence of disease progression or unacceptable toxicity.
Related Clinical Trial
NCT Number	NCT02363283	Phase Status	PHASE2
Clinical Description	A Phase 2 Study of CDX-011 (Glembatumumab Vedotin) for Metastatic Uveal Melanoma
Primary Endpoint	Overall Response Rate Using Response Evaluation Criteria in Solid Tumors Version 1.1.
Other Endpoint	The Number of Participants With Change in Glycoprotein NMB Expression on Tumor Tissue Via Immunohistochemistry, Progression-free Survival, Number of Participants With Grade 3-4 Adverse Events According to the National Cancer Institute Common Toxicity Criteria Version 4.0, Overall Survival.
Experiment 13 Reporting the Activity Date of This ADC					[254]
Patients Enrolled	The patient has histologically confirmed, gpNMB expressing, metastatic triple-negative breast cancer.
Related Clinical Trial
NCT Number	NCT03067935	Phase Status	N.A.
Clinical Description	N.A.
Experiment 14 Reporting the Activity Date of This ADC					[255]
Patients Enrolled	Patients diagnosed with triple negative breast cancer, (stages II-III, or high risk T1c disease) found to have gpNMB expression at or above 25%), and who are appropriate candidates for neo-adjuvant therapy. Patients must be willing to undergo lumpectomy (with radiation therapy) or mastectomy following neo-adjuvant therapy.
Administration Dosage	Standard neo-adjuvant dose-dense doxorubicin 60 mg/m2 and Cytoxan 600 mg/m2 IV every 14 days for 4 cycles followed by GV 1.9 mg/kg IV every 21 days for 4 cycles.
Related Clinical Trial
NCT Number	NCT03473691	Phase Status	EARLY_PHASE1
Clinical Description	Pilot Study of the Antibody-drug Conjugate Glembatumumab Vedotin (CDX-011) Following Doxorubicin (Adriamycin) and Cytoxan as Neo-adjuvant Therapy in Glycoprotein NMB-expressing High Risk Triple Negative Breast Cancer
Primary Endpoint	Incidence of Adverse Events (AEs), Proportion of patients who complete the 4 cycles of GV within 15 weeks of the first dose of GV (without dose limiting adverse events)., Number of discontinuations due to AEs.
Other Endpoint	Efficacy, Growth Differentiation Factor-11 (GDF11) expression in the tumor, Glycoprotein-NMB (gpNMB) expression in the tumor.
Experiment 15 Reporting the Activity Date of This ADC					[256]
Patients Enrolled	Diagnosed with metastatic (i.e., cancer that has spread) TNBC, Documented progression of disease based on radiographic, clinical or pathologic, Breast cancer tumor confirmed to express gpNMB.
Administration Dosage	CDX-011 administered as an intravenous infusion on Day 1 of each 21 day cycle.
Related Clinical Trial
NCT Number	NCT01997333	Phase Status	PHASE2
Clinical Description	A Randomized Multicenter Pivotal Study of CDX-011 (CR011-vcMMAE)in Patients With Metastatic, gpNMB Over-Expressing, Triple Negative Breast Cancer (The METRIC Study)
Primary Endpoint	Progression Free Survival (PFS)
Other Endpoint	Objective Response Rate (ORR), Duration of Response, verall Survival, Adverse Events (AE), Pharmacokinetics (PK).
Experiment 16 Reporting the Activity Date of This ADC					[257]
Patients Enrolled	Patients must have histologically confirmed malignancy that is metastatic or unresectable and for which standard curative measures do not exist or are no longer effective. For TNBC and solid tumors other than melanoma: GPNMB expression as defined by at least 25% of malignant epithelial cells or tumor stromal cells expression GPNMB at any intensity via central immunohistochemistry on archived or biopsied tumor tissue (as per standard clinical care) from an advanced/metastatic disease site; for melanoma or uveal melanoma cohort: GPNMB testing results will not be required for eligibility assessment.    Click to Show/Hide
Administration Dosage	Patients receive glembatumumab vedotin IV over 90 minutes and nivolumab IV over 60 minutes on day 8 of course 1 and on day 1 of subsequent courses. Patients in melanoma expanded cohort also receive ipilimumab IV over 90 minutes on day 1. Treatment with ipilimumab repeats every 21 days for 4 courses in the absence of disease progression or unaccepted toxicity and courses with glembatumumab vedotin and nivolumab repeat every 21 days in the absence of disease progression or unaccepted toxicity.    Click to Show/Hide
Related Clinical Trial
NCT Number	NCT03326258	Phase Status	PHASE1|||PHASE2
Clinical Description	Phase Ib/II Clinical Trial of Glembatumumab Vedotin and Nivolumab in Advanced Solid Tumors
Primary Endpoint	Recommended phase 2 dose for the combination of glembatumumab vedotin and nivolumab (Phase Ib), Antitumor activity measured by Immune-Modified Response Evaluation Criteria in Solid Tumors (iRECIST)/Response Evaluation Criteria in Solid Tumors (RECIST) 1.1 (Phase II)
Other Endpoint	Incidence of adverse events, Overall response rate, Clinical benefit rate, Progression free survival, Pharmacokinetic parameters, Levels of plasma and tissue biomarkers.
Experiment 17 Reporting the Activity Date of This ADC					[258]
Patients Enrolled	Patients must have had histologic verification of osteosarcoma at original diagnosis or relapse, Patients must have measurable disease according to RECIST 1.1, and have relapsed or become refractory to conventional therapy, Patient must have archival tumor specimen available for submission, Patients must have a performance status corresponding to Eastern Cooperative Oncology Group (ECOG) scores of 0, 1 or 2; use Karnofsky for patients > 16 years of age and Lansky for patients =< 16 years of age.    Click to Show/Hide
Administration Dosage	Patients receive glembatumumab vedotin IV over 90 minutes on day 1. Treatment repeats every 21 days for up to 18 courses in the absence of disease progression or unacceptable toxicity.
Related Clinical Trial
NCT Number	NCT02487979	Phase Status	PHASE2
Clinical Description	A Phase 2 Study of GPNMB-Targeted Antibody-Drug Conjugate, CDX-011 (Glembatumumab Vedotin, CR011-vcMMAE; NSC# 763737), in Recurrent or Refractory Osteosarcoma
Primary Endpoint	Disease Control Success.
Other Endpoint	Twenty-two patients were enrolled, and all were evaluable for response. Antibody-drug conjugate levels were detectable in patients, although small numbers limit comparison to adult data. The toxicities observed were similar to the previous studies with GV. The most common grade III adverse event was rash. One death from end organ failure occurred possibly related to GV. Of the 22 patients, one patient had a partial response, and two had stable disease. There was no correlation between gpNMB expression and response to GV.    Click to Show/Hide
Experiment 18 Reporting the Activity Date of This ADC					[259]
Related Clinical Trial
NCT Number	NCT06813417	Phase Status	NA
Clinical Description	An Open Label Individual Patient Dose Escalation Study Investigating the Safety and Efficacy of Retreatment with GCAR1 in a Patient with Multiply Relapsed Alveolar Soft Part Sarcoma

Experiment 1 Reporting the Activity Date of This ADC					[245]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 93.33%	High GPNMB expression (GPNMB+++)
Method Description	Tumor xenografts were generated by injecting UOK124 cells subcutaneously into flanks of athymic nude mice. Mice were randomized into treatment groups (n = 10 mice/group) based on tumor volume and treated with the following agents, singly or in combination CDX-011.
In Vivo Model	UOK124 CDX model
In Vitro Model	Papillary renal cell carcinoma	UOK124 cells		CVCL_B105

Experiment 1 Reporting the Activity Date of This ADC					[229]
Efficacy Data	Objective Response Rate (ORR)	2.56%	High GCC expression (GCC+++)
Patients Enrolled	Advanced or metastatic adenocarcinoma of the pancreas expressing GCC (H-score 10, as indicated by immunohistochemistry [IHC]), and previously treated with one or more prior chemotherapies.
Administration Dosage	1.80 mg/kg on day 1 of 3-week cycles as single 30-min intravenous (IV) infusions for up to 1 year or until disease progression (PD) or unacceptable toxicity.
Related Clinical Trial
NCT Number	NCT02202785	Phase Status	Phase 2
Clinical Description	A phase 2 trial of mLN0264 in previously treated patients with advanced or metastatic pancreatic adenocarcinoma expressing guanylyl cyclase C (GCC).
Primary Endpoint	OrR (CR+PR)=2.56% (N=1/39), one patient achieving PR, DOR=103 days. Nine (23.07%) patients achieved SD, among those nine patients, two patients (18%, low-GCC),four patients (31%, intermediate-GCC), and three patients (20%, high-GCC).
Other Endpoint	Median OS=162 days (range 36-282) and PFS=9-82 days in the low-cohort,median OS=140 days (range 43-443) and PFS=1-218 days in the intermediate-cohort,median OS=162 days (range 49-435) and PFS=16-137 days in the high-cohort,.
Experiment 2 Reporting the Activity Date of This ADC					[230]
Efficacy Data	Objective Response Rate (ORR)	2.63%	High GCC expression (GCC+++)
Patients Enrolled	GI carcinoma expressing GCC (H-score 10, as indicated by immunohistochemistry [IHC]), included gastric carcinoma, esophageal carcinoma, colorectal carcinoma, small intestine carcinoma, pancreatic carcinoma, and biliary carcinoma.
Administration Dosage	1.80 mg/kg on day 1 of 3-week cycles as single 30-min intravenous (IV) infusions for up to 1 year or until disease progression (PD) or unacceptable toxicity.
Related Clinical Trial
NCT Number	NCT02202785	Phase Status	Phase 2
Clinical Description	A phase 2 trial of mLN0264 in previously treated patients with advanced or metastatic pancreatic adenocarcinoma expressing guanylyl cyclase C (GCC).
Primary Endpoint	OrR (CR+PR)=2.63% (N=1/38), one patient identified as PR, nine patients (23.68%) had stable disease.
Experiment 3 Reporting the Activity Date of This ADC					[231]
Efficacy Data	Objective Response Rate (ORR)	5.56%	High GCC expression (GCC+++)
Patients Enrolled	Metastatic or recurrent adenocarcinoma of the stomach or gastroesophageal junction expressing GCC (H-score 10, as indicated by immunohistochemistry [IHC]) who progressed on at least one line of treatment.
Administration Dosage	TAK-264 1.80 mg/kg was administered as a 30 minute intravenous (IV) infusion on day 1 of a 21-day cycle for up to 1 year or until disease progression or unacceptable toxicity.
Related Clinical Trial
NCT Number	NCT02202759	Phase Status	Phase 2
Clinical Description	A phase 2 trial of mLN0264 in previously treated patients with metastatic or recurrent adenocarcinoma of the stomach or gastroesophageal junction expressing guanylyl cyclase C (GCC).
Primary Endpoint	OrR (CR+PR)=5.56% (N=2/36),2 patients achieved a PR with intermediate GCC expression.
Other Endpoint	The disease control rate (CR+PR+SD with a minimum duration of 12 weeks)=36.00%, 7 patients with high GCC expression, 4 patients with intermediate GCC expression, 4 patients with low GCC expression.
Experiment 4 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Objective Response Rate (ORR)	0%	High GCC expression (GCC+++)
Patients Enrolled	GI carcinoma expressing GCC (H-score 10, as indicated by immunohistochemistry [IHC]), included gastric carcinoma, esophageal carcinoma, colorectal carcinoma, small intestine carcinoma, pancreatic carcinoma, and biliary carcinoma.
Administration Dosage	A conventional 3+3 dose-escalation scheme, TAK-264 doses (planned dose levels, 1.20, 1.50, 1.80, 2.10, 2.40, and 2.70 mg/kg) on day 1 of 3-week cycles as 30-minute intravenous infusions for up to 1 year or until disease progression or unacceptable toxicity.
Related Clinical Trial
NCT Number	NCT02391038	Phase Status	Phase 1
Clinical Description	A phase 1/2 trial of mLN0264 in previously treated asian patients with advanced gastrointestinal (GI) carcinoma (phase 1) or metastatic or recurrent gastric or gastroesophageal junction adenocarcinoma (phase 2) expressing guanylyl cyclase C (GCC).
Primary Endpoint	None of the patients experienced a DLT and the MTD was not determined.
Other Endpoint	There were no objective responses; three patients had stable disease.
Experiment 5 Reporting the Activity Date of This ADC					[240]
Related Clinical Trial
NCT Number	NCT02391038	Phase Status	Phase 1
Clinical Description	A phase 1/2 trial of mLN0264 in previously treated asian patients with advanced gastrointestinal (GI) carcinoma (phase 1) or Metastatic or recurrent gastric or gastroesophageal junction adenocarcinoma (phase 2) expressing guanylyl cyclase C (GCC).
Experiment 6 Reporting the Activity Date of This ADC					[241]
Patients Enrolled	GCC-expressing gastrointestinal malignancy (H-score 10, derivation described below), for whom standard treatment was no longer effective or did not offer curative or life-prolonging potential, metastatic colorectal cancer, gastric carcinoma, esophageal carcinoma, small intestine cancer, pancreatic cancer, and unknown primary malignancies.
Administration Dosage	Once every 3 weeks as a 30-minute intravenous infusion (day 1 of 21-day cycles) for up to 17 cycles or until disease progression or occurrence of unacceptable TAK-264related toxicity.
Related Clinical Trial
NCT Number	NCT01577758	Phase Status	Phase 1
Clinical Description	An open-label, dose escalation, phase 1, first-in-human study of mLN0264 in Adult patients with advanced gastrointestinal malignancies expressing guanylyl cyclase C.
Primary Endpoint	21 patients (53.85%, N=39) experienced progressive disease, 3 patients (7.69%, N=39) experienced stable disease. Median PFS=44 days (95% CI,39-83). No association between GCC expression and PFS.
Other Endpoint	MTD=1.80 mg/kg.
Experiment 7 Reporting the Activity Date of This ADC					[246]
Efficacy Data	stable disease (SD)	24%
Patients Enrolled	Eligibility requires GI malignancy with GCC expression, measurable RECIST disease, ECOG 0-1, and adequate organ function (specified per protocol). Exclusions: pregnancy/lactation, major surgery/study drug <4 weeks, uncontrolled infections, HIV/hepatitis, brain metastases, or other primary malignancies (<3 years remission). Additional criteria apply, with final determination by the study site.    Click to Show/Hide
Administration Dosage	TAK-264 1.8 mg/kg was administered as a single 30 minute intravenous infusion on day 1 of a 21-day cycle for up to 1 year or until disease progression or unacceptable toxicity.
Related Clinical Trial
NCT Number	NCT01577758	Phase Status	PHASE1
Clinical Description	An Open-Label, Dose Escalation, Phase 1, First-in-Human Study of MLN0264 in Adult Patients With Advanced Gastrointestinal Malignancies Expressing Guanylyl Cyclase C
Primary Endpoint	The primary safety assessment includes DLTs (Grade 4 neutropenia/thrombocytopenia, Grade 3+ toxicities despite management, treatment delays >2 weeks, or other severe AEs prompting discontinuation) over ~9 months. TEAEs/SAEs (death, hospitalization, disability, medically significant events) are monitored post-consent until 30 days post-treatment. The MTD of MLN0264 (1.8 mg/kg) was determined via dose-escalation, with PK analysis (Cmax and AUC0-21d for MLN0264/MMAE) at Cycle 1.    Click to Show/Hide
Other Endpoint	Best Overall Response per RECIST (CR: disappearance of all lesions; PR: ≥30% target lesion reduction; PD: ≥20% increase/new lesions; SD: neither PR nor PD) is evaluated every 2 cycles (~9 months). Antitherapeutic antibodies (ATA) are assessed per cycle to determine immunogenicity, with blood samples analyzed for MLN0264 binding antibodies.
Experiment 8 Reporting the Activity Date of This ADC					[246]
Efficacy Data	progressive disease (PD)	74%
Patients Enrolled	Eligibility requires GI malignancy with GCC expression, measurable RECIST disease, ECOG 0-1, and adequate organ function (specified per protocol). Exclusions: pregnancy/lactation, major surgery/study drug <4 weeks, uncontrolled infections, HIV/hepatitis, brain metastases, or other primary malignancies (<3 years remission). Additional criteria apply, with final determination by the study site.    Click to Show/Hide
Administration Dosage	TAK-264 1.8 mg/kg was administered as a single 30 minute intravenous infusion on day 1 of a 21-day cycle for up to 1 year or until disease progression or unacceptable toxicity.
Related Clinical Trial
NCT Number	NCT01577758	Phase Status	PHASE1
Clinical Description	An Open-Label, Dose Escalation, Phase 1, First-in-Human Study of MLN0264 in Adult Patients With Advanced Gastrointestinal Malignancies Expressing Guanylyl Cyclase C
Primary Endpoint	The primary safety assessment includes DLTs (Grade 4 neutropenia/thrombocytopenia, Grade 3+ toxicities despite management, treatment delays >2 weeks, or other severe AEs prompting discontinuation) over ~9 months. TEAEs/SAEs (death, hospitalization, disability, medically significant events) are monitored post-consent until 30 days post-treatment. The MTD of MLN0264 (1.8 mg/kg) was determined via dose-escalation, with PK analysis (Cmax and AUC0-21d for MLN0264/MMAE) at Cycle 1.    Click to Show/Hide
Other Endpoint	Best Overall Response per RECIST (CR: disappearance of all lesions; PR: ≥30% target lesion reduction; PD: ≥20% increase/new lesions; SD: neither PR nor PD) is evaluated every 2 cycles (~9 months). Antitherapeutic antibodies (ATA) are assessed per cycle to determine immunogenicity, with blood samples analyzed for MLN0264 binding antibodies.
Experiment 9 Reporting the Activity Date of This ADC					[246]
Efficacy Data	Objective Response Rate (ORR)	3%
Patients Enrolled	Eligibility requires GI malignancy with GCC expression, measurable RECIST disease, ECOG 0-1, and adequate organ function (specified per protocol). Exclusions: pregnancy/lactation, major surgery/study drug <4 weeks, uncontrolled infections, HIV/hepatitis, brain metastases, or other primary malignancies (<3 years remission). Additional criteria apply, with final determination by the study site.    Click to Show/Hide
Administration Dosage	TAK-264 1.8 mg/kg was administered as a single 30 minute intravenous infusion on day 1 of a 21-day cycle for up to 1 year or until disease progression or unacceptable toxicity.
Related Clinical Trial
NCT Number	NCT01577758	Phase Status	PHASE1
Clinical Description	An Open-Label, Dose Escalation, Phase 1, First-in-Human Study of MLN0264 in Adult Patients With Advanced Gastrointestinal Malignancies Expressing Guanylyl Cyclase C
Primary Endpoint	The primary safety assessment includes DLTs (Grade 4 neutropenia/thrombocytopenia, Grade 3+ toxicities despite management, treatment delays >2 weeks, or other severe AEs prompting discontinuation) over ~9 months. TEAEs/SAEs (death, hospitalization, disability, medically significant events) are monitored post-consent until 30 days post-treatment. The MTD of MLN0264 (1.8 mg/kg) was determined via dose-escalation, with PK analysis (Cmax and AUC0-21d for MLN0264/MMAE) at Cycle 1.    Click to Show/Hide
Other Endpoint	Best Overall Response per RECIST (CR: disappearance of all lesions; PR: ≥30% target lesion reduction; PD: ≥20% increase/new lesions; SD: neither PR nor PD) is evaluated every 2 cycles (~9 months). Antitherapeutic antibodies (ATA) are assessed per cycle to determine immunogenicity, with blood samples analyzed for MLN0264 binding antibodies.
Experiment 10 Reporting the Activity Date of This ADC					[265]
Patients Enrolled	The study emphasizes safety monitoring (AEs/SAEs up to 30 days post-treatment) and pharmacokinetic profiling (MLN0264/MMAE levels during Cycles 1-3 and beyond). Tumor assessments occur every 2 cycles (Day 21) until progression, with survival follow-up for 6 months post-last patient enrollment. Archival tumor samples are required for GCC IHC analysis (separate consent). Protocol adherence includes strict contraception and abstinence criteria to mitigate risks.    Click to Show/Hide
Administration Dosage	MLN0264 1.8 mg/kg, 30-minute intravenous (IV) infusion, Day 1 of each 21-day cycle, for up to 1 year or until disease progression or unacceptable toxicity occurs (Up to 10 cycles). The dose may be decreased, delayed or discontinued in participants who develop treatment-associated nonhematologic and hematologic toxicity to MLN0264.
Related Clinical Trial
NCT Number	NCT02202785	Phase Status	PHASE2
Clinical Description	A Phase 2 Trial of MLN0264 in Previously Treated Patients With Advanced or Metastatic Pancreatic Adenocarcinoma Expressing Guanylyl Cyclase C (GCC)
Primary Endpoint	The primary endpoint is Overall Response Rate (ORR) per RECIST v1.1, assessing CR (disappearance of all lesions) and PR (≥30% decrease in target lesions) from Cycle 2 until disease progression or study closure (up to 16 months). Secondary endpoints include lab abnormalities (Grade 3+ per NCI CTCAE), vital signs, PFS (time to progression/death), duration of response, disease control rate (CR+PR+SD≥12 weeks), OS (time to death), pharmacokinetics (Cmax, MMAE levels), GCC H-score (0-600 scale), AEs/SAEs, tumor reduction percentage, and anti-drug antibodies.    Click to Show/Hide
Other Endpoint	Eligible patients are adults (≥18) with histologically confirmed metastatic/inoperable pancreatic adenocarcinoma (GCC H-score≥10), ≥1 prior chemotherapy, measurable disease per RECIST v1.1, ECOG 0-1, adequate organ function (ANC≥1.5x10^9/L, platelets≥100x10^9/L, etc.), and resolved prior treatment toxicities (≤Grade 1). Fertile participants must use contraception. Key exclusions: recent radiotherapy/chemotherapy (≤4 weeks), pregnancy/lactation, uncontrolled cardiovascular disease, QTc-prolonging drugs, Grade 2+ neuropathy, active infection, brain metastases, or anticoagulant therapy.    Click to Show/Hide
Experiment 11 Reporting the Activity Date of This ADC					[266]
Patients Enrolled	Disease response was evaluated every 2 cycles using modified RECIST 1.1 (CR: lesion disappearance; PR: ≥30% target lesion reduction; PD: ≥20% increase/new lesions; SD: neither PR nor PD). Blood samples were collected pre-dose for ATA analysis. Safety monitoring included abnormal labs, vital signs, and PK parameters throughout treatment. Post-treatment follow-up continued for PFS/OS every 12 weeks until PD/subsequent therapy or 6 months post-discontinuation. The study was terminated early, limiting some data collection periods.    Click to Show/Hide
Administration Dosage	Phase 1: MLN0264 1.2 milligram per kilogram (mg/kg) starting dose, Intravenous (IV), on Day 1 of 3 week cycles, for up to 1 year or until disease progression or unacceptable toxicity. Dosage of MLN0264 will be increased to 1.5 mg/kg then 1.8 mg/kg using a 3 + 3 dose escalation design to determine a maximum tolerated dose (MTD) and/or recommended Phase 2 Dose (RP2D).Phase 2: MLN0264, IV, on Day 1 of 3 week cycles, for up to 1 year or until disease progression or unacceptable toxicity. Dosage for this phase will be determined from results of Phase 1 MTD/RP2D.    Click to Show/Hide
Related Clinical Trial
NCT Number	NCT02391038	Phase Status	PHASE1
Clinical Description	A Phase 1/2 Trial of MLN0264 in Previously Treated Asian Patients With Advanced Gastrointestinal (GI) Carcinoma (Phase 1) or Metastatic or Recurrent Gastric or Gastroesophageal Junction Adenocarcinoma (Phase 2) Expressing Guanylyl Cyclase C (GCC)
Primary Endpoint	The Phase 1 safety assessment monitored DLTs (Grade 4 hematologic toxicities, Grade 3+ non-hematologic events despite management, treatment delays >2 weeks) during Cycle 1 and TEAEs/SAEs up to 30 days post-treatment (~35 weeks). Pharmacokinetic analysis of MLN0264, MMAE, and total antibody (Cmax, Tmax, AUCinf, AUCint, Ctrough) was performed at Cycles 1-2. Key evaluations included lab abnormalities, vital signs, and RP2D determination (MTD defined as dose where ≤1/6 participants experienced DLT). Phase 2 assessed ORR per RECIST (CR+PR), PFS (time to progression/death), DOR (confirmed response to PD), DCR (CR+PR+SD≥12 weeks), OS, tumor reduction, GCC H-score (0-600), and ATAs over ~1 year.    Click to Show/Hide
Other Endpoint	Eligible patients had GI/gastric adenocarcinoma with GCC expression (H-score≥10), measurable RECIST disease, ECOG 0-1, and adequate organ function. Phase 1 included various GI carcinomas while Phase 2 focused on gastric/GEJ cancers. Key exclusions: recent chemotherapy/investigational drugs (<4 weeks), pregnancy/lactation, uncontrolled cardiovascular disease, CNS metastases, significant infections, neuropathy ≥Grade 2, strong CYP3A4 inhibitors (<2 weeks), or hepatitis/HIV. All prior treatment toxicities (except alopecia) must have resolved to ≤Grade 1.    Click to Show/Hide
Experiment 12 Reporting the Activity Date of This ADC					[267]
Patients Enrolled	Tumor assessments utilized RECIST 1.1 criteria: CR (lesion disappearance + normal markers), PR (≥30% target lesion reduction), SD (no qualifying shrinkage/growth), PD (≥20% increase/new lesions). Blood samples for PK/ATA analysis were collected pre-dose (all cycles) and at specified post-dose intervals (Cycles 1-3). Safety follow-up continued for 30 days post-treatment, while survival/PFS was monitored every 12 weeks until death/progression or 6 months post-discontinuation. Clinically significant findings were investigator-determined, including abnormal labs (serum chemistry, hematology, coagulation) and vital signs (BP, heart rate, temperature).    Click to Show/Hide
Administration Dosage	MLN0264 1.8 mg/kg, 30-minute intravenous (IV) infusion, Day 1 of each 21-day cycle, for up to 1 year or until disease progression or unacceptable toxicity occurs (Up to 14 cycles). The dose may be decreased, delayed or discontinued in participants who develop treatment-associated nonhematologic and hematologic toxicity to MLN0264.
Related Clinical Trial
NCT Number	NCT02202759	Phase Status	PHASE2
Clinical Description	A Phase 2 Trial of MLN0264 in Previously Treated Patients With Metastatic or Recurrent Adenocarcinoma of the Stomach or Gastroesophageal Junction Expressing Guanylyl Cyclase C (GCC)
Primary Endpoint	The study assessed efficacy endpoints including ORR (CR+PR per RECIST 1.1), PFS (time to progression/death), DOR (response duration), DCR (CR+PR+SD≥12 weeks), and OS (up to 17 months) in participants with GCC-positive gastric/GEJ adenocarcinoma (H-score≥10). Pharmacokinetic analysis measured serum concentrations of MLN0264, total antibodies (conjugated/unconjugated), and MMAE during Cycles 1-14 (pre/post-dose timepoints). Tumor response was evaluated via imaging every other cycle (Day 21), with GCC expression quantified by IHC H-score (0-600). Safety monitoring included AEs/SAEs, lab abnormalities (Grade 3+ per NCI CTCAE), vital signs, and ATA development (pre-dose each cycle).    Click to Show/Hide
Other Endpoint	Eligible participants had metastatic/unresectable gastric/GEJ adenocarcinoma (≥1 prior chemotherapy), measurable RECIST 1.1 lesions, ECOG 0-1, and adequate organ function (ANC≥1.5x10^9/L, platelets≥100x10^9/L, bilirubin≤1.5xULN). Key exclusions: recent radiotherapy/chemotherapy (<4 weeks), anticoagulant use, symptomatic brain metastases, Grade 2+ neuropathy, strong CYP3A4 inhibitors (<2 weeks), uncontrolled cardiovascular disease, or HIV. Females of childbearing potential required dual contraception, while males practiced barrier methods until 4 months post-treatment. Archival tumor GCC testing (H-score) was mandatory for enrollment.    Click to Show/Hide

Experiment 1 Reporting the Activity Date of This ADC					[244]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 34%	High GCC expression (GCC+++)
Method Description	To evaluate the efficacy of TAK-264 in mouse models of pancreatic cancer,ten pancreatic PDX models were treated with 10 mg/kg of TAK-264 for at least 17 days. Each treatment group contained 56 mice with tumor pieces (~3mm3 fragments) injected into the right and left flank to give ~10 evaluable tumors. Mice were randomized into control or TAK-264 groups when tumor volumes reached ~150-300 mm3.    Click to Show/Hide
In Vivo Model	Pancreatic cancer PDX model (PDX: PANC137)
Experiment 2 Reporting the Activity Date of This ADC					[244]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 46%	High GCC expression (GCC+++)
Method Description	To evaluate the efficacy of TAK-264 in mouse models of pancreatic cancer,ten pancreatic PDX models were treated with 10 mg/kg of TAK-264 for at least 17 days. Each treatment group contained 56 mice with tumor pieces (~3mm3 fragments) injected into the right and left flank to give ~10 evaluable tumors. Mice were randomized into control or TAK-264 groups when tumor volumes reached ~150-300 mm3.    Click to Show/Hide
In Vivo Model	Pancreatic cancer PDX model (PDX: PANC129)
Experiment 3 Reporting the Activity Date of This ADC					[244]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 48.70%	High GCC expression (GCC+++)
Method Description	To evaluate the efficacy of TAK-264 in mouse models of pancreatic cancer,ten pancreatic PDX models were treated with 10 mg/kg of TAK-264 for at least 17 days. Each treatment group contained 56 mice with tumor pieces (~3mm3 fragments) injected into the right and left flank to give ~10 evaluable tumors. Mice were randomized into control or TAK-264 groups when tumor volumes reached ~150-300 mm3.    Click to Show/Hide
In Vivo Model	Pancreatic cancer PDX model (PDX: PANC269)
Experiment 4 Reporting the Activity Date of This ADC					[244]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 60.90%	High GCC expression (GCC+++)
Method Description	To evaluate the efficacy of TAK-264 in mouse models of pancreatic cancer,ten pancreatic PDX models were treated with 10 mg/kg of TAK-264 for at least 17 days. Each treatment group contained 56 mice with tumor pieces (~3mm3 fragments) injected into the right and left flank to give ~10 evaluable tumors. Mice were randomized into control or TAK-264 groups when tumor volumes reached ~150-300 mm3.    Click to Show/Hide
In Vivo Model	Pancreatic cancer PDX model (PDX: PANC277)
Experiment 5 Reporting the Activity Date of This ADC					[244]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 61.90%	High GCC expression (GCC+++)
Method Description	To evaluate the efficacy of TAK-264 in mouse models of pancreatic cancer,ten pancreatic PDX models were treated with 10 mg/kg of TAK-264 for at least 17 days. Each treatment group contained 56 mice with tumor pieces (~3mm3 fragments) injected into the right and left flank to give ~10 evaluable tumors. Mice were randomized into control or TAK-264 groups when tumor volumes reached ~150-300 mm3.    Click to Show/Hide
In Vivo Model	Pancreatic cancer PDX model (PDX: PANC266)
Experiment 6 Reporting the Activity Date of This ADC					[244]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 64.20%	High GCC expression (GCC+++)
Method Description	To evaluate the efficacy of TAK-264 in mouse models of pancreatic cancer,ten pancreatic PDX models were treated with 10 mg/kg of TAK-264 for at least 17 days. Each treatment group contained 56 mice with tumor pieces (~3mm3 fragments) injected into the right and left flank to give ~10 evaluable tumors. Mice were randomized into control or TAK-264 groups when tumor volumes reached ~150-300 mm3.    Click to Show/Hide
In Vivo Model	Pancreatic cancer PDX model (PDX: PANC193)
Experiment 7 Reporting the Activity Date of This ADC					[244]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 67.50%	High GCC expression (GCC+++)
Method Description	To evaluate the efficacy of TAK-264 in mouse models of pancreatic cancer,ten pancreatic PDX models were treated with 10 mg/kg of TAK-264 for at least 17 days. Each treatment group contained 56 mice with tumor pieces (~3mm3 fragments) injected into the right and left flank to give ~10 evaluable tumors. Mice were randomized into control or TAK-264 groups when tumor volumes reached ~150-300 mm3.    Click to Show/Hide
In Vivo Model	Pancreatic cancer PDX model (PDX: PANC272)
Experiment 8 Reporting the Activity Date of This ADC					[244]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 69.60%	High GCC expression (GCC+++)
Method Description	To evaluate the efficacy of TAK-264 in mouse models of pancreatic cancer,ten pancreatic PDX models were treated with 10 mg/kg of TAK-264 for at least 17 days. Each treatment group contained 56 mice with tumor pieces (~3mm3 fragments) injected into the right and left flank to give ~10 evaluable tumors. Mice were randomized into control or TAK-264 groups when tumor volumes reached ~150-300 mm3.    Click to Show/Hide
In Vivo Model	Pancreatic cancer PDX model (PDX: PANC268)
Experiment 9 Reporting the Activity Date of This ADC					[244]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 69.60%	High GCC expression (GCC+++)
Method Description	To evaluate the efficacy of TAK-264 in mouse models of pancreatic cancer,ten pancreatic PDX models were treated with 10 mg/kg of TAK-264 for at least 17 days. Each treatment group contained 56 mice with tumor pieces (~3mm3 fragments) injected into the right and left flank to give ~10 evaluable tumors. Mice were randomized into control or TAK-264 groups when tumor volumes reached ~150-300 mm3.    Click to Show/Hide
In Vivo Model	Pancreatic cancer PDX model (PDX: PANC150)
Experiment 10 Reporting the Activity Date of This ADC					[244]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 70.10%	High GCC expression (GCC+++)
Method Description	To evaluate the efficacy of TAK-264 in mouse models of pancreatic cancer,ten pancreatic PDX models were treated with 10 mg/kg of TAK-264 for at least 17 days. Each treatment group contained 56 mice with tumor pieces (~3mm3 fragments) injected into the right and left flank to give ~10 evaluable tumors. Mice were randomized into control or TAK-264 groups when tumor volumes reached ~150-300 mm3.    Click to Show/Hide
In Vivo Model	Pancreatic cancer PDX model (PDX: PANC122)

Experiment 1 Reporting the Activity Date of This ADC					[244]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	< 25 ug/mL
Method Description	Anti-proliferative Effects of TAK-264 Against Pancreatic Cancer Cell Lines. Eleven pancreatic cancer cell lines were treated with TAK-264 (dose range 0.4-25 ug/mL) for 72 hours and analyzed by a SRB proliferation assay. Cell lines were deemed more responsive if proliferation was less than 50% after treatment with 25g/mL of TAK-264.
In Vitro Model	Pancreatic adenocarcinoma	Panc 02.03 cells		CVCL_1633
Experiment 2 Reporting the Activity Date of This ADC					[244]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	< 25 ug/mL	High GCC expression (GCC+++)
Method Description	Anti-proliferative Effects of TAK-264 Against Pancreatic Cancer Cell Lines. Eleven pancreatic cancer cell lines were treated with TAK-264 (dose range 0.4-25 ug/mL) for 72 hours and analyzed by a SRB proliferation assay. Cell lines were deemed more responsive if proliferation was less than 50% after treatment with 25g/mL of TAK-264.
In Vitro Model	Pancreatic ductal adenocarcinoma	Panc 05.04 cells		CVCL_1637
Experiment 3 Reporting the Activity Date of This ADC					[244]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	< 25 ug/mL
Method Description	Anti-proliferative Effects of TAK-264 Against Pancreatic Cancer Cell Lines. Eleven pancreatic cancer cell lines were treated with TAK-264 (dose range 0.4-25 ug/mL) for 72 hours and analyzed by a SRB proliferation assay. Cell lines were deemed more responsive if proliferation was less than 50% after treatment with 25g/mL of TAK-264.
In Vitro Model	Pancreatic adenocarcinoma	Panc 03.27 cells		CVCL_1635
Experiment 4 Reporting the Activity Date of This ADC					[244]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	< 25 ug/mL
Method Description	Anti-proliferative Effects of TAK-264 Against Pancreatic Cancer Cell Lines. Eleven pancreatic cancer cell lines were treated with TAK-264 (dose range 0.4-25 ug/mL) for 72 hours and analyzed by a SRB proliferation assay. Cell lines were deemed more responsive if proliferation was less than 50% after treatment with 25g/mL of TAK-264.
In Vitro Model	Pancreatic ductal adenocarcinoma	MIA PaCa-2 cells		CVCL_0428
Experiment 5 Reporting the Activity Date of This ADC					[244]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	< 25 ug/mL
Method Description	Anti-proliferative Effects of TAK-264 Against Pancreatic Cancer Cell Lines. Eleven pancreatic cancer cell lines were treated with TAK-264 (dose range 0.4-25 ug/mL) for 72 hours and analyzed by a SRB proliferation assay. Cell lines were deemed more responsive if proliferation was less than 50% after treatment with 25g/mL of TAK-264.
In Vitro Model	Pancreatic adenosquamous carcinoma	L3.6pl cells		CVCL_0384

Experiment 1 Reporting the Activity Date of This ADC					[260]
Patients Enrolled	Eligible patients (≥18 years, KPS >60) must have histologically confirmed GBM, prior progression post-standard therapy (≥4 weeks since chemo/bevacizumab, ≥3 weeks post-radiation), MRI-measurable disease, and stable organ/lab values (ANC ≥1000/mm 3, platelets ≥100k/mm 3, bilirubin ≤2.0 mg/dL). Exclusions: non-GBM malignancies (excluding specific low-risk cancers), QTc >500 msec, recent GBM treatment (within 3 weeks), PSMA ADC/MMAE exposure, pancreatitis history, or uncontrolled infections/cardiopulmonary disease. Effective contraception is mandatory.    Click to Show/Hide
Administration Dosage	2.5 mg/kg, IV, over 60 minutes every 3 weeks
Related Clinical Trial
NCT Number	NCT01856933	Phase Status	PHASE2
Clinical Description	BrUOG 263: PSMA ADC for Recurrent Glioblastoma Multiforme (GBM): A Phase II Brown University Oncology Research Group Study
Primary Endpoint	The study evaluates response rate (using RANO criteria) in recurrent glioblastoma patients previously treated with radiation, temozolomide, and bevacizumab, defining progression as >25% tumor increase, new lesions, or clinical deterioration (followed for up to 1 year).
Other Endpoint	Safety assessment tracks toxicities (including unrelated events) in patients receiving PSMA ADC for recurrent GBM, recorded every 3 weeks until 30 days post-treatment (approximately 6 months total).
Experiment 2 Reporting the Activity Date of This ADC					[261]
Patients Enrolled	Eligible participants must have confirmed progressive castration-resistant metastatic prostate cancer with prior taxane-based chemotherapy and ECOG status 0-1. Key exclusions include significant cardiac/pulmonary disease, active infections requiring antibiotics, prior PSMA-targeted therapy, or a history of substance abuse.
Administration Dosage	PSMA ADC administered IV
Related Clinical Trial
NCT Number	NCT01414283	Phase Status	PHASE1
Clinical Description	A Phase 1 Dose-escalation Study of PSMA ADC in Subjects With Progressive, Castration-resistant, Metastatic Prostate Cancer
Primary Endpoint	The study aims to determine the maximum tolerated dose (MTD) of PSMA ADC in patients with progressive, castration-resistant metastatic prostate cancer, with toxicity observation over a 13-week timeframe.
Experiment 3 Reporting the Activity Date of This ADC					[262]
Patients Enrolled	Eligible patients must have completed prior PSMA ADC 1301 study with observed treatment benefit, confirmed progressive castration-resistant metastatic prostate cancer, prior taxane chemotherapy, and ECOG 0-1. Exclusions: significant cardiac/pulmonary disease, active infections requiring antibiotics, or history of substance abuse.
Administration Dosage	PSMA ADC administered IV
Related Clinical Trial
NCT Number	NCT01414296	Phase Status	PHASE1
Clinical Description	Extended 39-Week Study of PSMA ADC Following the Initial 12-Week Dose-escalation Study in Subjects With Progressive, Castration-resistant, Metastatic Prostate Cancer
Primary Endpoint	The study evaluates the safety of PSMA ADC over 39 weeks by monitoring adverse events, laboratory results (hematology, chemistry, urinalysis), vital signs, ECG, and physical exams in eligible participants.
Experiment 4 Reporting the Activity Date of This ADC					[263]
Patients Enrolled	Eligible participants must have metastatic castration-resistant prostate cancer, either with prior taxane chemotherapy (requiring Sponsor approval if >2 regimens) or chemotherapy-naïve (if ineligible/refused Radium-223), plus progression on abiraterone/enzalutamide, ECOG 0-2, and ≥6-month life expectancy. Exclusions include recent radiation/chemotherapy/radiopharmaceuticals, PSMA ADC/MMAE-based ADC treatment (unless Sponsor-approved), significant cardiac/pulmonary disease, active infections, pancreatitis, or substance abuse history.    Click to Show/Hide
Administration Dosage	PSMA ADC administered IV at 2.5 mg/kg Q3W for 8 cycles or 2.3 mg/kg Q3W for 8 cycles.
Related Clinical Trial
NCT Number	NCT01695044	Phase Status	PHASE2
Clinical Description	A Phase 2, Open-label, Multicenter Study of PSMA ADC in Subjects With Metastatic Castration-resistant Prostate Cancer
Primary Endpoint	This study evaluates efficacy endpoints at 24 weeks including PSA response (≥30% or ≥50% decrease from baseline), CTC response (≥30% or ≥50% reduction), and radiologic response (assessed via CT/bone scans per RECIST 1.1, tracking target/non-target lesions and bone/visceral/nodal metastases for best overall response before progression).
Experiment 5 Reporting the Activity Date of This ADC					[264]
Patients Enrolled	Eligible subjects had completed the PSMA ADC 2301 trial with anticipated continued benefit, ECOG 0-2, and maintained androgen-deprivation therapy if applicable, with contraception compliance. Exclusions: active infections (e.g., UTIs), hypersensitivity to PSMA ADC components/monoclonal antibodies, severe cardiac/pulmonary disease, or conditions compromising study participation/Safety evaluation.    Click to Show/Hide
Administration Dosage	Upon recommendation from the PI and after Sponsor approval, a subject benefiting from treatment could have received up to eight additional doses Q3W. Subjects were weighed prior to each cycle and dosing was calculated on a mg/kg basis prior to each dose, with a maximum weight of 100 kg for dosing calculations.
Related Clinical Trial
NCT Number	NCT02020135	Phase Status	PHASE2
Clinical Description	An Open-label Treatment Extension of PSMA ADC in Subjects With Metastatic Castration-resistant Prostate Cancer (mCRPC)
Primary Endpoint	The trial assessed efficacy at 25 weeks through PSA response (≥30% or ≥50% decrease from baseline), CTC response (≥50% reduction), and radiologic response (using bone/CT scans per RECIST 1.1 to evaluate target/non-target lesions and metastatic sites), with responses defined by the maximum observed decreases post-baseline.

