Linker ID	LIN0TAFAV
Linker Name	Maleimido-caproyl
Linker Type	Flexible reactive (thiol) linker
Antibody-Linker Relation	Uncleavable
Structure
	3D MOL			2D MOL
Formula	C10H13NO4
Isosmiles	O=C(O)CCCCCN1C(=O)C=CC1=O
InChI	InChI=1S/C10H13NO4/c12-8-5-6-9(13)11(8)7-3-1-2-4-10(14)15/h5-6H,1-4,7H2,(H,14,15)
InChIKey	WOJKKJKETHYEAC-UHFFFAOYSA-N
Pharmaceutical Properties	Molecule Weight		211.217	Polar area		74.68
	Complexity		15	xlogp Value		0.5564
	Heavy Count		15	Rot Bonds		6
	Hbond acc		3	Hbond Donor		1

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Objective Response Rate (ORR)	56.30%	High BCMA expression (BCMA +++)
Patients Enrolled	Eligible adult (18 years of age) patients for part 2 had histologically or cytologically confirmed MM, Eastern Cooperative Oncology Group performance status 0 or 1, prior therapy with alkylators, proteasome inhibitors and immunomodulators, and were refractory to the last line of treatment.
Administration Dosage	GSK2857916 3.4 mg/kg was administered through 1-h intravenous infusions once every 3 weeks, for a maximum of 16 cycles.
Related Clinical Trial
NCT Number	NCT02064387	Clinical Status	Phase 1
Clinical Description	A Phase I open-label, dose escalation study to investigate the safety, pharmacokinetics, pharmacodynamics, immunogenicity and clinical activity of the antibody drug conjugate GSK2857916 in subjects with relapsed/refractory multiple myeloma and other advanced hematologic malignancies expressing BCMA.
Primary Endpoint	Objective response rate=60.00% (95% CI 42.10-76.10),comprising 3 (9.00%) complete responses and 14.00 (40%) partial responses.
Other Endpoint	The median progression-free survival was 12.00 months and the median duration of response was 14.30 months.
Experiment 2 Reporting the Activity Date of This ADC					[2]
Efficacy Data	Objective Response Rate (ORR)	60%
Patients Enrolled	Histologically or cytologically confirmed MM, a European Cooperative Oncology Group performance status of 0 or 1, prior therapy with alkylators, PI and IMiD, had undergone stem cell transplant (if eligible) and refractory to the last line of treatment (defined as progressive disease on or within 60 days of completion of the last therapy) that included stem cell transplant and those patients with a history of autologous stem cell transplant must have received the transplant >100 days prior to study enrolment and have no active infection.    Click to Show/Hide
Administration Dosage	Doses ranging between 0.03 mg/kg and 4.60 mg/kg was administered as a 1-hour intravenous infusion every 3 weeks for a maximum of 16 cycles.
Related Clinical Trial
NCT Number	NCT02064387	Clinical Status	Phase 1
Clinical Description	A phase 1 open-label, dose escalation study to investigate the safety, pharmacokinetics, pharmacodynamics, immunogenicity and clinical activity of the antibody drug conjugate GSK2857916 in subjects with relapsed/refractory multiple myeloma and other advanced hematologic malignancies expressing BCMA.
Primary Endpoint	The primary endpoints of the trial were to determine the safety, tolerability, maximum tolerated dose (MTD) and RP2D and schedule of GSK2857916. Median PFS (post hoc analysis) was 7.90 months (95% CI: 3.1-not estimable),Overall response rate at 3.40 mg/kg in Part 2 was 60.00% (21/35; 95% confidence interval: 42.10%-76.10%).
Other Endpoint	PK profile (single dose area under the curve, maximum serum concentration [Cmax], time to Cmax , clearance, steady-state volume of distribution [Vss], half-life [t]; repeat dose Cmax and trough plasma concentration), the incidence of anti-drug antibodies, and clinical activity measured as overall response rate (ORR), defined as the percentage of subjects achieving confirmed partial response or better (PR) and clinical benefit rate, defined as the percentages of subjects with minimal response or better (MR).    Click to Show/Hide
Experiment 3 Reporting the Activity Date of This ADC					[3]
Related Clinical Trial
NCT Number	NCT03769506	Clinical Status	Phase 3
Clinical Description	A phase 3, randomized, double-arm, open-label, controlled trial of ASP-1929 photoimmunotherapy versus physician's choice standard of care for the treatment of locoregional, recurrent head and neck squamous cell carcinoma in patients who have failed or progressed on or after at least two lines of therapy, of which at least one line must be systemic therapy.    Click to Show/Hide

Experiment 1 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Half Maximal Effective Concentration (EC50)	30.6 ug/mL	Moderate BCMA expression (BCMA++)
Method Description	Cells (5 x 105 cells/mL) were left untreated or exposed to the indicated treatments for the indicated time. Cells were counted on a Vi-Cell-XR Cell Viability Analyzer (Beckman Coulter).
In Vitro Model	Thymoma	EL4 cells (BCMA expression)		CVCL_0255

Experiment 1 Reporting the Activity Date of This ADC					[5]
Efficacy Data	Objective Response Rate (ORR)	41.40%
Patients Enrolled	Eligible patients must have HER2-positive (IHC 3+/ISH+) advanced breast/gastric cancer unamenable to standard therapy, measurable lesions (RECIST 1.1), ECOG 0-1, adequate organ function, and anthracycline exposure below doxorubicin-equivalent 360mg/m2. Exclusions cover active HBV/HCV/HIV, uncontrolled infections, severe cardiopulmonary diseases (NYHA ≥2, CHF, recent MI), symptomatic CNS metastases, or Grade ≥2 neuropathy.    Click to Show/Hide
Administration Dosage	This trial was conducted in subjects with histologically confirmed HER2-positive breast cancer (having evaluable lesions and an Eastern Cooperative Oncology Group performance status of 0 or 1) using a 3 + 3 design of escalating BAT8001 doses. Patients received BAT8001 intravenously in a 21-day cycle, with dose escalation in 5 cohorts: 1.2, 2.4, 3.6, 4.8, and 6.0 mg/kg. The primary objective was to evaluate the safety and tolerability of BAT8001. Preliminary activity of BAT8001 was also assessed as a secondary objective.    Click to Show/Hide
Related Clinical Trial
NCT Number	NCT04189211	Clinical Status	PHASE1
Clinical Description	An Open-Label, Dose Escalation Phase I Clinical Trial on Safety, Tolerability and Pharmacokinetics of BAT8001 for Injection in Patients With HER2-Positive Solid Tumors
Primary Endpoint	Primary safety endpoints include dose-limiting toxicity (DLT) criteria spanning hematologic, hepatic, cardiac (e.g., LVEF ≤45% with ≥10% decrease) and other organ toxicities (Grade ≥3) assessed over 21 days post-dose. Pharmacokinetic parameters (AUC, Cmax, t1/2) of BAT8001, total antibody, and batansine are evaluated during Cycles 1-4 (21-day cycles), alongside immunogenicity monitoring (ADA/NADA). Maximum tolerated dose (MTD) is determined when ≤1/6 patients experience DLT.    Click to Show/Hide
Other Endpoint	Efficacy measures comprise progression-free survival (PFS) and overall response rate (ORR) per RECIST v1.1, tracked from baseline until study conclusion (up to 3 years).
Experiment 2 Reporting the Activity Date of This ADC					[5]
Efficacy Data	Disease control rate (DCR)	82.80%
Patients Enrolled	Eligible patients must have HER2-positive (IHC 3+/ISH+) advanced breast/gastric cancer unamenable to standard therapy, measurable lesions (RECIST 1.1), ECOG 0-1, adequate organ function, and anthracycline exposure below doxorubicin-equivalent 360mg/m2. Exclusions cover active HBV/HCV/HIV, uncontrolled infections, severe cardiopulmonary diseases (NYHA ≥2, CHF, recent MI), symptomatic CNS metastases, or Grade ≥2 neuropathy.    Click to Show/Hide
Administration Dosage	This trial was conducted in subjects with histologically confirmed HER2-positive breast cancer (having evaluable lesions and an Eastern Cooperative Oncology Group performance status of 0 or 1) using a 3 + 3 design of escalating BAT8001 doses. Patients received BAT8001 intravenously in a 21-day cycle, with dose escalation in 5 cohorts: 1.2, 2.4, 3.6, 4.8, and 6.0 mg/kg. The primary objective was to evaluate the safety and tolerability of BAT8001. Preliminary activity of BAT8001 was also assessed as a secondary objective.    Click to Show/Hide
Related Clinical Trial
NCT Number	NCT04189211	Clinical Status	PHASE1
Clinical Description	An Open-Label, Dose Escalation Phase I Clinical Trial on Safety, Tolerability and Pharmacokinetics of BAT8001 for Injection in Patients With HER2-Positive Solid Tumors
Primary Endpoint	Primary safety endpoints include dose-limiting toxicity (DLT) criteria spanning hematologic, hepatic, cardiac (e.g., LVEF ≤45% with ≥10% decrease) and other organ toxicities (Grade ≥3) assessed over 21 days post-dose. Pharmacokinetic parameters (AUC, Cmax, t1/2) of BAT8001, total antibody, and batansine are evaluated during Cycles 1-4 (21-day cycles), alongside immunogenicity monitoring (ADA/NADA). Maximum tolerated dose (MTD) is determined when ≤1/6 patients experience DLT.    Click to Show/Hide
Other Endpoint	Efficacy measures comprise progression-free survival (PFS) and overall response rate (ORR) per RECIST v1.1, tracked from baseline until study conclusion (up to 3 years).
Experiment 3 Reporting the Activity Date of This ADC					[6]
Patients Enrolled	Inclusion criteria require HER2-positive breast cancer (IHC 3+/FISH+), prior taxane/trastuzumab therapy, measurable lesions (RECIST 1.1), ECOG 0-1, LVEF ≥50%, and contraception for participants of childbearing potential. Exclusion criteria include grade ≥2 neuropathy, active brain metastases, unresolved radiation toxicity, severe cardio-pulmonary diseases, recent myocardial infarction, uncontrolled systemic illness, malabsorption disorders, or intolerance to trastuzumab.    Click to Show/Hide
Administration Dosage	3.6 mg/kg, q3w, administered intravenously on day 1 of each treatment cycle, 21 days/treatment cycle.
Related Clinical Trial
NCT Number	NCT04185649	Clinical Status	PHASE3
Clinical Description	A Clinical Study Evaluating the Efficacy and Safety of BAT8001 Injection for the Treatment of HER2-positive Advanced Breast Cancer - A Multicenter, Randomized, Open-label, Positive-controlled, Superiority Phase III Clinical Trial in China
Primary Endpoint	The primary endpoint is progression-free survival (PFS), defined as time from randomization to disease progression (RECIST v1.1) or death, assessed up to 18 months.
Other Endpoint	Secondary endpoints include overall survival (OS), objective response rate (ORR), duration of response (DOR), clinical benefit rate (CBR), serum concentrations of BAT8001 and its total antibody, plasma concentration of batansine, and percentage of participants with anti-therapeutic antibodies (ATA), all measured up to 30 months.
Experiment 4 Reporting the Activity Date of This ADC					[7]
Patients Enrolled	Eligible patients (18-75 years) must have HER2-positive advanced solid tumors (IHC 3+/ISH+) with ECOG 0-1, measurable lesions (RECIST 1.1), and adequate organ function. Exclusions include recent anti-tumor therapy (≤4 weeks), uncontrolled CNS metastases, active autoimmune diseases, severe cardiovascular conditions, or prior anthracycline overdose (doxorubicin >360mg/m2 equivalent).    Click to Show/Hide
Administration Dosage	Experimental: 2.4mg/kg of BAT8001 Drug:BAT1306 100mg/4ml/box, 200mg IV infusions ,BAT8001 100mg/box, 2.4mg/kg IV infusions Experimental: 3.6mg/kg of BAT8001 Drug:BAT1306 100mg/4ml/box, 200mg IV infusions ,BAT8001 100mg/box,3.6mg/kg IV infusions
Related Clinical Trial
NCT Number	NCT04151329	Clinical Status	PHASE1|||PHASE2
Clinical Description	Evaluation for the Safety of BAT1306 and BAT8001 Injection for the Treatment of Patients With HER2-positive Advanced Solid Tumors Phase I/IIa Clinical Trials of Sexual, Tolerability and Pharmacokinetic Characteristics
Primary Endpoint	Primary endpoints include dose-limiting toxicity (DLT) for safety assessment over 3 weeks, along with pharmacokinetic parameters (AUC, Cmax, t1/2). Immunogenicity measures (ADA and NADA) are evaluated throughout the study period (avg. 6-12 months).
Other Endpoint	Efficacy assessments consist of ORR, PFS, DCR, and DOR as secondary endpoints, monitored through study completion (avg. 6-12 months).
Experiment 5 Reporting the Activity Date of This ADC					[8]
Efficacy Data	Objective Response Rate (ORR)	41.40%
Patients Enrolled	HER2-positive locally advanced or metastatic breast cancer.
Administration Dosage	Patients received BAT8001 intravenously in a 21-day cycle, with dose escalation in 5 cohorts: 1.20, 2.40, 3.60, 4.80, and 6.00 mg/kg.
Related Clinical Trial
NCT Number	NCT04189211	Clinical Status	Phase 1
Clinical Description	An open-label, dose escalation phase 1 clinical trial on safety, tolerability and pharmacokinetics of BAT8001 for injection in patients with HER2-positive solid tumors.
Primary Endpoint	For BAT8001, 3.60 mg/kg was determined to be the MTD.
Experiment 6 Reporting the Activity Date of This ADC					[9]
Related Clinical Trial
NCT Number	NCT04185649	Clinical Status	Phase 3
Clinical Description	A clinical study evaluating the efficacy and safety of BAT8001 injection for the treatment of HER2-positive advanced breast cancer - a multicenter, randomized, open-label, positive-controlled, superiority phase 3 clinical trial in china.
Experiment 7 Reporting the Activity Date of This ADC					[10]
Related Clinical Trial
NCT Number	NCT04151329	Clinical Status	Phase 1/2
Clinical Description	Evaluation for the safety of BAT1306 and BAT8001 injection for the treatment of patients with HER2-positive advanced solid tumors phase 1/2a clinical trials of sexual, tolerability and pharmacokinetic characteristics.
Experiment 8 Reporting the Activity Date of This ADC					[11]
Related Clinical Trial
NCT Number	NCT04189211	Clinical Status	Phase 1
Clinical Description	An open-label, dose escalation phase 1 clinical trial on safety, tolerability and pharmacokinetics of BAT8001 for injection in patients with HER2-positive solid tumors.

