General Information of This Antibody
Antibody ID
ANI0IPZXU
Antibody Name
Ifinatamab
Organization
Daiichi Sankyo, Inc.
Synonyms
MABX-9001a;
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Antibody Type
Monoclonal antibody (mAb)
Antibody Subtype
Humanized IgG1-kappa
Antigen Name
CD276 antigen (CD276)
 Antigen Info 
ChEMBI ID
CHEMBL5095125
Click to Show/Hide the Sequence Information of This Antibody
Heavy Chain Sequence
QVQLVQSGAEVKKPGSSVRVSCKASGYTFTNYVMHWVRQAPGQGLEWMGYINPYNDDVKY
NEKFKGRVTITADESTSTAYMELSSLRSEDTAVYYCARWGYYGSPLYYFDYWGQGTLVTV
SSASTKGPSVFPLAPSSKSTSGGTAALGCLVKDYFPEPVTVSWNSGALTSGVHTFPAVLQ
SSGLYSLSSVVTVPSSSLGTQTYICNVNHKPSNTKVDKRVEPKSCDKTHTCPPCPAPELL
GGPSVFLFPPKPKDTLMISRTPEVTCVVVDVSHEDPEVKENWYVDGVEVHNAKTKPREEQ
YNSTYRVVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKTTSKAKGQPREPQVYTLPPSR
EEMTKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSKLTVDKS
RWQQGNVESCSVMHEALHNHYTQKSLSLSPGK
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Heavy Chain Varible Domain
QVQLVQSGAEVKKPGSSVKVSCKASGYTFTNYVMHWVRQAPGQGLEWMGYINPYNDDVKY
NEKFKGRVTITADESTSTAYMELSSLRSEDTAVYYCARWGYYGSPLYYFDYWGQGTLVTV
SS
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Heavy Chain Constant Domain 1
ASTKGPSVFPLAPSSKSTSGGTAALGCLVKDYFPEPVTVSWNSGALTSGVHTFPAVLQSS
GLYSLSSVVTVPSSSLGTQTYICNVNHKPSNTKVDKRV
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Heavy Chain Constant Domain 2
APELLGGPSVFLFPPKPKDTLMISRTPEVTCVVVDVSHEDPEVKFNWYVDGVEVHNAKTK
PREEQYNSTYRVVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKTISKAK
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Heavy Chain Constant Domain 3
GQPREPQVYTLPPSREEMTKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDS
DGSFFLYSKLTVDKSRWQQGNVFSCSVMHEALHNHYTQKSLSLSPGK
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Heavy Chain Hinge Region
EPKSCDKTHTCPPCP
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Heavy Chain CDR 1
GYTFTNYV
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Heavy Chain CDR 2
INPYNDDV
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Heavy Chain CDR 3
ARWGYYGSPLYYFDY
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Light Chain Sequence
EIVLTQSPATLSLSPGERATLSCRASSRLIYMHWYQQKPGQAPRPLIYATSNLASGIPAR
FSGSGSGTDFTLTISSLEPEDFAVYYCQQWNSNPPTFGQGTKVEIKRTVAAPSVFIFPPS
DEQLKSGTASVVCLLNNFYPREAKVQWKVDNALQSGNSQESVTEQDSKDSTYSLSSTLTL
SKADYEKHKVYACEVTHQGLSSPVTKSFNRGEC
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Light Chain Varible Domain
EIVLTQSPATLSLSPGERATLSCRASSRLIYMHWYQQKPGQAPRPLIYATSNLASGIPAR
FSGSGSGTDFTLTISSLEPEDFAVYYCQQWNSNPPTFGQGTKVEIK
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Light Chain Constant Domain
RTVAAPSVFIFPPSDEQLKSGTASVVCLLNNFYPREAKVQWKVDNALQSGNSQESVTEQD
SKDSTYSLSSTLTLSKADYEKHKVYACEVTHQGLSSPVTKSFNRGEC
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Light Chain CDR 1
SRLIY
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Light Chain CDR 2
ATS
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Light Chain CDR 3
QQWNSNPPT
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Each Antibody-drug Conjugate Related to This Antibody
Full Information of The Activity Data of The ADC(s) Related to This Antibody
Ifinatamab deruxtecan [New Drug Application]
Identified from the Human Clinical Data
Click To Hide/Show 16 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data stable disease (SD)
49%
Patients Enrolled
Eligible participants are adults (≥18) with histologically confirmed ES-SCLC, measurable per RECIST 1.1, progressing after ≥1 platinum-based systemic therapy (≥2 cycles). Key exclusions: prior B7-H3/ADC (exatecan-based) therapy, active CNS metastases, uncontrolled cardiovascular/respiratory disease, ILD, unresolved toxicities (>Grade 1), active infections (HBV/HCV/HIV), or immunosuppressive steroid use (>10 mg/day prednisone equivalent). Live vaccines within 30 days or pregnancy also preclude enrollment.