Experiment 1 Reporting the Activity Date of This ADC					[269]
Efficacy Data	Partial Response (PR)	20.00 50.00 %	High CD71 expression (CD71+++)
Patients Enrolled	Metastatic or locally advanced unresectable solid tumors without approved life-prolonging treatment options.
Administration Dosage	CX-2029 (0.10, 0.25, 0.50, 1, 2, 3, 4, or 5 mg/kg) i.v. over 90 minutes [later increased to 180 minutes to mitigate infusion-related reactions (IRR)] every 3 weeks.
Related Clinical Trial
NCT Number	NCT03543813	Phase Status	Phase 1
Clinical Description	A phase 1-2, first-in-human study of CX-2029 in adults with metastatic or locally advanced unresectable solid tumors or diffuse large B-cell lymphomas (PROCLAIM-CX-2029).
Primary Endpoint	For the dose of 3 mg/kg, confirmed partial response rate=20.00% (n=2, 95% CI=2.50-55.60). For the dose of 5 mg/kg, confirmed partial response rate=50.00% (n=1, 95% CI=1.30-98.70).
Other Endpoint	For the dose of 0.5 mg/kg, Disease controla rate=50.00% (n=3, 95% CI=11.80-82.20). For the dose of 2 mg/kg, Disease controla rate=28.60% (n=2, 95% CI=3.7-71.0). For the dose of 3 mg/kg, Disease controla rate=50.00% (n=5, 95% CI 18.70-81.30). For the dose of 5 mg/kg, Disease controla rate=50.00% (n=1, 95% CI 1.30-98.70).
Experiment 2 Reporting the Activity Date of This ADC					[286]
Patients Enrolled	Eligible patients include adults (≥18) with metastatic/locally advanced unresectable tumors (specific histologies required for Arms B/C) progressing after standard therapies, who can provide tumor samples. Key exclusions include Grade 1+ neuropathy, active infections, cardiac/metabolic disorders, CNS conditions, anticoagulation use, hepatic impairment (Child-Pugh B/C), or recent major surgery. Additional criteria may apply.    Click to Show/Hide
Related Clinical Trial
NCT Number	NCT03543813	Phase Status	PHASE1|||PHASE2
Clinical Description	A Phase 1-2, First-in-Human Study of CX-2029 in Adults With Metastatic or Locally Advanced Unresectable Solid Tumors or Diffuse Large B-cell Lymphomas (PROCLAIM-CX-2029)
Primary Endpoint	The study evaluates dose-limiting toxicities (DLTs) of CX-2029 monotherapy across various dose levels during the initial 21-day observation period.
Other Endpoint	Anti-tumor activity is assessed by objective response rate (ORR) at different dose levels over a 2-year timeframe following CX-2029 monotherapy administration.

Experiment 1 Reporting the Activity Date of This ADC					[278]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 74.10%	High CD71 expression (CD71+++)
Method Description	Dosing started on the same day for all groups,and dosing volume was adjusted for each mouse based on body weight on day of dosing. PDX models were intravenously dosed with vehicle (PBS) , 3 mg/kg on day 0 and day 7. Mice were checked daily for morbidity and mortality. Tumors were measured twice weekly via calipers.
In Vivo Model	Pancreatic cancer PDX model (PDX: PA6237)
Experiment 2 Reporting the Activity Date of This ADC					[278]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 80.80%	High CD71 expression (CD71+++)
Method Description	Female BALB/c nude mice used for esophageal,gastric,pancreatic models,and NOD/SCID,NPG,or NOG mice used for DLBCL models and used at ages 5 to 7 weeks. Seven- to 8-week-old female Athymic Nude-Foxn1nu mice were used for breast,HNSCC,and NSCLC models (Envigo). Human cancer cell lines or tumor fragments 2 to 3 mm in diameter from stock mice inoculated with primary human tumor xenografts were harvested and used to inoculate study mice by subcutaneous injection into the right flank. When tumors reached approximately 100 to 200 mm3,mice were randomized into treatment groups based on tumor volume and body weight. Dosing started on the same day for all groups,and dosing volume was adjusted for each mouse based on body weight on day of dosing. PDX models were intravenously dosed with vehicle (PBS),1.5 mg/kg,3 mg/kg,or 6 mg anti-CD71 PDC on day 0 and day 9. Mice were checked daily for morbidity and mortality. Tumors were measured twice weekly via calipers.    Click to Show/Hide
In Vivo Model	CTG-820 PDX model
Experiment 3 Reporting the Activity Date of This ADC					[278]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 97.60%	High CD71 expression (CD71+++)
Method Description	Dosing started on the same day for all groups,and dosing volume was adjusted for each mouse based on body weight on day of dosing. PDX models were intravenously dosed with vehicle (PBS) , 6 mg/kg on day 0 and day 7. Mice were checked daily for morbidity and mortality. Tumors were measured twice weekly via calipers.
In Vivo Model	Non-small cell lung cancer PDX model (PDX: CTG-0860)
Experiment 4 Reporting the Activity Date of This ADC					[278]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 98%	High CD71 expression (CD71+++)
Method Description	Female BALB/c nude mice used for esophageal,gastric,pancreatic models,and NOD/SCID,NPG,or NOG mice used for DLBCL models and used at ages 5 to 7 weeks. Seven- to 8-week-old female Athymic Nude-Foxn1nu mice were used for breast,HNSCC,and NSCLC models (Envigo). Human cancer cell lines or tumor fragments 2 to 3 mm in diameter from stock mice inoculated with primary human tumor xenografts were harvested and used to inoculate study mice by subcutaneous injection into the right flank. When tumors reached approximately 100 to 200 mm3,mice were randomized into treatment groups based on tumor volume and body weight. Dosing started on the same day for all groups,and dosing volume was adjusted for each mouse based on body weight on day of dosing. PDX models were intravenously dosed with vehicle (PBS),1.5 mg/kg,3 mg/kg,or 6 mg anti-CD71 PDC on day 0 and day 13. Mice were checked daily for morbidity and mortality. Tumors were measured twice weekly via calipers.    Click to Show/Hide
In Vivo Model	CTG-820 PDX model
Experiment 5 Reporting the Activity Date of This ADC					[278]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 98%	High CD71 expression (CD71+++)
Method Description	Female BALB/c nude mice used for esophageal,gastric,pancreatic models,and NOD/SCID,NPG,or NOG mice used for DLBCL models and used at ages 5 to 7 weeks. Seven- to 8-week-old female Athymic Nude-Foxn1nu mice were used for breast,HNSCC,and NSCLC models (Envigo). Human cancer cell lines or tumor fragments 2 to 3 mm in diameter from stock mice inoculated with primary human tumor xenografts were harvested and used to inoculate study mice by subcutaneous injection into the right flank. When tumors reached approximately 100 to 200 mm3,mice were randomized into treatment groups based on tumor volume and body weight. Dosing started on the same day for all groups,and dosing volume was adjusted for each mouse based on body weight on day of dosing. PDX models were intravenously dosed with vehicle (PBS),1.5 mg/kg,3 mg/kg,or 6 mg anti-CD71 PDC on day 0 and day 10. Mice were checked daily for morbidity and mortality. Tumors were measured twice weekly via calipers.    Click to Show/Hide
In Vivo Model	CTG-820 PDX model
Experiment 6 Reporting the Activity Date of This ADC					[278]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 99.40%	High CD71 expression (CD71+++)
Method Description	Dosing started on the same day for all groups,and dosing volume was adjusted for each mouse based on body weight on day of dosing. PDX models were intravenously dosed with vehicle (PBS) , 3 mg/kg on day 0 and day 7. Mice were checked daily for morbidity and mortality. Tumors were measured twice weekly via calipers.
In Vivo Model	Gastric cancer PDX models (PDX: GA6881)
Experiment 7 Reporting the Activity Date of This ADC					[278]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 99.80%	High CD71 expression (CD71+++)
Method Description	Dosing started on the same day for all groups,and dosing volume was adjusted for each mouse based on body weight on day of dosing. PDX models were intravenously dosed with vehicle (PBS) , 3 mg/kg on day 0 and day 7. Mice were checked daily for morbidity and mortality. Tumors were measured twice weekly via calipers.
In Vivo Model	Breast cancer PDX model (PDX: CTG-0708)
Experiment 8 Reporting the Activity Date of This ADC					[278]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100%	High CD71 expression (CD71+++)
Method Description	Dosing started on the same day for all groups,and dosing volume was adjusted for each mouse based on body weight on day of dosing. PDX models were intravenously dosed with vehicle (PBS) , 6 mg/kg on day 0 and day 7. Mice were checked daily for morbidity and mortality. Tumors were measured twice weekly via calipers.
In Vivo Model	Esophageal caner PDX model (PDX: ES0136)
Experiment 9 Reporting the Activity Date of This ADC					[278]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100%	High CD71 expression (CD71+++)
Method Description	Dosing started on the same day for all groups,and dosing volume was adjusted for each mouse based on body weight on day of dosing. PDX models were intravenously dosed with vehicle (PBS) , 6 mg/kg on day 0 and day 7. Mice were checked daily for morbidity and mortality. Tumors were measured twice weekly via calipers.
In Vivo Model	Gastric cancer PDX models (PDX: GA6881)
Experiment 10 Reporting the Activity Date of This ADC					[278]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100%	High CD71 expression (CD71+++)
Method Description	Dosing started on the same day for all groups,and dosing volume was adjusted for each mouse based on body weight on day of dosing. PDX models were intravenously dosed with vehicle (PBS) , 6 mg/kg on day 0 and day 7. Mice were checked daily for morbidity and mortality. Tumors were measured twice weekly via calipers.
In Vivo Model	Breast cancer PDX model (PDX: CTG-0708)
Experiment 11 Reporting the Activity Date of This ADC					[278]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100%	High CD71 expression (CD71+++)
Method Description	Dosing started on the same day for all groups,and dosing volume was adjusted for each mouse based on body weight on day of dosing. PDX models were intravenously dosed with vehicle (PBS) , 6 mg/kg on day 0 and day 7. Mice were checked daily for morbidity and mortality. Tumors were measured twice weekly via calipers.
In Vivo Model	Head and neck squamous cell carcinoma PDX model (PDX: CTG-820)
Experiment 12 Reporting the Activity Date of This ADC					[278]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100%	High CD71 expression (CD71+++)
Method Description	Dosing started on the same day for all groups,and dosing volume was adjusted for each mouse based on body weight on day of dosing. PDX models were intravenously dosed with vehicle (PBS) , 6 mg/kg on day 0 and day 7. Mice were checked daily for morbidity and mortality. Tumors were measured twice weekly via calipers.
In Vivo Model	Diffuse large B-cell lymphoma PDX model (PDX: LY6934)
Experiment 13 Reporting the Activity Date of This ADC					[278]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100%	High CD71 expression (CD71+++)
Method Description	Dosing started on the same day for all groups,and dosing volume was adjusted for each mouse based on body weight on day of dosing. PDX models were intravenously dosed with vehicle (PBS) , 6 mg/kg on day 0 and day 7. Mice were checked daily for morbidity and mortality. Tumors were measured twice weekly via calipers.
In Vivo Model	Pancreatic cancer PDX model (PDX: PA6237)
Experiment 14 Reporting the Activity Date of This ADC					[278]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100%	High CD71 expression (CD71+++)
Method Description	Female BALB/c nude mice used for esophageal,gastric,pancreatic models,and NOD/SCID,NPG,or NOG mice used for DLBCL models and used at ages 5 to 7 weeks. Seven- to 8-week-old female Athymic Nude-Foxn1nu mice were used for breast,HNSCC,and NSCLC models (Envigo). Human cancer cell lines or tumor fragments 2 to 3 mm in diameter from stock mice inoculated with primary human tumor xenografts were harvested and used to inoculate study mice by subcutaneous injection into the right flank. When tumors reached approximately 100 to 200 mm3,mice were randomized into treatment groups based on tumor volume and body weight. Dosing started on the same day for all groups,and dosing volume was adjusted for each mouse based on body weight on day of dosing. PDX models were intravenously dosed with vehicle (PBS),1.5 mg/kg,3 mg/kg,or 6 mg anti-CD71 PDC on day 0 and day 12. Mice were checked daily for morbidity and mortality. Tumors were measured twice weekly via calipers.    Click to Show/Hide
In Vivo Model	Esophageal cancer PDX model (PDX: ES0136)
Experiment 15 Reporting the Activity Date of This ADC					[278]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100%	High CD71 expression (CD71+++)
Method Description	Female BALB/c nude mice used for esophageal,gastric,pancreatic models,and NOD/SCID,NPG,or NOG mice used for DLBCL models and used at ages 5 to 7 weeks. Seven- to 8-week-old female Athymic Nude-Foxn1nu mice were used for breast,HNSCC,and NSCLC models (Envigo). Human cancer cell lines or tumor fragments 2 to 3 mm in diameter from stock mice inoculated with primary human tumor xenografts were harvested and used to inoculate study mice by subcutaneous injection into the right flank. When tumors reached approximately 100 to 200 mm3,mice were randomized into treatment groups based on tumor volume and body weight. Dosing started on the same day for all groups,and dosing volume was adjusted for each mouse based on body weight on day of dosing. PDX models were intravenously dosed with vehicle (PBS),1.5 mg/kg,3 mg/kg,or 6 mg anti-CD71 PDC on day 0 and day 11. Mice were checked daily for morbidity and mortality. Tumors were measured twice weekly via calipers.    Click to Show/Hide
In Vivo Model	Gastric cancer PDX model (PDX: GA6881)
Experiment 16 Reporting the Activity Date of This ADC					[278]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100%	High CD71 expression (CD71+++)
Method Description	Female BALB/c nude mice used for esophageal,gastric,pancreatic models,and NOD/SCID,NPG,or NOG mice used for DLBCL models and used at ages 5 to 7 weeks. Seven- to 8-week-old female Athymic Nude-Foxn1nu mice were used for breast,HNSCC,and NSCLC models (Envigo). Human cancer cell lines or tumor fragments 2 to 3 mm in diameter from stock mice inoculated with primary human tumor xenografts were harvested and used to inoculate study mice by subcutaneous injection into the right flank. When tumors reached approximately 100 to 200 mm3,mice were randomized into treatment groups based on tumor volume and body weight. Dosing started on the same day for all groups,and dosing volume was adjusted for each mouse based on body weight on day of dosing. PDX models were intravenously dosed with vehicle (PBS),1.5 mg/kg,3 mg/kg,or 6 mg anti-CD71 PDC on day 0 and day 8. Mice were checked daily for morbidity and mortality. Tumors were measured twice weekly via calipers.    Click to Show/Hide
In Vivo Model	Diffuse large B-cell lymphoma PDX model (PDX: LY6934)
Experiment 17 Reporting the Activity Date of This ADC					[278]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100%	High CD71 expression (CD71+++)
Method Description	Female BALB/c nude mice used for esophageal,gastric,pancreatic models,and NOD/SCID,NPG,or NOG mice used for DLBCL models and used at ages 5 to 7 weeks. Seven- to 8-week-old female Athymic Nude-Foxn1nu mice were used for breast,HNSCC,and NSCLC models (Envigo). Human cancer cell lines or tumor fragments 2 to 3 mm in diameter from stock mice inoculated with primary human tumor xenografts were harvested and used to inoculate study mice by subcutaneous injection into the right flank. When tumors reached approximately 100 to 200 mm3,mice were randomized into treatment groups based on tumor volume and body weight. Dosing started on the same day for all groups,and dosing volume was adjusted for each mouse based on body weight on day of dosing. PDX models were intravenously dosed with vehicle (PBS),1.5 mg/kg,3 mg/kg,or 6 mg anti-CD71 PDC on day 0 and day 7. Mice were checked daily for morbidity and mortality. Tumors were measured twice weekly via calipers.    Click to Show/Hide
In Vivo Model	Pancreatic cancer PDX model (PDX: PA6237)

Experiment 1 Reporting the Activity Date of This ADC					[278]
Efficacy Data	Half Maximal Effective Concentration (EC50)	1.2 nM
Method Description	Suspension or adherent cells were plated at a density of 1, 000 cells/well in 50-mL complete media in a 96-well white-walled tissue culture plate and used immediately or allowed to adhere overnight. Cells were then incubated with 50 uL of a 2 final concentration of test article for 3 to 5 days at 37 and 5% CO2.
In Vitro Model	Lung squamous cell carcinoma	NCI-H520 cells		CVCL_1566
Experiment 2 Reporting the Activity Date of This ADC					[278]
Efficacy Data	Half Maximal Effective Concentration (EC50)	1.3 nM	High CD71 expression (CD71+++)
Method Description	Suspension or adherent cells were plated at a density of 1, 000 cells/well in 50-mL complete media in a 96-well white-walled tissue culture plate and used immediately or allowed to adhere overnight. Cells were then incubated with 50 uL of a 2 final concentration of test article for 3 to 5 days at 37 and 5% CO2.
In Vitro Model	Colon cancer	HT29 cells		CVCL_A8EZ

Experiment 1 Reporting the Activity Date of This ADC					[270]
Related Clinical Trial
NCT Number	NCT04681131	Phase Status	Phase 2
Clinical Description	A phase 2 study of BA3011 alone and in combination with PD-1 inhibitor in adult patients with metastatic non-small cell lung cancer (NSCLC) who had prior disease progression on a PD-1/L-1 inhibitor.
Experiment 2 Reporting the Activity Date of This ADC					[277]
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NCT Number	NCT03425279	Phase Status	Phase 1
Clinical Description	A phase 1/ 2 safety and efficacy dose escalation/dose expansion study of a CAB-AXL-ADC, alone and in combination with a PD-1 inhibitor in adult patients with advanced solid tumors (phase 1) and adult and adolescent patients with advanced, refractory sarcoma (phase 2).
Experiment 3 Reporting the Activity Date of This ADC					[281]
Efficacy Data	Disease control rate (DCR)	41.10%
Patients Enrolled	Eligible patients (≥12 years for Phase 2) require measurable disease, adequate organ function, ECOG 0-1, and ≥3-month life expectancy; exclusions include uncontrolled CNS metastases, severe allergies, recent major surgery, prior auristatin therapy, active HIV/HBV/HCV, pregnancy/lactation, or clinically significant cardiac disease.
Administration Dosage	This phase 2 part 1 open-label study evaluated BA3011 in adult and adolescent patients (pts) with AXL-expressing (tumor membrane percent score ≥50%) advanced refractory sarcoma who received either BA3011 monotherapy 1.8 mg/kg every 2 weeks (Q2W) or BA3011 1.8 mg/kg Q2W + nivolumab
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NCT Number	NCT03425279	Phase Status	PHASE1|||PHASE2
Clinical Description	A Phase 1/2 Dose Escalation and Dose Expansion Study of Mecbotamab Vedotin (BA3011) Alone and in Combination with Nivolumab in Adult and Adolescent Patients 12 Years and Older with Advanced Solid Tumors
Primary Endpoint	The study evaluates safety metrics including dose-limiting toxicity (DLT), maximum tolerated dose (MTD), and adverse events (AEs) over 24 months in Phase 1, while Phase 2 additionally assesses confirmed objective response rate (ORR) per RECIST v1.1 as the primary efficacy endpoint.
Other Endpoint	Pharmacokinetic analysis (ADC, total antibody, MMAE levels, Cmax, AUC), immunogenicity (ADA development), and clinical response assessments (ORR, DOR, PFS, BOR, DCR, TTR, OS, tumor size change) are tracked over 24 months across both phases to characterize drug behavior and therapeutic impact.
Experiment 4 Reporting the Activity Date of This ADC					[301]
Patients Enrolled	Key inclusion criteria require measurable disease, age ≥18 years, adequate organ function, ECOG 0-1, and ≥3-month life expectancy. Major exclusions include significant cardiac disease, uncontrolled CNS metastasis, prior auristatin therapy, severe allergies, recent major surgery, active infections (HIV/HBV/HCV), and pregnancy/breastfeeding.
Administration Dosage	In this phase II, multicenter, open-label study, we evaluated patients (pts) with advanced, treatment-refractory metastatic NSCLC. Eligible pts whose NSCLC tumors expressed AXL were treated on days 1 and 8 of a 3-week cycle or every other week with 1.8 mg/kg Mec-V±nivolumab.
Related Clinical Trial
NCT Number	NCT04681131	Phase Status	PHASE2
Clinical Description	A Phase 2 Study of BA3011 Alone and in Combination with PD-1 Inhibitor in Adult Patients with Metastatic Non-small Cell Lung Cancer (NSCLC) Who Had Prior Disease Progression on a PD-1/L-1 Inhibitor, EGFR, or ALK Inhibitor.
Primary Endpoint	The primary endpoints include confirmed objective response rate (ORR) per RECIST v1.1 and incidence of adverse events (AEs) or serious adverse events (SAEs) as assessed by CTCAE v4.03/v5, both evaluated over a 24-month period.
Other Endpoint	Secondary endpoints assessed over 24 months comprise duration of response (DOR), progression-free survival (PFS), best overall response (BOR), disease control rate (DCR), time to response (TTR), overall survival (OS), and percent change from baseline in target lesion sum of diameters.
Experiment 5 Reporting the Activity Date of This ADC					[216]
Patients Enrolled	Eligible participants are women ≥18 with confirmed platinum-resistant high-grade serous ovarian/fallopian tube/peritoneal cancer showing measurable disease and adequate organ function, while excluding those with severe comorbidities, uncontrolled CNS metastases, recent major surgery, active infections, pregnancy, or high-risk autoimmune conditions over 3 years prior to treatment.    Click to Show/Hide
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NCT Number	NCT04918186	Phase Status	PHASE2
Clinical Description	An Immunotherapy Platform Study in Platinum Resistant High Grade Serous Ovarian Cancer
Primary Endpoint	The study evaluates objective response rate (ORR) via RECIST 1.1 over 36 months to identify effective immunotherapy combinations for platinum-resistant high-grade serous ovarian cancer in preparation for randomized trials.
Other Endpoint	Secondary endpoints include ORR assessment, progression-free and overall survival using RECIST/iRECIST criteria, and adverse event monitoring over 36 months to evaluate immunotherapy regimen efficacy and safety.

Experiment 1 Reporting the Activity Date of This ADC					[271]
Patients Enrolled	Patients with malignant pleural mesothelioma and MSLN in advanced malignant solid tumors.
Administration Dosage	Dose of 0.10, 0.50, 1.00, 1.50, 2.00 and 2.50 mg/kg.
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NCT Number	NCT04175847	Phase Status	Phase 1/2
Clinical Description	To evaluate the safety of RC88 for injection in patients with advanced malignant solid tumors, multicenter, open, multi-cohort extension of efficacy and pharmacokinetic characteristics phase 1 /2a clinical study.
Experiment 2 Reporting the Activity Date of This ADC					[272]
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NCT Number	NCT04175847	Phase Status	Phase 1/2
Clinical Description	To evaluate the safety of RC88 for injection in patients with advanced malignant solid tumors, multicenter, open, multi-cohort extension of efficacy and pharmacokinetic characteristics phase 1 /2a clinical study.
Experiment 3 Reporting the Activity Date of This ADC					[276]
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NCT Number	NCT05508334	Phase Status	Phase 1
Clinical Description	An open-label, non-randomised, multicentre study to allow continued access to and assess the safety and tolerability of RC88 for patients with advanced solid tumours.
Experiment 4 Reporting the Activity Date of This ADC					[296]
Patients Enrolled	Additional exclusions include untreated brain metastases, HBV/HCV/HIV positivity (unless controlled), recent live vaccines, allergies to RC88 or excipients, and pregnancy/lactation. Subjects with psychiatric/substance abuse issues or poor compliance are also excluded, per investigator judgment.
Administration Dosage	Participants will receive RC88 2.0 mg/kg every 3 weeks (Q3W)
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NCT Number	NCT06173037	Phase Status	PHASE2
Clinical Description	A Multicenter, Single-arm, Phase 2 Study to Evaluate the Efficacy, Safety and Pharmacokinetics of RC88 Monotherapy in Platinum-resistant Recurrent Epithelial Ovarian, Fallopian Tube and Primary Peritoneal Cancer
Primary Endpoint	The study evaluates Overall Response Rate (ORR) by both IRC and investigators using RECIST v1.1, along with Duration of Response (DOR) and Progression-free Survival (PFS) assessed by both parties. Additionally, it measures Overall Survival (OS), CA-125 levels via GCIG criteria, and pharmacokinetic parameters like RC88 binding antibody concentrations (ADC, TAb, free MMAE). Safety assessments include adverse events, lab abnormalities, and ADA/NAb incidence over approximately 2 years.    Click to Show/Hide
Other Endpoint	Eligible subjects must be ≥18 years old with histologically confirmed high-grade serous ovarian, fallopian tube, or peritoneal cancer, platinum-resistant, and progressed after ≥3 prior therapies. Key requirements include measurable lesions (RECIST v1.1), ECOG 0-1, adequate organ function, and contraception use. Exclusion criteria encompass uncontrolled effusions, active infections, recent systemic therapies, prior mesothelin/MMAE-targeting treatments, significant comorbidities (e.g., uncontrolled cardiovascular disease, interstitial lung disease), and conditions affecting safety or compliance.    Click to Show/Hide
Experiment 5 Reporting the Activity Date of This ADC					[297]
Patients Enrolled	Eligibility includes age 18-70 (Phase I) or ≥18 (Phase IIa), ECOG 0-1, MSLN+ tumors, adequate organ function. Exclusions cover recent therapies, unresolved toxicity >Grade 1, active infections, cardiovascular/ocular conditions, CNS metastases, pregnancy, or protocol non-compliance.
Administration Dosage	Phase I:Participants will be allocated to one of the following dose groups: 0.1, 0.5, 1.0, 1.5, 2.0 and 2.5 mg/kg, and receive a treatment of RC88-ADC followed by 21 days of dose limited toxicity (DLT) observation period. Phase IIa indication exploration
Related Clinical Trial
NCT Number	NCT04175847	Phase Status	PHASE1|||PHASE2
Clinical Description	To Evaluate the Safety of RC88 for Injection in Patients with Advanced Malignant Solid Tumors,Multicenter, Open, Multi-cohort Extension of Efficacy and Pharmacokinetic Characteristics Phase I /IIa Clinical Study
Primary Endpoint	The study evaluates Phase 1 adverse events via NCI-CTCAE v4.03 from consent to 28 days post-treatment, determines MTD of RC88 as the dose where ≥2/6 patients experience DLT within 21 days, and Phase 2 assesses ORR via IRC over 24 weeks.
Other Endpoint	Phase 1 tracks ORR (CR+PR), PFS (RECIST v1.1 progression/death), and PK parameters (Cmax, Tmax, AUC, Ctrough, t1/2, CL) for TAb, ADC, and MMAE across cycles, with immunogenicity testing for anti-RC88 antibodies from Cycle 1-3.
Experiment 6 Reporting the Activity Date of This ADC					[298]
Patients Enrolled	Eligible patients are ≥18 years with ECOG 0-1, MSLN-positive advanced/metastatic solid tumors (Phase I: failed standard therapy; Phase II: confirmed MSLN+). Exclusions include brain metastases, active HBV/HCV, recent major surgery, uncontrolled cardiac conditions, or allergy to study drug components.
Administration Dosage	Subjects will receive intravenous infusion of RC88 once every 2 weeks in a dose escalation fashion until confirmed progression, unacceptable toxicity, or any criterion for withdrawal from the trial or investigational medicinal product (IMP) occurs.
Related Clinical Trial
NCT Number	NCT05508334	Phase Status	PHASE1
Clinical Description	An Open-label, Non-randomised, Multicentre Study to Allow Continued Access to and Assess the Safety and Tolerability of RC88 for Patients with Advanced Solid Tumours
Primary Endpoint	The study evaluates the recommended Phase 2 dose (RP2D) of RC88 by assessing dose-limiting toxicity (DLT) incidence within 28 days of initial treatment.
Other Endpoint	Key outcomes include 24-month Objective Response Rate (ORR, CR/PR rates), measured PK parameters (Cmax, t½), and Progression-Free Survival (PFS) per RECIST v1.1 criteria across dose escalation and expansion phases.
Experiment 7 Reporting the Activity Date of This ADC					[299]
Patients Enrolled	Exclusions include brain metastases, active/hepatitis infections, recent major surgery, uncontrolled heart conditions, and allergies to mesothelin antibodies/tubulysin/mAb-related compounds, ensuring participant safety and protocol compliance.
Administration Dosage	1.5mg/kg ,2.0mg/kg ,2.5mg/kg by intravenous (IV) infusion,every 3 weeks
Related Clinical Trial
NCT Number	NCT05804526	Phase Status	PHASE1|||PHASE2
Clinical Description	An Open-label, Non-randomised, Multi-center Study to Evaluate the Safety, and Efficacy Off RC88 Combined With Sintilimab in AdvancedSolid Tumours
Primary Endpoint	The study evaluates RP2D within 28 days post-treatment and assesses DLT incidence of RC88 combined with Sintilimab, while monitoring ORR over 24 months based on CR/PR rates and measuring RC88's Cmax at specified intervals during dose escalation.
Other Endpoint	PFS is tracked for 24 months, calculated from treatment initiation to disease progression or death. Inclusion requires consent, ECOG 0/1, ≥12-week survival, MSLN positivity (Phase I), adequate organ function, and contraception adherence, with some MSLN testing exemptions for advanced cancers.
Experiment 8 Reporting the Activity Date of This ADC					[300]
Patients Enrolled	Exclusions include pregnancy, active HBV/HIV, recent live vaccines, prior immune checkpoint toxicity, uncontrolled systemic/autoimmune diseases, bleeding risks, interstitial lung disease, or significant cardiac/metastatic history. Cohort-specific exclusions: non-eligible NSCLC/cervical/gastric/ovarian cancer subtypes, prior docetaxel/VEGF/ADC use, or recent major surgery. Central nervous system metastases require stability ≥28 days post-treatment.    Click to Show/Hide
Related Clinical Trial
NCT Number	NCT06016062	Phase Status	PHASE1|||PHASE2
Clinical Description	A Multi-center Phase I/II Trial to Evaluate the Efficacy and Safety of RC148 As a Single Agent and Combination Therapy in Patients with Locally Advanced Unresectable or Metastatic Malignant Solid Tumors
Primary Endpoint	Phase I evaluates MTD/MAD and DLT incidence within 28 days post-treatment, alongside AE assessment per NCI-CTCAE v5.0 until 28/90 days post-treatment, while RP2D is determined via safety committee consensus. Phase II assesses ORR, DCR, DoR, and PFS per RECIST v1.1 over 15 months.
Other Endpoint	Phase I tracks ORR, DCR, DoR, and PFS over 15 months, alongside RC148 pharmacodynamics (PD-1 receptor occupancy, VEGF levels) and PK/ADA analysis. Phase II monitors AE severity (NCI-CTCAE v5.0), vital signs, and ECOG status. Key inclusion: age ≥18 (Phase I) or 18-75 (Phase II), ECOG 0/1, measurable lesions (RECIST v1.1), and organ function criteria (ANC ≥1.5×10^9/L, bilirubin ≤1.5×ULN, LVEF ≥50%).    Click to Show/Hide

Experiment 1 Reporting the Activity Date of This ADC					[273]
Related Clinical Trial
NCT Number	NCT03895112	Phase Status	Phase 1
Clinical Description	Phase 1 study of AVID200 in patients with myelofibrosis (myeloproliferative neoplasms research consortium [MPN-RC] 118).
Experiment 2 Reporting the Activity Date of This ADC					[274]
Related Clinical Trial
NCT Number	NCT04914117	Phase Status	Phase 1
Clinical Description	Phase 1, first-in-human, multicentre, open-label study of RC118 for injection in patients with locally advanced unresectable/metastatic solid tumours.
Experiment 3 Reporting the Activity Date of This ADC					[275]
Related Clinical Trial
NCT Number	NCT05205850	Phase Status	Phase 1
Clinical Description	An open, multi-center phase 1/2a clinical study of RC118 for injection in patients with locally advanced unresectable or metastatic malignant solid tumors with positive expression of CLAUDIN 18.2.
Experiment 4 Reporting the Activity Date of This ADC					[302]
Patients Enrolled	Eligible patients (18-75 years, ECOG 0-1) must have unresectable/metastatic Claudin 18.2-positive tumors refractory to standard therapy, measurable disease per RECIST v1.1, and adequate organ function (ANC≥1.5×109/L, platelets≥100×109/L, bilirubin≤1.5×ULN). Key exclusions include active HBV/HCV/HIV, uncontrolled comorbidities (cardiac, CNS metastases, grade≥2 neuropathy), recent antitumor therapy (<4 weeks), immunosuppression, or third-space effusions; reproductive-age patients require contraception compliance. Investigators may exclude participants deemed unsuitable for protocol adherence.    Click to Show/Hide
Administration Dosage	Part A (Dose Escalation): RC118 will be administered through IV infusion at the various dose levels, including 0.25, 0.5, 1.0, 1.5, 2, 2.5, and 3 mg/kg, 1-12 subjects for each dose level. Part B (Dose Confirmation): RC118 will be administered at up to two dose levels, which is equal or lower than MTD/MAD, through IV infusion. Each dose level contains 3-6 subjects.    Click to Show/Hide
Related Clinical Trial
NCT Number	NCT04914117	Phase Status	PHASE1
Clinical Description	Phase 1, First-in-Human, Multicentre, Open-label Study of RC118 for Injection in Patients With Locally Advanced Unresectable/Metastatic Solid Tumours
Primary Endpoint	The primary objectives include determining the maximum tolerated dose (MTD)/maximum administered dose (MAD) based on dose-limiting toxicities (DLTs) graded per NCI-CTCAE v5.0 over 18 months, with RP2D selection informed by safety committee review, while adverse events will be monitored throughout the study duration to assess treatment tolerability.
Other Endpoint	Secondary efficacy endpoints encompass ORR (RECIST v1.1), PFS, DCR, and DOR, all evaluated over 18 months, alongside pharmacokinetic analyses (Cmax, AUC, Tmax of RC118/MMAE) and immunogenicity assessment (anti-drug antibody incidence) to characterize therapeutic response, drug exposure, and immunogenic potential.
Experiment 5 Reporting the Activity Date of This ADC					[303]
Patients Enrolled	Eligible participants (18-75 years, ECOG 0-1) must have CLDN18.2-positive unresectable/metastatic gastric/GEJ/pancreatic cancers refractory to standard therapy with measurable lesions (RECIST v1.1), adequate organ function (ANC≥1.5×109/L, platelets≥100×109/L), and commit to contraception. Exclusions: active HBV/HCV/HIV, prior CLDN18.2 therapy, uncontrolled comorbidities (CNS metastases, QTc>480ms, NYHA 3-4 heart failure), recent anti-tumor treatment (<4 weeks), or pregnancy/breastfeeding. Investigator discretion applies for borderline cases.    Click to Show/Hide
Administration Dosage	Participants will be allocated to one of the following dose groups: 0.25, 0.5, 1.0, 1.5, 2.0, 2.5, and 3.0mg/kg, and receive a treatment of RC118-ADC followed by 14 days of dose limited toxicity (DLT) observation period.
Related Clinical Trial
NCT Number	NCT05205850	Phase Status	PHASE1|||PHASE2
Clinical Description	An Open, Multi-center Phase I/IIa Clinical Study of RC118 for Injection in Patients with Locally Advanced Unresectable or Metastatic Malignant Solid Tumors with Positive Expression of Claudin 18.2
Primary Endpoint	This study evaluates dose-limiting toxicity (DLT) within 28 days post-initial RC118 treatment (NCI-CTCAE v5.0-graded) and monitors adverse events (AEs) from consent through 28 days post-treatment to define safety, while assessing objective response rate (ORR) over 15 months by RECIST v1.1 (CR+PR).
Other Endpoint	Secondary outcomes include disease control rate (DCR; CR+PR+SD), progression-free survival (PFS), duration of response (DOR) over 15 months, pharmacokinetics (Tmax), immunogenicity (ADA incidence), and overall survival (OS; up to 2 years) to comprehensively characterize therapeutic efficacy, drug exposure, and immune response.
Experiment 6 Reporting the Activity Date of This ADC					[304]
Patients Enrolled	Eligible patients (18-75 years, ECOG 0-1) have Claudin18.2-positive metastatic gastric/GEJ adenocarcinoma refractory to ≤2 prior therapies, measurable lesions (RECIST v1.1), and adequate organ function. Key exclusions: active HBV/HCV/HIV, prior CLDN18.2/MMAE-based therapies, unstable brain metastases, QTc>450/470ms (M/F), uncontrolled comorbidities (NYHA 3-4 heart failure, autoimmune diseases requiring systemic treatment), or recent antitumor therapy (≤4 weeks). Phase 2 excludes patients with prior immune checkpoint inhibitor discontinuation due to toxicity or recent PD-1/PD-L1/VEGFR-targeted therapy.    Click to Show/Hide
Administration Dosage	Participants receive RC118- ADC (dose A or dose B) Q2W and Toripalimab (fixed dose) Q3W. Referring to the results of the Part A, an extension cohort using RC118 plus Toripalimab /RC148 will be established.
Related Clinical Trial
NCT Number	NCT06038396	Phase Status	PHASE1|||PHASE2
Clinical Description	A Phase I/II Clinical Study to Evaluate the Safety and Efficacy of RC118 in Combination with Toripalimab / RC148 for Patients with Claudin 18.2-Positive, Locally Advanced Unresectable or Metastatic Malignant Solid Tumors
Primary Endpoint	This Phase 1/2 study evaluates RC118+Toripalimab's safety (DLTs in first 21 days, AE/SAE incidence over 15 months) and establishes MTD/RP2D within 12 months; Phase 2 focuses on ORR (RECIST v1.1-confirmed CR/PR) over 15 months.
Other Endpoint	Secondary efficacy metrics include DCR (CR+PR+SD), PFS, DOR, and OS (all 15-month endpoints); pharmacokinetics (RC118/MMAE peak/trough levels) and immunogenicity (ADA incidence/timing) are assessed to characterize drug exposure and immune responses.
Experiment 7 Reporting the Activity Date of This ADC					[305]
Patients Enrolled	Eligible patients (≥18 years) must have WHO-confirmed primary/secondary myelofibrosis (MF-2+, DIPSS intermediate-2/high risk), ECOG 0-2, and platelets ≥25×109/L; exclusions: prior TGF-beta inhibitors (e.g., galunisertib), active cardiovascular disease (uncontrolled hypertension, NYHA III-IV), active infections, or pregnancy. Women of childbearing potential require contraception. Organ function thresholds: ALT/AST ≤3x ULN (≤4x if MF-related), bilirubin ≤1.5x ULN (≤2x if MF-related/Gilbert's), creatinine ≤2.0 mg/dL.    Click to Show/Hide
Administration Dosage	intravenous in dose cohorts of 70mg/m2 or 180 mg/m2
Related Clinical Trial
NCT Number	NCT03895112	Phase Status	PHASE1
Clinical Description	Phase I Study of AVID200 in Patients With Myelofibrosis (Myeloproliferative Neoplasms Research Consortium [MPN-RC] 118)
Primary Endpoint	Phase 1 evaluates the MTD of AVID200 over 6 cycles (21 days each) using a 3+3 design (max 12 patients, target toxicity rate 30%); subjects achieving clinical improvement (per IWG/ELN) or ≥1-grade bone marrow fibrosis reduction may continue in the extension phase.
Other Endpoint	Efficacy assessments include IWG/ELN response criteria (CR, PR, clinical improvement, etc.) at Cycles 6/12, bone marrow fibrosis grade (MF-0 to MF-3), symptom burden (MFSAFv4.0; 0-100 scale), and quality of life (EORTC QLQ-C30; higher scores indicate poorer health), all evaluated up to Cycle 13.