Experiment 1 Reporting the Activity Date of This ADC					[12]
Efficacy Data	stable disease (SD)	50%
Patients Enrolled	Exclusion criteria comprise uncontrolled CNS metastases, investigational drug use within 4 weeks prior, AGS-16C3F hypersensitivity, thromboembolic events (≤3 months), severe cardiac conditions (e.g., CHF Class III/IV), major surgery within 4 weeks, pregnancy/lactation, HIV/hepatitis B/C positivity, active infections requiring systemic treatment, or recent eye surgery/cataracts affecting vision.    Click to Show/Hide
Administration Dosage	ADCs were given q3w until PD or unacceptable toxicity.AGS-16M8F and AGS-16C3F studies treated 26 and 34 subjects in dose range 0.6 - 4.8 and 1.8 - 4.8 mg/kg, respectively.
Related Clinical Trial
NCT Number	NCT01672775	Clinical Status	PHASE1
Clinical Description	A Phase 1, Open Label, Multi-center Study to Assess the Safety, Pharmacokinetics and Effectiveness of AGS-16C3F Monotherapy in Subjects With Renal Cell Carcinoma (RCC) of Clear Cell or Papillary Histology
Primary Endpoint	The study evaluates the incidence of adverse events over 24 months and assesses pharmacokinetics (TAb, ADC, MMAF) including Ceoi/Cmax, Ctrough, Tmax, AUCτ, t1/2, CL, Vss at specified time points up to Day 92. Secondary endpoints include antidrug antibody formation, tumor response (ORR, DCR), and bone scan changes during the study period.
Other Endpoint	Eligible participants include metastatic RCC patients (clear cell/non-clear cell or papillary histology) with prior anti-VEGFR therapy (clear cell) or ENPP3+ status (non-clear cell/papillary). Key requirements: measurable disease (RECIST 1.1), ECOG 0-1, adequate hematologic (ANC ≥1.5x109/L, platelet ≥100x109/L, Hb ≥9 g/dL), renal (creatinine ≤1.5xULN or GFR >50 mL/min), and hepatic function (AST/ALT ≤2.5xULN or ≤5xULN with metastases; bilirubin ≤1.5xULN). Contraception is mandated for participants of childbearing potential.    Click to Show/Hide
Experiment 2 Reporting the Activity Date of This ADC					[13]
Efficacy Data	Progression Free Survival	3.5 months
Patients Enrolled	Exclusion criteria comprised prior axitinib/AGS-16C3F treatment, untreated or unstable brain metastases (>3 months post-radiation/surgery if treated), uncontrolled hypertension (>150/90), GI disorders affecting absorption, active ocular conditions (e.g., infections, corneal ulcers, glaucoma), strong CYP3A4/5 inhibitors/inducers use within 14 days, thromboembolic events (≤4 weeks unless anticoagulated), bleeding disorders (≤2 months), severe cardiac disease (NYHA Class III/IV, MI ≤6 months), major surgery ≤4 weeks, pregnancy/lactation, unresolved infections, or inability to comply with study protocols.    Click to Show/Hide
Administration Dosage	Participants received 1.8 milligram per kilogram (mg/kg) of AGS-16C3F once every three weeks by single intravenous (IV) infusion.
Related Clinical Trial
NCT Number	NCT02639182	Clinical Status	PHASE2
Clinical Description	A Multi-Center, Open Label, Randomized Phase 2 Study of AGS-16C3F vs. Axitinib in Metastatic Renal Cell Carcinoma
Primary Endpoint	The study assessed Progression-Free Survival (PFS) per RECIST v1.1 by investigator (up to 53 months) and central radiology review (up to 40 months), along with Objective Response Rate (ORR), Duration of Response (DOR), Overall Survival (OS), and Disease Control Rate (DCR). Pharmacokinetic parameters (Cmax, Ctrough, Tmax, AUC0- 21, t1/ 2) for ADC, TAb, and Cys-mcMMAF were evaluated over 21-day cycles. Adverse events (AEs) were monitored for 53 months, with serious AEs requiring intervention or hospitalization.    Click to Show/Hide
Experiment 3 Reporting the Activity Date of This ADC					[12]
Efficacy Data	Partial Response (PR)	8.80%
Patients Enrolled	Exclusion criteria comprise uncontrolled CNS metastases, investigational drug use within 4 weeks prior, AGS-16C3F hypersensitivity, thromboembolic events (≤3 months), severe cardiac conditions (e.g., CHF Class III/IV), major surgery within 4 weeks, pregnancy/lactation, HIV/hepatitis B/C positivity, active infections requiring systemic treatment, or recent eye surgery/cataracts affecting vision.    Click to Show/Hide
Administration Dosage	ADCs were given q3w until PD or unacceptable toxicity.AGS-16M8F and AGS-16C3F studies treated 26 and 34 subjects in dose range 0.6 - 4.8 and 1.8 - 4.8 mg/kg, respectively.
Related Clinical Trial
NCT Number	NCT01672775	Clinical Status	PHASE1
Clinical Description	A Phase 1, Open Label, Multi-center Study to Assess the Safety, Pharmacokinetics and Effectiveness of AGS-16C3F Monotherapy in Subjects With Renal Cell Carcinoma (RCC) of Clear Cell or Papillary Histology
Primary Endpoint	The study evaluates the incidence of adverse events over 24 months and assesses pharmacokinetics (TAb, ADC, MMAF) including Ceoi/Cmax, Ctrough, Tmax, AUCτ, t1/2, CL, Vss at specified time points up to Day 92. Secondary endpoints include antidrug antibody formation, tumor response (ORR, DCR), and bone scan changes during the study period.
Other Endpoint	Eligible participants include metastatic RCC patients (clear cell/non-clear cell or papillary histology) with prior anti-VEGFR therapy (clear cell) or ENPP3+ status (non-clear cell/papillary). Key requirements: measurable disease (RECIST 1.1), ECOG 0-1, adequate hematologic (ANC ≥1.5x109/L, platelet ≥100x109/L, Hb ≥9 g/dL), renal (creatinine ≤1.5xULN or GFR >50 mL/min), and hepatic function (AST/ALT ≤2.5xULN or ≤5xULN with metastases; bilirubin ≤1.5xULN). Contraception is mandated for participants of childbearing potential.    Click to Show/Hide
Experiment 4 Reporting the Activity Date of This ADC					[13]
Efficacy Data	Objective Response Rate (ORR)	7.50%
Patients Enrolled	Exclusion criteria comprised prior axitinib/AGS-16C3F treatment, untreated or unstable brain metastases (>3 months post-radiation/surgery if treated), uncontrolled hypertension (>150/90), GI disorders affecting absorption, active ocular conditions (e.g., infections, corneal ulcers, glaucoma), strong CYP3A4/5 inhibitors/inducers use within 14 days, thromboembolic events (≤4 weeks unless anticoagulated), bleeding disorders (≤2 months), severe cardiac disease (NYHA Class III/IV, MI ≤6 months), major surgery ≤4 weeks, pregnancy/lactation, unresolved infections, or inability to comply with study protocols.    Click to Show/Hide
Administration Dosage	Participants received 1.8 milligram per kilogram (mg/kg) of AGS-16C3F once every three weeks by single intravenous (IV) infusion.
Related Clinical Trial
NCT Number	NCT02639182	Clinical Status	PHASE2
Clinical Description	A Multi-Center, Open Label, Randomized Phase 2 Study of AGS-16C3F vs. Axitinib in Metastatic Renal Cell Carcinoma
Primary Endpoint	The study assessed Progression-Free Survival (PFS) per RECIST v1.1 by investigator (up to 53 months) and central radiology review (up to 40 months), along with Objective Response Rate (ORR), Duration of Response (DOR), Overall Survival (OS), and Disease Control Rate (DCR). Pharmacokinetic parameters (Cmax, Ctrough, Tmax, AUC0- 21, t1/ 2) for ADC, TAb, and Cys-mcMMAF were evaluated over 21-day cycles. Adverse events (AEs) were monitored for 53 months, with serious AEs requiring intervention or hospitalization.    Click to Show/Hide
Experiment 5 Reporting the Activity Date of This ADC					[13]
Efficacy Data	Disease control rate (DCR)	13.40%
Patients Enrolled	Exclusion criteria comprised prior axitinib/AGS-16C3F treatment, untreated or unstable brain metastases (>3 months post-radiation/surgery if treated), uncontrolled hypertension (>150/90), GI disorders affecting absorption, active ocular conditions (e.g., infections, corneal ulcers, glaucoma), strong CYP3A4/5 inhibitors/inducers use within 14 days, thromboembolic events (≤4 weeks unless anticoagulated), bleeding disorders (≤2 months), severe cardiac disease (NYHA Class III/IV, MI ≤6 months), major surgery ≤4 weeks, pregnancy/lactation, unresolved infections, or inability to comply with study protocols.    Click to Show/Hide
Administration Dosage	Participants received 1.8 milligram per kilogram (mg/kg) of AGS-16C3F once every three weeks by single intravenous (IV) infusion.
Related Clinical Trial
NCT Number	NCT02639182	Clinical Status	PHASE2
Clinical Description	A Multi-Center, Open Label, Randomized Phase 2 Study of AGS-16C3F vs. Axitinib in Metastatic Renal Cell Carcinoma
Primary Endpoint	The study assessed Progression-Free Survival (PFS) per RECIST v1.1 by investigator (up to 53 months) and central radiology review (up to 40 months), along with Objective Response Rate (ORR), Duration of Response (DOR), Overall Survival (OS), and Disease Control Rate (DCR). Pharmacokinetic parameters (Cmax, Ctrough, Tmax, AUC0- 21, t1/ 2) for ADC, TAb, and Cys-mcMMAF were evaluated over 21-day cycles. Adverse events (AEs) were monitored for 53 months, with serious AEs requiring intervention or hospitalization.    Click to Show/Hide
Experiment 6 Reporting the Activity Date of This ADC					[14]
Efficacy Data	Partial Response (PR)	23.08%	High ENPP3 expression (ENPP3+++)
Patients Enrolled	Metastatic renal cell carcinoma (MRCC), Eastern Cooperative Oncology Group (ECOG) performance status 1, adequate organ and bone marrow function.
Administration Dosage	AGS-16M8F was administered intravenously every 3 weeks at 5 dose levels ranging from 0.60 to 4.80 mg/kg until unacceptable toxicity or progression. A second study with AGS-16C3F started with the AGS-16M8F bridging dose of 4.80 mg/kg given every 3 weeks.
Related Clinical Trial
NCT Number	NCT01672775	Clinical Status	Phase 1
Clinical Description	A phase 1, open label, multi-center study to assess the safety, pharmacokinetics and effectiveness of AGS-16C3F monotherapy in subjects with renal cell carcinoma (RCC) of clear cell or papillary histology.
Primary Endpoint	In the AGS-16C3F study (n = 34),the MTD was 3.60 mg/kg,but this was not tolerated. The 1.80 mg/kg dose was determined to be safe and was associated antitumor response.
Other Endpoint	3 subjects at 1.80 mg/kg achieved durable PR (3/13, 23.08%). The disease control rate at 1.80 mg/kg was 92.30% (N=12/13). The disease control rate for the entire study was 58.82% (N=20/34).
Experiment 7 Reporting the Activity Date of This ADC					[15]
Efficacy Data	Objective Response Rate (ORR)	7.50 18.20 %	Moderate ENPP3 expression (ENPP3++)
Patients Enrolled	Advanced renal cell carcinoma (RCC).
Administration Dosage	Intravenous AGS-16C3F 1.80 mg/kg every 3 weeks or oral axitinib 5 mg twice daily (starting dose).
Related Clinical Trial
NCT Number	NCT02639182	Clinical Status	Phase 2
Clinical Description	A multi-center, open label, randomized phase 2 study of AGS-16C3F vs. axitinib in metastatic renal cell carcinoma.
Primary Endpoint	Median PFS=2.90 months (95% CI,2.00-4.00) for AGS16C3F,Median PFS=5.7 months (95% CI,5.30-9.10) for axitinib.
Other Endpoint	Disease Control Rate (DCR)=13.40% (95% CI,6.3-24.0) for AGS16C3F, Disease Control Rate (DCR)=22.70% (95% CI,13.30-34.70) for axitinib. Median duration of Response (mDoR)=6.80 months (95% CI,3.80-18.40) for AGS16C3F, Median duration of Response (mDoR)=6.7 months (95% CI,1.80-9.20) for axitinib. Objective Response Rate (ORR)=7.50% (95% CI,2.50-16.60) for AGS16C3F, Objective Response Rate (ORR)=18.20% (95% CI,9.80-29.60) for axitinib. Median Overall Survival (mOS)=13.10 months for AGS16C3F, Median Overall Survival (mOS)=15.40 months for axitinib.    Click to Show/Hide