Experiment 1 Reporting the Activity Date of This ADC					[279]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100%	High GPRC5D expression (GPRC5D+++)
Method Description	The inhibitory activity of LM-305 against cancer cell growth was evaluated in Multiple myeloma CDX model in vivo. The dose of LM-305 was 3 mg/kg.
In Vivo Model	Multiple myeloma CDX model
In Vitro Model	Multiple myeloma	Multiple myeloma cells		Homo sapiens

Experiment 1 Reporting the Activity Date of This ADC					[279]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.10-0.30 nM	High GPRC5D expression (GPRC5D+++)
Method Description	LM-305 was evaluated in vitro for its cytotoxic activity against a panel of multiple myeloma cell lines. LM-305 was co-cultured with multiple myeloma cells.
In Vitro Model	Plasma cell myeloma	MM1.R cells		CVCL_8794
Experiment 2 Reporting the Activity Date of This ADC					[279]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.10-0.30 nM	High GPRC5D expression (GPRC5D+++)
Method Description	LM-305 was evaluated in vitro for its cytotoxic activity against a panel of multiple myeloma cell lines. LM-305 was co-cultured with multiple myeloma cells.
In Vitro Model	Plasma cell myeloma	NCI-H929 cells		CVCL_1600

Experiment 1 Reporting the Activity Date of This ADC					[282]
Patients Enrolled	Key inclusion criteria: signed ICF; age ≥18; ECOG 0-1; life expectancy ≥6 months; adequate hematologic/organ function (specific laboratory thresholds to be confirmed per protocol).
Administration Dosage	LM-305 Dose Escalation
Related Clinical Trial
NCT Number	NCT05647512	Phase Status	PHASE1|||PHASE2
Clinical Description	A Phase I/II, Open-Label, Multiple Centre Clinical Study to Evaluate the Safety, Tolerability, Pharmacokinetics, Immunogenicity and Preliminary Efficacy of LM-305 in Patients With Relapsed or Refractory Multiple Myeloma (RRMM) and Other Plasma Cell Diseases
Primary Endpoint	Primary safety endpoints include dose-limiting toxicity (DLT) assessment during Cycle 1 (21-day cycle) and comprehensive AE/SAE monitoring from ICF signing until 28 days post-EOT or alternative anticancer therapy initiation to evaluate LM-305 safety profile.

Experiment 1 Reporting the Activity Date of This ADC					[280]
Efficacy Data	Objective Response Rate (ORR)	38.50%
Patients Enrolled	Eligible patients (18-80 years, ECOG 0-1) must have advanced solid tumors (excluding sarcoma, with Nectin-4 testing in expansion cohorts), measurable disease (RECIST 1.1), and adequate organ function. Exclusions: recent anticancer therapies/surgeries (within 14-28 days), prior MMAE/nectin-4 ADCs, uncontrolled comorbidities (CNS metastases, diabetes, neuropathy ≥Grade 2), or CYP3A4/P-gp modifiers within 14 days. Contraception is mandatory during and for 6 months post-study    Click to Show/Hide
Administration Dosage	All subjects will receive a single intravenous (IV) infusion of 9MW2821 once weekly for the first 3 weeks of every 4 week cycle (i.e., on Days 1, 8 and 15).
Related Clinical Trial
NCT Number	NCT05216965	Phase Status	PHASE1|||PHASE2
Clinical Description	Phase I/II Clinical Study of the Safety, Tolerability, Pharmacokinetics and Preliminary Antitumor Activity of 9MW2821 in Subjects With Advanced Malignant Solid Tumors
Primary Endpoint	The primary safety outcome is adverse event incidence assessed until 28 days post-treatment, while the Phase 2 efficacy endpoint is confirmed objective response rate (ORR ≥28 days) evaluating complete/partial responses over 24 months.
Other Endpoint	Key secondary endpoints include pharmacokinetics (Cmax, AUC, t½, CL) for TAb/ADC/MMAE, along with disease control rate, duration of response, time to response, progression-free survival, overall survival (all 24-month assessments), and anti-drug antibody monitoring.
Experiment 2 Reporting the Activity Date of This ADC					[280]
Efficacy Data	Disease control rate (DCR)	84.60%
Patients Enrolled	Eligible patients (18-80 years, ECOG 0-1) must have advanced solid tumors (excluding sarcoma, with Nectin-4 testing in expansion cohorts), measurable disease (RECIST 1.1), and adequate organ function. Exclusions: recent anticancer therapies/surgeries (within 14-28 days), prior MMAE/nectin-4 ADCs, uncontrolled comorbidities (CNS metastases, diabetes, neuropathy ≥Grade 2), or CYP3A4/P-gp modifiers within 14 days. Contraception is mandatory during and for 6 months post-study    Click to Show/Hide
Administration Dosage	All subjects will receive a single intravenous (IV) infusion of 9MW2821 once weekly for the first 3 weeks of every 4 week cycle (i.e., on Days 1, 8 and 15).
Related Clinical Trial
NCT Number	NCT05216965	Phase Status	PHASE1|||PHASE2
Clinical Description	Phase I/II Clinical Study of the Safety, Tolerability, Pharmacokinetics and Preliminary Antitumor Activity of 9MW2821 in Subjects With Advanced Malignant Solid Tumors
Primary Endpoint	The primary safety outcome is adverse event incidence assessed until 28 days post-treatment, while the Phase 2 efficacy endpoint is confirmed objective response rate (ORR ≥28 days) evaluating complete/partial responses over 24 months.
Other Endpoint	Key secondary endpoints include pharmacokinetics (Cmax, AUC, t½, CL) for TAb/ADC/MMAE, along with disease control rate, duration of response, time to response, progression-free survival, overall survival (all 24-month assessments), and anti-drug antibody monitoring.
Experiment 3 Reporting the Activity Date of This ADC					[288]
Patients Enrolled	Eligible patients (18-75 years) must have ECOG 0-1, measurable disease (RECIST v1.1), adequate organ function, and ≥12-week life expectancy. Key exclusions: Grade ≥2 treatment-related toxicities or peripheral neuropathy; active autoimmune diseases; recent anticancer therapies (chemotherapy/radiotherapy within 21 days or immunotherapy within 14 days); prior nectin-4 targeted ADC treatment; major surgery within 28 days; significant cardiac/cerebrovascular events within 6 months; or other active malignancies within 3 years. Contraception is required during and for 6 months post-treatment.    Click to Show/Hide
Related Clinical Trial
NCT Number	NCT06492005	Phase Status	PHASE2
Clinical Description	A Phase II Clinical Study of Efficacy and Safety of 9MW2821Monotherapy or Combined With PD-1 Inhibitor in Locally Advanced or Metastatic Triple-Negative Breast Cancer
Primary Endpoint	The primary efficacy endpoint is objective response rate (ORR) according to RECIST v1.1, evaluated over a 24-month period in patients with locally advanced or metastatic triple-negative breast cancer.
Other Endpoint	Secondary outcomes include duration of response (DoR), time to response (TTR), disease control rate (DCR), progression-free survival (PFS), and overall survival (OS) all assessed over 24 months. Pharmacokinetic analysis will measure Cmax, AUC, t1/2, and CL of TAb, ADC, and MMAE. Anti-drug antibody (ADA) incidence will be monitored throughout the study period.    Click to Show/Hide
Experiment 4 Reporting the Activity Date of This ADC					[289]
Patients Enrolled	Eligible patients must have ECOG 0-1, ≥12-week life expectancy, measurable disease (RECIST v1.1), and ≤2 prior systemic therapies (including platinum-based chemo ± bevacizumab). Exclusions: non-HPV-associated histologies, recent anticancer treatments (chemotherapy/radiation within 21 days; investigational drugs within 28 days), Grade ≥2 toxicity, uncontrolled comorbidities (HbA1c ≥8%, active infections, CNS metastases), major surgery within 28 days, or prior nectin-4/MMAE-based ADCs. Contraception is required during and for 6 months post-study.    Click to Show/Hide
Administration Dosage	1.25mg/kg of 9MW2821 by intravenous infusion on days 1, 8 and 15 of every 28-day cycle
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NCT Number	NCT06692166	Phase Status	PHASE3
Clinical Description	A Randomized, Open-label, Phase 3 Study to Evaluate 9MW2821 vs Treatment of Physician's Choice in Subjects With Recurrent or Metastatic Cervical Cancer Who Progressed on or After Platinum-based Chemotherapy
Primary Endpoint	The primary endpoint is overall survival (OS), defined as the time from randomization to death from any cause, assessed over a 3-year study period in female patients (18-75 years) with recurrent/metastatic cervical cancer.
Other Endpoint	Secondary efficacy endpoints include objective response rate (ORR), disease control rate (DCR), progression-free survival (PFS), duration of response (DoR), and time to response (TTR), all investigator-assessed per RECIST v1.1 over 3 years. Safety endpoints cover adverse event incidence and anti-drug antibody (ADA) development.
Experiment 5 Reporting the Activity Date of This ADC					[290]
Patients Enrolled	Eligible patients (18-80 years, ECOG 0-1) must have advanced solid tumors (Phase Ia) or metastatic UC (Phase Ib), prior ICI/GC/GP therapy exposure, measurable disease (RECIST 1.1), adequate organ function, and provide tumor samples. Exclusions: recent anticancer therapies/surgeries (14-28 days), Grade ≥2 toxicity/neuropathy, MMAE-ADC treatment, uncontrolled comorbidities (CNS metastases, diabetes, cardiovascular disease), or strong CYP3A4/P-gp modifiers within 14 days. Contraception is mandatory during and 6 months post-study.    Click to Show/Hide
Administration Dosage	All subjects will receive a single intravenous (IV) infusion of 9MW2821 once weekly for the first 3 weeks of every 4 week cycle (i.e., on Days 1, 8 and 15).
Related Clinical Trial
NCT Number	NCT05773937	Phase Status	PHASE1
Clinical Description	A Phase I Clinical Study of the Safety, Tolerability, Pharmacokinetics and Preliminary Antitumor Activity of 9MW2821 in Advanced Malignant Solid Tumors
Primary Endpoint	The primary safety endpoint evaluates adverse event incidence monitored up to 28 days after the last dose administration.
Other Endpoint	Key secondary endpoints include PK parameters (Cmax, AUC, t1/2, CL for TAb/ADC/MMAE) and efficacy measures (ORR, DCR, DoR, TTR, PFS, OS) over 24 months, alongside anti-drug antibody (ADA) incidence assessment.
Experiment 6 Reporting the Activity Date of This ADC					[291]
Patients Enrolled	Eligible participants (18-80 years, ECOG 0-1) must have histologically confirmed locally advanced/metastatic urothelial cancer, prior standard therapy (or treatment-naïve), measurable lesions (RECIST 1.1), adequate organ function, and tumor tissue availability. Exclusions encompass recent anticancer treatments (within 21 days), prior MMAE-ADC/PD- (L)1 therapy, significant treatment-related toxicity (≥Grade 2), uncontrolled comorbidities (CNS metastases, infections, diabetes), major surgery (within 28 days), strong CYP3A4/P-gp modifiers (14 days), active corneal risks, or conditions posing significant safety concerns. Contraception is required during and for 6 months post-study.    Click to Show/Hide
Administration Dosage	1.0/1.25/1.5 mg/kg, intravenous (IV) infusion every cycle until disease progression or intolerable toxicity, etc.
Related Clinical Trial
NCT Number	NCT06079112	Phase Status	PHASE1|||PHASE2
Clinical Description	A Phase Ib/II, Open-label, Single Arm, Multicenter Clinical Study to Evaluate the Safety and Efficacy of 9MW2821 Combined With Toripalimab Injection in Subjects With Local Advanced or Metastatic Urothelial Cancer
Primary Endpoint	The primary safety endpoints include incidence rates of adverse events (AEs) and serious adverse events (SAEs), monitored continuously throughout the study period of up to 24 months.
Other Endpoint	The key efficacy assessments consist of Objective Response Rate (ORR), Duration of Response (DOR), Time to Response (TTR), Disease Control Rate (DCR), Progression-Free Survival (PFS), and Overall Survival (OS), all evaluated over a 24-month timeframe; additional PK parameters (9MW2821 concentration) and immunogenicity (ADA) data will be collected for up to 12 months.    Click to Show/Hide
Experiment 7 Reporting the Activity Date of This ADC					[292]
Patients Enrolled	Eligible subjects (18-75 years, ECOG 0-1) must have locally advanced/metastatic urothelial cancer (platinum/PD- (L)1-refractory), measurable disease (RECIST 1.1), and adequate organ function. Exclusions: recent anticancer therapies (21 days), prior nectin-4/MMAE-ADC treatment, major surgery (28 days), Grade ≥2 toxicity/neuropathy, uncontrolled comorbidities (CNS metastases, HbA1c ≥8%, cardiac/cerebrovascular disease within 6 months), strong CYP3A4 modifiers (14 days), active infections, or conditions posing safety risks. Contraception is mandatory during and post-study (6 months).    Click to Show/Hide
Administration Dosage	1.25mg/kg of 9MW2821 by intravenous infusion on days 1, 8 and 15 of every 28-day cycle
Related Clinical Trial
NCT Number	NCT06196736	Phase Status	PHASE3
Clinical Description	An Open-label, Randomized Phase 3 Study to Evaluate 9MW2821 vs Investigator's Choice of Chemotherapy in Subjects With Locally Advanced or Metastatic Urothelial Cancer Who Have Previously Received PD- (L)1 Inhibitor and Platinum-containing Chemotherapy
Primary Endpoint	Primary efficacy endpoints include Progression-Free Survival (PFS) and Overall Survival (OS), assessed via Blinded Independent Central Review (BICR) over 3 years, measuring time from randomization to disease progression or death (PFS) and time until death from any cause (OS).
Other Endpoint	Secondary endpoints evaluated over 3 years encompass Objective Response Rate (ORR), Duration of Response (DOR), Time to Response (TTR), Disease Control Rate (DCR) per BICR/investigator, plus investigator-assessed PFS, alongside safety metrics (AE/ADA incidence) and quality-of-life measures (EORTC QLQ-C30, EQ-5D-5L VAS changes from baseline).
Experiment 8 Reporting the Activity Date of This ADC					[293]
Patients Enrolled	Eligible participants (≥18 years) must have high-risk NMIBC (non-muscle invasive, BCG/gemcitabine-refractory) post-TURBT (within 6 weeks), ECOG 0-1, and adequate organ function. Exclusions: prior muscle-invasive/metastatic disease, recent anticancer therapies (3 weeks), unresolved toxicity (>Grade 1), active infections, cardiovascular events (6 months), Nectin-4/MMAE-ADC exposure, or positive HBV/HCV/HIV serology. Contraception is mandatory during and for 180 days post-treatment.    Click to Show/Hide
Related Clinical Trial
NCT Number	NCT06551233	Phase Status	PHASE1
Clinical Description	A Clinical Study on the Safety and Efficacy of 9MW2821 in Patients With High-risk Non-muscle-invasive Bladder Cancer (NMIBC) That Have Previously Failed to Intravesical Therapy
Primary Endpoint	The study will evaluate safety and tolerability over 12 months by assessing AE/SAE incidence while determining the Recommended Phase 2 Dose (RP2D) and Maximum Tolerated Dose (MTD) to establish safe dosing parameters.
Other Endpoint	Efficacy assessments include 12-month Disease-Free Survival (DFS) rate, Duration of Complete Response (DoR), CR rates at 3/6/12 months, long-term DFS (up to 20 months), time to/proportion of radical cystectomy, and biomarker analysis (Nectin-4 expression).
Experiment 9 Reporting the Activity Date of This ADC					[294]
Patients Enrolled	Eligible participants (18-80 years, ECOG 0-1) must have untreated locally advanced/metastatic urothelial cancer (RECIST v1.1-measurable, cisplatin/carboplatin-suitable), adequate organ function, and accessible tumor tissue. Exclusions: prior malignancies (3 years), autoimmune/cardiovascular conditions (6 months), recent therapies (surgery/radiotherapy/CYP3A4 modulators), Grade ≥2 residual toxicity (excluding alopecia), active infections, Nectin-4/MMAE-ADC or checkpoint inhibitor exposure, uncontrolled CNS metastases, HBV/HCV/HIV coinfection, drug allergies, or high-risk ocular/neurological conditions. Contraception and protocol compliance are mandatory.    Click to Show/Hide
Administration Dosage	9MW2821, 1.25mg/kg, intravenous (IV) infusion
Related Clinical Trial
NCT Number	NCT06592326	Phase Status	PHASE3
Clinical Description	A Randomized, Controlled, Open-label, Multicenter Phase 3 Clinical Study of 9MW2821 in Combination With Toripalimab Versus Standard Chemotherapy in First-line Locally Advanced or Metastatic Urothelial Cancer
Primary Endpoint	The primary endpoints include Blinded Independent Central Review-assessed Progression-Free Survival (BICR-PFS) and Overall Survival (OS), both evaluated over a 50-month timeframe.
Other Endpoint	Secondary outcomes comprise Objective Response Rate (ORR), Disease Control Rate (DCR), Duration of Response (DoR), investigator-assessed PFS, safety metrics (AE/SAE), and immunogenicity (Anti-Drug Antibodies against 9MW2821), all monitored for up to 50 months.
Experiment 10 Reporting the Activity Date of This ADC					[295]
Patients Enrolled	Eligible patients (18-80 years, ECOG 0-1) must have untreated, histologically confirmed inoperable locally advanced/metastatic urothelial carcinoma (>50% urothelial differentiation) with ≥1 measurable lesion (RECIST v1.1). Key exclusions: other malignancies (3 years), active autoimmune disease requiring immunosuppressants, recent major cardiovascular/thromboembolic events (6 months), prior PD-1/PD-L1/CTLA-4/Nectin-4/MMAE-ADC therapy, uncontrolled infections, untreated CNS metastases, positive HBV/HCV/HIV serology, or drug allergies. Contraception and protocol adherence are mandatory.    Click to Show/Hide
Related Clinical Trial
NCT Number	NCT06823427	Phase Status	PHASE2
Clinical Description	A Randomized Phase II Trial to Evaluate 9MW2821 in Combination With Toripalimab Compared With 9MW2821 Monotherapy for the 1st Line Treatment of Locally Advanced or Metastatic Urothelial Carcinoma
Primary Endpoint	The primary endpoint is Objective Response Rate (ORR) assessed by Blinded Independent Central Review (BICR) over a 3-year period.
Other Endpoint	Secondary efficacy assessments include Overall Survival (OS), Progression-Free Survival (PFS), Duration of Response (DoR), Disease Control Rate (DCR), and ORR (investigator- and BICR-assessed). Safety monitoring covers treatment-emergent and -related adverse events (CTCAE v5.0), serious adverse events, and vital/lab abnormalities. Immunogenicity analysis measures ADA/NAb incidence, rates, and titers over 3 years.    Click to Show/Hide

Experiment 1 Reporting the Activity Date of This ADC					[283]
Patients Enrolled	Eligible patients had advanced/metastatic PTK7-positive solid tumors (e.g., ovarian, NSCLC, TNBC) with measurable disease, ECOG 0-1, and no prior anti-PTK7 therapy or uncontrolled comorbidities; exclusions included recent ADC progression, active CNS metastases, or infections.
Administration Dosage	PRO1107 monotherapy in escalating doses in Part A and at the two recommended phase 2 doses in Part B
Related Clinical Trial
NCT Number	NCT06171789	Phase Status	PHASE1|||PHASE2
Clinical Description	A Phase 1/2 Study of PRO1107 in Patients With Advanced Solid Tumors
Primary Endpoint	The study assessed adverse events, lab abnormalities, and dose-limiting toxicities over 1 year, including type, incidence, severity, and relatedness.
Other Endpoint	Key efficacy outcomes included ORR, DCR, PFS, and duration of response per RECIST v1.1, alongside pharmacokinetic parameters (AUC, Cmax, Tmax, t1/2, Ctrough) for PRO1107 over 1 year.

Experiment 1 Reporting the Activity Date of This ADC					[284]
Patients Enrolled	Key eligibility: Adults (≥18) with advanced/metastatic solid tumors (ECOG ≤1, measurable disease per RECIST 1.1). Major exclusions: active/unstable CNS metastases, recent major surgery (6 weeks), cardiovascular events (6 months), grade ≥2 neuropathy, live vaccinations (4 weeks), or hypersensitivity to JK06 components. Requires archival tumor samples and acceptable organ function (ANC ≥1,500/uL, platelets ≥100,000, bilirubin ≤1.5×ULN).    Click to Show/Hide
Administration Dosage	Escalating repeated doses of JK06 administered intravenously. A cycle of treatment is defined as 21 days.
Related Clinical Trial
NCT Number	NCT06667960	Phase Status	PHASE1|||PHASE2
Clinical Description	A Phase 1/2, Multicenter, Open Label, Dose Escalation & Dose Expansion Study of JK06, a 5T4 Antibody Drug Conjugate, in Patients with Unresectable Locally Advanced or Metastatic Cancer
Primary Endpoint	Primary objectives assess safety through DLT incidence (first 21 days), MTD/RP2D determination (up to 14 months), and treatment-emergent AE/SAE monitoring (treatment period through 28 days post-last dose) in advanced solid tumor patients receiving JK06.
Other Endpoint	Secondary endpoints evaluate PK parameters (Cmax, AUC), immunogenicity (ADA levels), and efficacy measures (ORR/DCR by RECIST v1.1, PFS) through 104 weeks of treatment follow-up.

Experiment 1 Reporting the Activity Date of This ADC					[285]
Patients Enrolled	Key eligibility: Inclusion requires nectin-4+ advanced/metastatic solid tumors with ≥1 prior therapy failure; Exclusion criteria cover active CNS metastases, grade≥2 neuropathy, uncontrolled diabetes (HbA1c≥8%), ocular/liver/pulmonary diseases, and significant comorbidities.
Administration Dosage	CRB-701 Dose level 1, intravenous infusion over 30 mins, Dose schedule 1
Related Clinical Trial
NCT Number	NCT06265727	Phase Status	PHASE1|||PHASE2
Clinical Description	A Phase 1/2 Study to Investigate the Safety, Pharmacokinetics, and Efficacy of CRB-701, an Antibody-drug Conjugate Targeting Nectin-4, in Patients with Advanced Solid Tumors
Primary Endpoint	Primary endpoints include MTD/PADR determination via DLT assessment in Part A (21-day window) and efficacy evaluation through DCR (CR+PR+SD≥4 months) and ORR (CR+PR per RECIST 1.1) in Parts B&C (6-month follow-up).
Other Endpoint	Secondary objectives cover safety profiling (TEAEs by CTCAE v5.0) across all phases and PK analysis (9-week duration) of CRB-701 components including total ADC/free MMAE/total antibody parameters (Cmax/Tmax/AUC) for single/multiple dosing.

Experiment 1 Reporting the Activity Date of This ADC					[287]
Patients Enrolled	Eligible patients (ECOG 0-1) must have advanced solid tumors refractory to standard therapy (Phase 1: all types; Phase 2: selected indications). Prior TROP2-directed therapy is allowed. Key requirements: measurable disease (RECIST 1.1/RANO-BM), archival/pretreatment biopsy, and adequate organ function (ANC ≥1.5×109/L, platelets ≥100×109/L, Hb ≥9 g/dL, AST/ALT ≤2.5×ULN). Exclusions: active/progressing CNS metastases (unless stable for ≥1 month post-treatment without steroids >4 mg dexamethasone), unresolved Grade >1 toxicities (except alopecia/vitiligo), recent systemic therapy (within 4 weeks/5 half-lives), or high-dose steroids (>10 mg prednisone/day).    Click to Show/Hide
Related Clinical Trial
NCT Number	NCT05941507	Phase Status	PHASE1|||PHASE2
Clinical Description	A Phase 1/2 Study to Evaluate the Safety, Tolerability, and Efficacy of TROP2-Directed Antibody-Drug Conjugate LCB84, as a Single Agent and in Combination With an Anti-PD-1 Ab, in Patients With Advanced Solid Tumors
Primary Endpoint	The study assesses the safety of LCB84 monotherapy and combination therapy with anti-PD-1 antibodies over 48 months by monitoring AEs/SAEs. The recommended Phase 2 dose is determined within 24 months based on tolerability, PK data, and preliminary anti-tumor activity. Efficacy endpoints-ORR, clinical benefit rate (CBR), DOR, TTP, PFS, and OS-are evaluated over 24 months via RECIST 1.1, iRECIST, and RANO-BM criteria.    Click to Show/Hide
Other Endpoint	PK analysis measures LCB84 plasma concentrations over 48 months, while immunogenicity is assessed via ADA detection. Phase 1 also evaluates anti-tumor activity (ORR, DOR, TTP, PFS) per RECIST 1.1, iRECIST, and RANO-BM within 24 months.

Experiment 1 Reporting the Activity Date of This ADC					[306]
Patients Enrolled	Advanced solid tumors that had been previously treated with standard-of-care therapy and their physicians had determined that such therapy was no longer effective, or patients had declined to receive further standard-of-care treatments.
Administration Dosage	The starting dose of 0.40 mg/kg on day 1 of each 21-day cycle; A standard 3 + 3 dose-escalation design was used, and doses of 0.80, 1.20, and 1.60 mg/kg were also administered on day 1 of each 21-day cycle; intravenous infusion over 60 minutes.
Related Clinical Trial
NCT Number	NCT04084366	Phase Status	Phase 1
Clinical Description	A phase 1/2, open-label, dose-escalation and cohort-expansion study evaluating the safety, pharmacokinetics, and therapeutic activity of OBI-999 in patients with advanced solid tumors.
Primary Endpoint	The incidence of dose-limiting toxicities and adverse events and determination of the maximum tolerated dose (MTD)/recommended phase II dose.
Experiment 2 Reporting the Activity Date of This ADC					[315]
Patients Enrolled	Inclusion criteria require patients aged ≥18 with advanced solid tumors (refractory to/intolerant of standard therapy), measurable disease (RECIST 1.1), ECOG 0-1, adequate organ function (ALT/AST ≤3×ULN [≤5×ULN if liver mets], bilirubin ≤1.5×ULN, ANC ≥1,500/uL, platelets ≥100,000/uL), and Globo H H-score ≥100 (Cohort-Expansion). HIV/HBV/HCV-infected patients are eligible if controlled. Exclusions include recent chemotherapy/radiation (<3 weeks), major surgery (<28 days), Grade ≥2 neuropathy, prior Globo H-targeted therapy, uncontrolled CNS metastases, cardiac dysfunction, or concurrent prohibited medications.    Click to Show/Hide
Administration Dosage	Part A: Five cohorts at escalating dose levels 0.4, 0.8, 1.2, 1.6 and 2.0 mg/kg (capping calculations at a maximum at 100 kg) of OBI-999 liquid form via IV infusion to establish maximum tolerated dose (MTD) and Recommended phase 2 dose (RP2D).Part B: Five cohorts of patients at RP2D of OBI-999 liquid form, as determined from Part A, via IV infusion.    Click to Show/Hide
Related Clinical Trial
NCT Number	NCT04084366	Phase Status	PHASE1|||PHASE2
Clinical Description	A Phase 1/2, Open-Label, Dose-Escalation and Cohort-Expansion Study Evaluating the Safety, Pharmacokinetics, and Therapeutic Activity of OBI-999 in Patients with Advanced Solid Tumors
Primary Endpoint	The primary objective is to assess the clinical benefit of OBI-999 through Objective Response Rate (ORR: CR+PR) per RECIST 1.1, evaluated every 6 weeks (±7 days) during initial 3 months, then every 9 weeks (±7 days) until treatment discontinuation, progression, death, or new therapy initiation-whichever occurs first within ~2 years (up to 35 cycles).    Click to Show/Hide
Other Endpoint	Key secondary endpoints include preliminary efficacy (ORR, Clinical Benefit Rate [CBR], Duration of Response [DOR], PFS per RECIST 1.1) and immunogenicity (anti-drug antibodies [ADAs]), analyzed from Week 1 to Week 106. Pharmacokinetics (PK) of OBI-999 and its active metabolite (MMAE) will be assessed via non-compartmental methods during Cycles 1-2, measuring Cmax, AUC, t1/2, clearance (Cl), Tmax, and volume of distribution (Vd).    Click to Show/Hide

Experiment 1 Reporting the Activity Date of This ADC					[311]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 34%	Positive Globo H expression (Globo H+++/++)
Method Description	Mice were treated with an intravenous dose of the ADCs at 0.3 mg/kg, qw*6.
In Vivo Model	MCF-7 CDX model
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 2 Reporting the Activity Date of This ADC					[311]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 60%	Positive Globo H expression (Globo H+++/++)
Method Description	Mice were treated with an intravenous dose of the ADCs at 1 mg/kg, qw*6.
In Vivo Model	MCF-7 CDX model
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 3 Reporting the Activity Date of This ADC					[311]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 83%	Positive Globo H expression (Globo H+++/++)
Method Description	Mice were treated with an intravenous dose of the ADCs at 1 mg/kg, qw*4.
In Vivo Model	NCI-N87 CDX model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 4 Reporting the Activity Date of This ADC					[311]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 85%	Positive Globo H expression (Globo H+++/++)
Method Description	Mice were treated with an intravenous dose of the ADCs at 10 mg/kg, qw*4.
In Vivo Model	NCI-H526 CDX model
In Vitro Model	Lung small cell carcinoma	NCI-H526 cells		CVCL_1569
Experiment 5 Reporting the Activity Date of This ADC					[311]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 95%	Positive Globo H expression (Globo H+++/++)
Method Description	Mice were treated with an intravenous dose of the ADCs at 10 mg/kg, qw*2.
In Vivo Model	MCF-7 CDX model
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 6 Reporting the Activity Date of This ADC					[311]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 97%	Positive Globo H expression (Globo H+++/++)
Method Description	Mice were treated with an intravenous dose of the ADCs at 10 mg/kg, qw*4.
In Vivo Model	NCI-N87 CDX model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 7 Reporting the Activity Date of This ADC					[311]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 97%	Positive Globo H expression (Globo H+++/++)
Method Description	Mice were treated with an intravenous dose of the ADCs at 1-3 mg/kg, qw*4.
In Vivo Model	NCI-N87 CDX model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 8 Reporting the Activity Date of This ADC					[311]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 98%	Positive Globo H expression (Globo H+++/++)
Method Description	Mice were treated with an intravenous dose of the ADCs at 3 mg/kg, qw*6.
In Vivo Model	MCF-7 CDX model
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 9 Reporting the Activity Date of This ADC					[311]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 99%	Positive Globo H expression (Globo H+++/++)
Method Description	Mice were treated with an intravenous dose of the ADCs at 10 mg/kg, qw*4.
In Vivo Model	HPAC CDX model
In Vitro Model	Pancreatic adenocarcinoma	HPAC cells		CVCL_3517

Experiment 1 Reporting the Activity Date of This ADC					[312]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 70.70%
Method Description	In vivo , In each animal study,the antitumor efficacy was evaluated with doses of 1.00, 3.00, or 10.00 mg/kg of OBI-999 via i.v. injection. In NCI-N87 xenograft model,treatment groups of MMAE 0.191 mg/kg and Ctrl-ADC 3 mg/kg were also included. Each study utilized 6 to 8 mice per group.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062
	Breast adenocarcinoma	HCC1428 cells		CVCL_1252

Experiment 1 Reporting the Activity Date of This ADC					[307]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 0%	Positive AXL expression (AXL+++/++)
In Vivo Model	Non-small cell lung cancer PDX model (PDX: LXFE772; EGFR mutation)
Experiment 2 Reporting the Activity Date of This ADC					[307]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 6%	Positive AXL expression (AXL+++/++)
Method Description	Antitumor activity of EnaV in Nonresponder.
In Vivo Model	NSCLC PDX model
Experiment 3 Reporting the Activity Date of This ADC					[308]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 13.30%	Positive AXL expression (AXL+++/++)
Method Description	The antitumor activity of ADCT-601 was tested in a range of human solid tumor xenograft models covering multiple indications. Single-dose (0.30 mg/kg,q.d.). Enapotamab vedotin and isotype-control ADC (B12-PL1601) were administered intravenously (day 1) to treatment groups of 8 mice.
In Vivo Model	Pancreatic cancer PDX model (PDX: PAXF1657)
Experiment 4 Reporting the Activity Date of This ADC					[307]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 16.50%	Positive AXL expression (AXL+++/++)
In Vivo Model	Non-small cell lung cancer PDX model (PDX: LU0858; EGFR L858R mutation)
Experiment 5 Reporting the Activity Date of This ADC					[307]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 16.50%	Positive AXL expression (AXL+++/++)
In Vivo Model	Non-small cell lung cancer PDX model (PDX: LU2511; EGFR mutation)
Experiment 6 Reporting the Activity Date of This ADC					[307]
Efficacy Data	Tumor Growth Inhibition value (TGI)	29.60%	Positive AXL expression (AXL+++/++)
Method Description	EnaV=2 mg/kg.
In Vivo Model	Non-small cell lung cancer PDX model (PDX: LU0395)
Experiment 7 Reporting the Activity Date of This ADC					[307]
Efficacy Data	Tumor Growth Inhibition value (TGI)	46.90%	Positive AXL expression (AXL+++/++)
Method Description	EnaV=4 mg/kg.
In Vivo Model	Non-small cell lung cancer PDX model (PDX: LU0395)
Experiment 8 Reporting the Activity Date of This ADC					[307]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 50%	Positive AXL expression (AXL+++/++)
In Vivo Model	Non-small cell lung cancer PDX model (PDX: LCx-MR007; Osimertinib resistant)
Experiment 9 Reporting the Activity Date of This ADC					[307]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 50%	Positive AXL expression (AXL+++/++)
In Vivo Model	Non-small cell lung cancer PDX model (PDX: LU1868; EGFR L858R and T790Mmutations)
Experiment 10 Reporting the Activity Date of This ADC					[307]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 50%	Positive AXL expression (AXL+++/++)
In Vivo Model	Non-small cell lung cancer PDX model (PDX: LXFA677; EGFR mutation)
Experiment 11 Reporting the Activity Date of This ADC					[307]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 56.40%	Positive AXL expression (AXL+++/++)
Method Description	Antitumor activity of EnaV in intermediate.
In Vivo Model	NSCLC PDX model
Experiment 12 Reporting the Activity Date of This ADC					[307]
Efficacy Data	Tumor Growth Inhibition value (TGI)	60%	Moderate AXL expression (AXL++; IHC H-score=121)
Method Description	EnaV=4 mg/kg.
In Vivo Model	Non-small cell lung cancer PDX model (PDX: LU2511)
Experiment 13 Reporting the Activity Date of This ADC					[307]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 66.50%	Moderate AXL expression (AXL++; IHC H-score=101)
In Vivo Model	Non-small cell lung cancer PDX model (PDX: LXFA526)
Experiment 14 Reporting the Activity Date of This ADC					[307]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 67%	High AXL expression (AXL+++; IHC H-score=248)
In Vivo Model	Non-small cell lung cancer PDX model (PDX: LU0395; EGFR mutation)
Experiment 15 Reporting the Activity Date of This ADC					[309]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 72.70%	Moderate AXL expression (AXL++; IHC H-score=142)
Method Description	The in vivo activity of Enapotamab vedotin was evaluated in additional cell line-derived and patient-derived xenograft (PDX) models representing different cancer types, including pancreas ,esophageal, lung, thyroid, ovarian, cervical cancer, melanoma and sarcoma. Enapotamab vedotin was administered at a dose of 2 mg/kg once a week for two weeks.
In Vivo Model	Non-small cell lung cancer PDX model (PDX: LXFA526)
Experiment 16 Reporting the Activity Date of This ADC					[309]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 84.10%	Moderate AXL expression (AXL++; IHC H-score=141)
Method Description	The anti-tumor activity of ADCs were determined in the pancreas cancer patient-derived xenograft (PDX) model PAXF1657. Before treatment,mice were divided into groups of 68 mice each,with equal tumor size distribution (average and variance). ADC is administered at a dose of 2.00 mg/kg in a single dose.
In Vivo Model	Pancreatic cancer PDX model (PDX: PAXF1657)
Experiment 17 Reporting the Activity Date of This ADC					[309]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 94.80%	Moderate AXL expression (AXL++; IHC H-score=183)
Method Description	The in vivo activity of Enapotamab vedotin was evaluated in additional cell line-derived and patient-derived xenograft (PDX) models representing different cancer types, including pancreas, esophageal, lung, thyroid, ovarian, cervical cancer, melanoma and sarcoma. Enapotamab vedotin was administered at a dose of 2 mg/kg once a week for two weeks.
In Vivo Model	Cervical cancer PDX model (PDX: CV1664)
Experiment 18 Reporting the Activity Date of This ADC					[309]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 97.40%	Moderate AXL expression (AXL++; IHC H-score=104)
Method Description	The in vivo activity of Enapotamab vedotin was evaluated in additional cell line-derived and patient-derived xenograft (PDX) models representing different cancer types, including pancreas, esophageal, lung, thyroid, ovarian, cervical cancer, melanoma and sarcoma. Enapotamab vedotin was administered at a dose of 4 mg/kg once a week for two weeks.
In Vivo Model	Cervical cancer PDX model (PDX: CV1664)
Experiment 19 Reporting the Activity Date of This ADC					[309]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 98.30%	Negative AXL expression (AXL-; IHC H-score=0)
Method Description	The anti-tumor activity of ADCs were determined in the pancreas cancer patient-derived xenograft (PDX) model PAXF1657. Before treatment,mice were divided into groups of 68 mice each,with equal tumor size distribution (average and variance). ADC is administered at a dose of 4.00 mg/kg in a single dose.
In Vivo Model	Pancreatic cancer PDX model (PDX: PAXF1657)
Experiment 20 Reporting the Activity Date of This ADC					[308]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 99.30%	High AXL expression (AXL+++; IHC H-score=305)
Method Description	The antitumor activity of ADCT-601 was tested in a range of human solid tumor xenograft models covering multiple indications. Single-dose (4 mg/kg,q.d.). Enapotamab vedotin and isotype-control ADC (B12-PL1601) were administered intravenously (day 1) to treatment groups of 8 mice.
In Vivo Model	Pancreatic cancer PDX model (PDX: PAXF1657)
Experiment 21 Reporting the Activity Date of This ADC					[309]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 99.80%	Moderate AXL expression (AXL++; IHC H-score=117)
Method Description	The in vivo activity of Enapotamab vedotin was evaluated in additional cell line-derived and patient-derived xenograft (PDX) models representing different cancer types, including pancreas, esophageal, lung, thyroid, ovarian, cervical cancer, melanoma and sarcoma. Enapotamab vedotin was administered at a dose of 4 mg/kg once a week for two weeks.
In Vivo Model	Non-small cell lung cancer PDX model (PDX: LXFA526)
Experiment 22 Reporting the Activity Date of This ADC					[307]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100%	Positive AXL expression (AXL+++/++)
In Vivo Model	Non-small cell lung cancer PDX model (PDX: LXFA677_R, EGFRi resistant)
Experiment 23 Reporting the Activity Date of This ADC					[307]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100%	Positive AXL expression (AXL+++/++)
Method Description	Antitumor activity of EnaV in responder.
In Vivo Model	NSCLC PDX model
Experiment 24 Reporting the Activity Date of This ADC					[309]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	70.55 ng/mL	Moderate AXL expression (AXL++; 22,304 AXL receptor copy number)
Method Description	All cell lines except melanoma were seeded at 1 x103 cells per well in 96 well culture plates (Greiner) and incubated for 3 h at 37°C, 5% CO2.
In Vivo Model	Melanoma PDX model (PDX: M019R.X1.CL)
In Vitro Model	Melanoma	M019R.X1.CL cells		Homo sapiens