Experiment 1 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.1 nM
Method Description	Cells were incubated in triplicate in medium containing AGS-16C3F or cHmLYS-1c3.G2k-mcMMAF (0 [Control],0.001,0.003,0.008,0.02,0.07,0.21,0.62,1.82,5.57,16.67,50,150,450,and 1350 nM) in a 5% CO2 incubator at 37°C for 96 hours. IC50 values at day 5 for AGS-16C3F were calculated for each cell line.
In Vitro Model	Normal	ROSA KIT D816V cells		CVCL_5G50
Experiment 2 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	2.73 nM	Moderate ENPP3 expression (ENPP3++)
Method Description	Cells were incubated in triplicate in medium containing AGS-16C3F or cHmLYS-1c3.G2k-mcMMAF (0 [Control],0.001,0.003,0.008,0.02,0.07,0.21,0.62,1.82,5.57,16.67,50,150,450,and 1350 nM) in a 5% CO2 incubator at 37°C for 96 hours. IC50 values at day 5 for AGS-16C3F were calculated for each cell line.
In Vitro Model	Mast-cell sarcoma	ROSA KIT D816V Gluc cells		Homo sapiens
Experiment 3 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	109.9 nM	High ENPP3 expression (ENPP3+++)
Method Description	Cells were incubated in triplicate in medium containing AGS-16C3F or cHmLYS-1c3.G2k-mcMMAF (0 [Control],0.001,0.003,0.008,0.02,0.07,0.21,0.62,1.82,5.57,16.67,50,150,450,and 1350 nM) in a 5% CO2 incubator at 37°C for 96 hours. IC50 values at day 5 for AGS-16C3F were calculated for each cell line.
In Vitro Model	Mast cell leukemia	HMC-1.1 cells		CVCL_H206
Experiment 4 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	146.5 nM
Method Description	Cells were incubated in triplicate in medium containing AGS-16C3F or cHmLYS-1c3.G2k-mcMMAF (0 [Control],0.001,0.003,0.008,0.02,0.07,0.21,0.62,1.82,5.57,16.67,50,150,450,and 1350 nM) in a 5% CO2 incubator at 37°C for 96 hours. IC50 values at day 5 for AGS-16C3F were calculated for each cell line.
In Vitro Model	Mast cell leukemia	HMC-1.2 cells		CVCL_H205

Experiment 1 Reporting the Activity Date of This ADC					[17]
Efficacy Data	Progression Free Survival	2.1 months
Patients Enrolled	Japanese participants with WHO grade III or IV malignant glioma
Administration Dosage	ABT-414 administered every other weeks monotherapy
Related Clinical Trial
NCT Number	NCT02590263	Clinical Status	PHASE1|||PHASE2
Clinical Description	A Non-Randomized, Open-Label, Multi-Center Phase 1/2 Study Evaluating the Safety, Pharmacokinetics and Efficacy of ABT-414 in Japanese Subjects With Malignant Glioma
Primary Endpoint	For all patients in the 2L Depatux-M + CT arm, the 6-month PFS estimate by central review was 25.6% (95% CI 11.4-42.6) with a median PFS of 2.1 months (95% CI 1.9-3.9; Figure 3 A, B). The 6-month OS estimate was 89.7% (95% CI 71.3-96.5), and the median OS was 14.7 months (95% CI 10.7-15.4; Figure 4). ORR, analyzed in patients with at least one measurable disease at baseline, was 21.7% (5/23) by central review with all responses being PR and the median DoR was 5.5 months (95% CI 1.9-NE; Table 6). Seven patients were considered to have 6-month PFS by investigator review, but not by central review.    Click to Show/Hide
Other Endpoint	Objective Response Rate [Time Frame: At each visit for approximately 1 year], Overall Survival [Time Frame: At each visit for approximately 1 year], Duration of Overall Response [Time Frame: At each visit for approximately 1 year]
Experiment 2 Reporting the Activity Date of This ADC					[17]
Efficacy Data	Overall suvival (OS)	14.7 months
Patients Enrolled	Japanese participants with WHO grade III or IV malignant glioma
Administration Dosage	ABT-414 administered every other weeks monotherapy
Related Clinical Trial
NCT Number	NCT02590263	Clinical Status	PHASE1|||PHASE2
Clinical Description	A Non-Randomized, Open-Label, Multi-Center Phase 1/2 Study Evaluating the Safety, Pharmacokinetics and Efficacy of ABT-414 in Japanese Subjects With Malignant Glioma
Primary Endpoint	For all patients in the 2L Depatux-M + CT arm, the 6-month PFS estimate by central review was 25.6% (95% CI 11.4-42.6) with a median PFS of 2.1 months (95% CI 1.9-3.9; Figure 3 A, B). The 6-month OS estimate was 89.7% (95% CI 71.3-96.5), and the median OS was 14.7 months (95% CI 10.7-15.4; Figure 4). ORR, analyzed in patients with at least one measurable disease at baseline, was 21.7% (5/23) by central review with all responses being PR and the median DoR was 5.5 months (95% CI 1.9-NE; Table 6). Seven patients were considered to have 6-month PFS by investigator review, but not by central review.    Click to Show/Hide
Other Endpoint	Objective Response Rate [Time Frame: At each visit for approximately 1 year], Overall Survival [Time Frame: At each visit for approximately 1 year], Duration of Overall Response [Time Frame: At each visit for approximately 1 year]
Experiment 3 Reporting the Activity Date of This ADC					[18]
Efficacy Data	Overall suvival (OS)	15.5 months
Patients Enrolled	Must have a clinical diagnosis of glioblastoma (GBM).
Administration Dosage	Depatuxizumab mafodotin is given on Day 1 of Week 1, 3 and 5 along with the standard therapy of TMZ and radiation during the chemoradiation phase. Depatuxizumab mafodotin is given on Day 1 and 15 of each cycle along with TMZ (Days 1-5 of each cycle) per standard of care during the adjuvant phase.
Related Clinical Trial
NCT Number	NCT02573324	Clinical Status	PHASE3
Clinical Description	A Randomized, Placebo Controlled Phase 3 Study of ABT-414 With Concurrent Chemoradiation and Adjuvant Temozolomide in Subjects With Newly Diagnosed Glioblastoma (GBM) With Epidermal Growth Factor Receptor (EGFR) Amplification (Intellance1)
Primary Endpoint	Overall Survival (OS) [Time Frame: Overall median duration of follow-up was 15.5 months (range: 0.1, 35.6).]
Other Endpoint	OS for the O6-methylguaninemethlytransferese (MGMT) Unmethylated Group [Time Frame: Overall median duration of follow-up was 15.5 months (range: 0.1, 35.6).]
Experiment 4 Reporting the Activity Date of This ADC					[17]
Efficacy Data	During of response (DoR)	5.5 months
Patients Enrolled	Japanese participants with WHO grade III or IV malignant glioma
Administration Dosage	ABT-414 administered every other weeks monotherapy
Related Clinical Trial
NCT Number	NCT02590263	Clinical Status	PHASE1|||PHASE2
Clinical Description	A Non-Randomized, Open-Label, Multi-Center Phase 1/2 Study Evaluating the Safety, Pharmacokinetics and Efficacy of ABT-414 in Japanese Subjects With Malignant Glioma
Primary Endpoint	For all patients in the 2L Depatux-M + CT arm, the 6-month PFS estimate by central review was 25.6% (95% CI 11.4-42.6) with a median PFS of 2.1 months (95% CI 1.9-3.9; Figure 3 A, B). The 6-month OS estimate was 89.7% (95% CI 71.3-96.5), and the median OS was 14.7 months (95% CI 10.7-15.4; Figure 4). ORR, analyzed in patients with at least one measurable disease at baseline, was 21.7% (5/23) by central review with all responses being PR and the median DoR was 5.5 months (95% CI 1.9-NE; Table 6). Seven patients were considered to have 6-month PFS by investigator review, but not by central review.    Click to Show/Hide
Other Endpoint	Objective Response Rate [Time Frame: At each visit for approximately 1 year], Overall Survival [Time Frame: At each visit for approximately 1 year], Duration of Overall Response [Time Frame: At each visit for approximately 1 year]
Experiment 5 Reporting the Activity Date of This ADC					[19]
Patients Enrolled	Subjects must have a solid tumor type likely to over-express Epidermal Growth Factor Receptor (EGFR) (Phase 1)
Administration Dosage	Data from patients who received ABT-414 monotherapy at a dose of 1-4 mg/kg once every 3 weeks or 1 or 1.5 mg/kg weekly for 2 out of every 3 weeks (alternate schedule) by intravenous infusion were included in the analysis of triplicate 12-lead ECGs obtained before dosing and through 168 h after dosing.
Related Clinical Trial
NCT Number	NCT01741727	Clinical Status	PHASE1
Clinical Description	A Phase 1/2 Study Evaluating the Safety, Pharmacokinetics and Efficacy of ABT-414 in Subjects With Advanced Solid Tumors Likely to Over-Express the Epidermal Growth Factor Receptor (EGFR)
Primary Endpoint	Phase 1 - Safety (Number of subjects with adverse events and/or dose limiting toxicities) [Time Frame: Every 1-3 weeks for an average of 20 weeks]
Other Endpoint	Phase 2- Safety (Scheduled study visits occurring on average every 3 weeks) [Time Frame: Followed on average every 3 weeks for approximately 20 weeks]
Experiment 6 Reporting the Activity Date of This ADC					[20]
Patients Enrolled	Histologically confirmed de novo (primary) glioblastoma with unequivocal tumor progression or recurrence.
Administration Dosage	intravenous administration (1.25 mg/kg or 1.0 mg/kg body weight) over 30 to 40 minutes once every 2 weeks until one of the treatment withdrawal criteria was met. The dose was 1.25 mg/kg in the original protocol (Version 1) and Version 2, Amendment 1, and was lowered to 1.0 mg/kg in protocol Version 3, Amendment 2. Pediatric participants: Intravenous administration (1.0 mg/kg body weight for those who were 6 to 17 years old at the date of first dose, or 1.3 mg/kg for those who were 0 to 5 years old) over 30 to 40 minutes or as directed by the guidelines once every 2 weeks until one of the treatment withdrawal criteria was met, for a maximum of one year. If used in combination with temozolomide, depatuxizumab mafodotin was dosed on Day 1 and Day 15 of the TMZ cycle (assuming a standard regimen of 200 mg/m^2/day for 5 days of each 28-day cycle; for other TMZ schedules, timing of the depatuxizumab mafodotin dosing schedule were to be discussed with the medical monitor).    Click to Show/Hide
Related Clinical Trial
NCT Number	NCT02343406	Clinical Status	PHASE2
Clinical Description	INTELLANCE-2: ABT-414 Alone or ABT-414 Plus Temozolomide Versus Lomustine or Temozolomide for Recurrent Glioblastoma: A Randomized Phase 2 Study of the EORTC Brain Tumor Group
Primary Endpoint	Overall Survival (OS); Progression-Free Survival (PFS)
Other Endpoint	Objective Response Rate (ORR); Overall Survival in the Subgroup With Epidermal Growth Factor Receptor (EGFRvIII) Mutation
Experiment 7 Reporting the Activity Date of This ADC					[21]
Patients Enrolled	Newly diagnosed glioblastoma (GBM) histologically proven, World Health Organization (WHO) grade IV GBM or WHO grade IV gliosarcoma
Administration Dosage	During the Chemoradiation Phase, participants were to receive depatuxizumab mafodotin at 2.0 mg/kg IV infusion over 30 - 40 minutes once every 2 weeks (Day 1 of Weeks 1, 3, and 5 of the 6-week regimen). During the Adjuvant Therapy Phase, participants were to receive depatuxizumab mafodotin at 1.25 mg/kg on Day 1 (± 2 days) and Day 15 (± 2 days) of each 28-day cycle as a 30 - 40 minute infusion for 12 cycles.    Click to Show/Hide
Related Clinical Trial
NCT Number	NCT03419403	Clinical Status	PHASE3
Clinical Description	Phase 3b Study for Management of Ocular Side Effects in Subjects With EGFR-amplified Glioblastoma Receiving Depatuxizumab Mafodotin (ABT-414)
Primary Endpoint	Percentage of Participants Who Required a Change in Ocular Side Effect (OSE) Management [Time Frame: Within 8 weeks after the initial dose of depatuxizumab mafodotin]
Other Endpoint	Maximum Change From Baseline on the Logarithm of the Minimum Angle of Resolution (LogMAR) Scale; Time to Bandage Contact Lens (BCL) Intervention; Number of Participants With Depatuxizumab Mafodotin Dose Modifications Due to Ocular Side Effects (OSE)
Experiment 8 Reporting the Activity Date of This ADC					[22]
Patients Enrolled	Glioblastoma Multiforme (GBM)
Administration Dosage	ABT-414 will be administered by intravenous infusion
Related Clinical Trial
NCT Number	NCT01800695	Clinical Status	PHASE1
Clinical Description	A Phase 1 Study Evaluating the Safety and Pharmacokinetics of ABT-414 for Subjects With Glioblastoma Multiforme
Primary Endpoint	Number and percentage of participants with adverse events
Other Endpoint	Biomarker EGFR expression, Progression Free Survival, Overall Survival
Experiment 9 Reporting the Activity Date of This ADC					[23]
Patients Enrolled	Participant must have epidermal growth factor receptor (EGFR) amplification or EGFRvIII mutation.
Related Clinical Trial
NCT Number	NCT03123952	Clinical Status	N.A.
Clinical Description	This is an expanded access program (EAP) for eligible participants. This program is designed to provide access to ABT-414 prior to approval by the local regulatory agency. Availability will depend on territory eligibility. Participating sites will be added as they apply for and are approved for the EAP. A medical doctor must decide whether the potential benefit outweighs the risk of receiving an investigational therapy based on the individual patient's medical history and program eligibility criteria.    Click to Show/Hide
Experiment 10 Reporting the Activity Date of This ADC					[25]
Efficacy Data	Median progression-free survival (mPFS)	8.0 (depatux-m group); 6.3 (placebo group) Months	High EGFR expression (EGFR +++)
Patients Enrolled	EGFR-amp newly diagnosed GBM were randomized 1:1 to radiotherapy, temozolomide, and depatux-m/placebo.
Administration Dosage	Depatux-m was dosed at 2.0 mg/kg during RT, then 1.25 mg/kg thereafter on days 1 and 15/28, 19,21 and allowed to continue until disease progression.
Experiment 11 Reporting the Activity Date of This ADC					[25]
Efficacy Data	Median Overall Survival (mOS)	18.9 (depatux-m group); 18.7(placebo group) Months	High EGFR expression (EGFR +++)
Patients Enrolled	EGFR-amp newly diagnosed GBM were randomized 1:1 to radiotherapy, temozolomide, and depatux-m/placebo.
Administration Dosage	Depatux-m was dosed at 2.0 mg/kg during RT, then 1.25 mg/kg thereafter on days 1 and 15/2819, 21 and allowed to continue until disease progression.

Experiment 1 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 87.50%	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					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	10.00 - 35.00 ug/mL	Positive EGFR expression (EGFR+++/++)
Method Description	Cells lines were plated at 1,000-3,000 cells per well in complete growth medium containing 10% FCS in 96-well plates and allowed to adhere overnight.
In Vitro Model	Pleural mesothelioma	NCI-H2052 cells		CVCL_1518
Experiment 3 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	10.00 - 35.00 ug/mL	Positive EGFR expression (EGFR+++/++)
Method Description	Cells lines were plated at 1,000-3,000 cells per well in complete growth medium containing 10% FCS in 96-well plates and allowed to adhere overnight.
In Vitro Model	Pleural mesothelioma	NCI-H2052 cells		CVCL_1518
Experiment 4 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	10.00 - 35.00 ug/mL	Positive EGFR expression (EGFR+++/++)
Method Description	Cells lines were plated at 1,000-3,000 cells per well in complete growth medium containing 10% FCS in 96-well plates and allowed to adhere overnight.
In Vitro Model	Pleural mesothelioma	NCI-H28 cells		CVCL_1555
Experiment 5 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	10.00 - 35.00 ug/mL	Positive EGFR expression (EGFR+++/++)
Method Description	Cells lines were plated at 1,000-3,000 cells per well in complete growth medium containing 10% FCS in 96-well plates and allowed to adhere overnight.
In Vitro Model	Pleural biphasic mesothelioma	MSTO-211H cells		CVCL_1430

Experiment 1 Reporting the Activity Date of This ADC					[24]
Patients Enrolled	Eligible participants (&ge;18 years) must have advanced/metastatic (non-lymphoma) solid tumors refractory to standard therapy, ECOG 0-1, measurable disease per RECIST v1.1, and adequate organ function. Key exclusions include symptomatic CNS involvement, grade &ge;2 neuropathy, ocular abnormalities, QTc >470 msec, LVEF <45%, active systemic diseases, or recent biologic therapy (&le;4 weeks).    Click to Show/Hide
Administration Dosage	Drug: W0101 - Cohort A1 Administered once every 2 weeks Drug: W0101 - Cohort A2 Administered every 3 weeks Drug: W0101 - Expansion Phase Administered according to the recommended dose for expansion
Related Clinical Trial
NCT Number	NCT03316638	Clinical Status	PHASE1|||PHASE2
Clinical Description	Phase I/II Open Label Dose Escalation and Dose Expansion Study of Intravenous Infusion of W0101, an Antibody-drug Conjugate, in Patients with Advanced or Metastatic Solid Tumors. International, Multicenter, Open Label Study
Primary Endpoint	The primary safety analysis focuses on identifying dose-limiting toxicities (DLTs) over two intervals: within 28 days and up to 63 days post-treatment initiation. Adverse events will be systematically monitored and categorized to determine MTD and treatment tolerability.
Experiment 2 Reporting the Activity Date of This ADC					[26]
Related Clinical Trial
NCT Number	NCT03316638	Clinical Status	Phase 1/2
Clinical Description	Phase 1/2 open label dose escalation and dose expansion study of intravenous infusion of W0101, an antibody-drug conjugate, in patients with advanced or metastatic solid tumors. International, multicenter, open label study.

Experiment 1 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 0%	Low IGF1 expression (IGF1+)
Method Description	For the lung cancer models, 7-week-old female athymic nude mice (Envigo) were engrafted subcutaneously with 7 x106 SBC5 cells and treated with W0101 or isotype control ADC at 3 mg/kg every 4 days for 4 cycles.
In Vitro Model	Lung small cell carcinoma	SBC-5 cells		CVCL_1679
Experiment 2 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 80%	Moderate IGF1 expression (IGF1++)
Method Description	For the lung cancer models, 7-week-old female athymic nude mice (Envigo) were engrafted subcutaneously with 7 x106 NCI-H2122 cells and treated with W0101 or isotype control ADC at 3 mg/kg every 4 days for 4 cycles.
In Vitro Model	Lung adenocarcinoma	NCI-H2122 cells		CVCL_1531
Experiment 3 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100%	Moderate IGF1 expression (IGF1++)
Method Description	For the ovarian cancer model, 7-week-old female SCID mice (Charles River Laboratories) were engrafted subcutaneously with 10 x106 CaoV3 cells and treated with W0101 or isotype control ADC at 3 mg/kg every 4 days for 4 cycles.
In Vitro Model	Lung adenocarcinoma	NCI-H2122 cells		CVCL_1531
Experiment 4 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100%	High IGF1 expression (IGF1+++)
Method Description	For the breast cancer model, 7-week-old female Swiss nude mice (Charles River Laboratories) were engrafted subcutaneously with 5 x106 MCF-7 cells 1 day after subcutaneous implantation of 0.72 mg 17-estradiol 60-day releasing pellets (Innovative Research of America) and treated with W0101 or isotype control ADC at 3 mg/kg every 4 days for 4 cycles.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 5 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.01 nM	High IGF1 expression (IGF1+++)
Method Description	Tumor and normal cells were plated in 96-well flat bottomed microplates (100 L/well) in cell culture medium and incubated overnight at 37°C in 5% CO2. The next day, increasing concentrations of W0101 or isotype control ADC (010 ug/mL) were added into 3 replicate wells containing cells (10 L/well). Plates were incubated for 6 days at 37°C in 5% CO2. Cell viability was determined by measuring ATP using the CellTiter-Glo Luminescent Cell Viability Assay (Promega). Luminescence was read using a Multimode Microplate Reader (Mithras LB940, Berthold Technologies). The percentage cell viability was calculated for each concentration considering 0 ug/mL ADC as 100% viability. The IC50 was calculated using Prism software. Three independent experiments were performed.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 6 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.63 nM	Moderate IGF1 expression (IGF1++)
Method Description	Tumor and normal cells were plated in 96-well flat bottomed microplates (100 L/well) in cell culture medium and incubated overnight at 37°C in 5% CO2. The next day, increasing concentrations of W0101 or isotype control ADC (010 ug/mL) were added into 3 replicate wells containing cells (10 L/well). Plates were incubated for 6 days at 37°C in 5% CO2. Cell viability was determined by measuring ATP using the CellTiter-Glo Luminescent Cell Viability Assay (Promega). Luminescence was read using a Multimode Microplate Reader (Mithras LB940, Berthold Technologies). The percentage cell viability was calculated for each concentration considering 0 ug/mL ADC as 100% viability. The IC50 was calculated using Prism software. Three independent experiments were performed.    Click to Show/Hide
In Vitro Model	Lung adenocarcinoma	NCI-H2122 cells		CVCL_1531
Experiment 7 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 10 nM	Moderate IGF1 expression (IGF1++)
Method Description	Tumor and normal cells were plated in 96-well flat bottomed microplates (100 L/well) in cell culture medium and incubated overnight at 37°C in 5% CO2. The next day, increasing concentrations of W0101 or isotype control ADC (010 ug/mL) were added into 3 replicate wells containing cells (10 L/well). Plates were incubated for 6 days at 37°C in 5% CO2. Cell viability was determined by measuring ATP using the CellTiter-Glo Luminescent Cell Viability Assay (Promega). Luminescence was read using a Multimode Microplate Reader (Mithras LB940, Berthold Technologies). The percentage cell viability was calculated for each concentration considering 0 ug/mL ADC as 100% viability. The IC50 was calculated using Prism software. Three independent experiments were performed.    Click to Show/Hide
In Vitro Model	Ovarian serous adenocarcinoma	Caov-3 cells		CVCL_0201
Experiment 8 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 100 nM	Low IGF1 expression (IGF1+)
Method Description	Tumor and normal cells were plated in 96-well flat bottomed microplates (100 L/well) in cell culture medium and incubated overnight at 37°C in 5% CO2. The next day, increasing concentrations of W0101 or isotype control ADC (010 ug/mL) were added into 3 replicate wells containing cells (10 L/well). Plates were incubated for 6 days at 37°C in 5% CO2. Cell viability was determined by measuring ATP using the CellTiter-Glo Luminescent Cell Viability Assay (Promega). Luminescence was read using a Multimode Microplate Reader (Mithras LB940, Berthold Technologies). The percentage cell viability was calculated for each concentration considering 0 ug/mL ADC as 100% viability. The IC50 was calculated using Prism software. Three independent experiments were performed.    Click to Show/Hide
In Vitro Model	Lung small cell carcinoma	SBC-5 cells		CVCL_1679

Experiment 1 Reporting the Activity Date of This ADC					[29]
Efficacy Data	stable disease (SD)	7.60%
Patients Enrolled	Eligible participants had advanced/metastatic solid tumors refractory to standard therapy, ECOG 0-1, and adequate organ function. Exclusion criteria included uncontrolled brain metastases, recent major surgery/anticancer therapy, and active infections.
Administration Dosage	Drug: PF-06263507 Part 1 - PF-06263507 will be administered intravenously in 21-day cycles in cohorts of 2 or more patients starting at a dose of 0.05 mg/kg. Increases in dose will continue until MTD is determined. Drug: PF-06263507 Part 2 - Patients with select tumor types will be treated at the MTD or Recommended Phase 2 dose selected in Part 1.
Related Clinical Trial
NCT Number	NCT01891669	Clinical Status	PHASE1
Clinical Description	A PHASE 1, DOSE ESCALATION STUDY OF PF-06263507 IN PATIENTS WITH ADVANCED SOLID TUMORS
Primary Endpoint	The study assessed dose-limiting toxicities (DLTs) occurring within the first treatment cycle (21 days), including severe neutropenia, febrile neutropenia, thrombocytopenia with bleeding, non-hematologic toxicities, or cardiac troponin abnormalities. AEs were graded per CTCAE v4.0, and persistent toxicity delaying treatment by >2 weeks was considered a DLT.    Click to Show/Hide
Other Endpoint	Treatment-emergent adverse events (TEAEs) and treatment-related AEs were monitored from baseline through treatment cycles and follow-up, with severity graded per NCI CTCAE v4.0. Hematologic, chemistry, and urine protein abnormalities were tracked, along with vital sign changes meeting predefined criteria. Anti-drug antibodies and pharmacokinetic parameters (Tmax for PF-06263507 and metabolites) were also evaluated.    Click to Show/Hide

Experiment 1 Reporting the Activity Date of This ADC					[41]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 71.70%	Low 5T4 expression (5T4+)
Method Description	ASN004 was evaluated for efficacy in human tumor mouse xenograft models,derived from four different human tumor cell types,having a wide range of 5T4 expression levels. ASN004 was further evaluated in a tumor xenograft model derived from the H1975 human lung carcinoma cell line [5T4+; 15, 800 binding sites per cell]. Subcutaneous tumor xenografts were developed in nude mice with established mean tumor volumes of 150 mm3. The dose of PF-06263507 was 3 mg/kg Q4D 4.    Click to Show/Hide
In Vivo Model	Lung cancer CDX model
In Vitro Model	Lung cancer	Lung cancer cells		Homo sapiens
Experiment 2 Reporting the Activity Date of This ADC					[41]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100%	Low 5T4 expression (5T4+)
Method Description	ASN004 was evaluated for efficacy in human tumor mouse xenograft models,derived from four different human tumor cell types,having a wide range of 5T4 expression levels. ASN004 was further evaluated in a tumor xenograft model derived from the H1975 human lung carcinoma cell line [5T4+; 15, 800 binding sites per cell]. Subcutaneous tumor xenografts were developed in nude mice with established mean tumor volumes of 150 mm3. The dose of PF-06263507 was 10 mg/kg Q4D 4.    Click to Show/Hide
In Vivo Model	Lung cancer CDX model
In Vitro Model	Lung cancer	Lung cancer cells		Homo sapiens