Experiment 1 Reporting the Activity Date of This ADC					[310]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 1%	Positive AXL expression (AXL+++/++)
Method Description	Treated with MART-1 T cells.
In Vivo Model	SkMel-147 cell line xenograft model
In Vitro Model	Melanoma	SK-MEL-147 cells		CVCL_3876
Experiment 2 Reporting the Activity Date of This ADC					[310]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 17.70%	Positive AXL expression (AXL+++/++)
Method Description	Treated with MART-1 T cells + Ctrl ADC.
In Vivo Model	SkMel-147 cell line xenograft model
In Vitro Model	Melanoma	SK-MEL-147 cells		CVCL_3876
Experiment 3 Reporting the Activity Date of This ADC					[307]
Efficacy Data	Tumor Growth Inhibition value (TGI)	34.30%	Positive AXL expression (AXL+++/++)
Method Description	EnaV=2 mg/kg.
In Vivo Model	LU2511 in NSCLC CDX model
Experiment 4 Reporting the Activity Date of This ADC					[307]
Efficacy Data	Tumor Growth Inhibition value (TGI)	40.90%	Positive AXL expression (AXL+++/++)
Method Description	EnaV=0.5 mg/kg.
In Vivo Model	LCLC-103H in NSCLC CDX model
In Vitro Model	Lung large cell carcinoma	LCLC-103H cells		CVCL_1375
Experiment 5 Reporting the Activity Date of This ADC					[310]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 43.40%	Positive AXL expression (AXL+++/++)
Method Description	Treated with MART-1 T cells.
In Vivo Model	LCLC-103H xenograft model
In Vitro Model	Lung large cell carcinoma	LCLC-103H cells		CVCL_1375
Experiment 6 Reporting the Activity Date of This ADC					[310]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 64%	Positive AXL expression (AXL+++/++)
Method Description	Treated with Ctrl T cells + EnaV.
In Vivo Model	SkMel-147 cell line xenograft model
In Vitro Model	Melanoma	SK-MEL-147 cells		CVCL_3876
Experiment 7 Reporting the Activity Date of This ADC					[310]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 64.70%	Positive AXL expression (AXL+++/++)
Method Description	Treated with MART-1 T cells.
In Vivo Model	BLM cell line xenograft model
In Vitro Model	Amelanotic melanoma	BLM cells		CVCL_7035
Experiment 8 Reporting the Activity Date of This ADC					[307]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 66.50%	Positive AXL expression (AXL+++/++)
In Vivo Model	LCLC-103H CDX model
In Vitro Model	Lung large cell carcinoma	LCLC-103H cells		CVCL_1375
Experiment 9 Reporting the Activity Date of This ADC					[309]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 78.50%	Positive AXL expression (AXL+++/++)
Method Description	The in vivo activity of Enapotamab vedotin was evaluated in additional cell line-derived and patient-derived xenograft (PDX) models representing different cancer types, including pancreas, esophageal, lung, thyroid, ovarian, cervical cancer, melanoma and sarcoma. Enapotamab vedotin was administered at a dose of 2 mg/kg once a week for two weeks.
In Vivo Model	Melanoma CDX model
In Vitro Model	Melanoma	SK-MEL-147 cells		CVCL_3876
Experiment 10 Reporting the Activity Date of This ADC					[310]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 85.20%	Positive AXL expression (AXL+++/++)
Method Description	Treated with MART-1 T cells + EnaV.
In Vivo Model	SkMel-147 cell line xenograft model
In Vitro Model	Melanoma	SK-MEL-147 cells		CVCL_3876
Experiment 11 Reporting the Activity Date of This ADC					[309]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 92.70%	Positive AXL expression (AXL+++/++)
Method Description	In the LCLC-103H xenograft model,therapeutic treatment with a single dose of 1 mg/kg in anti-tumor activity in the AXL-ADC panel.
In Vivo Model	Lung cancer CDX model
In Vitro Model	Lung large cell carcinoma	LCLC-103H cells		CVCL_1375
Experiment 12 Reporting the Activity Date of This ADC					[309]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 93.60%	Positive AXL expression (AXL+++/++)
Method Description	The in vivo activity of Enapotamab vedotin was evaluated in additional cell line-derived and patient-derived xenograft (PDX) models representing different cancer types, including pancreas, esophageal, lung, thyroid, ovarian, cervical cancer, melanoma and sarcoma. Enapotamab vedotin was administered at a dose of 4 mg/kg once a week for two weeks.
In Vivo Model	Melanoma CDX model
In Vitro Model	Melanoma	SK-MEL-147 cells		CVCL_3876
Experiment 13 Reporting the Activity Date of This ADC					[307]
Efficacy Data	Tumor Growth Inhibition value (TGI)	96.80%	Positive AXL expression (AXL+++/++)
Method Description	EnaV=1 mg/kg.
In Vivo Model	LCLC-103H in NSCLC CDX model
In Vitro Model	Lung large cell carcinoma	LCLC-103H cells		CVCL_1375

Experiment 1 Reporting the Activity Date of This ADC					[313]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.08 nM	High AXL expression (AXL+++)
Method Description	Tumor cells were plated in 96-well plates at predetermined density, treated with AXL02-MMAE or hIgG1-MMAE for 5-8 days to ensure that the doubling of the cells is sufficient. Then MTS reagent solution was added with replacing fresh medium, and cells were incubated for an appropriate time.
In Vitro Model	Lung large cell carcinoma	LCLC-103H cells		CVCL_1375
Experiment 2 Reporting the Activity Date of This ADC					[313]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.09 nM	Moderate AXL expression (AXL++)
Method Description	Tumor cells were plated in 96-well plates at predetermined density, treated with AXL02-MMAE or hIgG1-MMAE for 5-8 days to ensure that the doubling of the cells is sufficient. Then MTS reagent solution was added with replacing fresh medium, and cells were incubated for an appropriate time.
In Vitro Model	Lung adenocarcinoma	PC-9 cells		CVCL_B260
Experiment 3 Reporting the Activity Date of This ADC					[313]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.09 nM	High AXL expression (AXL+++)
Method Description	Tumor cells were plated in 96-well plates at predetermined density, treated with AXL02-MMAE or hIgG1-MMAE for 5-8 days to ensure that the doubling of the cells is sufficient. Then MTS reagent solution was added with replacing fresh medium, and cells were incubated for an appropriate time.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062
Experiment 4 Reporting the Activity Date of This ADC					[313]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.17 nM	High AXL expression (AXL+++)
Method Description	Tumor cells were plated in 96-well plates at predetermined density, treated with AXL02-MMAE or hIgG1-MMAE for 5-8 days to ensure that the doubling of the cells is sufficient. Then MTS reagent solution was added with replacing fresh medium, and cells were incubated for an appropriate time.
In Vitro Model	Lung squamous cell carcinoma	Calu-1 cells		CVCL_0608
Experiment 5 Reporting the Activity Date of This ADC					[313]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 100 nM	Low AXL expression (AXL+)
Method Description	Tumor cells were plated in 96-well plates at predetermined density, treated with AXL02-MMAE or hIgG1-MMAE for 5-8 days to ensure that the doubling of the cells is sufficient. Then MTS reagent solution was added with replacing fresh medium, and cells were incubated for an appropriate time.
In Vitro Model	Breast adenocarcinoma	MDA-MB-453 cells		CVCL_0418
Experiment 6 Reporting the Activity Date of This ADC					[313]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 100 nM	Low AXL expression (AXL+)
Method Description	Tumor cells were plated in 96-well plates at predetermined density, treated with AXL02-MMAE or hIgG1-MMAE for 5-8 days to ensure that the doubling of the cells is sufficient. Then MTS reagent solution was added with replacing fresh medium, and cells were incubated for an appropriate time.
In Vitro Model	Lung large cell carcinoma	NCI-H460 cells		CVCL_0459
Experiment 7 Reporting the Activity Date of This ADC					[309]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	5.5 ng/mL	Moderate AXL expression (AXL++; 37,235 AXL receptor copy number)
Method Description	All cell lines except melanoma were seeded at 1 x103 cells per well in 96 well culture plates (Greiner) and incubated for 3 h at 37°C, 5% CO2.
In Vitro Model	Melanoma	A-875 cells		CVCL_4733
Experiment 8 Reporting the Activity Date of This ADC					[309]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	15.34 ng/mL	Moderate AXL expression (AXL++; 54,946 AXL receptor copy number)
Method Description	All cell lines except melanoma were seeded at 1 x103 cells per well in 96 well culture plates (Greiner) and incubated for 3 h at 37°C, 5% CO2.
In Vitro Model	Cutaneous melanoma	SK-MEL-28 cells (BRAF inhibitor resistant)		CVCL_0526
Experiment 9 Reporting the Activity Date of This ADC					[309]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	20.7 ng/mL	High AXL expression (AXL+++; 117,665 AXL receptor copy number)
Method Description	All cell lines except melanoma were seeded at 1 x103 cells per well in 96 well culture plates (Greiner) and incubated for 3 h at 37°C, 5% CO2.
In Vitro Model	Lung large cell carcinoma	LCLC-103H cells		CVCL_1375
Experiment 10 Reporting the Activity Date of This ADC					[309]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	24.3 ng/mL	Moderate AXL expression (AXL++; 46,701 AXL receptor copy number)
Method Description	All cell lines except melanoma were seeded at 1 x103 cells per well in 96 well culture plates (Greiner) and incubated for 3 h at 37°C, 5% CO2.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062
Experiment 11 Reporting the Activity Date of This ADC					[309]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	42.06 ng/mL	Moderate AXL expression (AXL++; 35,452 AXL receptor copy number)
Method Description	All cell lines except melanoma were seeded at 1 x103 cells per well in 96 well culture plates (Greiner) and incubated for 3 h at 37°C, 5% CO2.
In Vitro Model	Melanoma	SK-MEL-147 cells		CVCL_3876
Experiment 12 Reporting the Activity Date of This ADC					[309]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	68.54 ng/mL	High AXL expression (AXL+++; 169,192 AXL receptor copy number)
Method Description	All cell lines except melanoma were seeded at 1 x103 cells per well in 96 well culture plates (Greiner) and incubated for 3 h at 37°C, 5% CO2.
In Vitro Model	Lung squamous cell carcinoma	Calu-1 cells		CVCL_0608
Experiment 13 Reporting the Activity Date of This ADC					[309]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	189.3 ng/mL	Moderate AXL expression (AXL++; 70,222 AXL receptor copy number)
Method Description	All cell lines except melanoma were seeded at 1 x103 cells per well in 96 well culture plates (Greiner) and incubated for 3 h at 37°C, 5% CO2.
In Vitro Model	Melanoma	SK-MEL-2 cells (MEK inhibitor-resistant)		CVCL_0069
Experiment 14 Reporting the Activity Date of This ADC					[309]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	190.9 ng/mL	Moderate AXL expression (AXL++; 83,986 AXL receptor copy number)
Method Description	All cell lines except melanoma were seeded at 1 x103 cells per well in 96 well culture plates (Greiner) and incubated for 3 h at 37°C, 5% CO2.
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037
Experiment 15 Reporting the Activity Date of This ADC					[309]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	370.4 ng/mL	Moderate AXL expression (AXL++; 16,611 AXL receptor copy number)
Method Description	All cell lines except melanoma were seeded at 1 x103 cells per well in 96 well culture plates (Greiner) and incubated for 3 h at 37°C, 5% CO2.
In Vitro Model	Amelanotic melanoma	A375/R cells		CVCL_IW10
Experiment 16 Reporting the Activity Date of This ADC					[309]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	887.2 ng/mL	Moderate AXL expression (AXL++; 16,611 AXL receptor copy number)
Method Description	All cell lines except melanoma were seeded at 1 x103 cells per well in 96 well culture plates (Greiner) and incubated for 3 h at 37°C, 5% CO2.
In Vivo Model	Melanoma PDX model (PDX: M016.X1.CL)
In Vitro Model	Cutaneous melanoma	SK-MEL-5 cells		CVCL_0527
Experiment 17 Reporting the Activity Date of This ADC					[309]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1828.3 ng/mL	Moderate AXL expression (AXL++; 66,691 AXL receptor copy number)
Method Description	All cell lines except melanoma were seeded at 1 x103 cells per well in 96 well culture plates (Greiner) and incubated for 3 h at 37°C, 5% CO2.
In Vitro Model	Lung large cell carcinoma	NCI-H1299 cells		CVCL_0060
Experiment 18 Reporting the Activity Date of This ADC					[309]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	2090.3 ng/mL	Moderate AXL expression (AXL++; 34,978 AXL receptor copy number)
Method Description	All cell lines except melanoma were seeded at 1 x103 cells per well in 96 well culture plates (Greiner) and incubated for 3 h at 37°C, 5% CO2.
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 19 Reporting the Activity Date of This ADC					[309]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	2895.7 ng/mL	Moderate AXL expression (AXL++; 28,000 AXL receptor copy number)
Method Description	All cell lines except melanoma were seeded at 1 x103 cells per well in 96 well culture plates (Greiner) and incubated for 3 h at 37°C, 5% CO2.
In Vitro Model	Pancreatic ductal adenocarcinoma	BxPC-3 cells		CVCL_0186
Experiment 20 Reporting the Activity Date of This ADC					[309]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	6881 ng/mL	Low AXL expression (AXL+; 9,138 AXL receptor copy number)
Method Description	All cell lines except melanoma were seeded at 1 x103 cells per well in 96 well culture plates (Greiner) and incubated for 3 h at 37°C, 5% CO2.
In Vitro Model	Lung large cell carcinoma	NCI-H661 cells		CVCL_1577
Experiment 21 Reporting the Activity Date of This ADC					[309]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 10 ug/mL	Negative AXL expression (AXL-; 100 AXL receptor copy number)
Method Description	All cell lines except melanoma were seeded at 1 x103 cells per well in 96 well culture plates (Greiner) and incubated for 3 h at 37°C, 5% CO2.
In Vitro Model	Melanoma	SK-MEL-2 cells		CVCL_0069
Experiment 22 Reporting the Activity Date of This ADC					[309]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 10 ug/mL	Negative AXL expression (AXL-; 325 AXL receptor copy number)
Method Description	All cell lines except melanoma were seeded at 1 x103 cells per well in 96 well culture plates (Greiner) and incubated for 3 h at 37°C, 5% CO2.
In Vitro Model	Cutaneous melanoma	SK-MEL-28 cells		CVCL_0526
Experiment 23 Reporting the Activity Date of This ADC					[309]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 10 ug/mL	Negative AXL expression (AXL-; 250 AXL receptor copy number)
Method Description	All cell lines except melanoma were seeded at 1 x103 cells per well in 96 well culture plates (Greiner) and incubated for 3 h at 37°C, 5% CO2.
In Vitro Model	Cutaneous melanoma	SK-MEL-5 cells		CVCL_0527
Experiment 24 Reporting the Activity Date of This ADC					[309]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 10 ug/mL	Negative AXL expression (AXL-; 150 AXL receptor copy number)
Method Description	All cell lines except melanoma were seeded at 1 x103 cells per well in 96 well culture plates (Greiner) and incubated for 3 h at 37°C, 5% CO2.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 25 Reporting the Activity Date of This ADC					[309]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 10 ug/mL	Low AXL expression (AXL+; 2,326 AXL receptor copy number)
Method Description	All cell lines except melanoma were seeded at 1 x103 cells per well in 96 well culture plates (Greiner) and incubated for 3 h at 37°C, 5% CO2.
In Vitro Model	Pancreatic ductal adenocarcinoma	HPAF-II cells		CVCL_0313
Experiment 26 Reporting the Activity Date of This ADC					[309]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 10 ug/mL	Moderate AXL expression (AXL++; 37,506 AXL receptor copy number)
Method Description	All cell lines except melanoma were seeded at 1 x103 cells per well in 96 well culture plates (Greiner) and incubated for 3 h at 37°C, 5% CO2.
In Vitro Model	Pleural epithelioid mesothelioma	NCI-H226 cells		CVCL_1544
Experiment 27 Reporting the Activity Date of This ADC					[309]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 10 ug/mL	Negative AXL expression (AXL-; 528 AXL receptor copy number)
Method Description	All cell lines except melanoma were seeded at 1 x103 cells per well in 96 well culture plates (Greiner) and incubated for 3 h at 37°C, 5% CO2.
In Vitro Model	Colon adenocarcinoma	LS174T cells		CVCL_1384
Experiment 28 Reporting the Activity Date of This ADC					[313]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.2 .	Moderate AXL expression (AXL++)
Method Description	Tumor cells were plated in 96-well plates at predetermined density, treated with AXL02-MMAE or hIgG1-MMAE for 5-8 days to ensure that the doubling of the cells is sufficient. Then MTS reagent solution was added with replacing fresh medium, and cells were incubated for an appropriate time.
In Vitro Model	Glioblastoma	U-87MG cells		CVCL_0022

Experiment 1 Reporting the Activity Date of This ADC					[314]
Efficacy Data	Objective Response Rate (ORR)	19%
Patients Enrolled	Eligible participants must have advanced/metastatic solid tumors refractory to standard therapy, measurable disease, and adequate organ function (ECOG 0-1). Exclusions cover uncontrolled cardiac disease, recent thrombosis, active infections, prior auristatin therapy, major surgery within 4 weeks, pregnancy, and significant comorbidities (e.g., Grade 2+ neuropathy, pneumonitis).    Click to Show/Hide
Administration Dosage	Participants in all cohorts of the trial (both in escalation and expansion phase) will be administered enapotamab vedotin (HuMax-AXL-ADC) intravenously (IV).
Related Clinical Trial
NCT Number	NCT02988817	Phase Status	PHASE1|||PHASE2
Clinical Description	First-in-human, Open-label, Dose-escalation Trial With Expansion Cohorts to Evaluate Safety of Axl-specific Antibody-drug Conjugate (Enapotamab Vedotin, HuMax®-AXL-ADC) in Patients With Solid Tumors
Primary Endpoint	Safety measures include dose-limiting toxicities (DLTs) during Cycle 1 (Grade 4 hematologic events, severe non-hematologic AEs, and infusion reactions) and treatment-emergent adverse events (TEAEs), including serious events (TESAEs), ≥Grade 3 toxicities per NCI-CTCAE v4.03, and lab abnormalities, monitored up to 1130 days post-dose.
Other Endpoint	Pharmacokinetic analysis evaluates conjugated enapotamab vedotin and free MMAE parameters (AUC0-inf, AUC0-last, Cmax, CL, Tmax, t1/2, Vss) across dosing regimens (1Q3W, 3Q4W). Secondary outcomes include ADA development and efficacy metrics (OR per RECIST v1.1, CA-125 response, DoR, PFS, OS, AXL expression changes) in solid tumor patients.
Experiment 2 Reporting the Activity Date of This ADC					[314]
Efficacy Data	Disease control rate (DCR)	50%
Patients Enrolled	Eligible participants must have advanced/metastatic solid tumors refractory to standard therapy, measurable disease, and adequate organ function (ECOG 0-1). Exclusions cover uncontrolled cardiac disease, recent thrombosis, active infections, prior auristatin therapy, major surgery within 4 weeks, pregnancy, and significant comorbidities (e.g., Grade 2+ neuropathy, pneumonitis).    Click to Show/Hide
Administration Dosage	Participants in all cohorts of the trial (both in escalation and expansion phase) will be administered enapotamab vedotin (HuMax-AXL-ADC) intravenously (IV).
Related Clinical Trial
NCT Number	NCT02988817	Phase Status	PHASE1|||PHASE2
Clinical Description	First-in-human, Open-label, Dose-escalation Trial With Expansion Cohorts to Evaluate Safety of Axl-specific Antibody-drug Conjugate (Enapotamab Vedotin, HuMax®-AXL-ADC) in Patients With Solid Tumors
Primary Endpoint	Safety measures include dose-limiting toxicities (DLTs) during Cycle 1 (Grade 4 hematologic events, severe non-hematologic AEs, and infusion reactions) and treatment-emergent adverse events (TEAEs), including serious events (TESAEs), ≥Grade 3 toxicities per NCI-CTCAE v4.03, and lab abnormalities, monitored up to 1130 days post-dose.
Other Endpoint	Pharmacokinetic analysis evaluates conjugated enapotamab vedotin and free MMAE parameters (AUC0-inf, AUC0-last, Cmax, CL, Tmax, t1/2, Vss) across dosing regimens (1Q3W, 3Q4W). Secondary outcomes include ADA development and efficacy metrics (OR per RECIST v1.1, CA-125 response, DoR, PFS, OS, AXL expression changes) in solid tumor patients.

Experiment 1 Reporting the Activity Date of This ADC					[316]
Efficacy Data	Objective Response Rate (ORR)	42.20 52.90 26.30 60.00 66.70 0.00 42.90 33.30 43.80 50.00 %
Patients Enrolled	CD20-positive B-cell non Hodgkin lymphoma (NHL) and had failed 2 prior lines of standard treatment.
Administration Dosage	Seven dose cohorts (0.10, 0.50, 1.00, 1.50, 1.80, 2.10, 2.30 mg/kg iv d1,q21d).
Related Clinical Trial
NCT Number	NCT05395533	Phase Status	Phase 1
Clinical Description	A multicenter, single-arm, dose-escalating study to evaluate the safety, tolerability, pharmacokinetics and effectiveness of TRS005 in patients with relapsed or refractory CD20-positive B-NHL.
Experiment 2 Reporting the Activity Date of This ADC					[323]
Efficacy Data	Objective Response Rate (ORR)	56.70%
Patients Enrolled	Eligible participants are adults (≥18) with relapsed/refractory CD20+ B-cell NHL (≥2 prior therapies), measurable lesions (≥1.5cm), and adequate organ function. Exclusions include active HBV/HCV/HIV, uncontrolled cardiovascular/autoimmune diseases, recent rituximab/CAR-T therapy, or CNS involvement. Contraception and lab criteria (ANC ≥1.5×109/L, PLT ≥100×109/L, etc.) are mandatory.    Click to Show/Hide
Administration Dosage	The dose of the enrolled subjects was increased according to the following 7 dose groups: 0.1mg/kg, 0.5mg/kg, 1.0mg/kg, 1.5mg/kg, 1.8mg/kg, and 2.1mg/kg. (according to the data of the previous study, when the dose climbs to 1.5 mg / kg, there is a serious decline of neutrophils, which shall be subject to the principle of 3 + 3.
Related Clinical Trial
NCT Number	NCT05395533	Phase Status	PHASE1
Clinical Description	A Multicenter, Single-arm, Dose-escalating Study to Evaluate the Safety, Tolerability, Pharmacokinetics and Effectiveness of TRS005 in Patients With Relapsed or Refractory CD20-positive B-NHL
Primary Endpoint	The study evaluates dose-limiting toxicities (DLTs) including grade 4 neutropenia unresponsive to G-CSF, grade 4 thrombocytopenia, and grade ≥2 neurotoxicity. The maximum tolerated dose (MTD) will be determined as the highest dose with ≤33% DLT incidence.
Other Endpoint	Immunogenicity (anti-drug antibody/neutralizing antibody), pharmacokinetics (Cmax, AUC0-t, AUC0-∞, Tmax), and efficacy (ORR per CR/PR) will be tracked across treatment cycles (21-day intervals). PK parameters are derived from plasma concentration-time curves.
Experiment 3 Reporting the Activity Date of This ADC					[323]
Efficacy Data	Disease control rate (DCR)	86.70%
Patients Enrolled	Eligible participants are adults (≥18) with relapsed/refractory CD20+ B-cell NHL (≥2 prior therapies), measurable lesions (≥1.5cm), and adequate organ function. Exclusions include active HBV/HCV/HIV, uncontrolled cardiovascular/autoimmune diseases, recent rituximab/CAR-T therapy, or CNS involvement. Contraception and lab criteria (ANC ≥1.5×109/L, PLT ≥100×109/L, etc.) are mandatory.    Click to Show/Hide
Administration Dosage	The dose of the enrolled subjects was increased according to the following 7 dose groups: 0.1mg/kg, 0.5mg/kg, 1.0mg/kg, 1.5mg/kg, 1.8mg/kg, and 2.1mg/kg. (according to the data of the previous study, when the dose climbs to 1.5 mg / kg, there is a serious decline of neutrophils, which shall be subject to the principle of 3 + 3.
Related Clinical Trial
NCT Number	NCT05395533	Phase Status	PHASE1
Clinical Description	A Multicenter, Single-arm, Dose-escalating Study to Evaluate the Safety, Tolerability, Pharmacokinetics and Effectiveness of TRS005 in Patients With Relapsed or Refractory CD20-positive B-NHL
Primary Endpoint	The study evaluates dose-limiting toxicities (DLTs) including grade 4 neutropenia unresponsive to G-CSF, grade 4 thrombocytopenia, and grade ≥2 neurotoxicity. The maximum tolerated dose (MTD) will be determined as the highest dose with ≤33% DLT incidence.
Other Endpoint	Immunogenicity (anti-drug antibody/neutralizing antibody), pharmacokinetics (Cmax, AUC0-t, AUC0-∞, Tmax), and efficacy (ORR per CR/PR) will be tracked across treatment cycles (21-day intervals). PK parameters are derived from plasma concentration-time curves.

Experiment 1 Reporting the Activity Date of This ADC					[317]
Related Clinical Trial
NCT Number	NCT05652868	Phase Status	Phase 1
Clinical Description	A phase 1 multicenter dose escalation and dose expansion study of antibody-drug conjugate MYTX-011 in subjects with non-small cell lung cancer - kismet-01.
Experiment 2 Reporting the Activity Date of This ADC					[330]
Patients Enrolled	Inclusion: NSCLC patients (Part 1: advanced/metastatic; Part 2: stratified by cMET expression/EGFR status) with ≥1 measurable lesion, ECOG 0-1, prior SOC therapy. Exclusion: Recent radiation/surgery (6w/28d), active CNS metastases, interstitial lung disease, Grade>1 neuropathy, hepatic/corneal disorders, or uncontrolled infections. Contraception required for 6 months post-treatment.    Click to Show/Hide
Administration Dosage	MYTX-011 will be administered as an intravenous infusion every 21 days.
Related Clinical Trial
NCT Number	NCT05652868	Phase Status	PHASE1
Clinical Description	A Phase 1 Multicenter Dose Escalation and Dose Expansion Study of Antibody-Drug Conjugate MYTX-011 in Subjects With Non-Small Cell Lung Cancer - KisMET-01
Primary Endpoint	Primary endpoints include DLT assessment (treatment-related AEs) in Part 1 (21-day evaluation) and tumor response rate (CR+PR) in Part 2 (2-year follow-up).
Other Endpoint	Secondary objectives comprise PK analysis (total ADC/antibody/free MMAE), ADA detection, ORR/DOR/TTR/DCR assessment, and survival outcomes (PFS/OS) with 24-month monitoring in Part 1.

Experiment 1 Reporting the Activity Date of This ADC					[318]
Related Clinical Trial
NCT Number	NCT05718895	Phase Status	Phase 1
Clinical Description	An open, multi-center, phase 1 clinical study of ATG 022 in patients with advanced/metastatic solid tumors.
Experiment 2 Reporting the Activity Date of This ADC					[322]
Efficacy Data	Objective Response Rate (ORR)	41.70%
Patients Enrolled	Eligible participants were adults with advanced solid tumors (Claudin 18.2+ in expansion phase), measurable disease per RECIST 1.1, adequate organ function, and willingness for tumor biopsy. Exclusions included CNS involvement, prior Claudin 18.2 therapy, active infections, recent anticancer treatments, transplants, or other conditions compromising protocol adherence.    Click to Show/Hide
Administration Dosage	A treatment cycle of ATG-022 will be defined as 21 days. Dosing will begin at 0.3 mg/kg once every 3 weeks (Q3W) with 1 subject ,the following dose cohorts (0.9, 1.8, 2.4, 3.0, and 3.6 mg/kg Q3W) will require at least 3 and up to 6 evaluable subjects by using dose escalation plan of "3+3" design.
Related Clinical Trial
NCT Number	NCT05718895	Phase Status	PHASE1
Clinical Description	An Open, Multi-center, Phase I Clinical Study of ATG 022 in Patients With Advanced/Metastatic Solid Tumors
Primary Endpoint	The study assessed dose-limiting toxicities (DLTs), maximum tolerated dose (MTD), and recommended Phase 2 dose (RP2D) during the initial 21-day period in dose escalation cohorts.
Other Endpoint	Efficacy outcomes included progression-free survival (PFS), overall response rate (ORR), and duration of response (DOR), all evaluated 12 months post-enrollment of the last subject across study cohorts.
Experiment 3 Reporting the Activity Date of This ADC					[322]
Efficacy Data	Disease control rate (DCR)	100%
Patients Enrolled	Eligible participants were adults with advanced solid tumors (Claudin 18.2+ in expansion phase), measurable disease per RECIST 1.1, adequate organ function, and willingness for tumor biopsy. Exclusions included CNS involvement, prior Claudin 18.2 therapy, active infections, recent anticancer treatments, transplants, or other conditions compromising protocol adherence.    Click to Show/Hide
Administration Dosage	A treatment cycle of ATG-022 will be defined as 21 days. Dosing will begin at 0.3 mg/kg once every 3 weeks (Q3W) with 1 subject ,the following dose cohorts (0.9, 1.8, 2.4, 3.0, and 3.6 mg/kg Q3W) will require at least 3 and up to 6 evaluable subjects by using dose escalation plan of "3+3" design.
Related Clinical Trial
NCT Number	NCT05718895	Phase Status	PHASE1
Clinical Description	An Open, Multi-center, Phase I Clinical Study of ATG 022 in Patients With Advanced/Metastatic Solid Tumors
Primary Endpoint	The study assessed dose-limiting toxicities (DLTs), maximum tolerated dose (MTD), and recommended Phase 2 dose (RP2D) during the initial 21-day period in dose escalation cohorts.
Other Endpoint	Efficacy outcomes included progression-free survival (PFS), overall response rate (ORR), and duration of response (DOR), all evaluated 12 months post-enrollment of the last subject across study cohorts.

Experiment 1 Reporting the Activity Date of This ADC					[319]
Patients Enrolled	Locally advanced unresectable or metastatic solid tumors.
Related Clinical Trial
NCT Number	NCT05194072	Phase Status	Phase 1
Clinical Description	A phase 1 study of SGN-B7H4V in advanced solid tumors.
Experiment 2 Reporting the Activity Date of This ADC					[332]
Patients Enrolled	Eligible participants have locally advanced/metastatic solid tumors (ovarian, breast, lung, etc.), ECOG 0-1, measurable disease (RECIST v1.1), and tumor tissue for analysis. Key exclusions: recent malignancies (≤3 years), active brain metastases (unless stable ≥4 weeks post-treatment), prior MMAE/B7-H4 therapy, Grade ≥2 neuropathy, or active corneal disease.    Click to Show/Hide
Related Clinical Trial
NCT Number	NCT05194072	Phase Status	PHASE1
Clinical Description	A Phase 1 Study of SGN-B7H4V in Advanced Solid Tumors
Primary Endpoint	Safety will be assessed through AE monitoring up to 5 years post-treatment, including laboratory abnormalities and DLTs (within 28 days of dosing), with overall safety evaluated across dose levels.
Other Endpoint	Efficacy endpoints include confirmed ORR, CRR, DOR, PFS, and iDFS tracked up to 5 years per RECIST v1.1. PK parameters (AUC, Cmax, Tmax, t1/2, Ctrough) and ADA incidence will be analyzed descriptively over 3 years post-treatment.

Experiment 1 Reporting the Activity Date of This ADC					[320]
Related Clinical Trial
NCT Number	NCT05103683	Phase Status	Phase 1
Clinical Description	A phase 1, first in human, dose-escalation study of TORL-1-23 in participants with advanced cancer.
Experiment 2 Reporting the Activity Date of This ADC					[321]
Efficacy Data	Partial Response (PR)	33.30%
Patients Enrolled	Inclusion: Adults with advanced solid tumors (RECIST 1.1-measurable), ECOG 0-1, adequate organ function. Exclusion: Unresolved toxicities (>Grade 1), recent anticancer therapy (14-28 days prior), active brain metastases, uncontrolled comorbidities (cardiac/infectious), MDS/AML history, concurrent malignancies (except non-melanoma skin/indolent cancers), pregnancy/breastfeeding, or clinically significant conditions per investigator judgment.    Click to Show/Hide
Administration Dosage	19 patients with platinum-resistant/refractory ovarian cancer were evaluated across 8 dose levels (0.2 to 2.4 mg/kg IV every 3 weeks, 21 day cycles) (data cutoff 01APR2023).
Related Clinical Trial
NCT Number	NCT05103683	Phase Status	PHASE1
Clinical Description	A Phase 1, First in Human, Dose-Escalation Study of TORL-1-23 in Participants with Advanced Cancer
Primary Endpoint	The primary safety endpoints include incidence/severity of adverse events (AEs) and serious AEs per NCI-CTCAE v5.0 (monitored for 2 years), as well as determination of Maximum Tolerated Dose (MTD) (<33% DLT rate in first 28 days) and Recommended Phase 2 Dose (RP2D) based on accumulated safety/PK data over 2 years.
Other Endpoint	Key efficacy measures are Objective Response Rate (ORR; CR+PR per RECIST 1.1), Duration of Response (DOR), Progression-Free Survival (PFS), Time to Response (TTR), and 1-/2-Year Overall Survival rates (1YOS/2YOS). Immunogenicity (ADA-positive participants) and 12 detailed pharmacokinetic parameters (Cmax, Cmin, t1/2, AUCinf, etc.) are assessed over 21-63 days with multiple serum concentration metrics.    Click to Show/Hide
Experiment 3 Reporting the Activity Date of This ADC					[334]
Patients Enrolled	Inclusion criteria: Women ≥18 with CLDN6-positive (per central assay), histologically confirmed advanced/metastatic high-grade serous/endometrioid ovarian, primary peritoneal, or fallopian tube cancer; platinum-resistant (progression ≤6 months post-platinum); 1-3 prior lines; measurable disease; ECOG 0-1; adequate organ function. Exclusions: Platinum-refractory disease (progression ≤3 months post-first-line platinum), prior CLDN6/MMAE-ADC therapy, active brain metastases/leptomeningeal disease, Grade≥2 neuropathy, uncontrolled infections/cardiopulmonary conditions, strong CYP3A4/P-gp modifiers use, or concurrent malignancies within 3 years. CNS mets require prior stabilization.    Click to Show/Hide
Administration Dosage	2.4, 3.0, 3.4 mg/kg intravenous infusion on Day 1 of every 3-week cycle.
Related Clinical Trial
NCT Number	NCT06690775	Phase Status	PHASE2
Clinical Description	Catalina-2: a Phase 2 Study Evaluating the Efficacy and Safety of TORL-1-23 in Women with Advanced Platinum-Resistant Epithelial Ovarian Cancer (Including Primary Peritoneal and Fallopian Tube Cancers) Expressing Claudin 6
Primary Endpoint	The primary efficacy endpoint is Objective Response Rate (ORR) per RECIST v1.1, assessed by Blinded Independent Central Review (BICR), in women with advanced platinum-resistant ovarian cancer (PROC) expressing CLDN6, evaluated over approximately 40 months with periodic assessments from first dose until disease progression.
Other Endpoint	Secondary efficacy measures include Duration of Response (DOR), ORR by investigator assessment, Progression-Free Survival (PFS), Overall Survival (OS) (tracked over ~40 months), CA-125 response per GCIG criteria, and safety/tolerability profiles (AE incidence/severity per CTCAE v5.0 monitored until 30 days post-treatment). PK/PD effects are also evaluated.    Click to Show/Hide

Experiment 1 Reporting the Activity Date of This ADC					[324]
Patients Enrolled	Eligible participants (18-75 years) must have HER2-expressing/amplified/mutated advanced solid tumors (breast/urothelial/gastric/ovarian/endometrial/colorectal/NSCLC), ECOG 0-1, measurable/evaluable lesions, adequate organ function (hematologic/hepatic/renal), and reproductive safeguards (contraception for 6 months post-treatment), with HER2 status confirmed by IHC/ISH/NGS in archival/current biopsy samples.    Click to Show/Hide
Administration Dosage	1a: The program evaluated six dose levels, i.e., 0.1, 0.3, 0.6, 1.2, 1.8, 2.4 mg/kg, An accelerated titration was performed in the 0.1 and 0.3 mg/kg dose groups, and then a Bayesian optimal interval design was used to determine MTDS for four subsequent dose levels. Ib: The antitumor activity of KM501 monotherapy in subjects with specific types of tumors that are HER2-positive or express, amplify, or mutate will be evaluated at the RP2D dose level    Click to Show/Hide
Related Clinical Trial
NCT Number	NCT05804864	Phase Status	PHASE1
Clinical Description	A Single-arm, Open, Multicenter Phase I Study to Evaluate the Safety, Tolerability, Pharmacokinetic Profile, and Efficacy of the KM501 Double-antibody ADC in Subjects With Advanced Solid Tumors That Express, Amplify, or Mutate HER2
Primary Endpoint	The study evaluates MTD/RP2D determination and treatment-related AEs (CTCAE v5.0) in Part 1a (dose escalation), while Part 1b assesses ORR (investigator-assessed CR/PR per RECIST 1.1) and long-term efficacy outcomes (PFS/DCR/OS) over 2-3 years in HER2-altered solid tumors.
Other Endpoint	Pharmacokinetic analyses (AUC/Cmax/T-HALF) and immunogenicity (ADA) are conducted across both parts, with safety monitoring (AEs) extended through Part 1b, providing comprehensive drug exposure and tolerability data alongside efficacy measures (ORR/PFS/DCR/OS) for up to 3 years.