Experiment 1 Reporting the Activity Date of This ADC					[30]
Efficacy Data	stable disease (SD)	16.70%
Patients Enrolled	Eligible patients must have relapsed/refractory solid tumors (ovarian, prostate, NSCLC, etc.) with prior histologic confirmation, ECOG 0-2, adequate organ function, and measurable disease (for dose expansion). Exclusions include uncontrolled CNS metastases, active infections, significant cardiac history, recent stroke/TIA, uncontrolled hypertension, anticoagulant use, and pregnancy/lactation. Prior therapies must be completed ≥30 days before enrollment.    Click to Show/Hide
Administration Dosage	All 6 patients were exposed to MEDI-547 at a dose of 0.08 mg/kg once every 3 weeks.
Related Clinical Trial
NCT Number	NCT00796055	Clinical Status	PHASE1
Clinical Description	A Phase 1, Open-Label Study of MEDI-547 to Evaluate the Safety, Tolerability, Pharmacokinetics, and Biologic Activity of Intravenous Administration in Subjects With Relapsed or Refractory Solid Tumors Associated With EphA2 Expression
Primary Endpoint	The safety and tolerability of MEDI-547 will be evaluated through monitoring adverse events (AEs), serious AEs (SAEs), lab abnormalities, physical exam changes, treatment discontinuations due to toxicity, and drug-related deaths during treatment and up to 30 days post-treatment.
Other Endpoint	Antitumor activity will be assessed via objective response rate (ORR), time to response (TTR), duration of response (DR), time to progression (TTP), progression-free survival (PFS), and overall survival (OS), with measurements continuing until 30 days after the last MEDI-547 dose.
Experiment 2 Reporting the Activity Date of This ADC					[30]
Efficacy Data	progressive disease (PD)	83.30%
Patients Enrolled	Eligible patients must have relapsed/refractory solid tumors (ovarian, prostate, NSCLC, etc.) with prior histologic confirmation, ECOG 0-2, adequate organ function, and measurable disease (for dose expansion). Exclusions include uncontrolled CNS metastases, active infections, significant cardiac history, recent stroke/TIA, uncontrolled hypertension, anticoagulant use, and pregnancy/lactation. Prior therapies must be completed ≥30 days before enrollment.    Click to Show/Hide
Administration Dosage	All 6 patients were exposed to MEDI-547 at a dose of 0.08 mg/kg once every 3 weeks.
Related Clinical Trial
NCT Number	NCT00796055	Clinical Status	PHASE1
Clinical Description	A Phase 1, Open-Label Study of MEDI-547 to Evaluate the Safety, Tolerability, Pharmacokinetics, and Biologic Activity of Intravenous Administration in Subjects With Relapsed or Refractory Solid Tumors Associated With EphA2 Expression
Primary Endpoint	The safety and tolerability of MEDI-547 will be evaluated through monitoring adverse events (AEs), serious AEs (SAEs), lab abnormalities, physical exam changes, treatment discontinuations due to toxicity, and drug-related deaths during treatment and up to 30 days post-treatment.
Other Endpoint	Antitumor activity will be assessed via objective response rate (ORR), time to response (TTR), duration of response (DR), time to progression (TTP), progression-free survival (PFS), and overall survival (OS), with measurements continuing until 30 days after the last MEDI-547 dose.
Experiment 3 Reporting the Activity Date of This ADC					[38]
Efficacy Data	Objective Response Rate (ORR)	0%
Patients Enrolled	Malignant solid tumor thought to be associated with increased expression of EphA2 (endometrial, breast, ovarian, prostate, non-small cell lung, colon, esophageal, gastric, and bladder cancers, renal cell carcinoma, melanoma), relapsed or refractory to standard therapy, and an Eastern Cooperative Oncology Group (ECOG) performance status score of 0-2.    Click to Show/Hide
Administration Dosage	0.08 mg/kg, 1-h intravenous (IV) infusion once q3wks or qwk for 3 consecutive weeks until unacceptable toxicity, progressive disease.
Related Clinical Trial
NCT Number	NCT00796055	Clinical Status	Phase 1
Clinical Description	A phase 1, open-label study of MEDI-547 to evaluate the safety, tolerability, pharmacokinetics, and biologic activity of intravenous administration in subjects with relapsed or refractory solid tumors associated with epha2 expression.
Primary Endpoint	Best response included progressive disease (n=5, 83.33%) and stable disease (n=1, 16.67%), No complete or partial tumor responses.
Other Endpoint	MTD could not be selected.

Experiment 1 Reporting the Activity Date of This ADC					[40]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 48%	Negative EPHA2 expression (EPHA2-)
Method Description	Mice injected with EphA2-negative SPEC-2 cell was assigned to one of four groups (n = 10 mice per group),MEDI-547,3 mg/kg weekly.
In Vivo Model	Endometrial cancer CDX model
In Vitro Model	Endometrial cancer	Endometrial cancer cells		Homo sapiens
Experiment 2 Reporting the Activity Date of This ADC					[40]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 86.67%	Positive EPHA2 expression (EPHA2+++/++)
Method Description	Mice injected with either Hec-1A or Ishikawa were assigned to one of four groups (n = 10 mice per group),MEDI-547,3 mg/kg weekly.
In Vivo Model	Endometrial cancer CDX model
In Vitro Model	Endometrial adenocarcinoma	HEC-1-A cells		CVCL_0293
Experiment 3 Reporting the Activity Date of This ADC					[40]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 92%	Positive EPHA2 expression (EPHA2+++/++)
Method Description	Mice injected with either Hec-1A or Ishikawa were assigned to one of four groups (n = 10 mice per group),MEDI-547,3 mg/kg weekly.
In Vivo Model	Endometrial cancer CDX model
In Vitro Model	Endometrial adenocarcinoma	Ishikawa cells		CVCL_2529

Experiment 1 Reporting the Activity Date of This ADC					[31]
Efficacy Data	stable disease (SD)	58%
Patients Enrolled	Eligible participants require confirmed NHL/RCC with CD70+ status, &ge;1 prior systemic therapy failure, measurable lesions (NHL>1.5cm/RCC&ge;10mm). Key exclusions are prior allogeneic transplant, active secondary malignancy (<3y remission), or previous anti-CD70 therapy.
Administration Dosage	SGN-75 was administered as an intravenous (IV) infusion without premedication every 3 weeks (Q3Wk), or on Days 1, 8, and 15 of 28-day cycles (weekly). Dose levels assessed were 0.3, 1.0, 1.5, 2.0, 3.0, and 4.5 mg/kg administered Q3Wk and 0.3 and 0.6 mg/kg administered weekly.
Related Clinical Trial
NCT Number	NCT01015911	Clinical Status	PHASE1
Clinical Description	A Phase 1, Open-label, Dose-escalation Study to Evaluate the Safety and Tolerability of SGN-75 in Patients With CD70-positive Relapsed or Refractory Non-Hodgkin Lymphoma or Metastatic Renal Cell Carcinoma
Primary Endpoint	The study evaluates adverse events and lab abnormalities as primary safety outcomes, monitored until 1 month post-treatment.
Other Endpoint	Secondary objectives include clinical response (assessed every 2 months), duration parameters (every 3 months), pharmacokinetics of SGN-75, and immunogenicity (both tracked through 1 month post-treatment).
Experiment 2 Reporting the Activity Date of This ADC					[37]
Patients Enrolled	Eligible patients must have CD70+ metastatic renal cell carcinoma with &ge;1 prior TKI, measurable disease, ECOG 0-1, and adequate organ function. Exclusions involve prior anti-CD70 therapy or >1 mTOR inhibitor regimen.
Administration Dosage	1-2 mg/kg IV every 21 days
Related Clinical Trial
NCT Number	NCT01677390	Clinical Status	PHASE1
Clinical Description	A Phase 1b, Open-label, Dose-escalation Study to Evaluate the Safety and Tolerability of SGN-75 in Combination With Everolimus in Patients With CD70-positive Metastatic Renal Cell Carcinoma
Primary Endpoint	The primary outcome measures include incidence of adverse events and lab abnormalities assessed up to 1 month post last dose, with clinical response evaluated per RECIST 1.1.
Other Endpoint	Secondary endpoints cover progression-free survival (expected ~6 months), overall survival (expected ~1 year), SGN-75/metabolite blood levels monitored across cycles, and anti-therapeutic antibody incidence.

Experiment 1 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Partial Response (PR)	3%
Patients Enrolled	Eligible patients must be relapsed/refractory to prior therapies with disease confirmation (B-ALL, Burkitt's or B-lymphoblastic lymphoma) and measurable disease, excluding recent transplant recipients (<60 days) or those with active GVHD/immunosuppression.
Administration Dosage	SGN-CD19A (IV) once (Day 1) or twice (Days 1 and 8) every 21 days; dose range: 0.3-6 mg/kg
Related Clinical Trial
NCT Number	NCT01786096	Clinical Status	PHASE1
Clinical Description	A Phase 1, Open-Label, Dose-Escalation Study of SGN-CD19A in Patients With B-Lineage Acute Lymphoblastic Leukemia and Highly Aggressive Lymphomas
Primary Endpoint	The study evaluates adverse events and laboratory abnormalities occurring within 1 month post last dose as primary safety endpoints.
Other Endpoint	Key secondary endpoints include objective response per modified AML or lymphoma criteria, duration of response (expected 3 months), overall survival (expected 6 months), pharmacokinetics of SGN-CD19A measured at specific timepoints, and immunogenicity assessed through antitherapeutic antibodies.
Experiment 2 Reporting the Activity Date of This ADC					[33]
Efficacy Data	Objective Response Rate (ORR)	33%
Patients Enrolled	Patients eligible for enrollment must have confirmed B-cell malignancies (e.g., MCL, DLBCL, Burkitt lymphoma) and be relapsed/refractory post at least 1 prior therapy (intensive salvage required for DLBCL/Grade 3 FL), with ECOG 0-1 and measurable disease, excluding those with prior allogeneic SCT.
Administration Dosage	Denintuzumab mafodotin was administered IV every 3 weeks (q3wk; 0.5-6 mg/kg) for dose escalation and every 6 weeks (q6wk; 3 mg/kg) in a subsequent expansion cohort.
Related Clinical Trial
NCT Number	NCT01786135	Clinical Status	PHASE1
Clinical Description	A Phase 1, Open-Label, Dose-Escalation Study of SGN-CD19A in Patients With Relapsed or Refractory B-Lineage Non-Hodgkin Lymphoma
Primary Endpoint	The primary endpoints assess safety, including adverse events and laboratory abnormalities within 1 month post last dose.
Other Endpoint	Secondary objectives focus on efficacy outcomes, including objective response per Cheson 2007 (assessed at ~6 weeks post last dose), duration of response (~6 months), overall survival (~1 year), pharmacokinetics of SGN-CD19A, and immunogenicity (antitherapeutic antibodies).
Experiment 3 Reporting the Activity Date of This ADC					[35]
Patients Enrolled	Secondary outcomes include adverse events (AEs) and lab abnormalities graded by NCI CTCAE v4.03, Objective Response Rate (ORR), duration of Complete Response (CR) and Objective Response (OR) up to 27.9 months, Progression-Free Survival (PFS) and Overall Survival (OS) tracked up to 30 months, alongside PBSC mobilization success and autologous stem cell transplant (ASCT) rates post-treatment.    Click to Show/Hide
Related Clinical Trial
NCT Number	NCT02592876	Clinical Status	PHASE2
Clinical Description	A Randomized, Open-Label Phase 2 Study of Denintuzumab Mafodotin (SGN-CD19A) Plus Rituximab, Ifosfamide, Carboplatin, and Etoposide (19A+RICE) Chemotherapy vs. RICE in the Treatment of Patients With Relapsed or Refractory Diffuse Large B-Cell Lymphoma (DLBCL) Who Are Candidates for Autologous Stem Cell Transplant
Primary Endpoint	The primary endpoint is the Complete Remission Rate assessed via PET and CT scans (or CT alone) over 4 months, measuring the number of patients achieving complete metabolic or radiologic responses as evaluated by an independent review facility.
Other Endpoint	Secondary outcomes include adverse events (AEs) and lab abnormalities graded by NCI CTCAE v4.03, Objective Response Rate (ORR), duration of Complete Response (CR) and Objective Response (OR) up to 27.9 months, Progression-Free Survival (PFS) and Overall Survival (OS) tracked up to 30 months, alongside PBSC mobilization success and autologous stem cell transplant (ASCT) rates post-treatment.    Click to Show/Hide
Experiment 4 Reporting the Activity Date of This ADC					[36]
Patients Enrolled	Eligible patients had untreated systemic DLBCL (de novo or transformed) or Grade 3b FL with high-intermediate/high-risk disease, measurable FDG-avid lesions, ECOG &le;2, and adequate baseline labs. Exclusions included prior lymphoma treatment, untreated CNS involvement, active cancers not in 3-year remission, PML history, or significant ocular conditions.    Click to Show/Hide
Administration Dosage	SGN-CD19A at 3 mg/kg will be administered every 6 weeks via intravenous (IV) infusion, up to a maximum of three (3) doses, on Day 1 of Cycles 1, 3, and 5 of 21-day cycles
Related Clinical Trial
NCT Number	NCT02855359	Clinical Status	PHASE2
Clinical Description	An Open Label Phase 2 Study of Denintuzumab Mafodotin (SGN-CD19A) in Combination With RCHOP (Rituximab, Cyclophosphamide, Doxorubicin, Vincristine, and Prednisone) or RCHP (Rituximab, Cyclophosphamide, Doxorubicin, and Prednisone) Compared With RCHOP Alone as Frontline Therapy in Patients With Diffuse Large B-cell Lymphoma (DLBCL) or Follicular Lymphoma (FL) Grade 3b    Click to Show/Hide
Primary Endpoint	The study did not advance to Part B, so the Complete Response Rate (CR) was not assessed. Adverse events and laboratory abnormalities (Grade 1+) were recorded in Part A only, with safety data collected over 54.7 weeks and lab assessments up to 183 days.
Other Endpoint	As the study did not proceed to Part B, none of the efficacy endpoints (Event-Free Survival, Progression-Free Survival, Overall Survival, Objective Response Rate, or Duration of Response) were evaluated, with no comparative data between study arms available.

Experiment 1 Reporting the Activity Date of This ADC					[34]
Patients Enrolled	Eligible patients are aged 18-75 with advanced Trop2-positive epithelial cancer, measurable lesions (RECIST 1.1), ECOG 0-1, adequate organ function, and recovery from prior therapy (≤Grade 1 AEs, except alopecia). Exclusion criteria include active HBV/HCV/syphilis, immunodeficiency, uncontrolled infections, severe cardiopulmonary disease, CNS metastases, Grade ≥2 neuropathy, recent clinical trial participation, major surgery, strong CYP3A4 inhibitor use, allergies, pregnancy, substance abuse, or other investigator-deemed ineligibility.    Click to Show/Hide
Administration Dosage	Phase 1 dose titration study from BAT8003 0.2mg/kg to 10mg/kg, then choose a proper dose for amplification study based on DLT result
Related Clinical Trial
NCT Number	NCT03884517	Clinical Status	PHASE1
Clinical Description	An Open, Escalating Phase I Clinical Trial of BAT8003 (for Injection) on the Safety, Tolerability and Pharmacokinetics for Patients With Advanced Epithelial Cancer
Primary Endpoint	The study assesses dose-limiting toxicity (DLT) and maximum tolerated dose (MTD) as safety/tolerability endpoints over 3 weeks. Pharmacokinetic parameters include AUC, Cmax, t1/2, and Tmax, measured within 24 weeks.
Experiment 2 Reporting the Activity Date of This ADC					[39]
Related Clinical Trial
NCT Number	NCT03884517	Clinical Status	Phase 1
Clinical Description	An open, escalating phase 1 clinical trial of BAT8003 (for injection) on the safety, tolerability and pharmacokinetics for patients with advanced epithelial cancer.

Experiment 1 Reporting the Activity Date of This ADC					[42]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 36.75%	Positive ASPH expression (ASPH +++/++)
Method Description	Mice bearing an approximately 100 mm3 tumor xenograft were intravenously injected weekly with 2.5 mg/kg of SNS-622 or SNS-622-DM1, and tumor growth was monitored.
In Vivo Model	Pancreatic ductal adenocarcinoma PDX model

Experiment 1 Reporting the Activity Date of This ADC					[42]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 55.56%	Positive ASPH expression (ASPH +++/++)
Method Description	MIA PaCa2-empty vector and MIA-PaCa2-ASPH cell lines generated sc tumors in the NSG mice were treated with SNS-622-DM1 (5 mg/kg. every 7 day) and a non-relevant IgG mAb also conjugated with DM1.
In Vivo Model	MIA PaCa2 CDX model
In Vitro Model	Pancreatic ductal adenocarcinoma	MIA PaCa-2 cells		CVCL_0428

Experiment 1 Reporting the Activity Date of This ADC					[43]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 62.90%	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,ASG-15MF 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					[43]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 63.40%	High SLITRK6 expression (SLITRK6+++; IHC H-score=230)
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,ASG-15MF 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					[43]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 80%	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,ASG-15MF 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					[43]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 35.20%	Moderate SLITRK6 expression (SLITRK6++; IHC H-score=185)
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. ASG-15MF was administered twice weekly at 3 mg/kg (n = 6) starting when the tumor volume reached approximately 200 mm3.
In Vivo Model	NCI-322M CDX model
In Vitro Model	Lung cancer	NCI-322M cells		Homo sapiens
Experiment 2 Reporting the Activity Date of This ADC					[43]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 81.30%	High SLITRK6 expression (SLITRK6+++; IHC H-score=280)
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 ASG-15MF, 5 mg/kg intravenously, was administered intravenously (iv) to the mice.
In Vivo Model	Bladder cancer CDX model
In Vitro Model	Bladder cancer	Bladder cancer cells		Homo sapiens

Experiment 1 Reporting the Activity Date of This ADC					[44]
Efficacy Data	Tumor Growth Inhibition value (TGI)	0%	Positive LRRC15 expression (LRRC15 +++/++)
Method Description	LRRC15 expression on stromal cells asassessed by IHC in an untreated xenograft tumor of 200-800 mm in volume, representative for eachxenograft model. In vivo activity of huM25-MCMMAF-E2 (12 mg/kg) was demonstrated in PANC-1 xenografts.
In Vivo Model	PANC-1 CDX model
In Vitro Model	Pancreatic ductal adenocarcinoma	PANC-1 cells		CVCL_0480
Experiment 2 Reporting the Activity Date of This ADC					[44]
Efficacy Data	Tumor Growth Inhibition value (TGI)	8.47%	High LRRC15 expression (LRRC15+++; IHC 3+)
Method Description	LRRC15 expression on stromal cells asassessed by IHC in an untreated xenograft tumor of 200-800 mm in volume, representative for eachxenograft model. In vivo activity of huM25-MCMMAF-E2 (6 mg/kg) was demonstrated in EBC-1 xenografts.
In Vivo Model	EBC-1 CDX model
In Vitro Model	Lung squamous cell carcinoma	EBC-1 cells		CVCL_2891

Experiment 1 Reporting the Activity Date of This ADC					[44]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.01 - 0.10 nM	Positive LRRC15 expression (LRRC15 +++/++)
Method Description	Cancer cell lines were incubated with compounds for 72 h. IC50 values were determined by quantitating viable cells using a CellTiter-Glo luminescent assay.
In Vitro Model	Colon carcinoma	HCT 116 cells		CVCL_0291

Experiment 1 Reporting the Activity Date of This ADC					[45]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 24.38%	High BCMA expression (BCMA+++)
Method Description	Mice were treated with either a single intravenous dose of the ADCs at 0.3 mg/kg or dosed intravenously with J6M0-mc-MMAFweekly at a dose of 0.3 mg/kg for 2 weeks.
In Vivo Model	NCI-H929 CDX model
In Vitro Model	Plasma cell myeloma	NCI-H929 cells		CVCL_1600
Experiment 2 Reporting the Activity Date of This ADC					[45]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 65.09%	Moderate BCMA expression (BCMA++)
Method Description	Mice were treated with either a single intravenous dose of ADCs at 1 mg/kg, or dosed intravenously with J6M0-mc-MMAF ADC weekly at a dose of 1 mg/kg for 4 weeks. Control mice were left untreated.
In Vivo Model	MM.1S CDX model
In Vitro Model	Plasma cell myeloma	MM1.S cells		CVCL_8792
Experiment 3 Reporting the Activity Date of This ADC					[45]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 66.25%	Moderate BCMA expression (BCMA++)
Method Description	Mice were treated with either a single intravenous dose of ADCs at 1 mg/kg, or dosed intravenously with J6M0-mc-MMAF ADC weekly at a dose of 1 mg/kg for 3 weeks. Control mice were left untreated.
In Vivo Model	JJN-3 CDX model
In Vitro Model	Plasma cell myeloma	JJN-3 cells		CVCL_2078
Experiment 4 Reporting the Activity Date of This ADC					[45]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 84.86%	High BCMA expression (BCMA+++)
Method Description	Mice were treated with either a single intravenous dose of ADCs at 1 mg/kg, or dosed intravenously with J6M0-mc-MMAF ADC weekly at a dose of 3 mg/kg for 4 weeks. Control mice were left untreated.
In Vivo Model	MM.1R CDX model
In Vitro Model	Plasma cell myeloma	MM1.R cells		CVCL_8794

Experiment 1 Reporting the Activity Date of This ADC					[45]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	29.28 nM	Moderate BCMA expression (BCMA++)
Method Description	The ability of the ADCs to kill multiple myeloma cells in vitro inthe presence of soluble BCMA (sBCMA, 0 ng/ml) as compared to the 09-SG3249 ADC was evaluated in MM.1S cells, except that tested cell lines also were treated with BCMA-containing conditioned media collected from Ad293 cells expressing human BCMA.
In Vitro Model	Plasma cell myeloma	MM1.S cells		CVCL_8792
Experiment 2 Reporting the Activity Date of This ADC					[45]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	55.55 nM	Moderate BCMA expression (BCMA++)
Method Description	The ability of the ADCs to kill multiple myeloma cells in vitro inthe presence of soluble BCMA (sBCMA, 75 ng/ml) as compared to the 09-SG3249 ADC was evaluated in MM.1S cells, except that tested cell lines also were treated with BCMA-containing conditioned media collected from Ad293 cells expressing human BCMA.
In Vitro Model	Plasma cell myeloma	MM1.S cells		CVCL_8792
Experiment 3 Reporting the Activity Date of This ADC					[45]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	159.7 nM	Moderate BCMA expression (BCMA++)
Method Description	The ability of the ADCs to kill multiple myeloma cells in vitro inthe presence of soluble BCMA (sBCMA, 270 ng/ml) as compared to the 09-SG3249 ADC was evaluated in MM.1S cells, except that tested cell lines also were treated with BCMA-containing conditioned media collected from Ad293 cells expressing human BCMA.
In Vitro Model	Plasma cell myeloma	MM1.S cells		CVCL_8792
Experiment 4 Reporting the Activity Date of This ADC					[45]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.46 uM	Moderate BCMA expression (BCMA++)
Method Description	The ability of the ADCs to kill multiple myeloma cells in vitro inthe presence of soluble BCMA (sBCMA, 720 ng/ml) as compared to the 09-SG3249 ADC was evaluated in MM.1S cells, except that tested cell lines also were treated with BCMA-containing conditioned media collected from Ad293 cells expressing human BCMA.
In Vitro Model	Plasma cell myeloma	MM1.S cells		CVCL_8792

Experiment 1 Reporting the Activity Date of This ADC					[46]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 30.23%	Positive EGFR expression (EGFR+++/++)
Method Description	Cells were subcutaneously inoculated at a dose of 1,000,000 cells to the right flank region of each female nude mouse (Day 0). On the day 7 of grouping, the antibody-drug conjugate was intravenously administered at doses of 3 mg/kg to thetail of each mouse.
In Vivo Model	EBC-1 CDX model
In Vitro Model	Lung squamous cell carcinoma	EBC-1 cells		CVCL_2891

Experiment 1 Reporting the Activity Date of This ADC					[43]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 35.90%	High SLITRK6 expression (SLITRK6+++; IHC H-score=280)
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 Ha15-1c25F, 5 mg/kg intravenously, was administered intravenously (iv) to the mice.
In Vivo Model	Bladder cancer CDX model
In Vitro Model	Bladder cancer	Bladder cancer cells		Homo sapiens

Experiment 1 Reporting the Activity Date of This ADC					[43]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 44.70%	High SLITRK6 expression (SLITRK6+++; IHC H-score=280)
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 Ha15-1abe16F, 5 mg/kg intravenously, was administered intravenously (iv) to the mice.
In Vivo Model	Bladder cancer CDX model
In Vitro Model	Bladder cancer	Bladder cancer cells		Homo sapiens

Experiment 1 Reporting the Activity Date of This ADC					[47]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 60%	Positive RAGE expression (RAGE+++/++)
Method Description	Nude athymic mice were divided into three treatment groups of six mice each. Mice were treated with PBS (control) or RBGO1 ADC at either 3 mg/kg or 20mg/kg N intravenous injection. Bodyweight was measured at days 3, 6, 8, 13, 17 and 21 and mouse health assessed daily.
In Vivo Model	HEC-1-A CDX model
In Vitro Model	Endometrial adenocarcinoma	HEC-1-A cells		CVCL_0293

Experiment 1 Reporting the Activity Date of This ADC					[43]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 64.30%	High SLITRK6 expression (SLITRK6+++; IHC H-score=280)
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 Ha15-10ac14F, 5 mg/kg intravenously, was administered intravenously (iv) to the mice.
In Vivo Model	Bladder cancer CDX model
In Vitro Model	Bladder cancer	Bladder cancer cells		Homo sapiens

Experiment 1 Reporting the Activity Date of This ADC					[48]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 76.44%	Positive CD19 expression (CD19+++/++)
Method Description	To establish DOHH1 tumors, 5 x 106 cells were implanted into the right flank of athymic nu/nu female donor mice (Harlan,Indianapolis, IN). When tumors reached ~100 mm3 mice were randomly allocated to treatment groups. The dose of ADC was 4 mg/kg single.
In Vivo Model	DOHH1 CDX model
In Vitro Model	Diffuse large B-cell lymphoma germinal center B-cell type	DoHH2 cells		CVCL_1179
Experiment 2 Reporting the Activity Date of This ADC					[48]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 96.21%	Positive CD70 expression (CD70+++/++)
Method Description	To establish 786-O tumors, 5 x 106 cells were implanted into the right flank of athymic nu/nu female donor mice. When tumors reached ~100 mm3 mice were randomly allocated to treatment groups. The dose of ADC was 0.5 mg/kg single.
In Vivo Model	786-O CDX model
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051

Experiment 1 Reporting the Activity Date of This ADC					[48]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	12 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234
Experiment 2 Reporting the Activity Date of This ADC					[48]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	34 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051

Experiment 1 Reporting the Activity Date of This ADC					[46]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 81.39%	Positive EGFR expression (EGFR+++/++)
Method Description	Cells were subcutaneously inoculated at a dose of 1,000,000 cells to the right flank region of each female nude mouse (Day 0). On the day 7 of grouping, the antibody-drug conjugate was intravenously administered at doses of 3 mg/kg to thetail of each mouse.
In Vivo Model	EBC-1 CDX model
In Vitro Model	Lung squamous cell carcinoma	EBC-1 cells		CVCL_2891
Experiment 2 Reporting the Activity Date of This ADC					[46]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 86.40%	Positive EGFR expression (EGFR+++/++)
Method Description	Cells were subcutaneously inoculated at a dose of 1,000,000 cells to the right flank region of each female nude mouse (Day 0). On the day 7 of grouping, the antibody-drug conjugate was intravenously administered at doses of 1 mg/kg to thetail of each mouse.
In Vivo Model	NCI-H1703 CDX model
In Vitro Model	Lung squamous cell carcinoma	NCI-H1703 cells		CVCL_1490

Experiment 1 Reporting the Activity Date of This ADC					[49]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 84.30%	Positive ICAM1 expression (ICAM1 +++/++)
Method Description	IC1-MMAE (5 m ug/kg, every seven days x3) induces efficient tumor cell killing in cell line-derived models of MDA-MB-436 or MDA-MB-231 cells with ICAM1 expression with high expression.
In Vivo Model	MDA-MB-231 CDX model
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062
Experiment 2 Reporting the Activity Date of This ADC					[49]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 99%	Positive ICAM1 expression (ICAM1 +++/++)
Method Description	IC1-MMAE (5 m ug/kg, every seven days x3) induces efficient tumor cell killing in cell line-derived models of MDA-MB-436 or MDA-MB-231 cells with ICAM1 expression with high expression.
In Vivo Model	MDA-MB-436 CDX model
In Vitro Model	Metastasis of ductal carcinoma	MDA-MB-436 cells		CVCL_0623