Experiment 1 Reporting the Activity Date of This ADC					[325]
Patients Enrolled	Key inclusion criteria: age ≥18/21 years (US/Singapore); weight 40-120kg; advanced/metastatic solid tumors refractory to standard therapy; ECOG PS ≤2 (Part A) or 0-1 (Parts B-D); adequate hepatic/renal/bone marrow function per protocol.
Administration Dosage	EBC-129 will be administered on Day 1 of each 21-Day cycle (Parts A, B, and C), and Day 1 of each 21- or 28-Day cycle (Part D) via a 30-120-minute intravenous (IV) fusion.
Related Clinical Trial
NCT Number	NCT05701527	Phase Status	PHASE1
Clinical Description	A Phase 1A/B Study to Evaluate the Safety and Tolerability of EBC-129 As a Single Agent and in Combination with Pembrolizumab in Advanced Solid Tumours
Primary Endpoint	Primary endpoints include SAE/TEAE incidence (pre-screening to EOS), MTD/RP2D determination (Parts A/B/D), and ORR assessment (Parts C/D per RECIST v1.1) over 2 years.
Other Endpoint	Secondary endpoints comprise efficacy measures (DCR, DoR, TTP, PFS, OS), PK parameters (Cmax, Ctrough, AUC, Tmax, t1/2 for EBC-129/pembrolizumab), immunogenicity (ADA/neutralizing antibodies), and tumor response comparisons (Part A) evaluated over 3.3 years.

Experiment 1 Reporting the Activity Date of This ADC					[326]
Patients Enrolled	Key inclusion criteria: age ≥18; ECOG 0-1; adequate organ function; histologically confirmed advanced/metastatic solid tumors (NSCLC, HR+ BC, HNSCC, ESCC, TNBC); protocol compliance capability with signed informed consent.
Administration Dosage	IV administration of XB010
Related Clinical Trial
NCT Number	NCT06545331	Phase Status	PHASE1
Clinical Description	A Dose-Escalation and Expansion Study of XB010 as a Single Agent and Combination Therapy in Subjects With Locally Advanced or Metastatic Solid Tumors
Primary Endpoint	Primary endpoints include MTD/RDE determination (18 months), safety profile (AE/SAE incidence), tolerability (exposure duration/dose intensity), and preliminary antitumor activity (ORR per RECIST 1.1) for XB010 monotherapy and combination therapy.
Other Endpoint	Secondary endpoints comprise PK parameters (Cmax, Tmax, clearance, AUC, Cmin) and immunogenicity (ADA analysis) for both dose-escalation (18 months) and cohort-expansion stages (24 months), along with continued tolerability assessments.

Experiment 1 Reporting the Activity Date of This ADC					[327]
Patients Enrolled	Key eligibility criteria: Patients aged 18-75 with histologically confirmed locally advanced/metastatic solid tumors, ECOG 0-1, measurable lesions, and adequate organ function. Major exclusions: prior CLDN18.2-targeted therapy, severe allergies to JS107 components, recent anticancer treatments (within 4 weeks), uncontrolled infections (HBV/HCV/HIV), symptomatic CNS metastases, or significant cardiopulmonary comorbidities.    Click to Show/Hide
Related Clinical Trial
NCT Number	NCT05657418	Phase Status	PHASE1
Clinical Description	A Phase I Clinical Study Evaluating the Safety, Tolerability, Pharmacokinetics of JS107 in Patients With Advanced Pancreatic Cancer
Primary Endpoint	Primary endpoints focus on determining the maximum tolerated dose (MTD) and recommended Phase 2 dose (RP2D) for JS107 monotherapy and combination therapy, with evaluation timelines up to 12 and 24 months respectively from first patient enrollment.
Other Endpoint	Secondary objectives include pharmacokinetic analysis of drug plasma concentrations, immunogenicity assessment (ADA/Nab incidence and titers), and efficacy evaluation through objective response rate (ORR) per RECIST v1.1 criteria, all monitored over 24 months.
Experiment 2 Reporting the Activity Date of This ADC					[328]
Patients Enrolled	Key eligibility: Adults (18-75) with histologically confirmed advanced/metastatic solid tumors (ECOG 0-1, measurable lesions). Major exclusions: prior CLDN18.2 therapy, severe allergies to JS107 components, recent anticancer treatments (4 weeks), active infections (HBV/HCV/HIV/TB), uncontrolled CNS metastases, significant cardiopulmonary disease, or autoimmune disorders.    Click to Show/Hide
Administration Dosage	JS107, i.v., q3w
Related Clinical Trial
NCT Number	NCT05502393	Phase Status	PHASE1
Clinical Description	A Phase I Clinical Study Evaluating the Safety, Tolerability, Pharmacokinetics of JS107 in Patients With Advanced Solid Tumors
Primary Endpoint	Primary endpoints include MTD determination (12 months) and RP2D establishment (24 months) for JS107 monotherapy/combination therapy in advanced solid tumor patients.
Other Endpoint	Secondary objectives cover PK analysis (drug concentrations), immunogenicity (ADA/Nab incidence/titers), and efficacy (ORR per RECIST v1.1), all monitored over 24 months.

Experiment 1 Reporting the Activity Date of This ADC					[329]
Patients Enrolled	Eligible patients must have histologically confirmed metastatic solid tumors (RECIST 1.1 measurable), ECOG 0-1, and life expectancy ≥12 weeks. Key exclusions include recent anti-cancer therapies (within 2-4 weeks depending on type), active CNS metastases, grade ≥2 neuropathy, uncontrolled infections (HIV/HBV/HCV), pregnancy, or hypersensitivity to BB-1709 components.    Click to Show/Hide
Administration Dosage	BB-1709 will be administered as an intravenous infusion by Q3W or Q2W as long as they continue to show clinical benefit as judged by the investigator, until disease progression or intolerable toxicity, withdrawal of consent, death, or termination of the study.
Related Clinical Trial
NCT Number	NCT06241898	Phase Status	PHASE1
Clinical Description	A Phase I, Open Label, Multicenter, Dose Escalation and Dose Expansion Study to Evaluate the Safety, Tolerability, Pharmacokinetics and Preliminary Antitumor Activity of BB-1709 in Patients With Locally Advanced/Metastatic Solid Tumors
Primary Endpoint	The primary safety evaluation focuses on adverse events (AEs) and serious adverse events (SAEs) occurring within 3 years to assess BB-1709's safety profile.
Other Endpoint	Pharmacokinetic analysis includes area under the serum concentration-time curve (AUC0-inf) measured during Cycles 1-8 (21-day cycles) to characterize BB-1709's exposure.

Experiment 1 Reporting the Activity Date of This ADC					[331]
Patients Enrolled	Eligible subjects (≥18 years, ECOG 0-1) must have advanced c-Kit+ tumors (GIST, SCLC, ACC, uveal melanoma, NET ChRCC/ccRCC) refractory to standard therapies, including imatinib for GIST. Required washout periods: 21 days (chemotherapy), 14 days (targeted therapy), 28 days (immunotherapy). Exclusions include active brain metastases, uncontrolled infections, significant cardiovascular disease, recent major surgery, COVID-19 infection, or pregnancy. Adequate organ function and contraception (120 days post-treatment) are mandatory.    Click to Show/Hide
Related Clinical Trial
NCT Number	NCT06805825	Phase Status	PHASE1
Clinical Description	A Phase 1 Dose Escalation and Expansion Study of the C-Kit Specific Antibody-Drug Conjugate NN3201 in Subjects with Advanced And/or Metastatic Solid Tumors Known to Express C-Kit
Primary Endpoint	The study evaluates safety by assessing dose-limiting toxicities (DLTs) within 3 weeks post-treatment, defined as clinically relevant AEs per NCI CTCAE v5.0 that are attributed to NN3201. Adverse event incidence (severity, seriousness, and drug relationship) is monitored over 1 year.
Other Endpoint	The trial determines optimal doses for expansion cohorts (within 1 year) by analyzing anti-tumor efficacy and acceptable safety profiles. Pharmacokinetic (PK) analysis measures NN3201 serum concentration over 3 years, while RECIST 1.1 assesses anti-tumor activity. Promising doses may advance to future studies based on sustained efficacy and safety (3-year timeframe).    Click to Show/Hide

Experiment 1 Reporting the Activity Date of This ADC					[333]
Patients Enrolled	Inclusion criteria require histologically confirmed metastatic/unresectable solid tumors (Part A: any advanced solid tumors; Part B: specific cancers including melanoma, breast cancer, NSCLC, or pancreatic adenocarcinoma) with progression after standard therapy, ECOG ≤1, measurable disease by RECIST v1.1, and available tumor tissue for biomarker analysis. Exclusions comprise other active malignancies within 5 years (except certain cured cancers), recent anticancer treatments (≤28 days), severe drug hypersensitivity, pregnancy/lactation, or conditions compromising safety/study compliance.    Click to Show/Hide
Related Clinical Trial
NCT Number	NCT06596915	Phase Status	PHASE1
Clinical Description	A Phase I Study to Evaluate the Safety, Tolerability, Pharmacokinetic, and Preliminary Efficacy of BA1302 in Patients With Advanced Solid Malignancies
Primary Endpoint	The primary safety endpoints include the number of participants experiencing dose-limiting toxicities (DLTs) within the first 21 days and adverse events (AEs) recorded through 28 days after the last treatment.
Other Endpoint	Key secondary endpoints focus on pharmacokinetics (AUC0-t, AUC0-inf, Cmax, t1/2, and AUC at steady state) and immunogenicity (ADA incidence), all evaluated over approximately one year. Efficacy measures comprise objective response rate (ORR) and duration of response (DOR) per RECIST v1.1.

Experiment 1 Reporting the Activity Date of This ADC					[335]
Patients Enrolled	Inclusion: Adults (≥18) with advanced/metastatic solid tumors (RECIST 1.1-measurable), ECOG 0-1, life expectancy ≥12 weeks, adequate organ function, willingness for biopsies, and contraception compliance. Exclusion: Prior MMAE-ADC therapy, platinum-refractory disease, active CNS metastases, Grade≥2 neuropathy/corneal disease, uncontrolled infections (HIV/HBV/HCV), recent anticancer therapies (chemotherapy within 2 weeks, antibodies within 4 weeks, radiotherapy within 2-4 weeks), immunosuppression, or significant comorbidities (cardiovascular, interstitial lung disease, bowel obstruction). Pregnancy, breastfeeding, or unresolved toxicities (>Grade 1) also exclude participation.    Click to Show/Hide
Administration Dosage	LNCB74 is an antibody drug conjugate being evaluated as a potential treatment for participants with advanced solid tumors. Participants will receive LNCB74 into the vein (IV; intravenously) in 21-day dosing cycles. Participants will continue treatment in the absence of unacceptable toxicities and unequivocal disease progression.
Related Clinical Trial
NCT Number	NCT06774963	Phase Status	PHASE1
Clinical Description	A Phase 1, Open-label, Dose Escalation and Dose Expansion Study for LNCB74, a B7-H4 Targeted Antibody Drug Conjugate, as Monotherapy in Participants With Advanced Solid Tumors
Primary Endpoint	The study aims to evaluate the safety and tolerability of LNCB74 over 24 months, assessing incidence of AEs, SAEs, DLTs, discontinuations, and deaths per NCI CTCAE v5.0. Additionally, it seeks to determine the RP2D (based on MTD, MAD, and cumulative safety/PK data) and define the maximum tolerated/feasible dose.
Other Endpoint	Efficacy measures include ORR, DOR, DCR, and PFS at 6/24 months (per RECIST 1.1), alongside correlations between B7-H4 expression (via central IHC) and clinical outcomes (ORR, DOR, DCR, PFS). Pharmacokinetics (Tmax, AUC, T1/2, Cmax) are evaluated across multiple cycles (Days 1-15, Cycles 1-9). Immunogenicity (anti-drug antibodies) is monitored for 24 months.    Click to Show/Hide

Experiment 1 Reporting the Activity Date of This ADC					[336]
Patients Enrolled	Eligible adults (≥18 y, ECOG 0-1) must have CDH3-expressing metastatic solid tumors, measurable lesions (RECIST 1.1), ≥3-month life expectancy, and adequate organ function. Exclusions include prior allogeneic transplants, uncontrolled hypertension, active CNS metastases, ocular/cardiac/pulmonary comorbidities, recent immunosuppression or CYP3A4 modulators, or pregnancy. Contraception is mandatory for 6 months post-treatment.    Click to Show/Hide
Related Clinical Trial
NCT Number	NCT06548672	Phase Status	PHASE1
Clinical Description	A Phase Ia/Ib, Open-Label, Dose Escalation and Dose Expansion Study to Evaluate the Safety, Tolerability, Pharmacokinetics (PK), and Preliminary Efficacy of BC3195 in Patients With Locally Advanced or Metastatic Solid Tumors
Primary Endpoint	The study evaluates Dose Limiting Toxicities (DLTs) within the first 21 days of treatment to determine the Maximum Tolerated Dose (MTD) and/or Recommended Phase 2 Dose (RP2D). Incidence and severity of all Adverse Events (AEs) are monitored from screening through 12 weeks post-treatment.
Other Endpoint	Efficacy is assessed via ORR, DCR, DoR, TTP, PFS (per RECIST 1.1), and OS (up to 100 months). Pharmacokinetics (AUC, Cmax, Tmax, t1/2, Vd, CL) are analyzed for BC3195 through 21 days post-last dose, alongside immunogenicity (ADA) monitoring for 30 days.
Experiment 2 Reporting the Activity Date of This ADC					[337]
Patients Enrolled	Eligible participants (≥18 years, ECOG 0-1) must provide informed consent and have metastatic solid tumors refractory to standard therapies with ≥3-month life expectancy. Key exclusions include pregnancy, recent anticancer treatment, uncontrolled hypertension, active infections, cardiovascular disease, or poor compliance potential as judged by investigators. Effective contraception is required for 6 months post-treatment.    Click to Show/Hide
Administration Dosage	BC3195 is administered as 1 hour (h) IV infusion every 3 weeks. An evaluation of seven dose levels (DLs) is planned: 0.3, 0.6, 1.2, 1.8, 2.4, 3.0 and 3.6 mg/kg with a BOIN design guiding dose escalation.
Related Clinical Trial
NCT Number	NCT05957471	Phase Status	PHASE1
Clinical Description	A Phase Ia/Ib, Open-Label, First-in-human, Dose Escalation and Dose Expansion Study to Evaluate the Safety, Tolerability, Pharmacokinetics, and Preliminary Efficacy of BC3195 in Patients With Locally Advanced or Metastatic Solid Tumors
Primary Endpoint	The trial will assess dose limiting toxicities (DLTs) observed during the first treatment cycle (21 days) to evaluate safety parameters.

Experiment 1 Reporting the Activity Date of This ADC					[338]
Patients Enrolled	Eligible patients include adults (≥18 years) with relapsed/refractory ALL, AML, or MPAL (WHO 2016, CD71+ ≥20% blasts), controlled blast count (<20,000/mm 3), adequate organ function, and ECOG 0-2. Exclusions cover APL, prior anti-TfR therapy, recent transplant, CNS disease, uncontrolled cardiac/liver disease, active infection, pregnancy, and major surgery within 4 weeks.    Click to Show/Hide
Administration Dosage	INA03 will be administered IV on Day 1, Day 14 of 28-day cycles. The administration of INA03 will begin at 0.02 mg/kg. Study Part I is a titration study to determine the dose for the first INA03 infusion. Patients will be enrolled in sequential cohorts of 2 patients to receive ascending starting doses of INA03, starting from the lowest starting dose (0.02 mg/kg), and followed by subsequent administrations of INA03 (D14 and beyond) at a fixed dose of 0.1 mg/kg. The starting dose will be increased every cohort of 2 patients until evidence of absence of marrow residual erythroblasts by D14 myelogram. This dose is referred to as the MEID and will be selected as the D1 dose for the study Part 2. Patient accumulation in Part I of the study will continue until no evidence of non-hematological DLT within 28 days post dosing    Click to Show/Hide
Related Clinical Trial
NCT Number	NCT03957915	Phase Status	EARLY_PHASE1
Clinical Description	A Phase I, First in Human, Open-label Study of Escalating Doses of INA03 Administered Intravenously as Single Agent in Adult Patients With Relapse/Refractory Acute Leukemia
Primary Endpoint	The study assesses the minimal erythroblastopenia-inducing dose (MEID) of INA03 in adults with refractory/relapsed acute leukemia within 2 weeks post-dose, defined by erythroblast depletion or Grade ≥2 non-hematologic toxicity, followed by determining the maximum tolerated dose (MTD) for subsequent administrations (Day 15 onwards) over 28 days.
Other Endpoint	Safety is evaluated via NCI-CTCAE v5.0-graded adverse events. Pharmacokinetic analysis includes Cmax, AUC, and half-life (t½) from dosing to Day 42, while pharmacodynamics tracks erythroblast/blast reduction via bone marrow aspirates. Anti-INA03 antibodies are measured, and preliminary efficacy is assessed per ELN 2017 criteria for up to 182 days.    Click to Show/Hide

Experiment 1 Reporting the Activity Date of This ADC					[339]
Patients Enrolled	Eligible patients must have advanced solid tumors (RECIST 1.1 measurable) with ECOG 0-1 and adequate organ function. Exclusions include: unresolved treatment toxicities (>Grade 1); recent anticancer therapy (14-day/28-day washout for small molecules/biologics); active brain metastases; uncontrolled medical conditions/organ dysfunction; significant cardiac disease; MDS/AML history; recent malignancies (except cured skin cancers/low-risk DCIS/prostate cancer); and pregnancy/breastfeeding.    Click to Show/Hide
Related Clinical Trial
NCT Number	NCT06005740	Phase Status	PHASE1
Clinical Description	A Phase 1, First in Human Study of TORL-4-500 in Patients with Advanced Cancer
Primary Endpoint	The safety profile including AE/SAE incidence and severity (graded by NCI-CTCAE v5.0) will be monitored for two years. The study will establish the MTD (highest dose with <33% DLTs among 6 evaluable participants in 28 days) and determine RP2D based on MTD, safety data, and pharmacokinetics.
Other Endpoint	Efficacy measures include ORR (CR+PR per RECIST 1.1), DOR from first response to progression/death, PFS from treatment initiation to progression/death, and TTR over two years. Survival rates (1-/2-year OS) will be tracked. Immunogenicity (ADA positivity) and comprehensive PK parameters (Cmax/Cmin/Tmax/AUC/Vz/CL/Rac) for TORL-4-500 will be assessed at single-dose (21-day) and steady-state (63-day) timepoints.    Click to Show/Hide

Experiment 1 Reporting the Activity Date of This ADC					[340]
Patients Enrolled	Eligible participants require histologically confirmed lymphoid malignancies (Parts A/B: CD30+ ≥1% except cHL/ALCL; Part C: CD30-independent) with specific prior therapy requirements: cHL (≥3 lines, anti-PD-1 exposed), PTCL (≥2 lines), or ALCL (brentuximab-containing regimens). Key exclusions: >2 brentuximab lines, recent malignancies (<3 years), active CNS disease, allogeneic SCT complications (<100 days/GVHD/CMV reactivation), or significant pulmonary conditions (Grade≥2 ILD, steroid-dependent lung disease). ECOG≤1 and measurable FDG-avid disease (per Lugano criteria) are mandatory.    Click to Show/Hide
Related Clinical Trial
NCT Number	NCT06120504	Phase Status	PHASE1
Clinical Description	An Open-label Phase 1 Study to Evaluate the Safety of SGN-35T in Adults With Advanced Malignancies
Primary Endpoint	The safety assessment will track adverse events, laboratory abnormalities, dose modifications, and dose-limiting toxicities (including by dose level) through 30-37 days post-treatment (approximately 1 year). AE reporting will include all medically significant occurrences regardless of causality, with DLT evaluations specifically during the initial 21-day period.    Click to Show/Hide
Other Endpoint	Pharmacokinetic analysis will assess AUC, Cmax, and Tmax through 30-37 days post-treatment (≈1 year), summarized descriptively alongside antidrug antibody incidence. Efficacy endpoints include investigator-assessed ORR (CR+PR), CR rate, and DOR (time from first response to progression/death), all evaluated over ≈1 year using disease-specific criteria.    Click to Show/Hide

Experiment 1 Reporting the Activity Date of This ADC					[341]
Patients Enrolled	Eligible patients must have advanced solid tumors with measurable disease (RECIST v1.1), ECOG 0-1, and adequate organ function. Exclusions include unresolved toxicities (>Grade 1, except alopecia), recent anticancer therapy (14-28 days prior), active brain metastases, uncontrolled comorbidities, cardiac disease, MDS/AML history, concurrent malignancies (except certain low-risk cases), and pregnancy/breastfeeding.    Click to Show/Hide
Related Clinical Trial
NCT Number	NCT05948826	Phase Status	PHASE1
Clinical Description	A Phase 1, First in Human, Dose-Escalation Study of TORL-3-600 in Participants With Advanced Cancer
Primary Endpoint	The study will assess the incidence and severity of adverse events (AEs) and serious adverse events (SAEs) graded by NCI-CTCAE v5.0 over 2 years, while determining Maximum Tolerated Dose (MTD) based on dose-limiting toxicities (DLTs) in the first 6 evaluable participants within 28 days, and Recommended Phase 2 Dose (RP2D) using safety, tolerability, and pharmacokinetic data.    Click to Show/Hide
Other Endpoint	Efficacy endpoints include Objective Response Rate (ORR), Duration of Response (DOR), Progression-Free Survival (PFS), Time to Response (TTR), 1-Year and 2-Year Overall Survival (1YOS, 2YOS), and immunogenicity via anti-drug antibody (ADA) assessment. Pharmacokinetic parameters [Cmax, Cmin, AUC, t1/2, CL, Vz, Rac, etc.] for TORL-3-600 will be evaluated over 21-63 days.    Click to Show/Hide

Experiment 1 Reporting the Activity Date of This ADC					[342]
Efficacy Data	Partial Response (PR)	4%
Patients Enrolled	Metastatic castration-resistant prostate cancer (CRPC).
Administration Dosage	3 + 3 dose escalation study, 0.30 to 2.80 mg/kg intravenously given once every 3 weeks followed by cohort expansion at the recommended phase II dose or weekly (0.80 to 1.00 mg/kg).
Related Clinical Trial
NCT Number	NCT01283373	Phase Status	Phase 1
Clinical Description	A phase 1, open-label study of the safety and pharmacokinetics of escalating doses of DSTP3086S in patients with metastatic castration-resistant prostate cancer.
Primary Endpoint	DsTP3086S has acceptable safety at the recommended phase II dose level of 2.40 mg/kg once every 3 weeks.
Experiment 2 Reporting the Activity Date of This ADC					[354]
Related Clinical Trial
NCT Number	NCT01283373	Phase Status	Phase 1
Clinical Description	A phase 1, open-label study of the safety and pharmacokinetics of escalating doses of DSTP3086S in patients with metastatic castration-resistant prostate cancer.
Experiment 3 Reporting the Activity Date of This ADC					[400]
Patients Enrolled	Eligible patients require metastatic castration-resistant prostate cancer (≤2 prior chemo regimens for expansion cohort), ECOG 0-2, and measurable disease. Key exclusions include recent anticancer therapy (4-week washout), active infections, uncontrolled CNS metastases (>8 weeks post-radiotherapy if treated), corticosteroids >10mg/day prednisone, or prior mAb hypersensitivity.    Click to Show/Hide
Administration Dosage	This study evaluated safety and activity of DSTP3086S (0.3-2.8 mg/kg IV) given every 3 weeks (q3w) to pts with CRPC.
Related Clinical Trial
NCT Number	NCT01283373	Phase Status	PHASE1
Clinical Description	A Phase I, Open-Label Study of the Safety and Pharmacokinetics of Escalating Doses of DSTP3086S in Patients With Metastatic Castration-Resistant Prostate Cancer
Primary Endpoint	Safety will be assessed through DLT monitoring during the first 21-day cycle to determine treatment tolerability.
Other Endpoint	Comprehensive PK analyses including AUC, Cmax/Cmin, clearance, half-life, and volume of distribution will be conducted over a 1-year period to characterize drug exposure and metabolism.

Experiment 1 Reporting the Activity Date of This ADC					[343]
Efficacy Data	Partial Response (PR)	6.20%
Patients Enrolled	Advanced clear cell or papillary renal cell carcinoma (RCC) who experienced progression after at least two lines of systemic therapy, including at least one TKI were included; Additional main inclusion criteria included measurable disease by Response Criteria in Solid Tumors (RECIST) 1.1 criteria, a Karnofsky performance status 70%, and adequate renal, hepatic, and hematological laboratory values.    Click to Show/Hide
Administration Dosage	Intravenously at doses ranging from 0.15 to 2.00 mg/kg every 2 or 3 weeks until progression or unacceptable toxicity.
Related Clinical Trial
NCT Number	NCT02837991	Phase Status	Phase 1
Clinical Description	A phase l open-label, dose escalation and cohort expansion study, to assess the safety and activity of the antibody-drug conjugate CDX-014 in advanced or metastatic renal cell carcinoma (RCC) and advanced or metastatic ovarian clear cell carcinoma (OCCC).
Primary Endpoint	One patient (6.20%) treated at 0.3 mg/kg every 3 weeks exhibited PR as best overall response,ongoing after 17 months on therapy; this patient had been on single agent PD-1 inhibition prior to initiating therapy with CDX-014. Five patients (31.00%) exhibited clinical benefit from CDX-014. PFS and OS were 2.70 months (95%CI 1.2-8.0) and 12.6 months (95%CI 5.7-12.6),respectively.    Click to Show/Hide
Other Endpoint	Partial response (PR) = 6.00% of one patient treated at 0.30 mg/kg every 3 weeks as best overall response, clinical benefit from CDX-014 of five patients = (31.25%) exhibited of at least 6 months. PFS = 2.7 months (95%CI, 1.20-8.00) ,OS =12.6 months (95%CI, 5.70-12.60).
Experiment 2 Reporting the Activity Date of This ADC					[393]
Patients Enrolled	Eligible patients must have advanced/metastatic clear cell/papillary renal cell carcinoma (RCC; ≥2 prior therapies including VEGF-TKI) or clear cell ovarian carcinoma (OCCC; ≥1 platinum-taxane regimen), measurable disease, life expectancy ≥3 months, and available TIM-1-expressing tumor tissue. Key exclusions: prior MMAE therapy, recent cytotoxic/TKI/mAb treatments (within 2-4 weeks), uncontrolled comorbidities, active infections (excluding oral-therapy-controlled cases), untreated brain metastases, significant cardiovascular disease, concurrent malignancies (except cured skin/in situ cancers), and chronic high-dose corticosteroid use (>5mg prednisone/day). Effective contraception is mandatory during and for 6 months post-treatment.    Click to Show/Hide
Administration Dosage	During the treatment phase of the study, patients will receive CDX-014 treatment every 3 weeks (RCC or OCCC) or every 2 weeks (RCC) as long as they remain eligible. Patients may be discontinued from CDX-014 treatment based on the results of disease assessments or if experiencing side effects that make study therapy intolerable.
Related Clinical Trial
NCT Number	NCT02837991	Phase Status	PHASE1
Clinical Description	A Phase l Open-Label, Dose Escalation and Cohort Expansion Study, to Assess the Safety and Activity of the Antibody-Drug Conjugate CDX-014 in Advanced or Metastatic Renal Cell Carcinoma (RCC) and Advanced or Metastatic Ovarian Clear Cell Carcinoma (OCCC)
Primary Endpoint	The dose escalation phase aims to determine the maximum tolerated dose (MTD) and recommended phase II dose (RP2D) of CDX-014, defined as the highest dose with <33% incidence of dose-limiting toxicities (DLTs) within 21 days post-first dose. The expansion cohort will evaluate objective response rate (ORR) per RECIST v1.1, assessed every 6-9 weeks until discontinuation or progression (up to 5 years).    Click to Show/Hide

Experiment 1 Reporting the Activity Date of This ADC					[372]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 20%	Positive TIM1 expression (TIM1+++/++)
Method Description	Anti-TIM-1-vcMMAE (CDX-014=300 g), CDX-014 inhibited the increase in tumor volumes relative to saline control treatment.
In Vivo Model	IGROV-1 xenograft mouse models
In Vitro Model	Ovarian endometrioid adenocarcinoma	IGROV-1 cells		CVCL_1304
Experiment 2 Reporting the Activity Date of This ADC					[372]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 21%	Positive TIM1 expression (TIM1+++/++)
Method Description	Anti-TIM-1-vcMMAE (CDX-014=300 g).
In Vivo Model	A549 xenograft mouse models
In Vitro Model	Lung adenocarcinoma	A-549 cells		CVCL_0023
Experiment 3 Reporting the Activity Date of This ADC					[372]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 22.90%	Positive TIM1 expression (TIM1+++/++)
Method Description	Anti-TIM-1-vcMMAE (CDX-014=300 g).
In Vivo Model	Caki-1 xenograft mouse model
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234
Experiment 4 Reporting the Activity Date of This ADC					[372]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 40.50%	Positive TIM1 expression (TIM1+++/++)
Method Description	Extended dosing of CDX-014 ADC in the A549 tumor model. Three cycles of four doses of CDX-014 prolong the inhibition of tumor growth.
In Vivo Model	A549 xenograft mouse models
In Vitro Model	Lung adenocarcinoma	A-549 cells		CVCL_0023

Experiment 1 Reporting the Activity Date of This ADC					[344]
Efficacy Data	Objective Response Rate (ORR)	2.10 10.80 20.00 20.00 20.00 %
Patients Enrolled	Patients with LRRC15 positive squamous cell carcinoma of the head and neck, NSCKC, breast cancer, undifferentiated pleomorphic sarcoma or osteosarcoma.
Administration Dosage	0.30 up to 6.00 mg/kg on day 1, once every 2 weeks.
Related Clinical Trial
NCT Number	NCT02565758	Phase Status	Phase 1
Clinical Description	A multicenter, phase 1, open-label, dose-escalation study of ABBV-085, an antibody drug conjugate, in subjects with advanced solid tumors.
Experiment 2 Reporting the Activity Date of This ADC					[363]
Related Clinical Trial
NCT Number	NCT02565758	Phase Status	Phase 1
Clinical Description	A multicenter, phase 1, open-label, dose-escalation study of ABBV-085, an antibody drug conjugate, in subjects with advanced solid tumors.
Experiment 3 Reporting the Activity Date of This ADC					[383]
Patients Enrolled	Eligible participants have advanced solid tumors (ECOG 0-2, measurable/evaluable disease per RECIST 1.1 or tumor antigen criteria) and adequate organ function. Exclusions include recent anticancer therapy, uncontrolled CNS metastases, unresolved Grade 2+ toxicities, hemolysis, major surgery within 28 days, or auristatin/IgG hypersensitivity.
Administration Dosage	ABBV-085 administered on at 28 day cycle and enrolling at MD Anderson
Related Clinical Trial
NCT Number	NCT02565758	Phase Status	PHASE1
Clinical Description	A Multicenter, Phase 1, Open-Label, Dose-Escalation Study of ABBV-085, an Antibody Drug Conjugate, in Subjects With Advanced Solid Tumors
Primary Endpoint	The study evaluates ABBV-085's terminal elimination half-life, Cmax, AUC (0-t), and adverse events over 24 months, with continuous monitoring of safety and pharmacokinetics.
Other Endpoint	Key efficacy endpoints include ORR (CR+PR rate), PFS (time to progression/death), and DOR (response duration), all assessed over a 24-month period to determine treatment impact.

Experiment 1 Reporting the Activity Date of This ADC					[366]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 27.90%	Negative LRRC15 (LRRC15-)
Method Description	The efficacy of ABBV-085 directed against LRRC15 was assessed in several patient-derived xenograft models of UPS,LMS,and DDLPS. For efficacy study,tumors were allowed to establish to 200±50 mm3 in size before randomization into various treatment groups with 7-9 mice per group. Isotype-control,isotype-MMAE,and ABBV-085,diluted in PBS were administered at 6 mg/kg once every 4 days intraperitoneally for a total of six injections.    Click to Show/Hide
In Vivo Model	Liposarcoma PDX model (PDX: LPS28)
Experiment 2 Reporting the Activity Date of This ADC					[366]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 34.50%	Negative LRRC15 (LRRC15-)
Method Description	The efficacy of ABBV-085 directed against LRRC15 was assessed in several patient-derived xenograft models of UPS,LMS,and DDLPS. For efficacy study,tumors were allowed to establish to 200±50 mm3 in size before randomization into various treatment groups with 7-9 mice per group. Isotype-control,isotype-MMAE,and ABBV-085,diluted in PBS were administered at 6 mg/kg once every 4 days intraperitoneally for a total of six injections.    Click to Show/Hide
In Vivo Model	Leiomyosarcoma PDX model (PDX: LMS33)
Experiment 3 Reporting the Activity Date of This ADC					[366]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 38.10%	Negative LRRC15 (LRRC15-)
Method Description	The efficacy of ABBV-085 directed against LRRC15 was assessed in several patient-derived xenograft models of UPS,LMS,and DDLPS. For efficacy study,tumors were allowed to establish to 200±50 mm3 in size before randomization into various treatment groups with 7-9 mice per group. Isotype-control,isotype-MMAE,and ABBV-085,diluted in PBS were administered at 6 mg/kg once every 4 days intraperitoneally for a total of six injections.    Click to Show/Hide
In Vivo Model	Liposarcoma PDX model (PDX: LPS28)
Experiment 4 Reporting the Activity Date of This ADC					[366]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 87.20%	High LRRC15 expression (LRRC15+++)
Method Description	The efficacy of ABBV-085 directed against LRRC15 was assessed in several patient-derived xenograft models of UPS,LMS,and DDLPS. For efficacy study,tumors were allowed to establish to 200±50 mm3 in size before randomization into various treatment groups with 7-9 mice per group. Isotype-control,isotype-MMAE,and ABBV-085,diluted in PBS were administered at 6 mg/kg once every 4 days intraperitoneally for a total of six injections.    Click to Show/Hide
In Vivo Model	Liposarcoma PDX model (PDX: LPS28)
Experiment 5 Reporting the Activity Date of This ADC					[366]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 88.70%	High LRRC15 expression (LRRC15+++)
Method Description	The efficacy of ABBV-085 directed against LRRC15 was assessed in several patient-derived xenograft models of UPS,LMS,and DDLPS. For efficacy study,tumors were allowed to establish to 200±50 mm3 in size before randomization into various treatment groups with 7-9 mice per group. Isotype-control,isotype-MMAE,and ABBV-085,diluted in PBS were administered at 6 mg/kg once every 4 days intraperitoneally for a total of six injections.    Click to Show/Hide
In Vivo Model	Leiomyosarcoma PDX model (PDX: LMS33)
Experiment 6 Reporting the Activity Date of This ADC					[366]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 95.20%	High LRRC15 expression (LRRC15+++)
Method Description	The efficacy of ABBV-085 directed against LRRC15 was assessed in several patient-derived xenograft models of UPS,LMS,and DDLPS. For efficacy study,tumors were allowed to establish to 200±50 mm3 in size before randomization into various treatment groups with 7-9 mice per group. Isotype-control,isotype-MMAE,and ABBV-085,diluted in PBS were administered at 6 mg/kg once every 4 days intraperitoneally for a total of six injections.    Click to Show/Hide
In Vivo Model	Leiomyosarcoma and undifferentiated sarcomas PDX model, (PDX: UPS7)
Experiment 7 Reporting the Activity Date of This ADC					[366]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100%	High LRRC15 expression (LRRC15+++)
Method Description	The efficacy of ABBV-085 directed against LRRC15 was assessed in several patient-derived xenograft models of UPS,LMS,and DDLPS. For efficacy study,tumors were allowed to establish to 200±50 mm3 in size before randomization into various treatment groups with 7-9 mice per group. Isotype-control,isotype-MMAE,and ABBV-085,diluted in PBS were administered at 6 mg/kg once every 4 days intraperitoneally for a total of six injections.    Click to Show/Hide
In Vivo Model	Leiomyosarcoma and undifferentiated sarcomas PDX model, (PDX: UPS7)

Experiment 1 Reporting the Activity Date of This ADC					[345]
Efficacy Data	Objective Response Rate (ORR)	10.67%
Patients Enrolled	Relapsed or refractory multiple myeloma (RRMM) and Eastern Cooperative Oncology Group (ECOG) performance status of 0-2; were not eligible for stem cell/bone marrow transplant or had refused stem cell/bone marrow transplant, or had relapsed after autologous or allogeneic stem cell/bone marrow transplant.
Administration Dosage	ABBV-838 (3+3 design) intravenously starting from 0.60 mg/kg up to 6.00 mg/kg for 3-week dosing intervals (Q3W). Patients could continue ABBV-838 for up to 24 months. Assessment of alternate dosing intervals (Q1W and Q2W) was conducted in parallel.
Related Clinical Trial
NCT Number	NCT02462525	Phase Status	Phase 1
Clinical Description	A multicenter, phase 1/1b, open-label, dose-escalation study of ABBV-838, an antibody drug conjugate, in subjects with relapsed and refractory multiple myeloma.
Primary Endpoint	OrR=10.67% (N=8/75, 95% Cl 4.7-19.9), very good partial response (VGPR)=2.67% (N=2), PR=8.00% (N=6). Median DOR=4 months.
Other Endpoint	The MTD was not reached. The selected recommended dose for the expansion cohort was 5.00 mg/kg Q3W.
Experiment 2 Reporting the Activity Date of This ADC					[355]
Related Clinical Trial
NCT Number	NCT02951117	Phase Status	Phase 1
Clinical Description	A phase 1b, open label, multicenter, dose escalation study of venetoclax and ABBV-838 combination therapy with dexamethasone in subjects with relapsed or refractory multiple myeloma.
Experiment 3 Reporting the Activity Date of This ADC					[356]
Related Clinical Trial
NCT Number	NCT02462525	Phase Status	Phase 1
Clinical Description	A multicenter, phase 1/1b, open-label, dose-escalation study of ABBV-838, an antibody drug conjugate, in subjects with relapsed and refractory multiple myeloma.
Experiment 4 Reporting the Activity Date of This ADC					[391]
Patients Enrolled	Eligible participants had relapsed/refractory multiple myeloma (≥3 prior lines including proteasome inhibitors/immunomodulatory drugs) with measurable disease, adequate organ function, and LVEF ≥45% if applicable. Exclusions included recent anticancer therapy (<21 days), solid tumors, unresolved toxicities (≥Grade 2), uncontrolled conditions, active infections, strong CYP3A4 inhibitors, HIV/hepatitis, or prior pomalidomide exposure for combination-arm participants.    Click to Show/Hide
Administration Dosage	Eligible patients (≥18 years) received ABBV-838 (3+3 design) intravenously starting from 0.6 mg/kg up to 6.0 mg/kg for 3-week dosing intervals (Q3W). Patients could continue ABBV-838 for up to 24 months. Assessment of alternate dosing intervals (Q1W and Q2W) was conducted in parallel.
Related Clinical Trial
NCT Number	NCT02462525	Phase Status	PHASE1
Clinical Description	A Multicenter, Phase 1/1b, Open-Label, Dose-Escalation Study of ABBV-838, an Antibody Drug Conjugate, in Subjects With Relapsed and Refractory Multiple Myeloma
Primary Endpoint	Pharmacokinetic evaluation of ABBV-838 included maximum plasma concentration (Cmax, ng/ml) measured at multiple timepoints (Cycles 1-3) and maximum tolerated dose assessment (over ~2 years), with dose-limiting toxicities monitored to determine safety thresholds.
Other Endpoint	Preliminary efficacy of ABBV-838 monotherapy was based on International Myeloma Working Group (IMWG) response criteria, assessed radiologically at screening, Cycle 1 Day 15, and periodically thereafter (~3 years).
Experiment 5 Reporting the Activity Date of This ADC					[392]
Patients Enrolled	Eligible participants had relapsed/refractory multiple myeloma (≥2 prior therapies including IMiD + proteasome inhibitor), measurable disease (serum/urine M-protein or sFLC), and ECOG ≤1 (dose escalation) or ≤2 (expansion). Exclusions included recent anti-myeloma therapy (within 5 half-lives/14 days for non-mAbs; 6 weeks for mAbs), uncontrolled comorbidities, or corticosteroid use (≥4 mg/day dexamethasone within 3 weeks).    Click to Show/Hide
Related Clinical Trial
NCT Number	NCT02951117	Phase Status	PHASE1
Clinical Description	A Phase 1b, Open Label, Multicenter, Dose Escalation Study of Venetoclax and ABBV-838 Combination Therapy With Dexamethasone in Subjects With Relapsed or Refractory Multiple Myeloma
Primary Endpoint	The study aims to determine the maximum tolerated dose (MTD) and recommended phase two dose (RPTD) of venetoclax + ABBV-838 + dexamethasone during dose escalation (1 cycle, 21-28 days). Safety will be monitored via adverse events (AEs) for ~2 years post-enrollment.
Other Endpoint	Pharmacokinetic parameters (Cmax, Tmax, AUC) of venetoclax and ABBV-838 will be assessed over ~43-57 days, alongside efficacy (ORR per IMWG criteria), toxin levels (MMAE), total mAb, and MRD negativity (10^-5 threshold by NGS). Terminal elimination (t1/2, beta) of ABBV-838 will be analyzed on Cycle 1 Day 1.

Experiment 1 Reporting the Activity Date of This ADC					[346]
Efficacy Data	Objective Response Rate (ORR)	13.00 29.00 40.00 40.00 %	High SLITRK6 expression (SLITRK6+++; IHC H-score=230)
Patients Enrolled	Metastatic uroepithelial carcinoma (mUC) patients unselected for SLITRK6 expression (determined by an IHC assay) and previously treated with 1 prior chemo regimen or unfit for cisplatin.
Administration Dosage	Administered IV weekly for 3 out of every 4 weeks.
Related Clinical Trial
NCT Number	NCT01963052	Phase Status	Phase 1
Clinical Description	A phase 1 study of the safety and pharmacokinetics of escalating doses of AGS15E given as monotherapy in subjects with metastatic urothelial cancer.
Experiment 2 Reporting the Activity Date of This ADC					[378]
Efficacy Data	Progression Free Survival	16 weeks
Patients Enrolled	Eligible patients must have histologically confirmed TCCU with specific prior treatment requirements per cohort (Parts A, B, C). Key inclusion criteria include measurable disease, ECOG status 0-2, life expectancy ≥3 months, and adequate organ function. Exclusion criteria cover severe neuropathy, uncontrolled CNS metastases, recent investigational/cancer therapy, significant cardiac disease, active infections, major surgery within 28 days, and specific ocular conditions.    Click to Show/Hide
Administration Dosage	ASG-15ME was administered IV weekly for 3 out of every 4 wks until no further benefit. 6 dose levels were studied: 0.1, .25, .5, 0.75, 1, or 1.25 mg/kg.
Related Clinical Trial
NCT Number	NCT01963052	Phase Status	PHASE1
Clinical Description	A Phase 1 Study of the Safety and Pharmacokinetics of Escalating Doses of AGS15E Given as Monotherapy in Subjects With Metastatic Urothelial Cancer
Primary Endpoint	The primary safety endpoint is the incidence of adverse events over 36 months, while pharmacokinetic parameters for total antibody (TAb), antibody drug conjugate (ADC), and Monomethyl Auristatin E (MMAE) including CEOI, Cmax, Ctrough, Tmax, AUC0-7, t1/2, CL, and Vss are assessed during specific dosing cycles up to 6 months.
Other Endpoint	Secondary endpoints include Anti-Drug Antibody (ADA) incidence and tumor response (CR/PR per RECIST 1.1 confirmed ≥28 days), objective response rate, disease control rate (CR/PR/SD), progression-free survival (time from first infusion to progression/death), and duration of response (time from first CR/PR to progression/death) evaluated over 26-36 months.    Click to Show/Hide
Experiment 3 Reporting the Activity Date of This ADC					[378]
Efficacy Data	Objective Response Rate (ORR)	30%
Patients Enrolled	Eligible patients must have histologically confirmed TCCU with specific prior treatment requirements per cohort (Parts A, B, C). Key inclusion criteria include measurable disease, ECOG status 0-2, life expectancy ≥3 months, and adequate organ function. Exclusion criteria cover severe neuropathy, uncontrolled CNS metastases, recent investigational/cancer therapy, significant cardiac disease, active infections, major surgery within 28 days, and specific ocular conditions.    Click to Show/Hide
Administration Dosage	ASG-15ME was administered IV weekly for 3 out of every 4 wks until no further benefit. 6 dose levels were studied: 0.1, .25, .5, 0.75, 1, or 1.25 mg/kg.
Related Clinical Trial
NCT Number	NCT01963052	Phase Status	PHASE1
Clinical Description	A Phase 1 Study of the Safety and Pharmacokinetics of Escalating Doses of AGS15E Given as Monotherapy in Subjects With Metastatic Urothelial Cancer
Primary Endpoint	The primary safety endpoint is the incidence of adverse events over 36 months, while pharmacokinetic parameters for total antibody (TAb), antibody drug conjugate (ADC), and Monomethyl Auristatin E (MMAE) including CEOI, Cmax, Ctrough, Tmax, AUC0-7, t1/2, CL, and Vss are assessed during specific dosing cycles up to 6 months.
Other Endpoint	Secondary endpoints include Anti-Drug Antibody (ADA) incidence and tumor response (CR/PR per RECIST 1.1 confirmed ≥28 days), objective response rate, disease control rate (CR/PR/SD), progression-free survival (time from first infusion to progression/death), and duration of response (time from first CR/PR to progression/death) evaluated over 26-36 months.    Click to Show/Hide

Experiment 1 Reporting the Activity Date of This ADC					[367]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 73.40%	Moderate SLITRK6 expression (SLITRK6++; IHC H-score=185)
Method Description	PDX models were established by subcutaneous implantation of xenograft fragments (AG-B7 or AG-B8) in the flanks of SCID mice. When the tumor volume reached approximately 200 mm3,Sirtratumab Vedotin was dosed at 0.25 mg/kg,2x per week i.v in AG-B8 PDX model. The last dose was given on day 14.
In Vivo Model	Bladder cancer PDX model (PDX: AG-B8)
Experiment 2 Reporting the Activity Date of This ADC					[367]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 86.90%	High SLITRK6 expression (SLITRK6+++; IHC H-score=280)
Method Description	PDX models were established by subcutaneous implantation of xenograft fragments (AG-B7 or AG-B8) in the flanks of SCID mice. When the tumor volume reached approximately 200 mm3,Sirtratumab Vedotin was dosed at 0.5 mg/kg,2x per week i.v in AG-B7 PDX model. The last dose was given on day 21.
In Vivo Model	Bladder cancer PDX model (PDX: AG-B7)
Experiment 3 Reporting the Activity Date of This ADC					[367]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 88.40%	High SLITRK6 expression (SLITRK6+++; IHC H-score=250)
Method Description	PDX models were established by subcutaneous implantation of xenograft fragments (AG-B7 or AG-B8) in the flanks of SCID mice. When the tumor volume reached approximately 200 mm3,Sirtratumab Vedotin was dosed at 0.5 mg/kg,2x per week i.v in AG-B8 PDX model. The last dose was given on day 14.
In Vivo Model	Bladder cancer PDX model (PDX: AG-B8)

Experiment 1 Reporting the Activity Date of This ADC					[367]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 88.90%	High SLITRK6 expression (SLITRK6+++)
Method Description	CDX models were established by subcutaneous injection of between 2 and 10 million SW780, RT4 (ATCC) or NCI-H322M (NCI) cells in SCID mice. When the tumor volume reached approximately 230 mm3, a single dose of Sirtratumab Vedotin, 5 mg/kg intravenously, was administered intravenously (iv) to the mice.
In Vivo Model	Bladder cancer CDX model
In Vitro Model	Bladder carcinoma	RT-4 cells		CVCL_0036
Experiment 2 Reporting the Activity Date of This ADC					[367]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 91.10%	Negative SLITRK6 expression (SLITRK6-)
Method Description	CDX models were established by subcutaneous injection of between 2 and 10 million SW780, RT4 (ATCC) or NCI-H322M (NCI) cells in SCID mice. Sirtratumab Vedotin was administered twice weekly at 3 mg/kg (n = 6) starting when the tumor volume reached approximately 200 mm3.
In Vivo Model	Lung cancer NCI-322M CDX model
In Vitro Model	Lung cancer	NCI-322M cells		Homo sapiens

Experiment 1 Reporting the Activity Date of This ADC					[367]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.99 nM
Method Description	ASG-15ME was tested for its ability to kill several SLITRK6-positive cell lines in vitro. The viability of CHP-212 cells treated with ASG-15ME was compared with that of target negative cells (IGR-OV1) or cells treated with an isotype control antibody to determine IC50 values.
In Vitro Model	Neuroblastoma	CHP-212 cells		CVCL_1125
Experiment 2 Reporting the Activity Date of This ADC					[367]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 10 uM	High SLITRK6 expression (SLITRK6+++; IHC H-score=250)
Method Description	ASG-15ME was tested for its ability to kill several SLITRK6-positive cell lines in vitro. The viability of CHP-212 cells treated with ASG-15ME was compared with that of target negative cells (IGR-OV1) or cells treated with an isotype control antibody to determine IC50 values.
In Vitro Model	Ovarian endometrioid adenocarcinoma	IGROV-1 cells		CVCL_1304

Experiment 1 Reporting the Activity Date of This ADC					[347]
Efficacy Data	Objective Response Rate (ORR)	13.30%
Patients Enrolled	Patients with HER2-positive advanced breast cancer progressive to at least two kinds of prior anti-HER2 treatment.
Administration Dosage	0.30-4.80 mg/kg iv administered once every 3 weeks.
Related Clinical Trial
NCT Number	NCT03281824	Phase Status	Phase 1
Clinical Description	Open-label, dose increase and phase 1 study of ALT-P7 to determine safety, tolerability, pharmacokinetics for HER2 positive metastatic breast cancer patients who have progressed on previous trastuzumab-based therapy.
Experiment 2 Reporting the Activity Date of This ADC					[377]
Efficacy Data	Progression Free Survival	6.2 months
Patients Enrolled	Eligible patients must be ≥19 years old with ECOG 0-1, adequate organ function (hematologic/renal/hepatic), and negative pregnancy status. Key exclusions include trastuzumab intolerance, active CNS metastases, unresolved Grade ≥2 toxicities, recent anticancer therapies (<3 weeks), significant cardiopulmonary dysfunction (LVEF<50%, NYHA II-IV), active infections (HIV/HBV/HCV), or other malignancies within 5 years (except specified cured cancers).    Click to Show/Hide
Administration Dosage	8 groups: 0.3 mg/kg, 0.6 mg/kg, 1.2 mg/kg, 2.4 mg/kg, 3.6 mg/kg, 4.2 mg/kg, 4.5 mg/kg, 4.8 mg/kg, Administration: Day 1 of each 3-week cycle
Related Clinical Trial
NCT Number	NCT03281824	Phase Status	PHASE1
Clinical Description	Open-Label, Dose Increase and Phase I Study of ALT-P7 to Determine Safety, Tolerability, Pharmacokinetics for HER2 Positive Metastatic Breast Cancer Patients Who Have Progressed on Previous Trastuzumab-Based Therapy
Primary Endpoint	The study evaluates safety endpoints including dose-limiting toxicities (DLTs) during the 21-day assessment period to determine maximum tolerated dose (MTD) or recommended phase II dose (RP2D), along with treatment-emergent adverse events (TEAEs) graded by CTCAE v4.03 with special focus on immune-related adverse events (irAEs) monitored for up to 4 weeks post-treatment.    Click to Show/Hide
Other Endpoint	Pharmacokinetic analysis assesses ALT-P7 metabolism across dose groups (1.2-5.4 mg/kg) from administration to elimination, while immunogenicity testing evaluates anti-drug antibody responses. Efficacy outcomes are analyzed descriptively after Cycle 2 (42 days), including subject counts, means, standard deviations, and ranges for each dose cohort.
Experiment 3 Reporting the Activity Date of This ADC					[377]
Efficacy Data	Disease control rate (DCR)	77.30%
Patients Enrolled	Eligible patients must be ≥19 years old with ECOG 0-1, adequate organ function (hematologic/renal/hepatic), and negative pregnancy status. Key exclusions include trastuzumab intolerance, active CNS metastases, unresolved Grade ≥2 toxicities, recent anticancer therapies (<3 weeks), significant cardiopulmonary dysfunction (LVEF<50%, NYHA II-IV), active infections (HIV/HBV/HCV), or other malignancies within 5 years (except specified cured cancers).    Click to Show/Hide
Administration Dosage	8 groups: 0.3 mg/kg, 0.6 mg/kg, 1.2 mg/kg, 2.4 mg/kg, 3.6 mg/kg, 4.2 mg/kg, 4.5 mg/kg, 4.8 mg/kg, Administration: Day 1 of each 3-week cycle
Related Clinical Trial
NCT Number	NCT03281824	Phase Status	PHASE1
Clinical Description	Open-Label, Dose Increase and Phase I Study of ALT-P7 to Determine Safety, Tolerability, Pharmacokinetics for HER2 Positive Metastatic Breast Cancer Patients Who Have Progressed on Previous Trastuzumab-Based Therapy
Primary Endpoint	The study evaluates safety endpoints including dose-limiting toxicities (DLTs) during the 21-day assessment period to determine maximum tolerated dose (MTD) or recommended phase II dose (RP2D), along with treatment-emergent adverse events (TEAEs) graded by CTCAE v4.03 with special focus on immune-related adverse events (irAEs) monitored for up to 4 weeks post-treatment.    Click to Show/Hide
Other Endpoint	Pharmacokinetic analysis assesses ALT-P7 metabolism across dose groups (1.2-5.4 mg/kg) from administration to elimination, while immunogenicity testing evaluates anti-drug antibody responses. Efficacy outcomes are analyzed descriptively after Cycle 2 (42 days), including subject counts, means, standard deviations, and ranges for each dose cohort.

Experiment 1 Reporting the Activity Date of This ADC					[348]
Efficacy Data	Objective Response Rate (ORR)	17.76%
Patients Enrolled	Eastern Cooperative Oncology Group (ECOG) performance status of 0-1, histologically or cytologically documented advanced or metastatic breast, ovarian, pancreatic, NSCLC, head and neck squamous cell carcinoma, or gastric cancer in dose escalation, adequate hematologic and end organ function, and measurable disease per RECIST v1.1.
Administration Dosage	Intravenously at doses of 0.20, 0.40, 0.80, 1.60, or 2.40 mg/kg once every 3 weeks (Q3W).
Related Clinical Trial
NCT Number	NCT02092792	Phase Status	Phase 1
Clinical Description	A phase 1, open-label study evaluating the safety and tolerability of escalating doses of DLYE5953A in patients with refractory solid tumors.
Primary Endpoint	The confirmed overall objective response rate was 17.76%. All responders (8/68 patients) had PR,and all had received the RP2D dose of 2.40 mg/kg. This included three patients with MBC, and five patients in the NSCLC expansion cohort (5/25; 20%).
Other Endpoint	The recommended phase II dose (RP2D) was 2.40 mg/kg Q3W. No dose-limiting toxicities were identified during dose escalation (0.20-2.40 mg/kg; n = 20).
Experiment 2 Reporting the Activity Date of This ADC					[389]
Patients Enrolled	Eligible participants (≥18 years, ECOG 0-1) must have measurable advanced/metastatic solid tumors with no effective standard therapies. Exclusions: recent anticancer treatments (chemotherapy/radiation within 4 weeks; oral kinase inhibitors within 2 weeks unless toxicity resolves).
Related Clinical Trial
NCT Number	NCT02092792	Phase Status	PHASE1
Clinical Description	A PHASE I, OPEN-LABEL STUDY EVALUATING THE SAFETY AND TOLERABILITY OF ESCALATING DOSES OF DLYE5953A IN PATIENTS WITH REFRACTORY SOLID TUMORS
Primary Endpoint	The study evaluates safety through dose-limiting toxicities (Days 1-21) and adverse events (up to 32 months) in patients with advanced solid tumors, while also assessing efficacy and drug exposure.
Other Endpoint	Key outcomes include total drug exposure (AUC), immunogenicity (anti-DLYE5953A antibodies), and efficacy measures like objective response (RECIST v1.1), duration of response, and progression-free survival (all tracked up to 32 months).

Experiment 1 Reporting the Activity Date of This ADC					[349]
Efficacy Data	Objective Response Rate (ORR)	24%	Low CD37 expression (CD37+; CD37 MFI ratio=82)
Patients Enrolled	Relapsed / refractory non Hodgkin lymphomas (NHLs) and chronic lymphocytic leukemia (CLL).
Administration Dosage	Administered intravenously (IV) once every 3 weeks (Q3 weeks) until disease progression or unacceptable toxicity.
Related Clinical Trial
NCT Number	NCT02175433	Phase Status	Phase 1
Clinical Description	A phase 1 study evaluating safety, tolerability, and pharmacokinetics of escalating doses of AGS67E given as monotherapy in subjects with refractory or relapsed lymphoid malignancies.
Experiment 2 Reporting the Activity Date of This ADC					[364]
Related Clinical Trial
NCT Number	NCT02610062	Phase Status	Phase 1
Clinical Description	A phase 1 study evaluating safety, tolerability, and pharmacokinetics of escalating doses of AGS67E given as monotherapy in subjects with acute myeloid leukemia (AML).
Experiment 3 Reporting the Activity Date of This ADC					[385]
Patients Enrolled	Site-specific conjugation through the engineered C-terminal cysteine
Administration Dosage	Participants will receive 1.2, 1.8, 2.4, 0.6, 0.9 mg/kg of AGS67E as an intravenous infusion once every three weeks (Q3).
Related Clinical Trial
NCT Number	NCT02610062	Phase Status	PHASE1
Clinical Description	A Phase 1 Study Evaluating Safety, Tolerability, and Pharmacokinetics of Escalating Doses of AGS67E Given as Monotherapy in Subjects With Acute Myeloid Leukemia (AML)
Primary Endpoint	This clinical trial evaluates AGS67E, an antibody-drug conjugate (ADC), in acute myeloid leukemia (AML) patients, focusing on safety (adverse events, anti-drug antibodies), pharmacokinetics (Cmax, AUC, half-life of AGS67E components), and efficacy (complete remission rate, response duration). Key inclusion: relapsed/refractory or untreated AML (WHO 2008 criteria), ECOG ≤2, adequate organ function. Exclusion: APL, active GVHD, neuropathy ≥G2, recent chemo (<14 days), uncontrolled infections, or cardiac disease.    Click to Show/Hide
Other Endpoint	The study includes dose escalation (Q3W/weekly) and expansion phases with PK sampling (up to 12 months). Primary endpoints: safety/tolerability (AEs, ADA incidence) and PK parameters (TAb, ADC, MMAE). Secondary endpoints: efficacy (CR/CRc rates, best response). Hydroxyurea is permitted for blast control; P-gp/CYP3A modulators are restricted unless prophylactic.    Click to Show/Hide
Experiment 4 Reporting the Activity Date of This ADC					[386]
Patients Enrolled	Site-specific conjugation through unnatural amino acid (pAF 121).
Administration Dosage	Participants will receive 0.05, 0.1, 0.3, 0.6, 0.9, 1.2 milligram per kilogram (mg/kg) AGS67E without growth factor (GF) by intravenous infusion once every three weeks.
Related Clinical Trial
NCT Number	NCT02175433	Phase Status	PHASE1
Clinical Description	A Phase 1 Study Evaluating Safety, Tolerability, and Pharmacokinetics of Escalating Doses of AGS67E Given as Monotherapy in Subjects With Refractory or Relapsed Lymphoid Malignancies
Primary Endpoint	Safety evaluation included the incidence and severity of adverse events over 34 months, alongside comprehensive pharmacokinetic assessments of total antibody (TAb), antibody-drug conjugate (ADC), and MMAE at defined intervals during escalation and expansion phases, covering key metrics such as CEOI, Cmax, Tmax, AUC, half-life, systemic clearance, and volume of distribution.    Click to Show/Hide
Other Endpoint	Immunogenicity was assessed through Anti-Drug Antibody (ADA) formation against AGS67C/AGS67E, while efficacy endpoints included tumor response rates (CR/PR) and objective response rate (ORR), measured over the 34-month study period.

Experiment 1 Reporting the Activity Date of This ADC					[370]
Efficacy Data	Tumor Growth Inhibition value (TGI)	0%	Low CD37 expression (CD37+; CD37 MFI ratio=82)
Method Description	The in vivo antitumor activity of AGS-67E was evaluated in a CD37 positive NHL,CLL and AmL cell line xenograft models. Depending on the cell line,110e6 cells were injected into the flanks of individual SCID mice,and tumor volumes were allowed to reach 100 to 300 mm3. Animals and their tumors were size matched and randomized into treatment and control groups. Depending on the study,AGS67E and an isotype control ADC were dosed by i.v. bolus injection either at 0.25,0.75,1.5,or 3.0 mg/kg at biweekly (BIW) or weekly (QW) frequencies and for a total of 2 to 4 doses.    Click to Show/Hide
In Vivo Model	CD37-expressing Hel 92.1.7 AmL cancer xenograft model
In Vitro Model	Erythroleukemia	HEL 92.1.7 cells		CVCL_2481
Experiment 2 Reporting the Activity Date of This ADC					[370]
Efficacy Data	Tumor Growth Inhibition value (TGI)	27%	High CD37 expression (CD37+++; CD37 MFI ratio=580)
Method Description	The in vivo antitumor activity of AGS-67E was evaluated in a CD37 positive NHL,CLL and AmL cell line xenograft models. Depending on the cell line,110e6 cells were injected into the flanks of individual SCID mice,and tumor volumes were allowed to reach 100 to 300 mm3. Animals and their tumors were size matched and randomized into treatment and control groups. Depending on the study,AGS67E and an isotype control ADC were dosed by i.v. bolus injection either at 0.25,0.75,1.5,or 3.0 mg/kg at biweekly (BIW) or weekly (QW) frequencies and for a total of 2 to 4 doses.    Click to Show/Hide
In Vivo Model	CD37-expressing DOHH2 FL cancer xenograft model
In Vitro Model	Diffuse large B-cell lymphoma germinal center B-cell type	DoHH2 cells		CVCL_1179
Experiment 3 Reporting the Activity Date of This ADC					[370]
Efficacy Data	Tumor Growth Inhibition value (TGI)	31%	High CD37 expression (CD37+++; CD37 MFI ratio=554)
Method Description	The in vivo antitumor activity of AGS-67E was evaluated in a CD37 positive NHL,CLL and AmL cell line xenograft models. Depending on the cell line,110e6 cells were injected into the flanks of individual SCID mice,and tumor volumes were allowed to reach 100 to 300 mm3. Animals and their tumors were size matched and randomized into treatment and control groups. Depending on the study,AGS67E and an isotype control ADC were dosed by i.v. bolus injection either at 0.25,0.75,1.5,or 3.0 mg/kg at biweekly (BIW) or weekly (QW) frequencies and for a total of 2 to 4 doses.    Click to Show/Hide
In Vivo Model	CD37-expressing WSU-DLCL2 DBCL cancer xenograft model
In Vitro Model	Diffuse large B-cell lymphoma	WSU-DLCL2 cells		CVCL_1902
Experiment 4 Reporting the Activity Date of This ADC					[370]
Efficacy Data	Tumor Growth Inhibition value (TGI)	41%	Low CD37 expression (CD37+; CD37 MFI ratio=20)
Method Description	The in vivo antitumor activity of AGS-67E was evaluated in a CD37 positive NHL,CLL and AmL cell line xenograft models. Depending on the cell line,110e6 cells were injected into the flanks of individual SCID mice,and tumor volumes were allowed to reach 100 to 300 mm3. Animals and their tumors were size matched and randomized into treatment and control groups. Depending on the study,AGS67E and an isotype control ADC were dosed by i.v. bolus injection either at 0.25,0.75,1.5,or 3.0 mg/kg at biweekly (BIW) or weekly (QW) frequencies and for a total of 2 to 4 doses.    Click to Show/Hide
In Vivo Model	CD37-expressing KG-1 AmL cancer xenograft model
In Vitro Model	Adult acute myeloid leukemia	KG-1 cells		CVCL_0374
Experiment 5 Reporting the Activity Date of This ADC					[370]
Efficacy Data	Tumor Growth Inhibition value (TGI)	51%	High CD37 expression (CD37+++; CD37 MFI ratio=300)
Method Description	The in vivo antitumor activity of AGS-67E was evaluated in a CD37 positive NHL,CLL and AmL cell line xenograft models. Depending on the cell line,110e6 cells were injected into the flanks of individual SCID mice,and tumor volumes were allowed to reach 100 to 300 mm3. Animals and their tumors were size matched and randomized into treatment and control groups. Depending on the study,AGS67E and an isotype control ADC were dosed by i.v. bolus injection either at 0.25,0.75,1.5,or 3.0 mg/kg at biweekly (BIW) or weekly (QW) frequencies and for a total of 2 to 4 doses.    Click to Show/Hide
In Vivo Model	CD37-expressing Mino MCL cancer xenograft model
In Vitro Model	Mantle cell lymphoma	Mino cells		CVCL_1872
Experiment 6 Reporting the Activity Date of This ADC					[370]
Efficacy Data	Tumor Growth Inhibition value (TGI)	63%	Moderate CD37 expression (CD37++; CD37 MFI ratio=140)
Method Description	The in vivo antitumor activity of AGS-67E was evaluated in a CD37 positive NHL,CLL and AmL cell line xenograft models. Depending on the cell line,110e6 cells were injected into the flanks of individual SCID mice,and tumor volumes were allowed to reach 100 to 300 mm3. Animals and their tumors were size matched and randomized into treatment and control groups. Depending on the study,AGS67E and an isotype control ADC were dosed by i.v. bolus injection either at 0.25,0.75,1.5,or 3.0 mg/kg at biweekly (BIW) or weekly (QW) frequencies and for a total of 2 to 4 doses.    Click to Show/Hide
In Vivo Model	CD37-expressing Ramos-RR-XcL Burkitt lymphoma cancer xenograft model
In Vitro Model	Burkitt lymphoma	Ramos cells		CVCL_0597
Experiment 7 Reporting the Activity Date of This ADC					[370]
Efficacy Data	Tumor Growth Inhibition value (TGI)	66%	High CD37 expression (CD37+++; CD37 MFI ratio=580)
Method Description	The in vivo antitumor activity of AGS-67E was evaluated in a CD37 positive NHL,CLL and AmL cell line xenograft models. Depending on the cell line,110e6 cells were injected into the flanks of individual SCID mice,and tumor volumes were allowed to reach 100 to 300 mm3. Animals and their tumors were size matched and randomized into treatment and control groups. Depending on the study,AGS67E and an isotype control ADC were dosed by i.v. bolus injection either at 0.25,0.75,1.5,or 3.0 mg/kg at biweekly (BIW) or weekly (QW) frequencies and for a total of 2 to 4 doses.    Click to Show/Hide
In Vivo Model	CD37-expressing DOHH2 FL cancer xenograft model
In Vitro Model	Diffuse large B-cell lymphoma germinal center B-cell type	DoHH2 cells		CVCL_1179
Experiment 8 Reporting the Activity Date of This ADC					[370]
Efficacy Data	Tumor Growth Inhibition value (TGI)	69%	Low CD37 expression (CD37+; CD37 MFI ratio=25)
Method Description	The in vivo antitumor activity of AGS-67E was evaluated in a CD37 positive NHL,CLL and AmL cell line xenograft models. Depending on the cell line,110e6 cells were injected into the flanks of individual SCID mice,and tumor volumes were allowed to reach 100 to 300 mm3. Animals and their tumors were size matched and randomized into treatment and control groups. Depending on the study,AGS67E and an isotype control ADC were dosed by i.v. bolus injection either at 0.25,0.75,1.5,or 3.0 mg/kg at biweekly (BIW) or weekly (QW) frequencies and for a total of 2 to 4 doses.    Click to Show/Hide
In Vivo Model	CD37-expressing MOLM-13 AmL cancer xenograft model
In Vitro Model	Adult acute myeloid leukemia	MOLM-13 cells		CVCL_2119
Experiment 9 Reporting the Activity Date of This ADC					[370]
Efficacy Data	Tumor Growth Inhibition value (TGI)	86%	Moderate CD37 expression (CD37++; CD37 MFI ratio=140)
Method Description	The in vivo antitumor activity of AGS-67E was evaluated in a CD37 positive NHL,CLL and AmL cell line xenograft models. Depending on the cell line,110e6 cells were injected into the flanks of individual SCID mice,and tumor volumes were allowed to reach 100 to 300 mm3. Animals and their tumors were size matched and randomized into treatment and control groups. Depending on the study,AGS67E and an isotype control ADC were dosed by i.v. bolus injection either at 0.25,0.75,1.5,or 3.0 mg/kg at biweekly (BIW) or weekly (QW) frequencies and for a total of 2 to 4 doses.    Click to Show/Hide
In Vivo Model	CD37-expressing Ramos-RR-XcL Burkitt lymphoma cancer xenograft model
In Vitro Model	Burkitt lymphoma	Ramos cells		CVCL_0597
Experiment 10 Reporting the Activity Date of This ADC					[370]
Efficacy Data	Tumor Growth Inhibition value (TGI)	92%	High CD37 expression (CD37+++; CD37 MFI ratio=300)
Method Description	The in vivo antitumor activity of AGS-67E was evaluated in a CD37 positive NHL,CLL and AmL cell line xenograft models. Depending on the cell line,110e6 cells were injected into the flanks of individual SCID mice,and tumor volumes were allowed to reach 100 to 300 mm3. Animals and their tumors were size matched and randomized into treatment and control groups. Depending on the study,AGS67E and an isotype control ADC were dosed by i.v. bolus injection either at 0.25,0.75,1.5,or 3.0 mg/kg at biweekly (BIW) or weekly (QW) frequencies and for a total of 2 to 4 doses.    Click to Show/Hide
In Vivo Model	CD37-expressing Mino MCL cancer xenograft model
In Vitro Model	Mantle cell lymphoma	Mino cells		CVCL_1872
Experiment 11 Reporting the Activity Date of This ADC					[370]
Efficacy Data	Tumor Growth Inhibition value (TGI)	95%	Low CD37 expression (CD37+; CD37 MFI ratio=23)
Method Description	The in vivo antitumor activity of AGS-67E was evaluated in a CD37 positive NHL,CLL and AmL cell line xenograft models. Depending on the cell line,110e6 cells were injected into the flanks of individual SCID mice,and tumor volumes were allowed to reach 100 to 300 mm3. Animals and their tumors were size matched and randomized into treatment and control groups. Depending on the study,AGS67E and an isotype control ADC were dosed by i.v. bolus injection either at 0.25,0.75,1.5,or 3.0 mg/kg at biweekly (BIW) or weekly (QW) frequencies and for a total of 2 to 4 doses.    Click to Show/Hide
In Vivo Model	CD37-expressing THP-1 AmL cancer xenograft models
In Vitro Model	Childhood acute monocytic leukemia	THP-1 cells		CVCL_0006
Experiment 12 Reporting the Activity Date of This ADC					[370]
Efficacy Data	Tumor Growth Inhibition value (TGI)	95%	High CD37 expression (CD37+++; CD37 MFI ratio=580)
Method Description	The in vivo antitumor activity of AGS-67E was evaluated in a CD37 positive NHL,CLL and AmL cell line xenograft models. Depending on the cell line,110e6 cells were injected into the flanks of individual SCID mice,and tumor volumes were allowed to reach 100 to 300 mm3. Animals and their tumors were size matched and randomized into treatment and control groups. Depending on the study,AGS67E and an isotype control ADC were dosed by i.v. bolus injection either at 0.25,0.75,1.5,or 3.0 mg/kg at biweekly (BIW) or weekly (QW) frequencies and for a total of 2 to 4 doses.    Click to Show/Hide
In Vivo Model	CD37-expressing DOHH2 FL cancer xenograft model
In Vitro Model	Diffuse large B-cell lymphoma germinal center B-cell type	DoHH2 cells		CVCL_1179
Experiment 13 Reporting the Activity Date of This ADC					[370]
Efficacy Data	Tumor Growth Inhibition value (TGI)	96%	High CD37 expression (CD37+++; CD37 MFI ratio=554)
Method Description	The in vivo antitumor activity of AGS-67E was evaluated in a CD37 positive NHL,CLL and AmL cell line xenograft models. Depending on the cell line,110e6 cells were injected into the flanks of individual SCID mice,and tumor volumes were allowed to reach 100 to 300 mm3. Animals and their tumors were size matched and randomized into treatment and control groups. Depending on the study,AGS67E and an isotype control ADC were dosed by i.v. bolus injection either at 0.25,0.75,1.5,or 3.0 mg/kg at biweekly (BIW) or weekly (QW) frequencies and for a total of 2 to 4 doses.    Click to Show/Hide
In Vivo Model	CD37-expressing WSU-DLCL2 DBCL cancer xenograft model
In Vitro Model	Diffuse large B-cell lymphoma	WSU-DLCL2 cells		CVCL_1902
Experiment 14 Reporting the Activity Date of This ADC					[370]
Efficacy Data	Tumor Growth Inhibition value (TGI)	97%	Moderate CD37 expression (CD37++; CD37 MFI ratio=140)
Method Description	The in vivo antitumor activity of AGS-67E was evaluated in a CD37 positive NHL,CLL and AmL cell line xenograft models. Depending on the cell line,110e6 cells were injected into the flanks of individual SCID mice,and tumor volumes were allowed to reach 100 to 300 mm3. Animals and their tumors were size matched and randomized into treatment and control groups. Depending on the study,AGS67E and an isotype control ADC were dosed by i.v. bolus injection either at 0.25,0.75,1.5,or 3.0 mg/kg at biweekly (BIW) or weekly (QW) frequencies and for a total of 2 to 4 doses.    Click to Show/Hide
In Vivo Model	CD37-expressing Ramos-RR-XcL Burkitt lymphoma cancer xenograft model
In Vitro Model	Burkitt lymphoma	Ramos cells		CVCL_0597
Experiment 15 Reporting the Activity Date of This ADC					[370]
Efficacy Data	Tumor Growth Inhibition value (TGI)	100%	Low CD37 expression (CD37+; CD37 MFI ratio=25)
Method Description	The in vivo antitumor activity of AGS-67E was evaluated in a CD37 positive NHL,CLL and AmL cell line xenograft models. Depending on the cell line,110e6 cells were injected into the flanks of individual SCID mice,and tumor volumes were allowed to reach 100 to 300 mm3. Animals and their tumors were size matched and randomized into treatment and control groups. Depending on the study,AGS67E and an isotype control ADC were dosed by i.v. bolus injection either at 0.25,0.75,1.5,or 3.0 mg/kg at biweekly (BIW) or weekly (QW) frequencies and for a total of 2 to 4 doses.    Click to Show/Hide
In Vivo Model	CD37-expressing MOLM-13 AmL cancer xenograft model
In Vitro Model	Adult acute myeloid leukemia	MOLM-13 cells		CVCL_2119
Experiment 16 Reporting the Activity Date of This ADC					[370]
Efficacy Data	Tumor Growth Inhibition value (TGI)	100%	Low CD37 expression (CD37+; CD37 MFI ratio=25)
Method Description	The in vivo antitumor activity of AGS-67E was evaluated in a CD37 positive NHL,CLL and AmL cell line xenograft models. Depending on the cell line,110e6 cells were injected into the flanks of individual SCID mice,and tumor volumes were allowed to reach 100 to 300 mm3. Animals and their tumors were size matched and randomized into treatment and control groups. Depending on the study,AGS67E and an isotype control ADC were dosed by i.v. bolus injection either at 0.25,0.75,1.5,or 3.0 mg/kg at biweekly (BIW) or weekly (QW) frequencies and for a total of 2 to 4 doses.    Click to Show/Hide
In Vivo Model	CD37-expressing MOLM-13 AmL cancer xenograft model
In Vitro Model	Adult acute myeloid leukemia	MOLM-13 cells		CVCL_2119
Experiment 17 Reporting the Activity Date of This ADC					[370]
Efficacy Data	Tumor Growth Inhibition value (TGI)	100%	Low CD37 expression (CD37+; CD37 MFI ratio=22)
Method Description	The in vivo antitumor activity of AGS-67E was evaluated in a CD37 positive NHL,CLL and AmL cell line xenograft models. Depending on the cell line,110e6 cells were injected into the flanks of individual SCID mice,and tumor volumes were allowed to reach 100 to 300 mm3. Animals and their tumors were size matched and randomized into treatment and control groups. Depending on the study,AGS67E and an isotype control ADC were dosed by i.v. bolus injection either at 0.25,0.75,1.5,or 3.0 mg/kg at biweekly (BIW) or weekly (QW) frequencies and for a total of 2 to 4 doses.    Click to Show/Hide
In Vivo Model	CD38-expressing MV-411 AmL cancer xenograft model
In Vitro Model	Childhood acute monocytic leukemia	MV4-11 cells		CVCL_0064
Experiment 18 Reporting the Activity Date of This ADC					[370]
Efficacy Data	Tumor Growth Inhibition value (TGI)	100%	Low CD37 expression (CD37+; CD37 MFI ratio=22)
Method Description	The in vivo antitumor activity of AGS-67E was evaluated in a CD37 positive NHL,CLL and AmL cell line xenograft models. Depending on the cell line,110e6 cells were injected into the flanks of individual SCID mice,and tumor volumes were allowed to reach 100 to 300 mm3. Animals and their tumors were size matched and randomized into treatment and control groups. Depending on the study,AGS67E and an isotype control ADC were dosed by i.v. bolus injection either at 0.25,0.75,1.5,or 3.0 mg/kg at biweekly (BIW) or weekly (QW) frequencies and for a total of 2 to 4 doses.    Click to Show/Hide
In Vivo Model	CD38-expressing MV-411 AmL cancer xenograft model
In Vitro Model	Childhood acute monocytic leukemia	MV4-11 cells		CVCL_0064
Experiment 19 Reporting the Activity Date of This ADC					[370]
Efficacy Data	Tumor Growth Inhibition value (TGI)	100%	Low CD37 expression (CD37+; CD37 MFI ratio=22)
Method Description	The in vivo antitumor activity of AGS-67E was evaluated in a CD37 positive NHL,CLL and AmL cell line xenograft models. Depending on the cell line,110e6 cells were injected into the flanks of individual SCID mice,and tumor volumes were allowed to reach 100 to 300 mm3. Animals and their tumors were size matched and randomized into treatment and control groups. Depending on the study,AGS67E and an isotype control ADC were dosed by i.v. bolus injection either at 0.25,0.75,1.5,or 3.0 mg/kg at biweekly (BIW) or weekly (QW) frequencies and for a total of 2 to 4 doses.    Click to Show/Hide
In Vivo Model	CD38-expressing MV-411 AmL cancer xenograft model
In Vitro Model	Childhood acute monocytic leukemia	MV4-11 cells		CVCL_0064
Experiment 20 Reporting the Activity Date of This ADC					[370]
Efficacy Data	Tumor Growth Inhibition value (TGI)	100%	Moderate CD37 expression (CD37++; CD37 MFI ratio=129)
Method Description	The in vivo antitumor activity of AGS-67E was evaluated in a CD37 positive NHL,CLL and AmL cell line xenograft models. Depending on the cell line,110e6 cells were injected into the flanks of individual SCID mice,and tumor volumes were allowed to reach 100 to 300 mm3. Animals and their tumors were size matched and randomized into treatment and control groups. Depending on the study,AGS67E and an isotype control ADC were dosed by i.v. bolus injection either at 0.25,0.75,1.5,or 3.0 mg/kg at biweekly (BIW) or weekly (QW) frequencies and for a total of 2 to 4 doses.    Click to Show/Hide
In Vivo Model	CD38-expressing JVM3 xenograft CLL cancer model
In Vitro Model	B-cell prolymphocytic leukemia	JVM-3 cells		CVCL_1320
Experiment 21 Reporting the Activity Date of This ADC					[370]
Efficacy Data	Tumor Growth Inhibition value (TGI)	100%	Moderate CD37 expression (CD37++; CD37 MFI ratio=129)
Method Description	The in vivo antitumor activity of AGS-67E was evaluated in a CD37 positive NHL,CLL and AmL cell line xenograft models. Depending on the cell line,110e6 cells were injected into the flanks of individual SCID mice,and tumor volumes were allowed to reach 100 to 300 mm3. Animals and their tumors were size matched and randomized into treatment and control groups. Depending on the study,AGS67E and an isotype control ADC were dosed by i.v. bolus injection either at 0.25,0.75,1.5,or 3.0 mg/kg at biweekly (BIW) or weekly (QW) frequencies and for a total of 2 to 4 doses.    Click to Show/Hide
In Vivo Model	CD38-expressing JVM3 xenograft CLL cancer model
In Vitro Model	B-cell prolymphocytic leukemia	JVM-3 cells		CVCL_1320
Experiment 22 Reporting the Activity Date of This ADC					[370]
Efficacy Data	Tumor Growth Inhibition value (TGI)	100%	Moderate CD37 expression (CD37++; CD37 MFI ratio=129)
Method Description	The in vivo antitumor activity of AGS-67E was evaluated in a CD37 positive NHL,CLL and AmL cell line xenograft models. Depending on the cell line,110e6 cells were injected into the flanks of individual SCID mice,and tumor volumes were allowed to reach 100 to 300 mm3. Animals and their tumors were size matched and randomized into treatment and control groups. Depending on the study,AGS67E and an isotype control ADC were dosed by i.v. bolus injection either at 0.25,0.75,1.5,or 3.0 mg/kg at biweekly (BIW) or weekly (QW) frequencies and for a total of 2 to 4 doses.    Click to Show/Hide
In Vivo Model	CD38-expressing JVM3 xenograft CLL cancer model
In Vitro Model	B-cell prolymphocytic leukemia	JVM-3 cells		CVCL_1320