Experiment 1 Reporting the Activity Date of This ADC					[49]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	7.3 pM	Positive ICAM1 expression (ICAM1 +++/++)
Method Description	In vitro cytotoxicity of four ICAM1 ADCs against a panel of four human TNBC cell lines.
In Vitro Model	Metastasis of ductal carcinoma	MDA-MB-436 cells		CVCL_0623
Experiment 2 Reporting the Activity Date of This ADC					[49]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	68.7 pM	Positive ICAM1 expression (ICAM1 +++/++)
Method Description	In vitro cytotoxicity of four ICAM1 ADCs against a panel of four human TNBC cell lines.
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 3 Reporting the Activity Date of This ADC					[49]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.12 nM	Positive ICAM1 expression (ICAM1 +++/++)
Method Description	In vitro cytotoxicity of four ICAM1 ADCs against a panel of four human TNBC cell lines.
In Vitro Model	Breast carcinoma	MDA-MB-157 cells		CVCL_0618

Experiment 1 Reporting the Activity Date of This ADC					[45]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 95.16%	Moderate BCMA expression (BCMA++)
Method Description	Mice were treated with either a single intravenous dose of ADCs at 1 mg/kg, or dosed intravenously with J6M0-mc-MMAF ADC weekly at a dose of 1 mg/kg for 3 weeks. Control mice were left untreated.
In Vivo Model	JJN-3 CDX model
In Vitro Model	Plasma cell myeloma	JJN-3 cells		CVCL_2078

Experiment 1 Reporting the Activity Date of This ADC					[46]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100%	Positive EGFR expression (EGFR+++/++)
Method Description	Cells were subcutaneously inoculated at a dose of 1,000,000 cells to the right flank region of each female nude mouse (Day 0). On the day 7 of grouping, the antibody-drug conjugate was intravenously administered at doses of 3 mg/kg to thetail of each mouse.
In Vivo Model	EBC-1 CDX model
In Vitro Model	Lung squamous cell carcinoma	EBC-1 cells		CVCL_2891

Experiment 1 Reporting the Activity Date of This ADC					[50]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	29 pM	Positive HER2 expression (HER2 +++/++)
Method Description	The cytotoxic activity in vitro of ADCs, which are comprising an anti-HER2 antibody carrying a D265C mutation (T-D265C, anti-HER2-D265C) conjugated tostructurally different amanitin derivatives via its D265C residue was tested on JIMT-1 cells NCI-N87 cells and SKBR-3 cells.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[50]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	57 pM	Positive HER2 expression (HER2+++/++; HER2 MFI=1016)
Method Description	The cytotoxic activity in vitro of ADCs, which are comprising an anti-HER2 antibody carrying a D265C mutation (T-D265C, anti-HER2-D265C) conjugated tostructurally different amanitin derivatives via its D265C residue was tested on JIMT-1 cells NCI-N87 cells and SKBR-3 cells.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[50]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	7.08 nM	Moderate HER2 expression (HER2++)
Method Description	The cytotoxic activity in vitro of ADCs, which are comprising an anti-HER2 antibody carrying a D265C mutation (T-D265C, anti-HER2-D265C) conjugated tostructurally different amanitin derivatives via its D265C residue was tested on JIMT-1 cells NCI-N87 cells and SKBR-3 cells.
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077

Experiment 1 Reporting the Activity Date of This ADC					[50]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	47 pM	Positive PSMA expression (PSMA +++/++)
Method Description	The cytotoxic activity in vitro of ADCs, which are comprising an anti-PSMA antibody carrying a D265C mutation conjugated tostructurally different amanitin derivatives via its D265C residue was tested on LNCaP cells and 22RV1 cells.
In Vitro Model	Prostate carcinoma	LNCaP cells		CVCL_0395
Experiment 2 Reporting the Activity Date of This ADC					[50]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.49 nM	Positive PSMA expression (PSMA +++/++)
Method Description	The cytotoxic activity in vitro of ADCs, which are comprising an anti-PSMA antibody carrying a D265C mutation conjugated tostructurally different amanitin derivatives via its D265C residue was tested on LNCaP cells and 22RV1 cells.
In Vitro Model	Prostate carcinoma	22RV1 cells		CVCL_1045

Experiment 1 Reporting the Activity Date of This ADC					[50]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	47 pM	Positive HER2 expression (HER2+++/++; HER2 MFI=1016)
Method Description	The cytotoxic activity in vitro of ADCs, which are comprising an anti-HER2 antibody carrying a D265C mutation (T-D265C, anti-HER2-D265C) conjugated tostructurally different amanitin derivatives via its D265C residue was tested on JIMT-1 cells NCI-N87 cells and SKBR-3 cells.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[50]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	58 pM	Positive HER2 expression (HER2 +++/++)
Method Description	The cytotoxic activity in vitro of ADCs, which are comprising an anti-HER2 antibody carrying a D265C mutation (T-D265C, anti-HER2-D265C) conjugated tostructurally different amanitin derivatives via its D265C residue was tested on JIMT-1 cells NCI-N87 cells and SKBR-3 cells.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC					[50]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	86 nM	Moderate HER2 expression (HER2++)
Method Description	The cytotoxic activity in vitro of ADCs, which are comprising an anti-HER2 antibody carrying a D265C mutation (T-D265C, anti-HER2-D265C) conjugated tostructurally different amanitin derivatives via its D265C residue was tested on JIMT-1 cells NCI-N87 cells and SKBR-3 cells.
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077

Experiment 1 Reporting the Activity Date of This ADC					[51]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.01 nM	High HER2 expression (HER2 +++)
Method Description	HER2-expressing cell lines were incubated with concentration series of the drug conjugates, and the viability of the cells was measured.
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 2 Reporting the Activity Date of This ADC					[51]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.2 nM	High HER2 expression (HER2 +++)
Method Description	HER2-expressing cell lines were incubated with concentration series of the drug conjugates, and the viability of the cells was measured.
In Vitro Model	Breast adenocarcinoma	AU565 cells		CVCL_1074
Experiment 3 Reporting the Activity Date of This ADC					[51]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.2 nM	High HER2 expression (HER2 +++)
Method Description	HER2-expressing cell lines were incubated with concentration series of the drug conjugates, and the viability of the cells was measured.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 4 Reporting the Activity Date of This ADC					[51]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	12 nM	High HER2 expression (HER2 +++)
Method Description	HER2-expressing cell lines were incubated with concentration series of the drug conjugates, and the viability of the cells was measured.
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 5 Reporting the Activity Date of This ADC					[51]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	215 nM	Moderate HER2 expression (HER2 ++)
Method Description	HER2-expressing cell lines were incubated with concentration series of the drug conjugates, and the viability of the cells was measured.
In Vitro Model	Lung adenocarcinoma	A-549 cells		CVCL_0023

Experiment 1 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.01 nM	High LYPD3 expression (LYPD3+++); High HER2 expression (HER2+++)
Method Description	The in vitro potency of NAMPTi-SMOLs and NAMPTi-ADCs was determined in human tumor cell lines. Cells (2000-4000 cells/well, were incubated at 37°C, 5% CO2 for 24 h and the compounds were added at concentrations of 3x10-12 - 3x10-8 Min triplicates. Cell viability was determined at the beginning (day 0) and after 72-96 h incubation in the presence or absence of NAMPTi-SMOLs or NAMPTi-ADCs.    Click to Show/Hide
In Vitro Model	Childhood acute monocytic leukemia	THP-1 cells		CVCL_0006
Experiment 2 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 10 uM	High LYPD3 expression (LYPD3+++)
Method Description	The in vitro potency of NAMPTi-SMOLs and NAMPTi-ADCs was determined in human tumor cell lines. Cells (2000-4000 cells/well, were incubated at 37°C, 5% CO2 for 24 h and the compounds were added at concentrations of 3x10-12 - 3x10-8 Min triplicates. Cell viability was determined at the beginning (day 0) and after 72-96 h incubation in the presence or absence of NAMPTi-SMOLs or NAMPTi-ADCs.    Click to Show/Hide
In Vitro Model	Lung adenocarcinoma	A549-C4.4a cells		CVCL_0023
Experiment 3 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 10 uM	High CD276 expression (CD276+++)
Method Description	The in vitro potency of NAMPTi-SMOLs and NAMPTi-ADCs was determined in human tumor cell lines. Cells (2000-4000 cells/well, were incubated at 37°C, 5% CO2 for 24 h and the compounds were added at concentrations of 3x10-12 - 3x10-8 Min triplicates. Cell viability was determined at the beginning (day 0) and after 72-96 h incubation in the presence or absence of NAMPTi-SMOLs or NAMPTi-ADCs.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-453 cells		CVCL_0418

Experiment 1 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.08 nM	High CD276 expression (CD276+++)
Method Description	The in vitro potency of NAMPTi-SMOLs and NAMPTi-ADCs was determined in human tumor cell lines. Cells (2000-4000 cells/well, were incubated at 37°C, 5% CO2 for 24 h and the compounds were added at concentrations of 3x10-12 - 3x10-8 Min triplicates. Cell viability was determined at the beginning (day 0) and after 72-96 h incubation in the presence or absence of NAMPTi-SMOLs or NAMPTi-ADCs.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-453 cells		CVCL_0418
Experiment 2 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 10 uM	High LYPD3 expression (LYPD3+++); High HER2 expression (HER2+++)
Method Description	The in vitro potency of NAMPTi-SMOLs and NAMPTi-ADCs was determined in human tumor cell lines. Cells (2000-4000 cells/well, were incubated at 37°C, 5% CO2 for 24 h and the compounds were added at concentrations of 3x10-12 - 3x10-8 Min triplicates. Cell viability was determined at the beginning (day 0) and after 72-96 h incubation in the presence or absence of NAMPTi-SMOLs or NAMPTi-ADCs.    Click to Show/Hide
In Vitro Model	Childhood acute monocytic leukemia	THP-1 cells		CVCL_0006
Experiment 3 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 10 uM	High LYPD3 expression (LYPD3+++)
Method Description	The in vitro potency of NAMPTi-SMOLs and NAMPTi-ADCs was determined in human tumor cell lines. Cells (2000-4000 cells/well, were incubated at 37°C, 5% CO2 for 24 h and the compounds were added at concentrations of 3x10-12 - 3x10-8 Min triplicates. Cell viability was determined at the beginning (day 0) and after 72-96 h incubation in the presence or absence of NAMPTi-SMOLs or NAMPTi-ADCs.    Click to Show/Hide
In Vitro Model	Lung adenocarcinoma	A549-C4.4a cells		CVCL_0023

Experiment 1 Reporting the Activity Date of This ADC					[50]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.11 nM	Positive PSMA expression (PSMA +++/++)
Method Description	The cytotoxic activity in vitro of ADCs, which are comprising an anti-PSMA antibody carrying a D265C mutation conjugated tostructurally different amanitin derivatives via its D265C residue was tested on LNCaP cells and 22RV1 cells.
In Vitro Model	Prostate carcinoma	LNCaP cells		CVCL_0395
Experiment 2 Reporting the Activity Date of This ADC					[50]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.57 nM	Positive PSMA expression (PSMA +++/++)
Method Description	The cytotoxic activity in vitro of ADCs, which are comprising an anti-PSMA antibody carrying a D265C mutation conjugated tostructurally different amanitin derivatives via its D265C residue was tested on LNCaP cells and 22RV1 cells.
In Vitro Model	Prostate carcinoma	22RV1 cells		CVCL_1045

Experiment 1 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.19 nM	High LYPD3 expression (LYPD3+++); High HER2 expression (HER2+++)
Method Description	The in vitro potency of NAMPTi-SMOLs and NAMPTi-ADCs was determined in human tumor cell lines. Cells (2000-4000 cells/well, were incubated at 37°C, 5% CO2 for 24 h and the compounds were added at concentrations of 3x10-12 - 3x10-8 Min triplicates. Cell viability was determined at the beginning (day 0) and after 72-96 h incubation in the presence or absence of NAMPTi-SMOLs or NAMPTi-ADCs.    Click to Show/Hide
In Vitro Model	Childhood acute monocytic leukemia	THP-1 cells		CVCL_0006
Experiment 2 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 10 uM	High LYPD3 expression (LYPD3+++)
Method Description	The in vitro potency of NAMPTi-SMOLs and NAMPTi-ADCs was determined in human tumor cell lines. Cells (2000-4000 cells/well, were incubated at 37°C, 5% CO2 for 24 h and the compounds were added at concentrations of 3x10-12 - 3x10-8 Min triplicates. Cell viability was determined at the beginning (day 0) and after 72-96 h incubation in the presence or absence of NAMPTi-SMOLs or NAMPTi-ADCs.    Click to Show/Hide
In Vitro Model	Lung adenocarcinoma	A549-C4.4a cells		CVCL_0023
Experiment 3 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 10 uM	High CD276 expression (CD276+++)
Method Description	The in vitro potency of NAMPTi-SMOLs and NAMPTi-ADCs was determined in human tumor cell lines. Cells (2000-4000 cells/well, were incubated at 37°C, 5% CO2 for 24 h and the compounds were added at concentrations of 3x10-12 - 3x10-8 Min triplicates. Cell viability was determined at the beginning (day 0) and after 72-96 h incubation in the presence or absence of NAMPTi-SMOLs or NAMPTi-ADCs.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-453 cells		CVCL_0418