Experiment 1 Reporting the Activity Date of This ADC					[370]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.05±0.03 nM	Low CD37 expression (CD37+; CD37 MFI ratio=25)
Method Description	The inhibitory activity of AGS-67E against cancer cell growth was evaluated in various human cancer cell lines in vitro. Exponentially growing cells with a viability of 95% or greater were plated in fresh RPMI-1640 (Gibco-Invitrogen) media containing phenol red supplemented with 10% FBS (heat inactivated),10 mmol/L Hepes,and 1 mmol/L sodium pyruvate. Cells were left overnight and treated with AGS67E and an isotype control. After 5 days of treatment and incubation at 37°C and 5% CO2,cell viability was measured following a 1 hour incubation at 37°C with Presto Blue Reagent (Invitrogen).    Click to Show/Hide
In Vitro Model	Burkitt lymphoma	Ramos cells		CVCL_0597
Experiment 2 Reporting the Activity Date of This ADC					[370]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.07±0.49 nM	Low CD37 expression (CD37+; CD37 MFI ratio=18)
Method Description	The inhibitory activity of AGS-67E against cancer cell growth was evaluated in various human cancer cell lines in vitro. Exponentially growing cells with a viability of 95% or greater were plated in fresh RPMI-1640 (Gibco-Invitrogen) media containing phenol red supplemented with 10% FBS (heat inactivated),10 mmol/L Hepes,and 1 mmol/L sodium pyruvate. Cells were left overnight and treated with AGS67E and an isotype control. After 5 days of treatment and incubation at 37°C and 5% CO2,cell viability was measured following a 1 hour incubation at 37°C with Presto Blue Reagent (Invitrogen).    Click to Show/Hide
In Vitro Model	Mantle cell lymphoma	Mino cells		CVCL_1872
Experiment 3 Reporting the Activity Date of This ADC					[370]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.08±0.61 nM	Negative CD37 expression (CD37-; CD37 MFI ratio=3)
Method Description	The inhibitory activity of AGS-67E against cancer cell growth was evaluated in various human cancer cell lines in vitro. Exponentially growing cells with a viability of 95% or greater were plated in fresh RPMI-1640 (Gibco-Invitrogen) media containing phenol red supplemented with 10% FBS (heat inactivated),10 mmol/L Hepes,and 1 mmol/L sodium pyruvate. Cells were left overnight and treated with AGS67E and an isotype control. After 5 days of treatment and incubation at 37°C and 5% CO2,cell viability was measured following a 1 hour incubation at 37°C with Presto Blue Reagent (Invitrogen).    Click to Show/Hide
In Vitro Model	Mantle cell lymphoma	Granta-519 cells		CVCL_1818
Experiment 4 Reporting the Activity Date of This ADC					[370]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.08±0.02 nM
Method Description	The inhibitory activity of AGS-67E against cancer cell growth was evaluated in various human cancer cell lines in vitro. Exponentially growing cells with a viability of 95% or greater were plated in fresh RPMI-1640 (Gibco-Invitrogen) media containing phenol red supplemented with 10% FBS (heat inactivated),10 mmol/L Hepes,and 1 mmol/L sodium pyruvate. Cells were left overnight and treated with AGS67E and an isotype control. After 5 days of treatment and incubation at 37°C and 5% CO2,cell viability was measured following a 1 hour incubation at 37°C with Presto Blue Reagent (Invitrogen).    Click to Show/Hide
In Vitro Model	Burkitt lymphoma	Daudi cells		CVCL_0008
Experiment 5 Reporting the Activity Date of This ADC					[370]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.13±0.08 nM	High CD37 expression (CD37+++; CD37 MFI ratio=662)
Method Description	The inhibitory activity of AGS-67E against cancer cell growth was evaluated in various human cancer cell lines in vitro. Exponentially growing cells with a viability of 95% or greater were plated in fresh RPMI-1640 (Gibco-Invitrogen) media containing phenol red supplemented with 10% FBS (heat inactivated),10 mmol/L Hepes,and 1 mmol/L sodium pyruvate. Cells were left overnight and treated with AGS67E and an isotype control. After 5 days of treatment and incubation at 37°C and 5% CO2,cell viability was measured following a 1 hour incubation at 37°C with Presto Blue Reagent (Invitrogen).    Click to Show/Hide
In Vitro Model	Childhood acute monocytic leukemia	THP-1 cells		CVCL_0006
Experiment 6 Reporting the Activity Date of This ADC					[370]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.23±0.30 nM	High CD37 expression (CD37+++; CD37 MFI ratio=534)
Method Description	The inhibitory activity of AGS-67E against cancer cell growth was evaluated in various human cancer cell lines in vitro. Exponentially growing cells with a viability of 95% or greater were plated in fresh RPMI-1640 (Gibco-Invitrogen) media containing phenol red supplemented with 10% FBS (heat inactivated),10 mmol/L Hepes,and 1 mmol/L sodium pyruvate. Cells were left overnight and treated with AGS67E and an isotype control. After 5 days of treatment and incubation at 37°C and 5% CO2,cell viability was measured following a 1 hour incubation at 37°C with Presto Blue Reagent (Invitrogen).    Click to Show/Hide
In Vitro Model	Diffuse large B-cell lymphoma	SU-DHL-4 cells		CVCL_0539
Experiment 7 Reporting the Activity Date of This ADC					[370]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.50±0.72 nM	High CD37 expression (CD37+++; CD37 MFI ratio=581)
Method Description	The inhibitory activity of AGS-67E against cancer cell growth was evaluated in various human cancer cell lines in vitro. Exponentially growing cells with a viability of 95% or greater were plated in fresh RPMI-1640 (Gibco-Invitrogen) media containing phenol red supplemented with 10% FBS (heat inactivated),10 mmol/L Hepes,and 1 mmol/L sodium pyruvate. Cells were left overnight and treated with AGS67E and an isotype control. After 5 days of treatment and incubation at 37°C and 5% CO2,cell viability was measured following a 1 hour incubation at 37°C with Presto Blue Reagent (Invitrogen).    Click to Show/Hide
In Vitro Model	B-cell prolymphocytic leukemia	JVM-3 cells		CVCL_1320
Experiment 8 Reporting the Activity Date of This ADC					[370]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.71±0.20 nM	Low CD37 expression (CD37+; CD37 MFI ratio=22)
Method Description	The inhibitory activity of AGS-67E against cancer cell growth was evaluated in various human cancer cell lines in vitro. Exponentially growing cells with a viability of 95% or greater were plated in fresh RPMI-1640 (Gibco-Invitrogen) media containing phenol red supplemented with 10% FBS (heat inactivated),10 mmol/L Hepes,and 1 mmol/L sodium pyruvate. Cells were left overnight and treated with AGS67E and an isotype control. After 5 days of treatment and incubation at 37°C and 5% CO2,cell viability was measured following a 1 hour incubation at 37°C with Presto Blue Reagent (Invitrogen).    Click to Show/Hide
In Vitro Model	Acute myeloid leukemia	SKM-1 cells		CVCL_0098
Experiment 9 Reporting the Activity Date of This ADC					[370]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.98±1.10 nM	Negative CD37 expression (CD37-; CD37 MFI ratio=9)
Method Description	The inhibitory activity of AGS-67E against cancer cell growth was evaluated in various human cancer cell lines in vitro. Exponentially growing cells with a viability of 95% or greater were plated in fresh RPMI-1640 (Gibco-Invitrogen) media containing phenol red supplemented with 10% FBS (heat inactivated),10 mmol/L Hepes,and 1 mmol/L sodium pyruvate. Cells were left overnight and treated with AGS67E and an isotype control. After 5 days of treatment and incubation at 37°C and 5% CO2,cell viability was measured following a 1 hour incubation at 37°C with Presto Blue Reagent (Invitrogen).    Click to Show/Hide
In Vitro Model	Diffuse large B-cell lymphoma germinal center B-cell type	DoHH2 cells		CVCL_1179
Experiment 10 Reporting the Activity Date of This ADC					[370]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.10±0.60 nM	Moderate CD37 expression (CD37++; CD37 MFI ratio=129)
Method Description	The inhibitory activity of AGS-67E against cancer cell growth was evaluated in various human cancer cell lines in vitro. Exponentially growing cells with a viability of 95% or greater were plated in fresh RPMI-1640 (Gibco-Invitrogen) media containing phenol red supplemented with 10% FBS (heat inactivated),10 mmol/L Hepes,and 1 mmol/L sodium pyruvate. Cells were left overnight and treated with AGS67E and an isotype control. After 5 days of treatment and incubation at 37°C and 5% CO2,cell viability was measured following a 1 hour incubation at 37°C with Presto Blue Reagent (Invitrogen).    Click to Show/Hide
In Vitro Model	Adult acute myeloid leukemia	OCI-AML-2 cells		CVCL_1619
Experiment 11 Reporting the Activity Date of This ADC					[370]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.20±0.90 nM	Negative CD37 expression (CD37-; CD37 MFI ratio=1)
Method Description	The inhibitory activity of AGS-67E against cancer cell growth was evaluated in various human cancer cell lines in vitro. Exponentially growing cells with a viability of 95% or greater were plated in fresh RPMI-1640 (Gibco-Invitrogen) media containing phenol red supplemented with 10% FBS (heat inactivated),10 mmol/L Hepes,and 1 mmol/L sodium pyruvate. Cells were left overnight and treated with AGS67E and an isotype control. After 5 days of treatment and incubation at 37°C and 5% CO2,cell viability was measured following a 1 hour incubation at 37°C with Presto Blue Reagent (Invitrogen).    Click to Show/Hide
In Vitro Model	Childhood acute monocytic leukemia	MV4-11 cells		CVCL_0064
Experiment 12 Reporting the Activity Date of This ADC					[370]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.30±0.50 nM	Low CD37 expression (CD37+; CD37 MFI ratio=20)
Method Description	The inhibitory activity of AGS-67E against cancer cell growth was evaluated in various human cancer cell lines in vitro. Exponentially growing cells with a viability of 95% or greater were plated in fresh RPMI-1640 (Gibco-Invitrogen) media containing phenol red supplemented with 10% FBS (heat inactivated),10 mmol/L Hepes,and 1 mmol/L sodium pyruvate. Cells were left overnight and treated with AGS67E and an isotype control. After 5 days of treatment and incubation at 37°C and 5% CO2,cell viability was measured following a 1 hour incubation at 37°C with Presto Blue Reagent (Invitrogen).    Click to Show/Hide
In Vitro Model	Adult acute myeloid leukemia	MOLM-13 cells		CVCL_2119
Experiment 13 Reporting the Activity Date of This ADC					[370]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	3.50±0.70 nM	Low CD37 expression (CD37+; CD37 MFI ratio=11)
Method Description	The inhibitory activity of AGS-67E against cancer cell growth was evaluated in various human cancer cell lines in vitro. Exponentially growing cells with a viability of 95% or greater were plated in fresh RPMI-1640 (Gibco-Invitrogen) media containing phenol red supplemented with 10% FBS (heat inactivated),10 mmol/L Hepes,and 1 mmol/L sodium pyruvate. Cells were left overnight and treated with AGS67E and an isotype control. After 5 days of treatment and incubation at 37°C and 5% CO2,cell viability was measured following a 1 hour incubation at 37°C with Presto Blue Reagent (Invitrogen).    Click to Show/Hide
In Vitro Model	Myeloid leukemia with maturation	Kasumi-1 cells		CVCL_0589
Experiment 14 Reporting the Activity Date of This ADC					[370]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	5.70±1.60 nM	Low CD37 expression (CD37+; CD37 MFI ratio=26)
Method Description	The inhibitory activity of AGS-67E against cancer cell growth was evaluated in various human cancer cell lines in vitro. Exponentially growing cells with a viability of 95% or greater were plated in fresh RPMI-1640 (Gibco-Invitrogen) media containing phenol red supplemented with 10% FBS (heat inactivated),10 mmol/L Hepes,and 1 mmol/L sodium pyruvate. Cells were left overnight and treated with AGS67E and an isotype control. After 5 days of treatment and incubation at 37°C and 5% CO2,cell viability was measured following a 1 hour incubation at 37°C with Presto Blue Reagent (Invitrogen).    Click to Show/Hide
In Vitro Model	Acute myeloid leukemia	BDCM cells		CVCL_4613
Experiment 15 Reporting the Activity Date of This ADC					[370]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	19.70±3.00 nM	High CD37 expression (CD37+++; CD37 MFI ratio=341)
Method Description	The inhibitory activity of AGS-67E against cancer cell growth was evaluated in various human cancer cell lines in vitro. Exponentially growing cells with a viability of 95% or greater were plated in fresh RPMI-1640 (Gibco-Invitrogen) media containing phenol red supplemented with 10% FBS (heat inactivated),10 mmol/L Hepes,and 1 mmol/L sodium pyruvate. Cells were left overnight and treated with AGS67E and an isotype control. After 5 days of treatment and incubation at 37°C and 5% CO2,cell viability was measured following a 1 hour incubation at 37°C with Presto Blue Reagent (Invitrogen).    Click to Show/Hide
In Vitro Model	Diffuse large B-cell lymphoma	WSU-DLCL2 cells		CVCL_1902
Experiment 16 Reporting the Activity Date of This ADC					[370]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 10 uM	Low CD37 expression (CD37+; CD37 MFI ratio=23)
Method Description	The inhibitory activity of AGS-67E against cancer cell growth was evaluated in various human cancer cell lines in vitro. Exponentially growing cells with a viability of 95% or greater were plated in fresh RPMI-1640 (Gibco-Invitrogen) media containing phenol red supplemented with 10% FBS (heat inactivated),10 mmol/L Hepes,and 1 mmol/L sodium pyruvate. Cells were left overnight and treated with AGS67E and an isotype control. After 5 days of treatment and incubation at 37°C and 5% CO2,cell viability was measured following a 1 hour incubation at 37°C with Presto Blue Reagent (Invitrogen).    Click to Show/Hide
In Vitro Model	Adult T acute lymphoblastic leukemia	MOLT-4 cells		CVCL_0013
Experiment 17 Reporting the Activity Date of This ADC					[370]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 10 uM	Low CD37 expression (CD37+; CD37 MFI ratio=64)
Method Description	The inhibitory activity of AGS-67E against cancer cell growth was evaluated in various human cancer cell lines in vitro. Exponentially growing cells with a viability of 95% or greater were plated in fresh RPMI-1640 (Gibco-Invitrogen) media containing phenol red supplemented with 10% FBS (heat inactivated),10 mmol/L Hepes,and 1 mmol/L sodium pyruvate. Cells were left overnight and treated with AGS67E and an isotype control. After 5 days of treatment and incubation at 37°C and 5% CO2,cell viability was measured following a 1 hour incubation at 37°C with Presto Blue Reagent (Invitrogen).    Click to Show/Hide
In Vitro Model	Acute erythroid leukemia	HEL 92.1 cells		CVCL_2481
Experiment 18 Reporting the Activity Date of This ADC					[370]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 10 uM	Low CD37 expression (CD37+; CD37 MFI ratio=10)
Method Description	The inhibitory activity of AGS-67E against cancer cell growth was evaluated in various human cancer cell lines in vitro. Exponentially growing cells with a viability of 95% or greater were plated in fresh RPMI-1640 (Gibco-Invitrogen) media containing phenol red supplemented with 10% FBS (heat inactivated),10 mmol/L Hepes,and 1 mmol/L sodium pyruvate. Cells were left overnight and treated with AGS67E and an isotype control. After 5 days of treatment and incubation at 37°C and 5% CO2,cell viability was measured following a 1 hour incubation at 37°C with Presto Blue Reagent (Invitrogen).    Click to Show/Hide
In Vitro Model	Acute erythroid leukemia	TF-1a cells		CVCL_3608
Experiment 19 Reporting the Activity Date of This ADC					[370]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 10 uM	Low CD37 expression (CD37+; CD37 MFI ratio=30)
Method Description	The inhibitory activity of AGS-67E against cancer cell growth was evaluated in various human cancer cell lines in vitro. Exponentially growing cells with a viability of 95% or greater were plated in fresh RPMI-1640 (Gibco-Invitrogen) media containing phenol red supplemented with 10% FBS (heat inactivated),10 mmol/L Hepes,and 1 mmol/L sodium pyruvate. Cells were left overnight and treated with AGS67E and an isotype control. After 5 days of treatment and incubation at 37°C and 5% CO2,cell viability was measured following a 1 hour incubation at 37°C with Presto Blue Reagent (Invitrogen).    Click to Show/Hide
In Vitro Model	Down syndrome	CMK cells		CVCL_0216
Experiment 20 Reporting the Activity Date of This ADC					[370]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 10 uM	Negative CD37 expression (CD37-; CD37 MFI ratio=5)
Method Description	The inhibitory activity of AGS-67E against cancer cell growth was evaluated in various human cancer cell lines in vitro. Exponentially growing cells with a viability of 95% or greater were plated in fresh RPMI-1640 (Gibco-Invitrogen) media containing phenol red supplemented with 10% FBS (heat inactivated),10 mmol/L Hepes,and 1 mmol/L sodium pyruvate. Cells were left overnight and treated with AGS67E and an isotype control. After 5 days of treatment and incubation at 37°C and 5% CO2,cell viability was measured following a 1 hour incubation at 37°C with Presto Blue Reagent (Invitrogen).    Click to Show/Hide
In Vitro Model	Adult acute myeloid leukemia	KG-1 cells		CVCL_0374
Experiment 21 Reporting the Activity Date of This ADC					[370]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 10 uM	Negative CD37 expression (CD37-; CD37 MFI ratio=4)
Method Description	The inhibitory activity of AGS-67E against cancer cell growth was evaluated in various human cancer cell lines in vitro. Exponentially growing cells with a viability of 95% or greater were plated in fresh RPMI-1640 (Gibco-Invitrogen) media containing phenol red supplemented with 10% FBS (heat inactivated),10 mmol/L Hepes,and 1 mmol/L sodium pyruvate. Cells were left overnight and treated with AGS67E and an isotype control. After 5 days of treatment and incubation at 37°C and 5% CO2,cell viability was measured following a 1 hour incubation at 37°C with Presto Blue Reagent (Invitrogen).    Click to Show/Hide
In Vitro Model	Adult acute megakaryoblastic leukemia	UT-7 cells		CVCL_2233
Experiment 22 Reporting the Activity Date of This ADC					[370]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 10 uM	High CD37 expression (CD37+++; CD37 MFI ratio=372)
Method Description	The inhibitory activity of AGS-67E against cancer cell growth was evaluated in various human cancer cell lines in vitro. Exponentially growing cells with a viability of 95% or greater were plated in fresh RPMI-1640 (Gibco-Invitrogen) media containing phenol red supplemented with 10% FBS (heat inactivated),10 mmol/L Hepes,and 1 mmol/L sodium pyruvate. Cells were left overnight and treated with AGS67E and an isotype control. After 5 days of treatment and incubation at 37°C and 5% CO2,cell viability was measured following a 1 hour incubation at 37°C with Presto Blue Reagent (Invitrogen).    Click to Show/Hide
In Vitro Model	Adult acute myeloid leukemia	HL-60 cells		CVCL_0002
Experiment 23 Reporting the Activity Date of This ADC					[370]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 10 uM	Low CD37 expression (CD37+; CD37 MFI ratio=39)
Method Description	The inhibitory activity of AGS-67E against cancer cell growth was evaluated in various human cancer cell lines in vitro. Exponentially growing cells with a viability of 95% or greater were plated in fresh RPMI-1640 (Gibco-Invitrogen) media containing phenol red supplemented with 10% FBS (heat inactivated),10 mmol/L Hepes,and 1 mmol/L sodium pyruvate. Cells were left overnight and treated with AGS67E and an isotype control. After 5 days of treatment and incubation at 37°C and 5% CO2,cell viability was measured following a 1 hour incubation at 37°C with Presto Blue Reagent (Invitrogen).    Click to Show/Hide
In Vitro Model	Chronic eosinophilic leukemia	EoL-1 cells		CVCL_0258
Experiment 24 Reporting the Activity Date of This ADC					[370]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 10 uM	High CD37 expression (CD37+++; CD37 MFI ratio=554)
Method Description	The inhibitory activity of AGS-67E against cancer cell growth was evaluated in various human cancer cell lines in vitro. Exponentially growing cells with a viability of 95% or greater were plated in fresh RPMI-1640 (Gibco-Invitrogen) media containing phenol red supplemented with 10% FBS (heat inactivated),10 mmol/L Hepes,and 1 mmol/L sodium pyruvate. Cells were left overnight and treated with AGS67E and an isotype control. After 5 days of treatment and incubation at 37°C and 5% CO2,cell viability was measured following a 1 hour incubation at 37°C with Presto Blue Reagent (Invitrogen).    Click to Show/Hide
In Vitro Model	Acute myeloid leukemia	PL-21 cells		CVCL_2161
Experiment 25 Reporting the Activity Date of This ADC					[370]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 10 uM	High CD37 expression (CD37+++; CD37 MFI ratio=301)
Method Description	The inhibitory activity of AGS-67E against cancer cell growth was evaluated in various human cancer cell lines in vitro. Exponentially growing cells with a viability of 95% or greater were plated in fresh RPMI-1640 (Gibco-Invitrogen) media containing phenol red supplemented with 10% FBS (heat inactivated),10 mmol/L Hepes,and 1 mmol/L sodium pyruvate. Cells were left overnight and treated with AGS67E and an isotype control. After 5 days of treatment and incubation at 37°C and 5% CO2,cell viability was measured following a 1 hour incubation at 37°C with Presto Blue Reagent (Invitrogen).    Click to Show/Hide
In Vitro Model	Mantle cell lymphoma	REC-1 cells		CVCL_1884

Experiment 1 Reporting the Activity Date of This ADC					[350]
Efficacy Data	Objective Response Rate (ORR)	36.00 50.00 %
Patients Enrolled	Relapsed/refractory (r/r) diffuse diffuse large B-cell lymphoma (DLBCL), iNHL (including follicular lymphoma, marginal zone lymphoma, and small lymphocytic lymphoma), mantle cell lymphoma (MCL), and chronic lymphocytic leukemia (CLL), and for whom no suitable therapy of curative intent or higher priority existed.
Administration Dosage	Intravenously over 30-90 minutes in 21-day cycles, starting dose of 0.10 mg/kg.
Related Clinical Trial
NCT Number	NCT01209130	Phase Status	Phase 1
Clinical Description	An open-label, multicenter, phase 1 trial of the safety and pharmacokinetics of escalating doses of DCDT2980S in patients with relapsed or refractory B-cell non-Hodgkin's lymphoma and chronic lymphocytic leukemia and DCDT2980S in combination with rituximab in patients with relapsed or refractory B-cell non Hodgkin's lymphoma.
Primary Endpoint	On the basis of these observations, while 3.20 mg/kg did not exceed the protocol-defined MTD.
Experiment 2 Reporting the Activity Date of This ADC					[353]
Efficacy Data	Objective Response Rate (ORR)	54.05 66.67 %
Patients Enrolled	R/R diffuse large B-cell lymphoma (DLBCL), R/R follicular lymphoma (FL).
Administration Dosage	PiV + RTX (ADC 2.40 mg/kg + RTX 375 mg/m2) every 21 days.
Related Clinical Trial
NCT Number	NCT01691898	Phase Status	Phase 1
Clinical Description	A randomized, open-label, multicenter, phase 2 trial evaluating the safety and activity of pinatuzumab vedotin (DCDT2980S) in combination with rituximab or polatuzumab vedotin (DCDS4501A) in combination with rituximab and a non-randomized phase 1b/2 evaluation of polatuzumab vedotin in combination with obinutuzumab in patients with relapsed or refractory B-cell non-Hodgkin's lymphoma.    Click to Show/Hide
Primary Endpoint	For R/R DLBCL, ORR=51.35% (N=19/37, 95% Cl, 34.00-68.00), CR rate=13.51% (N=5/37, 95% Cl, 5.00-29.00) and PR rate=37.84% (N=14/37,95% Cl, 23.00-55.00) in patients treated with PoV (CD79b) + RTX. For R/R DLBCL, ORR=54.05% (N=20/37,95% Cl, 37.00-71.00),CR rate=18.92% (N=7/37,95% Cl, 8.00-35.00) and PR rate=35.14% (N=13/37,95% Cl, 20.00-53.00) in patients treated with PiV (CD22) + RTX.    Click to Show/Hide
Other Endpoint	For R/R FL, ORR=60.00% (N=12/20,95% Cl 36.00-81.00), CR rate=30.00% (N=6/20, 95% Cl 12.00-54.00) and PR rate=30.00% (N=6/20,95% Cl 12.00-54.00) in patients treated with PoV (CD79b) + RTX. For R/R FL, ORR=66.67% (N=14/21,95% Cl 43.00-85.00), CR rate=4.76% (N=1/21, 95% Cl 0.10-24.00) and PR rate=61.90% (N=13/21,95% Cl 38.00-52.00) in patients treated with PiV (CD22) + RTX.    Click to Show/Hide
Experiment 3 Reporting the Activity Date of This ADC					[44]
Efficacy Data	Objective Response Rate (ORR)	60.00 62.00 %
Patients Enrolled	Relapsed or refractory diffuse large B-cell lymphoma or relapsed or refractory grade 13a follicular lymphoma.
Administration Dosage	R-pina (375 mg/m2 rituximab plus 24 mg/kg ADCs) every 21 days until disease progression or unacceptable toxicity up to 1 year.
Related Clinical Trial
NCT Number	NCT01691898	Phase Status	Phase 1
Clinical Description	A randomized, open-label, multicenter, phase 2 trial evaluating the safety and activity of pinatuzumab vedotin (DCDT2980S) in combination with rituximab or polatuzumab vedotin (DCDS4501A) in combination with rituximab and a non-randomized phase 1b/2 evaluation of polatuzumab vedotin in combination with obinutuzumab in patients with relapsed or refractory B-cell non-Hodgkin's lymphoma.    Click to Show/Hide
Primary Endpoint	Pr=60.00%, CR=26.00% for large B-cell lymphoma. PR=62.00%,CR=70.00% for follicular lymphoma.
Experiment 4 Reporting the Activity Date of This ADC					[401]
Patients Enrolled	Eligible patients must have measurable relapsed/refractory hematologic malignancies (NHL, DLBCL, MCL, CLL) with ≥12-week life expectancy. Key exclusions include recent antibody/ADC therapies (4-week washout), chemotherapy/radiation (2-week washout), or stem cell transplants (autologous <100 days, allogeneic prohibited).
Related Clinical Trial
NCT Number	NCT01209130	Phase Status	PHASE1
Clinical Description	An Open-Label, Multicenter, Phase I Trial of the Safety and Pharmacokinetics of Escalating Doses of DCDT2980S in Patients With Relapsed or Refractory B-Cell Non-Hodgkin's Lymphoma and Chronic Lymphocytic Leukemia And DCDT2980S in Combination With Rituximab in Patients With Relapsed or Refractory B-Cell Non Hodgkin's Lymphoma
Primary Endpoint	DLTs will be monitored continuously throughout the study to evaluate treatment safety and tolerability, with data collected until early discontinuation if applicable.
Other Endpoint	Objective tumor response (CR/PR) will be assessed per standard criteria as a key efficacy measure, with evaluations ongoing until study completion or patient discontinuation.
Experiment 5 Reporting the Activity Date of This ADC					[402]
Patients Enrolled	Eligible patients require ECOG 0-2, measurable r/r NHL/DLBCL (≥1 lesion >1.5cm), and archived tissue. Key exclusions: prior mAb/ADC ≤4 weeks, chemo/RT ≤2 weeks, unresolved grade >2 AEs (excluding neuropathy), allo/auto-SCT within 100 days, active CNS lymphoma, or live vaccines ≤28 days.
Administration Dosage	Pinatuzumab Vedotin 1.8 or 2.4 mg/kg administered by IV infusion on Day 1 or 2 of every 21-day cycle.
Related Clinical Trial
NCT Number	NCT01691898	Phase Status	PHASE1|||PHASE2
Clinical Description	A Randomized, Open-Label, Multicenter, Phase II Trial Evaluating the Safety and Activity of Pinatuzumab Vedotin (DCDT2980S) in Combination With Rituximab or Polatuzumab Vedotin (DCDS4501A) in Combination With Rituximab and a Non-Randomized Phase Ib/II Evaluation of Polatuzumab Vedotin in Combination With Obinutuzumab in Patients With Relapsed or Refractory B-Cell Non-Hodgkin's Lymphoma    Click to Show/Hide
Primary Endpoint	Tumor response endpoints will evaluate OR (CR/PR) per modified Cheson criteria (NHL) in rituximab/polatuzumab vedotin arms (A/B, Cohort C) and PET/CT-based CR (Lugano 2014) in obinutuzumab cohorts (E/G/H), with secondary assessments of DOR, PFS, OS, and progression rates across 3.5-5.5 years follow-up.
Other Endpoint	Immunogenicity (ADAs against pinatuzumab/polatuzumab vedotin/obinutuzumab) and pharmacokinetics (AUCinf, Cmax, CL, t½, Vss of rituximab/ADCs, plus MMAE-conjugated/unconjugated drug levels) will be serially monitored through 1.5-5.5 years to assess treatment sustainability and exposure-response relationships.

Experiment 1 Reporting the Activity Date of This ADC					[351]
Efficacy Data	Objective Response Rate (ORR)	46.67%
Patients Enrolled	B-non Hodgkin lymphoma (NHL) that had relapsed after or failed to respond to at least one prior treatment regimen and for which no suitable therapy of curative intent or higher priority existed.
Administration Dosage	The phase Ia, starting dose of 0.30 mg/kg administered intravenously once every 3 weeks (Q3W; 1 cycle = 21 days); The phase Ib portion evaluated DCDS0780A in dose-escalation cohorts starting at one dose level below that tolerated by completed monotherapy cohorts, and in combination with a fixed dose of rituximab (375 mg/m2); up to approximately 1 year or until disease progression or unacceptable toxicity.    Click to Show/Hide
Related Clinical Trial
NCT Number	NCT02453087	Phase Status	Phase 1
Clinical Description	An open-label, multicenter, phase 1/1b dose escalation study evaluating the pharmacokinetics, safety, tolerability, and preliminary efficacy of DCDS0780A, alone or in combination with rituximab, or obinutuzumab, in patients with relapsed/refractory B-cell non-Hodgkin's lymphoma.
Primary Endpoint	Response rate in all-treated patients (N=60) was 46.67% (n=28), including 17 complete responses (28.33%) and 11 partial responses (18.33%). The median duration of response (15.20 months) was the same for all responders (n=28) and patients with DLBCL (n=20).
Other Endpoint	The median PFS for all patients on study (N =60) was 4.40 months [95% CI,2.60-13.20], and 3.90 months (95% CI,2.40-9.50) for patients with DLBCL (n=41); PFS for pooled subgroups are indicated. The median DoR for the 28 responders among all patients was 15.20 months (95% CI,8.40-N.E.).
Experiment 2 Reporting the Activity Date of This ADC					[384]
Patients Enrolled	Eligible participants have relapsed/refractory B-cell NHL (ECOG 0-1, adequate organ function), while exclusions include recent anticancer therapy (4 weeks for mAbs, 2 weeks for chemo/radiation), active CNS lymphoma, uncontrolled infections, HBV/HCV/HIV positivity, or significant comorbidities (e.g., diabetes with HbA1c ≥7.5%, Grade 2+ neuropathy).    Click to Show/Hide
Administration Dosage	Participants will receive escalating doses of DCDS0780A as intravenous infusion as monotherapy on Day 1 of each 21-day cycle up to approximately 1 year or until disease progression or unacceptable toxicity (whichever comes first).
Related Clinical Trial
NCT Number	NCT02453087	Phase Status	PHASE1
Clinical Description	An Open-label, Multicenter, Phase 1/1b Dose Escalation Study Evaluating the Pharmacokinetics, Safety, Tolerability, and Preliminary Efficacy of DCDS0780A, Alone or in Combination With Rituximab, or Obinutuzumab, in Patients With Relapsed/Refractory B-Cell Non-Hodgkin's Lymphoma
Primary Endpoint	The study assesses DCDS0780A safety (AEs, dose-limiting toxicities), MTD/RP2D determination (Days 1-21), and pharmacokinetics (AUC, Cmax, CL, t½, Vss for total antibody, acMMAE, unconjugated MMAE) via intensive sampling across monotherapy/combination arms (21-day cycles, up to 1 year).
Other Endpoint	Key efficacy endpoints include ORR (Lugano criteria), PFS, DOR, and B-cell recovery metrics, alongside immunogenicity (anti-drug antibodies) and pharmacodynamic markers (lymphocyte counts), all monitored over 24 months with standardized infusion protocols.