Experiment 1 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.37 nM	High CD276 expression (CD276+++)
Method Description	The in vitro potency of NAMPTi-SMOLs and NAMPTi-ADCs was determined in human tumor cell lines. Cells (2000-4000 cells/well, were incubated at 37°C, 5% CO2 for 24 h and the compounds were added at concentrations of 3x10-12 - 3x10-8 Min triplicates. Cell viability was determined at the beginning (day 0) and after 72-96 h incubation in the presence or absence of NAMPTi-SMOLs or NAMPTi-ADCs.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-453 cells		CVCL_0418
Experiment 2 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	88 nM	High LYPD3 expression (LYPD3+++)
Method Description	The in vitro potency of NAMPTi-SMOLs and NAMPTi-ADCs was determined in human tumor cell lines. Cells (2000-4000 cells/well, were incubated at 37°C, 5% CO2 for 24 h and the compounds were added at concentrations of 3x10-12 - 3x10-8 Min triplicates. Cell viability was determined at the beginning (day 0) and after 72-96 h incubation in the presence or absence of NAMPTi-SMOLs or NAMPTi-ADCs.    Click to Show/Hide
In Vitro Model	Lung adenocarcinoma	A549-C4.4a cells		CVCL_0023
Experiment 3 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 10 uM	High LYPD3 expression (LYPD3+++); High HER2 expression (HER2+++)
Method Description	The in vitro potency of NAMPTi-SMOLs and NAMPTi-ADCs was determined in human tumor cell lines. Cells (2000-4000 cells/well, were incubated at 37°C, 5% CO2 for 24 h and the compounds were added at concentrations of 3x10-12 - 3x10-8 Min triplicates. Cell viability was determined at the beginning (day 0) and after 72-96 h incubation in the presence or absence of NAMPTi-SMOLs or NAMPTi-ADCs.    Click to Show/Hide
In Vitro Model	Childhood acute monocytic leukemia	THP-1 cells		CVCL_0006

Experiment 1 Reporting the Activity Date of This ADC					[51]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	8.2 nM	High HER2 expression (HER2 +++)
Method Description	HER2-expressing cell lines were incubated with concentration series of the drug conjugates, and the viability of the cells was measured.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[51]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	24 nM	High HER2 expression (HER2 +++)
Method Description	HER2-expressing cell lines were incubated with concentration series of the drug conjugates, and the viability of the cells was measured.
In Vitro Model	Breast adenocarcinoma	AU565 cells		CVCL_1074

Experiment 1 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	10 nM	High CD276 expression (CD276+++)
Method Description	The in vitro potency of NAMPTi-SMOLs and NAMPTi-ADCs was determined in human tumor cell lines. Cells (2000-4000 cells/well, were incubated at 37°C, 5% CO2 for 24 h and the compounds were added at concentrations of 3x10-12 - 3x10-8 Min triplicates. Cell viability was determined at the beginning (day 0) and after 72-96 h incubation in the presence or absence of NAMPTi-SMOLs or NAMPTi-ADCs.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-453 cells		CVCL_0418
Experiment 2 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	240 nM	High LYPD3 expression (LYPD3+++)
Method Description	The in vitro potency of NAMPTi-SMOLs and NAMPTi-ADCs was determined in human tumor cell lines. Cells (2000-4000 cells/well, were incubated at 37°C, 5% CO2 for 24 h and the compounds were added at concentrations of 3x10-12 - 3x10-8 Min triplicates. Cell viability was determined at the beginning (day 0) and after 72-96 h incubation in the presence or absence of NAMPTi-SMOLs or NAMPTi-ADCs.    Click to Show/Hide
In Vitro Model	Lung adenocarcinoma	A549-C4.4a cells		CVCL_0023
Experiment 3 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 10 uM	High LYPD3 expression (LYPD3+++); High HER2 expression (HER2+++)
Method Description	The in vitro potency of NAMPTi-SMOLs and NAMPTi-ADCs was determined in human tumor cell lines. Cells (2000-4000 cells/well, were incubated at 37°C, 5% CO2 for 24 h and the compounds were added at concentrations of 3x10-12 - 3x10-8 Min triplicates. Cell viability was determined at the beginning (day 0) and after 72-96 h incubation in the presence or absence of NAMPTi-SMOLs or NAMPTi-ADCs.    Click to Show/Hide
In Vitro Model	Childhood acute monocytic leukemia	THP-1 cells		CVCL_0006

Experiment 1 Reporting the Activity Date of This ADC					[53]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 100 nM	Negative MUC16 expression (MUC16-)
Method Description	Cells were seeded in 96 well plates at 3000 cells per well in complete growth media and grown overnight. For cell viability curves, serially diluted conjugates or payloads were added to the cells at final concentrations ranging from 300 nM to 5 pM and incubated for 8 days.
In Vitro Model	Normal	HEK293 cells		CVCL_0045
Experiment 2 Reporting the Activity Date of This ADC					[53]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 100 nM	Positive MUC16 expression (MUC16 +++/++)
Method Description	Cells were seeded in 96 well plates at 3000 cells per well in complete growth media and grown overnight. For cell viability curves, serially diluted conjugates or payloads were added to the cells at final concentrations ranging from 300 nM to 5 pM and incubated for 8 days.
In Vitro Model	Ovarian serous adenocarcinoma	OVCAR-3 cells		CVCL_0465

Ref 1	Antibody-drug conjugate, GSK2857916, in relapsed/refractory multiple myeloma: an update on safety and efficacy from dose expansion phase I study. Blood Cancer J. 2019 Mar 20;9(4):37. doi: 10.1038/s41408-019-0196-6.
Ref 2	Targeting B-cell maturation antigen with GSK2857916 antibody-drug conjugate in relapsed or refractory multiple myeloma (BMA117159): a dose escalation and expansion phase 1 trial. Lancet Oncol. 2018 Dec;19(12):1641-1653.
Ref 3	Near-infrared photoimmunotherapy of cancer: a new approach that kills cancer cells and enhances anti-cancer host immunity. Int Immunol. 2021 Jan 1;33(1):7-15.
Ref 4	Belantamab Mafodotin (GSK2857916) Drives Immunogenic Cell Death and Immune-mediated Antitumor Responses In Vivo. Mol Cancer Ther. 2021 Oct;20(10):1941-1955. doi: 10.1158/1535-7163.MCT-21-0035.
Ref 5	Safety, tolerability, and pharmacokinetics of BAT8001 in patients with HER2-positive breast cancer: An open-label, dose-escalation, phase I study
Ref 6	The Efficacy and Safety of BAT8001 Injection for the Treatment of HER2-positive Advanced Breast Cancer
Ref 7	A Phase I Clinical Trial of BAT1306 and BAT8001 Injection in Patients With Solid Tumor
Ref 8	Safety, tolerability, and pharmacokinetics of BAT8001 in patients with HER2-positive breast cancer: An open-label, dose-escalation, phase I study. Cancer Commun (Lond). 2021 Feb;41(2):171-182.
Ref 9	A Clinical Study Evaluating the Efficacy and Safety of BAT8001 Injection for the Treatment of HER2-positive Advanced Breast Cancer - A Multicenter, Randomized, Open-label, Positive-controlled, Superiority Phase III Clinical Trial in China, NCT04185649
Ref 10	Evaluation for the Safety of BAT1306 and BAT8001 Injection for the Treatment of Patients With HER2-positive Advanced Solid Tumors Phase I/IIa Clinical Trials of Sexual, Tolerability and Pharmacokinetic Characteristics, NCT04151329
Ref 11	An Open-Label, Dose Escalation Phase I Clinical Trial on Safety, Tolerability and Pharmacokinetics of BAT8001 for Injection in Patients With HER2-Positive Solid Tumors, NCT04189211
Ref 12	A Study to Assess the Safety, Pharmacokinetics and Effectiveness of AGS-16C3F Monotherapy in Subjects With Renal Cell Carcinoma (RCC) of Clear Cell or Papillary Histology
Ref 13	A Randomized Phase II Study of AGS-16C3F Versus Axitinib in Previously Treated Patients with Metastatic Renal Cell Carcinoma
Ref 14	Phase I Trials of Anti-ENPP3 Antibody-Drug Conjugates in Advanced Refractory Renal Cell Carcinomas. Clin Cancer Res. 2018 Sep 15;24(18):4399-4406.
Ref 15	A Randomized Phase II Study of AGS-16C3F Versus Axitinib in Previously Treated Patients with Metastatic Renal Cell Carcinoma. Oncologist. 2021 Mar;26(3):182-e361.
Ref 16	In vitro and in vivo efficacy of an anti-CD203c conjugated antibody (AGS-16C3F) in mouse models of advanced systemic mastocytosis. Blood Adv. 2019 Feb 26;3(4):633-643.
Ref 17	Study Evaluating ABT-414 in Japanese Subjects With Malignant Glioma
Ref 18	A Study of ABT-414 in Participants With Newly Diagnosed Glioblastoma (GBM) With Epidermal Growth Factor Receptor (EGFR) Amplification
Ref 19	A Study of ABT-414 in Subjects With Solid Tumors
Ref 20	Adult Study: ABT-414 Alone or ABT-414 Plus Temozolomide vs. Lomustine or Temozolomide for Recurrent Glioblastoma Pediatric Study: Evaluation of ABT-414 in Children With High Grade Gliomas
Ref 21	UNITE Study: Understanding New Interventions With GBM ThErapy
Ref 22	Evaluating the Safety and Pharmacokinetics of ABT-414 for Subjects With Glioblastoma Multiforme
Ref 23	Expanded Access to ABT-414
Ref 24	A Study of a New Investigational Medicinal Product to Treat Patients with Advanced or Metastatic Solid Tumors
Ref 25	Depatuxizumab mafodotin in EGFR-amplified newly diagnosed glioblastoma: A phase III randomized clinical trial. Neuro Oncol. 2023 Feb 14;25(2):339-350. doi: 10.1093/neuonc/noac173.
Ref 26	Phase I/II Open Label Dose Escalation and Dose Expansion Study of Intravenous Infusion of W0101, an Antibody-drug Conjugate, in Patients With Advanced or Metastatic Solid Tumors. International, Multicenter, Open Label Study, NCT03316638
Ref 27	Efficacy of the Antibody-Drug Conjugate W0101 in Preclinical Models of IGF-1 Receptor Overexpressing Solid Tumors. Mol Cancer Ther. 2020 Jan;19(1):168-177.
Ref 28	Targeting and Efficacy of Novel mAb806-Antibody-Drug Conjugates in Malignant Mesothelioma. Pharmaceuticals (Basel). 2020 Oct 2;13(10):289. doi: 10.3390/ph13100289.
Ref 29	First-in-human trial of an anti-5T4 antibody-monomethylauristatin conjugate, PF-06263507, in patients with advanced solid tumors
Ref 30	Study of MEDI-547 to Evaluate the Safety, Tolerability, and Biologic Activity of IV Administration in Subjects With Relapsed or Refractory Solid Tumors
Ref 31	Phase I dose-escalation study of SGN-75 in patients with CD70-positive relapsed/refractory non-Hodgkin lymphoma or metastatic renal cell carcinoma
Ref 32	A Safety Study of SGN-CD19A for Leukemia and Lymphoma
Ref 33	A Safety Study of SGN-CD19A for B-Cell Lymphoma
Ref 34	Clinical Trial of BAT8003 (for Injection) for Patients With Advanced Epithelial Cancer
Ref 35	Treatment Study of Denintuzumab Mafodotin (SGN-CD19A) Plus RICE Versus RICE Alone for Diffuse Large B-Cell Lymphoma
Ref 36	Denintuzumab Mafodotin (SGN-CD19A) Combined With RCHOP or RCHP Versus RCHOP Alone in Diffuse Large B-Cell Lymphoma or Follicular Lymphoma
Ref 37	A Phase 1b Study of SGN-75 in Combination With Everolimus in Patients With Renal Cell Carcinoma
Ref 38	Phase 1, open-label study of MEDI-547 in patients with relapsed or refractory solid tumors. Invest New Drugs. 2013 Feb;31(1):77-84.
Ref 39	An Open, Escalating Phase I Clinical Trial of BAT8003 (for Injection) on the Safety, Tolerability and Pharmacokinetics for Patients With Advanced Epithelial Cancer
Ref 40	EphA2 targeted chemotherapy using an antibody drug conjugate in endometrial carcinoma. Clin Cancer Res. 2010 May 1;16(9):2562-70.
Ref 41	ASN004, A 5T4-targeting scFv-Fc Antibody-Drug Conjugate with High Drug-to-Antibody Ratio, Induces Complete and Durable Tumor Regressions in Preclinical Models. Mol Cancer Ther. 2021 Aug;20(8):1327-1337.
Ref 42	Anti-tumor activity of antibody drug conjugate targeting aspartate--hydroxylase in pancreatic ductal adenocarcinoma. Cancer Lett. 2019 May 1;449:87-98. doi: 10.1016/j.canlet.2019.02.006. Epub 2019 Feb 12.
Ref 43	Development of ASG-15ME, a Novel Antibody-Drug Conjugate Targeting SLITRK6, a New Urothelial Cancer Biomarker. Mol Cancer Ther. 2016 Jun;15(6):1301-10.
Ref 44	Anti-huLRRC15 antibody drug conjugates and methods for their use. 2017-06-08
Ref 45	Bcma monoclonal antibody-drug conjugate.
Ref 46	Anti-egfr antibodies and antibody drug conjugates.
Ref 47	Antibody drug conjugates against the receptor for advanced glycation end products (RAGE), a novel therapeutic target in endometrial cancer. J Immunother Cancer. 2019 Oct 29;7(1):280. doi: 10.1186/s40425-019-0765-z.
Ref 48	Hydrophilic antibody-drug conjugates; 2015-08-20.
Ref 49	A rationally designed ICAM1 antibody drug conjugate eradicates late-stage and refractory triple-negative breast tumors in vivo. Sci Adv. 2023 May 5;9(18):eabq7866. doi: 10.1126/sciadv.abq7866. Epub 2023 May 5.
Ref 50	Amatoxin antibody-drug conjugates and uses thereof; 2020-10-29.
Ref 51	Comparison of HER2-targeted affibody conjugates loaded with auristatin- and maytansine-derived drugs. J Control Release. 2023 Mar;355:515-527. doi: 10.1016/j.jconrel.2023.02.005. Epub 2023 Feb 14.
Ref 52	A Novel NAMPT Inhibitor-Based Antibody-Drug Conjugate Payload Class for Cancer Therapy. Bioconjug Chem. 2022 Jun 15;33(6):1210-1221.
Ref 53	Antibody drug conjugates of cleavable amino-benzoyl-maytansinoids. Bioorg Med Chem. 2020 Dec 1;28(23):115785. doi: 10.1016/j.bmc.2020.115785. Epub 2020 Oct 11.