Experiment 1 Reporting the Activity Date of This ADC					[352]
Efficacy Data	Objective Response Rate (ORR)	47.10 33.30 40.00 100.00 20.00 38.10 %
Patients Enrolled	Patients with resistant/refractory solid tumors that express CLDN18.2 who progressed on or were intolerant to standard treatment, or had no standard treatment were recruited.. ECOG score of 0-2.
Administration Dosage	0.50 up to 3.00 mg/kg on day 1, administered once every 3 weeks.
Related Clinical Trial
NCT Number	NCT05009966	Phase Status	Phase 1
Clinical Description	A phase 1 trial to evaluate safety, tolerability, pharmacokinetics, immunogenicity and initial efficacy of SYSA1801 in the treatment of CLDN 18.2 positive advanced malignant solid tumor.
Experiment 2 Reporting the Activity Date of This ADC					[381]
Patients Enrolled	Inclusion criteria for Parts A/B: histologically confirmed pancreatic/gastric/esophagogastric junction cancer with ≥50% tumor cells showing moderate-to-strong claudin 18.2 staining (IHC 2+/3+), archived/fresh tumor tissue, adequate organ function, life expectancy >12 weeks, age ≥18, ECOG PS 0/1, informed consent, and negative pregnancy test for reproductive-potential females within 48h prior to enrollment.    Click to Show/Hide
Administration Dosage	Part A will follow the standard 3+3 dose-escalation design and will be enrolled at dose levels of CPO102 at (0.5, 1, 1.8, 2.5, 3.5, 4.5, 5.5 mg/kg).
Related Clinical Trial
NCT Number	NCT05043987	Phase Status	PHASE1
Clinical Description	A Phase 1, Multicenter, Dose Escalation and Dose Expansion Study to Evaluate Safety of CPO102, an Anti-claudin 18.2 Antibody-MMAE Drug Conjugate Administered Intravenously in Patients With Advanced Pancreatic and Gastric Cancers
Primary Endpoint	The study will assess the number of participants with dose-limiting toxicities (DLTs) during the DLT evaluation period (first 21-day cycle) to determine the maximum tolerated dose (MTD) and/or recommended phase 2 dose (RP2D), with data collected over an average of 3 years.
Other Endpoint	Safety evaluations include treatment-emergent adverse events (TEAEs) graded by NCI-CTCAE v5.0 (Grade ≥3, serious, or fatal TEAEs with causality assessment), clinically significant changes in vital signs and lab tests, and CPO102 pharmacokinetics (AUC, Cmax, Tmax, t½, CL). Efficacy is measured by objective response rate (ORR per RECIST v1.1), while immunogenicity tracks anti-drug-antibody (ADA) incidence, all monitored over ~3 years.    Click to Show/Hide

Experiment 1 Reporting the Activity Date of This ADC					[357]
Related Clinical Trial
NCT Number	NCT01065623	Phase Status	Phase 1
Clinical Description	An open label phase 1 dose-escalation study to evaluate the safety, tolerability, pharmacokinetics, and maximum tolerated dose of BAY79-4620 administered as an intravenous infusion once every 2 weeks in patients with advanced solid tumors.
Experiment 2 Reporting the Activity Date of This ADC					[358]
Related Clinical Trial
NCT Number	NCT01028755	Phase Status	Phase 1
Clinical Description	An open label phase 1 study to evaluate the safety, tolerability, pharmacokinetics and maximum tolerated dose of BAY79-4620 in patients with advanced solid tumors.
Experiment 3 Reporting the Activity Date of This ADC					[398]
Patients Enrolled	Eligible participants must be ≥18 years with ECOG 0-2, ≥12-week life expectancy, confirmed advanced solid tumors refractory to standard therapy, and evaluable disease. Required lab values include: Hgb>10, ANC≥1500, platelets≥100K, bilirubin≤1.5xULN, ALT/AST≤2.5xULN (5x if liver mets), creatinine≤1.5xULN. Exclusions include significant cardiac disease (CHF III/IV, recent MI, arrhythmias, LVEF<40%), pancreatic abnormalities, uncontrolled HTN, active CNS mets (<6mos stable), renal failure, active HBV/HCV/HIV, grade≥3 infections, unhealed wounds, drug allergies, or other malignancies (except cured cancers >3yrs prior).    Click to Show/Hide
Administration Dosage	BAY79-4620 will be administered as 1 hour IV infusion. Dose escalation will be dependent on any dose limiting toxicities
Related Clinical Trial
NCT Number	NCT01028755	Phase Status	PHASE1
Clinical Description	An Open Label Phase I Study to Evaluate the Safety, Tolerability, Pharmacokinetics and Maximum Tolerated Dose of BAY79-4620 in Patients With Advanced Solid Tumors
Primary Endpoint	The study will evaluate the safety profile, tolerability, and determine the maximum tolerated dose of BAY79-4620 over two years, while simultaneously characterizing the pharmacokinetics of the drug and its key metabolites throughout the same duration.
Other Endpoint	Comprehensive biomarker assessments will be conducted, along with tumor response evaluations (following standard criteria), and immunogenicity testing - all assessed continuously over the two-year study period as key secondary endpoints.
Experiment 4 Reporting the Activity Date of This ADC					[399]
Patients Enrolled	Eligible patients must be ≥18 years old with ECOG 0-2, ≥12-week life expectancy, and advanced refractory solid tumors (histologically confirmed) who either lack standard options or decline standard therapy, with evaluable disease and adequate organ function. Key exclusions include significant cardiac disease (CHF Class III/IV, recent MI, unstable angina), uncontrolled hypertension (>160/95 mmHg), untreated CNS metastases, severe renal impairment, active HBV/HCV/HIV infections requiring treatment, serious unhealed wounds, recent major surgery/trauma, or anticancer treatments within protocol-specified washout periods.    Click to Show/Hide
Administration Dosage	1-hour infusion every 14 days. Starting dose will be 0.15 mg/ kg and dose will be escalated dependent on any dose limiting toxicities
Related Clinical Trial
NCT Number	NCT01065623	Phase Status	PHASE1
Clinical Description	An Open Label Phase I Dose-escalation Study to Evaluate the Safety, Tolerability, Pharmacokinetics, and Maximum Tolerated Dose of BAY79-4620 Administered as an Intravenous Infusion Once Every 2 Weeks in Patients With Advanced Solid Tumors
Primary Endpoint	The trial will monitor adverse events for approximately 3 years while characterizing the pharmacokinetics of BAY79-4620 at the end of cycle 2 (14-day cycles).
Other Endpoint	Biomarker patterns, tumor response outcomes, and immunogenicity will be systematically evaluated throughout the study's 3-year duration.

Experiment 1 Reporting the Activity Date of This ADC					[359]
Related Clinical Trial
NCT Number	NCT05229900	Phase Status	Phase 1
Clinical Description	A phase 1 study of SGN-ALPV in advanced solid tumors.
Experiment 2 Reporting the Activity Date of This ADC					[382]
Patients Enrolled	Eligible participants must have specified advanced solid tumors (ovarian/endometrial/NSCLC/gastric/cervical/GCT cancers) with measurable disease (RECIST v1.1), ECOG 0-1, and biopsy compliance for biomarker analysis. Key exclusions include active CNS metastases, prior MMAE/ALPP-targeted therapy, or Grade≥2 neuropathy (CTCAE v5.0). Ovarian cancer cohorts require platinum-resistant HGSOC with prior bevacizumab exposure.    Click to Show/Hide
Related Clinical Trial
NCT Number	NCT05229900	Phase Status	PHASE1
Clinical Description	A Phase 1 Study of SGN-ALPV in Advanced Solid Tumors
Primary Endpoint	Primary endpoints focus on safety evaluation including AE incidence (6 months post-treatment), DLT occurrence (28 days), and laboratory abnormalities, with dose-level toxicity analysis.
Other Endpoint	Secondary objectives assess immunogenicity (ADA incidence over 6 months), PK parameters (AUC/Cmax/Tmax/t½/Ctrough within 14 days post-treatment), efficacy measures (ORR/DOR/PFS/OS per RECIST v1.1 over 2 years), and ovarian cancer-specific CA-125 responses (GCIG criteria).

Experiment 1 Reporting the Activity Date of This ADC					[360]
Related Clinical Trial
NCT Number	NCT04665921	Phase Status	Phase 1
Clinical Description	A phase 1 study of SGN-STNV in advanced solid tumors.
Experiment 2 Reporting the Activity Date of This ADC					[396]
Patients Enrolled	Eligible participants had advanced solid tumors (NSCLC, breast, GI, and gynecologic cancers) refractory to standard therapies, measurable disease per RECIST v1.1, and adequate organ function. Key exclusions included active CNS metastases, prior MMAE therapy, ≥Grade 2 neuropathy, or uncontrolled ≥Grade 3 infections. Biopsies were required for specific cohorts.    Click to Show/Hide
Administration Dosage	Part A (dose escalation) and Part B (dose expansion) will include up to 25 and 180 patients (in up to 6 expansion cohorts), respectively.
Related Clinical Trial
NCT Number	NCT04665921	Phase Status	PHASE1
Clinical Description	A Phase 1 Study of SGN-STNV in Advanced Solid Tumors
Primary Endpoint	Safety endpoints included incidence of AEs, lab abnormalities, and dose-limiting toxicities monitored up to 30-37 days post-treatment or approximately 3 years, analyzed descriptively.
Other Endpoint	Efficacy measures (ORR, PFS, OS, DOR) and PK/immunogenicity parameters (AUC, Tmax, Cmax, Ctrough, ADA) were evaluated over approximately 3 years to assess treatment response and drug exposure characteristics.

Experiment 1 Reporting the Activity Date of This ADC					[361]
Related Clinical Trial
NCT Number	NCT04042480	Phase Status	Phase 1
Clinical Description	A phase 1 study of SGN-CD228A in select advanced solid tumors.
Experiment 2 Reporting the Activity Date of This ADC					[394]
Patients Enrolled	Inclusion: Metastatic/unresectable, relapsed/refractory solid tumors (melanoma, mesothelioma, HER2- breast cancer, NSCLC, CRC, PDAC) with prior therapies per tumor type, measurable disease (RECIST v1.1), ECOG 0-1. Exclusion: Recent malignancies, Grade 2+ neuropathy, retinal disease, prior SGN-CD228A/MMAE exposure.
Administration Dosage	SGN-CD228A administered into the vein (IV; intravenously)
Related Clinical Trial
NCT Number	NCT04042480	Phase Status	PHASE1
Clinical Description	A Phase 1 Study of SGN-CD228A in Select Advanced Solid Tumors
Primary Endpoint	The study monitors adverse events (AEs), lab abnormalities, and dose-limiting toxicities (DLTs) over 3.5 years, tracking any untoward medical occurrences in participants administered the investigational drug.
Other Endpoint	Efficacy endpoints include RECIST v1.1/mRECIST response (for mesothelioma), ORR (CR/PR post-treatment), PFS, OS, and DOR. PK analysis covers Cmax, Tmax, AUC (0-last), and Ctrough for acMMAE, free MMAE, and total antibody, alongside ADA incidence, all assessed over 3.5 years.

Experiment 1 Reporting the Activity Date of This ADC					[368]
Efficacy Data	Tumor Growth Inhibition value (TGI)	75%	Positive CD228 expression (CD228+++/++)
Method Description	SGN-CD228A was evaluated for antitumor activity in melanoma and NSCLC xenograft and PDX models.SGN-CD228A was administered at a single dose of 3.00 mg/kg.
In Vivo Model	NSCLC PDX model
Experiment 2 Reporting the Activity Date of This ADC					[368]
Efficacy Data	Tumor Growth Inhibition value (TGI)	100%	Positive CD228 expression (CD228+++/++)
Method Description	SGN-CD228A was evaluated for antitumor activity in melanoma and NSCLC xenograft and PDX models.SGN-CD228A was administered at a single dose of 1.00 mg/kg.
In Vivo Model	NSCLC PDX model

Experiment 1 Reporting the Activity Date of This ADC					[368]
Efficacy Data	Tumor Growth Inhibition value (TGI)	50%	Positive CD228 expression (CD228+++/++)
Method Description	SGN-CD228A was evaluated for antitumor activity in melanoma and NSCLC xenograft and PDX models.SGN-CD228A was administered at a single dose of 1.00 mg/kg.
In Vivo Model	Melanoma CDX model
In Vitro Model	Cutaneous melanoma	SK-MEL-5 cells		CVCL_0527
Experiment 2 Reporting the Activity Date of This ADC					[368]
Efficacy Data	Tumor Growth Inhibition value (TGI)	62.50%	Positive CD228 expression (CD228+++/++)
Method Description	SGN-CD228A was evaluated for antitumor activity in melanoma and NSCLC xenograft and PDX models.SGN-CD228A was administered at a single dose of 1.00 mg/kg.
In Vivo Model	Melanoma CDX model
In Vitro Model	Cutaneous melanoma	COLO 853 cells		CVCL_2003
Experiment 3 Reporting the Activity Date of This ADC					[368]
Efficacy Data	Tumor Growth Inhibition value (TGI)	100%	Positive CD228 expression (CD228+++/++)
Method Description	SGN-CD228A was evaluated for antitumor activity in melanoma and NSCLC xenograft and PDX models.SGN-CD228A was administered at a single dose of 1.00 mg/kg.
In Vivo Model	Squamous NSCLC CDX model
In Vitro Model	Lung squamous cell carcinoma	Calu-1 cells		CVCL_0608

Experiment 1 Reporting the Activity Date of This ADC					[362]
Related Clinical Trial
NCT Number	NCT03379584	Phase Status	Phase 1
Clinical Description	A phase 1 study of SGN-CD48A in patients with relapsed or refractory multiple myeloma.
Experiment 2 Reporting the Activity Date of This ADC					[395]
Patients Enrolled	Eligible patients must have MM requiring systemic treatment (per IMWG) refractory to prior PI, IMiD, and anti-CD38 antibody therapy, with measurable disease and adequate organ function (ECOG 0-1). Key exclusions: Grade 2+ neuropathy, recent malignancies (past 3 years), active CNS disease, uncontrolled infections (HIV/HBV/HCV), prior allogeneic transplant, recent cardiovascular events, or use of P-gp/CYP3A modulators within 14 days.    Click to Show/Hide
Administration Dosage	Intravenous (IV) infusion on days 1, 8, and 15 of a 28-day cycle
Related Clinical Trial
NCT Number	NCT03379584	Phase Status	PHASE1
Clinical Description	A Phase 1 Study of SGN-CD48A in Patients With Relapsed or Refractory Multiple Myeloma
Primary Endpoint	Safety outcomes monitor adverse events (AEs) including severity, seriousness, and relatedness through 1 month after the last dose, along with laboratory abnormalities and dose-limiting toxicities (DLTs) within 3 weeks of first treatment.
Other Endpoint	Efficacy measures include objective response rate (ORR; stringent CR/CR/VGPR/PR), CR rate, duration of response (DOR and CR duration up to ~3 years), PFS, OS, pharmacokinetics (blood concentrations of SGN-CD48A/metabolites), and incidence of antitherapeutic antibodies.

Experiment 1 Reporting the Activity Date of This ADC					[373]
Efficacy Data	Tumor Growth Inhibition value (TGI)	75%	Positive SLAMF2 expression (SLAMF2+++/++)
Method Description	SGN-CD48A was evaluated in vivo for antitumor activity in a diffuse MM cell line xenograft model in mice. SGN-CD48A was administered at a single dose of 0.30 mg/kg.
In Vivo Model	Multiple myeloma CDX model
In Vitro Model	Plasma cell myeloma	EJM cells		CVCL_2030
Experiment 2 Reporting the Activity Date of This ADC					[373]
Efficacy Data	Tumor Growth Inhibition value (TGI)	87.50%	Positive SLAMF2 expression (SLAMF2+++/++)
Method Description	SGN-CD48A was evaluated in vivo for antitumor activity in a diffuse MM cell line xenograft model in mice. SGN-CD48A was administered at a single dose of 1.00 mg/kg.
In Vivo Model	Multiple myeloma CDX model
In Vitro Model	Plasma cell myeloma	U-266 cells		CVCL_0015
Experiment 3 Reporting the Activity Date of This ADC					[373]
Efficacy Data	Tumor Growth Inhibition value (TGI)	100%	Positive SLAMF2 expression (SLAMF2+++/++)
Method Description	SGN-CD48A was evaluated in vivo for antitumor activity in a diffuse MM cell line xenograft model in mice. SGN-CD48A was administered at a single dose of 0.30 mg/kg.
In Vivo Model	Multiple myeloma CDX model
In Vitro Model	Plasma cell myeloma	NCI-H929 cells		CVCL_1600

Experiment 1 Reporting the Activity Date of This ADC					[373]
Efficacy Data	Half Maximal Effective Concentration (EC50)	1.00-11.00 ng/mL	High CD48 expresion (CD48+++/++; 1260 MSLN molecules/cell)
Method Description	Cytotoxic activity of SGN-CD48A was demonstrated in a panel of human MM cell lines in vitro.
In Vitro Model	Multiple myeloma	Multiple myeloma cells		Homo sapiens

Experiment 1 Reporting the Activity Date of This ADC					[365]
Patients Enrolled	Patients with advanced solid tumor types typically associated with elevated levels of EGFR expression (e.g., head and neck squamous cell carcinoma [HNC], non-small cell lung cancer [NSCLC], triple-negative breast cancer, colorectal carcinoma, and GBM.
Administration Dosage	A standard 3+3 design; intravenous (IV) infusion to groups of 3 to 6 patients. An every-3-week dosing cycle (0.30, 0.45, 0.67, 1.00, 1.50, 2.00, or 2.25 mg/kg losatuxizumab vedotin every 3 weeks [Q3W]) or alternative dosing schedules were evaluated (2.00 or 3.00 mg/kg losatuxizumab vedotin for 2 weeks on, 1 week off, or 4.50 or 6.00 mg/kg losatuxizumab vedotin weekly [over 3 weeks total]).    Click to Show/Hide
Related Clinical Trial
NCT Number	NCT02365662	Phase Status	Phase 1
Clinical Description	A phase 1 study of ABBV-221 in subjects with advanced solid tumor types likely to exhibit elevated levels of epidermal growth factor receptor.
Primary Endpoint	The maximum tolerated dose (MTD) was not achieved.
Other Endpoint	Stable disease (SD) for at least 2 cycles was observed in 19 patients (42.20%).
Experiment 2 Reporting the Activity Date of This ADC					[375]
Efficacy Data	stable disease (SD)	38%
Patients Enrolled	Eligible participants (ECOG 0-2) must have EGFR-elevated solid tumors (e.g., HNSCC, NSCLC, TNBC) with archived tissue and adequate organ function; expanded safety cohort requires platinum-refractory metastatic lung cancer. Exclusions include recent EGFR antibody use (>Grade 1 unresolved toxicities), IgG-related hypersensitivity, or high-risk conditions per investigator judgment.    Click to Show/Hide
Administration Dosage	ABBV-221 will be given either every 3 weeks or 2 weeks on, 1 week off or weekly dosing by intravenous infusion approximately over 30 minutes to 3 hours. This is a dose escalation study, therefore the dose of ABBV-221 will change throughout the study.
Related Clinical Trial
NCT Number	NCT02365662	Phase Status	PHASE1
Clinical Description	A Phase 1 Study of ABBV-221 in Subjects With Advanced Solid Tumor Types Likely to Exhibit Elevated Levels of Epidermal Growth Factor Receptor
Primary Endpoint	This study evaluates the safety profile of ABBV-221 through adverse event monitoring (4 years) and pharmacokinetics (Cmax, AUCt) with blood sampling across multiple cycles (up to ~2 years). The primary objectives include determining the maximum tolerated dose (MTD) and recommended Phase 2 dose (RPTD), where RPTD selection considers DLT patterns if MTD is reached or PK/safety data if MTD is not achieved.    Click to Show/Hide
Other Endpoint	Secondary objectives assess ABBV-221's effect on QT prolongation via ECG monitoring (Cycle 1 Days 1-8, then per cycle) and efficacy via objective response rate (ORR by RECIST 1.1) measured every 2-3 cycles for ~2 years in participants with baseline measurable lesions.

Experiment 1 Reporting the Activity Date of This ADC					[369]
Efficacy Data	Tumor Growth Inhibition value (TGI)	94.90%	High HER2 expression (HER2+++)
Method Description	In vivo therapy studies were conducted in mesothelioma xenograft and patient-derived xenograft (PDX) tumor model.ABT-414 treatment 3 mg/kg q4 days.
In Vivo Model	Malignant Mesothelioma PDX model (PDX: MSTO-211H)
Experiment 2 Reporting the Activity Date of This ADC					[369]
Efficacy Data	Tumor Growth Inhibition value (TGI)	98.30%	High HER2 expression (HER2+++)
Method Description	In vivo therapy studies were conducted in mesothelioma xenograft and patient-derived xenograft (PDX) tumor model.ABBV-221 treatment 3 mg/kg q4 days.
In Vivo Model	Malignant Mesothelioma PDX model (PDX: MSTO-211H)

Experiment 1 Reporting the Activity Date of This ADC					[371]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 0.23%	Low EGFR expression (EGFR+)
Method Description	To generate xenografts, a suspension of viable tumors cells mixed with an equal amount of Matrigel was injected subcutaneously into the flank of 6- to 8-week old mice. The injection volume was 0.2 mL composed of a 1:1 mixture of S-MEM and Matrigel. Tumors were size matched at approximately 200-250 mm3. Treatments ABBV-221 at 6 mg/kg every 4th day by intraperitoneal injection.    Click to Show/Hide
In Vivo Model	NCI-H292 lung xenograft tumor model
In Vitro Model	Lung mucoepidermoid carcinoma	NCI-H292 cells		CVCL_0455
Experiment 2 Reporting the Activity Date of This ADC					[371]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 5.45%	Low EGFR expression (EGFR+)
Method Description	To generate xenografts, a suspension of viable tumors cells mixed with an equal amount of Matrigel was injected subcutaneously into the flank of 6- to 8-week old mice. The injection volume was 0.2 mL composed of a 1:1 mixture of S-MEM and Matrigel. Tumors were size matched at approximately 200-250 mm3. Treatments ABBV-221 at 3 mg/kg every 4th day by intraperitoneal injection.    Click to Show/Hide
In Vivo Model	NCI-H441 lung xenograft tumor model
In Vitro Model	Lung papillary adenocarcinoma	NCI-H441 cells		CVCL_1561
Experiment 3 Reporting the Activity Date of This ADC					[371]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 66.60%	High EGFR expression (EGFR+++)
Method Description	To generate xenografts, a suspension of viable tumors cells mixed with an equal amount of Matrigel was injected subcutaneously into the flank of 6- to 8-week old mice. The injection volume was 0.2 mL composed of a 1:1 mixture of S-MEM and Matrigel. Tumors were size matched at approximately 200-250 mm3. Treatments ABBV-221 at 4 mg/kg every 4th day by intraperitoneal injection.    Click to Show/Hide
In Vivo Model	EBC1 lung xenograft tumor model
In Vitro Model	Lung squamous cell carcinoma	EBC-1 cells		CVCL_2891
Experiment 4 Reporting the Activity Date of This ADC					[371]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100%	High EGFR expression (EGFR+++)
Method Description	To generate xenografts, a suspension of viable tumors cells mixed with an equal amount of Matrigel was injected subcutaneously into the flank of 6- to 8-week old mice. The injection volume was 0.2 mL composed of a 1:1 mixture of S-MEM and Matrigel. Tumors were size matched at approximately 200-250 mm3. Treatments ABBV-221 at 1 mg/kg every 4th day by intraperitoneal injection.    Click to Show/Hide
In Vivo Model	NCI-H1703 lung xenograft tumor model
In Vitro Model	Lung squamous cell carcinoma	NCI-H1703 cells		CVCL_1490

Experiment 1 Reporting the Activity Date of This ADC					[374]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 89.80%	Positive EGFR expression (EGFR+++/++)
Method Description	To establish xenografts, 2 x 106 MSTO-211H cells mixed with 75-uL Matrigel were injected subcutaneously in the right flank of 5 to 6-week-old female BALB/c nu/nu miceFor the MSTO-211H study, mice received either ABT-414, ABBV-221 or ADC control (3 mg/kg) every 4 days.
In Vivo Model	MSTO-211H CDX model
In Vitro Model	Pleural biphasic mesothelioma	MSTO-211H cells		CVCL_1430
Experiment 2 Reporting the Activity Date of This ADC					[371]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.2 nM	Positive EGFR vIII expression (EGFR vIII+++/++)
Method Description	Cells were plated at 1,000 to 3,000 cells/well in complete growth medium containing 10% FBS in 96-well plates. The following day medium was removed and replaced with fresh media containing titrations of antibodies or ADCs, and cells were incubated for 72 hours at 37°C in a humidified CO2 incubator. Cell viability was then assessed using an ATPlite luminescence assay.Cell viability was determined following incubation with ABBV-221 for 72 hours.    Click to Show/Hide
In Vitro Model	Glioblastoma	U87MGde2-7 cells (EGFRvIII overexpression)		CVCL_0022
Experiment 3 Reporting the Activity Date of This ADC					[371]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1 nM	High EGFR expression (EGFR+++)
Method Description	Cells were plated at 1,000 to 3,000 cells/well in complete growth medium containing 10% FBS in 96-well plates. The following day medium was removed and replaced with fresh media containing titrations of antibodies or ADCs, and cells were incubated for 72 hours at 37°C in a humidified CO2 incubator. Cell viability was then assessed using an ATPlite luminescence assay.Cell viability was determined following incubation with ABBV-221 for 72 hours.    Click to Show/Hide
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037
Experiment 4 Reporting the Activity Date of This ADC					[371]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	4 nM	High EGFR expression (EGFR+++)
Method Description	Cells were plated at 1,000 to 3,000 cells/well in complete growth medium containing 10% FBS in 96-well plates. The following day medium was removed and replaced with fresh media containing titrations of antibodies or ADCs, and cells were incubated for 72 hours at 37°C in a humidified CO2 incubator. Cell viability was then assessed using an ATPlite luminescence assay.Cell viability was determined following incubation with ABBV-221 for 72 hours.    Click to Show/Hide
In Vitro Model	Lung squamous cell carcinoma	NCI-H1703 cells		CVCL_1490
Experiment 5 Reporting the Activity Date of This ADC					[371]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	8 nM	High EGFR expression (EGFR+++)
Method Description	Cells were plated at 1,000 to 3,000 cells/well in complete growth medium containing 10% FBS in 96-well plates. The following day medium was removed and replaced with fresh media containing titrations of antibodies or ADCs, and cells were incubated for 72 hours at 37°C in a humidified CO2 incubator. Cell viability was then assessed using an ATPlite luminescence assay.Cell viability was determined following incubation with ABBV-221 for 72 hours.    Click to Show/Hide
In Vitro Model	Colon adenocarcinoma	LoVo cells		CVCL_0399
Experiment 6 Reporting the Activity Date of This ADC					[371]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	8 nM	High EGFR expression (EGFR+++)
Method Description	Cells were plated at 1,000 to 3,000 cells/well in complete growth medium containing 10% FBS in 96-well plates. The following day medium was removed and replaced with fresh media containing titrations of antibodies or ADCs, and cells were incubated for 72 hours at 37°C in a humidified CO2 incubator. Cell viability was then assessed using an ATPlite luminescence assay.Cell viability was determined following incubation with ABBV-221 for 72 hours.    Click to Show/Hide
In Vitro Model	Lung mucoepidermoid carcinoma	NCI-H292 cells		CVCL_0455
Experiment 7 Reporting the Activity Date of This ADC					[371]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	11 nM	High EGFR expression (EGFR+++)
Method Description	Cells were plated at 1,000 to 3,000 cells/well in complete growth medium containing 10% FBS in 96-well plates. The following day medium was removed and replaced with fresh media containing titrations of antibodies or ADCs, and cells were incubated for 72 hours at 37°C in a humidified CO2 incubator. Cell viability was then assessed using an ATPlite luminescence assay.Cell viability was determined following incubation with ABBV-221 for 72 hours.    Click to Show/Hide
In Vitro Model	Lung adenocarcinoma	HCC827ER cells		CVCL_V408
Experiment 8 Reporting the Activity Date of This ADC					[371]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	69 nM	Moderate EGFR expression (EGFR++)
Method Description	Cells were plated at 1,000 to 3,000 cells/well in complete growth medium containing 10% FBS in 96-well plates. The following day medium was removed and replaced with fresh media containing titrations of antibodies or ADCs, and cells were incubated for 72 hours at 37°C in a humidified CO2 incubator. Cell viability was then assessed using an ATPlite luminescence assay.Cell viability was determined following incubation with ABBV-221 for 72 hours.    Click to Show/Hide
In Vitro Model	Lung squamous cell carcinoma	EBC-1 cells		CVCL_2891
Experiment 9 Reporting the Activity Date of This ADC					[371]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	80 nM	Moderate EGFR expression (EGFR++)
Method Description	Cells were plated at 1,000 to 3,000 cells/well in complete growth medium containing 10% FBS in 96-well plates. The following day medium was removed and replaced with fresh media containing titrations of antibodies or ADCs, and cells were incubated for 72 hours at 37°C in a humidified CO2 incubator. Cell viability was then assessed using an ATPlite luminescence assay.Cell viability was determined following incubation with ABBV-221 for 72 hours.    Click to Show/Hide
In Vitro Model	Lung papillary adenocarcinoma	NCI-H441 cells		CVCL_1561
Experiment 10 Reporting the Activity Date of This ADC					[371]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1000 nM	Low EGFR expression (EGFR+)
Method Description	Cells were plated at 1,000 to 3,000 cells/well in complete growth medium containing 10% FBS in 96-well plates. The following day medium was removed and replaced with fresh media containing titrations of antibodies or ADCs, and cells were incubated for 72 hours at 37°C in a humidified CO2 incubator. Cell viability was then assessed using an ATPlite luminescence assay.Cell viability was determined following incubation with ABBV-221 for 72 hours.    Click to Show/Hide
In Vitro Model	Colon adenocarcinoma	SW620 cells		CVCL_0547
Experiment 11 Reporting the Activity Date of This ADC					[371]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1000 nM	Low EGFR expression (EGFR+)
Method Description	Cells were plated at 1,000 to 3,000 cells/well in complete growth medium containing 10% FBS in 96-well plates. The following day medium was removed and replaced with fresh media containing titrations of antibodies or ADCs, and cells were incubated for 72 hours at 37°C in a humidified CO2 incubator. Cell viability was then assessed using an ATPlite luminescence assay.Cell viability was determined following incubation with ABBV-221 for 72 hours.    Click to Show/Hide
In Vitro Model	Colon adenocarcinoma	HCT 15 cells		CVCL_0292

Experiment 1 Reporting the Activity Date of This ADC					[376]
Efficacy Data	Progression Free Survival	5.8 months
Patients Enrolled	Eligible patients include those with MUC16+ ovarian/pancreatic cancers (ECOG 0-1, measurable disease) who progressed after 1-2 prior therapies, excluding those with recent anti-tumor therapy, MUC16/MMAE-targeted treatment, active infections, uncontrolled comorbidities, CNS metastases, or Grade >1 toxicities from prior treatment.
Administration Dosage	DMUC4064A will be administered to participants at a starting dose of 1.0 milligram per kilogram (mg/kg) by IV infusion q3w and would be monitored for DLTs for 21 days after first infusion of Cycle 1 (cycle length=21 days).
Related Clinical Trial
NCT Number	NCT02146313	Phase Status	PHASE1
Clinical Description	A Phase I, Open-Label, Dose-Escalation Study of the Safety, Tolerability, and Pharmacokinetics of DMUC4064A Administered Intravenously to Patients With Platinum-Resistant Ovarian Cancer or Unresectable Pancreatic Cancer
Primary Endpoint	The study evaluates dose-limiting toxicities (DLTs) during Cycle 1 (21 days) to determine maximum tolerated dose (MTD) and recommended Phase II dose of DMUC4064A, while monitoring adverse events (AEs/SAEs) over approximately 3.5 years.
Other Endpoint	Key outcomes include immunogenicity (anti-DMUC4064A antibodies), pharmacokinetic profile, objective response rate (RECIST v1.1), duration of response, and progression-free survival in platinum-resistant ovarian cancer and unresectable pancreatic cancer patients over 3.5 years.

Experiment 1 Reporting the Activity Date of This ADC					[379]
Patients Enrolled	Histologically documented, incurable, locally advanced or metastatic disease for which no standard therapy exists, consisting of one of the following: Unresectable pancreatic ductal adenocarcinoma or platinum-resistant ovarian cancer
Administration Dosage	Injection of 89Zr-MMOT0530A followed by 2 or 3 PET scans at different time points
Related Clinical Trial
NCT Number	NCT01832116	Phase Status	PHASE1
Clinical Description	89Zr-MMOT0530A PET Imaging in Patients With Unresectable Pancreatic or Platinum-resistant Ovarian Cancer Before Treatment With DMOT4039A. A Separate Study to the Phase I Study Protocol DMO4993g
Primary Endpoint	The in vivo biodistribution measured in SUV values and organ pharmacokinetics (PK) of 89Zr-MMOT0530A [Time Frame: Approximately 1 year]
Other Endpoint	The 89Zr-MMOT0530A tumor uptake measured in SUV related to the response to DMOT4039A therapy according to RECISt 1.1 criteria [Time Frame: Approximately 1 year], Number of patients with adverse events after 89Zr-MMOT0530A injection as a measure of safety and tolerability [Time Frame: Approximately 1 year]
Experiment 2 Reporting the Activity Date of This ADC					[380]
Patients Enrolled	Eastern Cooperative Oncology Group (ECOG) performance status 0 or 1.Histologically documented, incurable, locally advanced or metastatic disease for which no standard therapy exists, consisting of one of the following: Unresectable pancreatic ductal adenocarcinoma or platinum-resistant ovarian cancer.
Administration Dosage	Participants in different cohorts will receive DMOT4039A at various escalating dose levels, starting with 0.2 milligrams per kilogram (mg/kg), as intravenous infusion every 3 weeks (Q3W) to determine the maximum tolerated dose (MTD) of DMOT4039A for until disease progression, loss of clinical benefit or unacceptable toxicity, whichever occurred first (up to approximately 2.5 years    Click to Show/Hide
Related Clinical Trial
NCT Number	NCT01469793	Phase Status	PHASE1
Clinical Description	A Phase I, Open Label Study of the Safety and Pharmacokinetics of Escalating Doses of DMOT4039A in Patients With Unresectable Pancreatic or Platinum-Resistant Ovarian Cancer
Primary Endpoint	Maximum Tolerated Dose (MTD) of DMOT4039A, Number of Participants With Dose-Limiting Toxicities (DLTs), Recommended Phase 2 Dose (RP2D) of DMOT4039A.
Other Endpoint	Pharmacokinetics: area under the concentration-time curve (AUC), Serum anti-therapeutic antibody levels, Objective response (complete response or partial response), tumor assessments according to RECIST criteria, Duration of response, Progression-free survival.

Experiment 1 Reporting the Activity Date of This ADC					[387]
Patients Enrolled	Inclusion: Metastatic pancreatic adenocarcinoma or AGS-5+ gastric/GEJ adenocarcinoma (measurable disease ≥10-15 mm), ECOG 0-1; untreated or ≤1 prior systemic therapy (2/4-week washout). Exclusion: CNS metastases, active malignancy (<3y remission), recent cardiac/CV events (NYHA III-IV), or untreated major organ dysfunction.
Administration Dosage	0.3-3.0 mg/kg IV on Days 1, 8, and 15 of 28-day cycles
Related Clinical Trial
NCT Number	NCT01166490	Phase Status	PHASE1
Clinical Description	A Phase 1, Open-Label, Dose Escalation Study of ASG-5ME in Patients With Pancreatic or Gastric Adenocarcinoma
Primary Endpoint	Safety analysis includes incidence of adverse events and lab abnormalities (assessed until 1 month post-treatment), ASG-5ME/metabolite blood concentrations, and antitherapeutic antibody development.
Other Endpoint	Efficacy measures involve best clinical response (assessed every 2 months), overall survival, progression-free survival (monthly until death/study closure), and pharmacokinetic monitoring of ASG-5ME.
Experiment 2 Reporting the Activity Date of This ADC					[388]
Patients Enrolled	Inclusion: Castration-resistant prostate cancer (progression post-standard therapy, no effective therapy, or patient declines), testosterone ≤50 ng/dL, ECOG 0-1, life expectancy >6 months, adequate hematologic/renal/hepatic function, stable LHRH/GnRH therapy, prior docetaxel allowed only if refractory/intolerant. Exclusion: CNS metastases, active malignancy (<3-year remission), significant cardiac disease, recent chemo/radiation/anti-androgens, neuropathy ≥grade 2, major surgery/infection, HIV/HepB/HepC positivity, recent thromboembolic events.    Click to Show/Hide
Related Clinical Trial
NCT Number	NCT01228760	Phase Status	PHASE1
Clinical Description	A Phase 1, Open-label, Multi-center, Dose Escalation Study of the Safety and Pharmacokinetics of ASG-5ME Monotherapy in Subjects With Castration-Resistant Prostate Cancer (CRPC)
Primary Endpoint	Safety is evaluated through adverse events, lab tests (hematology, biochemistry), and vital signs during the 12-week treatment and 4-week follow-up. Pharmacokinetics of ASG-5ME is analyzed via blood samples (Cycle 1 & 4, pre-dose Cycles 2 & 3, and periodically thereafter if treatment continues).
Other Endpoint	Efficacy measures include anti-ASG-5ME antibody formation, tumor response (every 12 weeks), PSA levels, bone scans, circulating tumor cells, and cytokeratin-18 levels (assessed periodically during treatment).

Experiment 1 Reporting the Activity Date of This ADC					[390]
Patients Enrolled	Eligibility requires adults (≥18) with ECOG 0-2, relapsed/refractory myeloma (prior proteasome inhibitor/immunomodulatory therapy), and measurable disease. Exclusions: recent mAb/chemotherapy (≤4/2 weeks), unresolved toxicities (except neuropathy), recent transplants, antibody allergies, active infections, or hepatitis/HIV. Pregnancy is prohibited.    Click to Show/Hide
Administration Dosage	multiple ascending doses
Related Clinical Trial
NCT Number	NCT01432353	Phase Status	PHASE1
Clinical Description	An Open-label, Multicenter, Phase I Trial of the Safety and Pharmacokinetics of Escalating Doses of DFRF4539A in Patients With Relapsed or Refractory Multiple Myeloma
Primary Endpoint	The study evaluates safety outcomes including AE incidence over 3.5 years, MTD/DLT determination within 1.5 years, and establishes the RP2D for DFRF4539A administered every 3 weeks or weekly.
Other Endpoint	Immunogenicity (serum ATA levels) and PK (AUC) are monitored over 3.5 years. Efficacy is assessed via IMWG/EBMT criteria for objective response, DoR (time to progression/death), and PFS (from treatment initiation to progression/death within 30 days post-treatment).

Experiment 1 Reporting the Activity Date of This ADC					[397]
Patients Enrolled	Eligible patients were adults with advanced melanoma (Stage III/IV) resistant to prior therapies, adequate organ function, and measurable disease. Exclusions included recent anticancer treatments (21 days for cytotoxic/antibody therapies), active infections, CNS metastases, prior MMAE-ADC treatment, or significant comorbidities.
Administration Dosage	DEDN6526A (0.3-2.8 mg/kg) was given intravenously every 3 weeks (q3w) to pts with metastatic or unresectable cutaneous, mucosal, or ocular (uveal) melanoma in a 3+3 design to determine the maximum-tolerated dose, followed by cohort expansion at the recommended phase II dose (RP2D).
Related Clinical Trial
NCT Number	NCT01522664	Phase Status	PHASE1
Clinical Description	A Phase I, Open-Label Study of the Safety and Pharmacokinetics of Escalating Doses of DEDN6526A in Patients With Metastatic or Unresectable Melanoma
Primary Endpoint	Safety evaluation included ongoing monitoring of adverse events (up to 90 days post-treatment), determination of maximum tolerated dose/dose-limiting toxicities, and establishment of recommended Phase II dose over approximately 2 years.
Other Endpoint	Pharmacokinetic assessments covered concentration-time curve analysis and anti-therapeutic antibody monitoring during treatment cycles, with tumor response evaluated via RECIST criteria for approximately 1 year.
Experiment 2 Reporting the Activity Date of This ADC					[397]
Patients Enrolled	Eligibility requires adult Stage III/IV melanoma patients (ECOG 0-1, failed ≥1 prior therapies) with adequate organ function. Key exclusions include recent anticancer treatments (21-day washout), active CNS metastases, Grade ≥2 toxicities, MMAE-ADC exposure, or uncontrolled comorbidities. Contraception is mandated for 6 months post-treatment.
Administration Dosage	DEDN6526A (0.3-2.8 mg/kg) was given intravenously every 3 weeks (q3w) to pts with metastatic or unresectable cutaneous, mucosal, or ocular (uveal) melanoma in a 3+3 design to determine the maximum-tolerated dose, followed by cohort expansion at the recommended phase II dose (RP2D).
Related Clinical Trial
NCT Number	NCT01522664	Phase Status	PHASE1
Clinical Description	A Phase I, Open-Label Study of the Safety and Pharmacokinetics of Escalating Doses of DEDN6526A in Patients With Metastatic or Unresectable Melanoma
Primary Endpoint	Safety will be continuously monitored for adverse events through 90 days post-treatment, while dose-limiting toxicities and MTD will be evaluated over one year to establish the recommended Phase II dose within approximately two years.
Other Endpoint	PK parameters including AUC will be assessed through serial sampling (pre/post-dose during Cycles 1-5), alongside ATA monitoring and tumor response evaluations per RECIST criteria for approximately one year.