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Administration Dosage
I-DXd will be administered as an intravenous (IV) infusion on Day 1 of each 21-day cycle (every Q3W), 8/12 mg/kg.
Related Clinical Trial
NCT Number NCT05280470  Clinical Status PHASE2
Clinical Description
A Phase 2, Multicenter, Randomized, Open-label Study of Ifinatamab Deruxtecan (I-DXd), a B7-H3 Antibody Drug Conjugate (ADC), in Subjects With Pretreated Extensive-stage Small Cell Lung Cancer (ES-SCLC) (IDeate-Lung01)
Primary Endpoint
The primary endpoint is Objective Response Rate (ORR) assessed by BICR (36 months), defined as confirmed CR (complete disappearance of lesions) or PR (≥30% reduction in lesion diameters) per RECIST 1.1. Safety is measured via treatment-emergent adverse events (TEAEs) occurring after treatment initiation.
Other Endpoint
Secondary endpoints include progression-free survival (PFS), duration of response (DoR), overall survival (OS), time to response (TTR), and disease control rate (DCR) assessed up to 36 months by BICR/investigator. Pharmacokinetic evaluations (Cmax, Tmax, Ctrough, AUC, T1/2) track I-DXd, anti-B7-H3 antibody, and MAAA-1181a levels; immunogenicity assesses treatment-emergent antidrug antibodies (ADAs).

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Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data progressive disease (PD)
3%
Patients Enrolled
Eligible participants are adults (≥18) with histologically confirmed ES-SCLC, measurable per RECIST 1.1, progressing after ≥1 platinum-based systemic therapy (≥2 cycles). Key exclusions: prior B7-H3/ADC (exatecan-based) therapy, active CNS metastases, uncontrolled cardiovascular/respiratory disease, ILD, unresolved toxicities (>Grade 1), active infections (HBV/HCV/HIV), or immunosuppressive steroid use (>10 mg/day prednisone equivalent). Live vaccines within 30 days or pregnancy also preclude enrollment.

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Administration Dosage
I-DXd will be administered as an intravenous (IV) infusion on Day 1 of each 21-day cycle (every Q3W), 8/12 mg/kg.
Related Clinical Trial
NCT Number NCT05280470  Clinical Status PHASE2
Clinical Description
A Phase 2, Multicenter, Randomized, Open-label Study of Ifinatamab Deruxtecan (I-DXd), a B7-H3 Antibody Drug Conjugate (ADC), in Subjects With Pretreated Extensive-stage Small Cell Lung Cancer (ES-SCLC) (IDeate-Lung01)
Primary Endpoint
The primary endpoint is Objective Response Rate (ORR) assessed by BICR (36 months), defined as confirmed CR (complete disappearance of lesions) or PR (≥30% reduction in lesion diameters) per RECIST 1.1. Safety is measured via treatment-emergent adverse events (TEAEs) occurring after treatment initiation.
Other Endpoint
Secondary endpoints include progression-free survival (PFS), duration of response (DoR), overall survival (OS), time to response (TTR), and disease control rate (DCR) assessed up to 36 months by BICR/investigator. Pharmacokinetic evaluations (Cmax, Tmax, Ctrough, AUC, T1/2) track I-DXd, anti-B7-H3 antibody, and MAAA-1181a levels; immunogenicity assesses treatment-emergent antidrug antibodies (ADAs).

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Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Partial Response (PR)
16%
Patients Enrolled
Eligible participants are adults (≥18) with histologically confirmed ES-SCLC, measurable per RECIST 1.1, progressing after ≥1 platinum-based systemic therapy (≥2 cycles). Key exclusions: prior B7-H3/ADC (exatecan-based) therapy, active CNS metastases, uncontrolled cardiovascular/respiratory disease, ILD, unresolved toxicities (>Grade 1), active infections (HBV/HCV/HIV), or immunosuppressive steroid use (>10 mg/day prednisone equivalent). Live vaccines within 30 days or pregnancy also preclude enrollment.

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Administration Dosage
I-DXd will be administered as an intravenous (IV) infusion on Day 1 of each 21-day cycle (every Q3W), 8/12 mg/kg.
Related Clinical Trial
NCT Number NCT05280470  Clinical Status PHASE2
Clinical Description
A Phase 2, Multicenter, Randomized, Open-label Study of Ifinatamab Deruxtecan (I-DXd), a B7-H3 Antibody Drug Conjugate (ADC), in Subjects With Pretreated Extensive-stage Small Cell Lung Cancer (ES-SCLC) (IDeate-Lung01)
Primary Endpoint
The primary endpoint is Objective Response Rate (ORR) assessed by BICR (36 months), defined as confirmed CR (complete disappearance of lesions) or PR (≥30% reduction in lesion diameters) per RECIST 1.1. Safety is measured via treatment-emergent adverse events (TEAEs) occurring after treatment initiation.
Other Endpoint
Secondary endpoints include progression-free survival (PFS), duration of response (DoR), overall survival (OS), time to response (TTR), and disease control rate (DCR) assessed up to 36 months by BICR/investigator. Pharmacokinetic evaluations (Cmax, Tmax, Ctrough, AUC, T1/2) track I-DXd, anti-B7-H3 antibody, and MAAA-1181a levels; immunogenicity assesses treatment-emergent antidrug antibodies (ADAs).

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Experiment 4 Reporting the Activity Date of This ADC [1]
Efficacy Data Complete response (CR)
22%
Patients Enrolled
Eligible participants are adults (≥18) with histologically confirmed ES-SCLC, measurable per RECIST 1.1, progressing after ≥1 platinum-based systemic therapy (≥2 cycles). Key exclusions: prior B7-H3/ADC (exatecan-based) therapy, active CNS metastases, uncontrolled cardiovascular/respiratory disease, ILD, unresolved toxicities (>Grade 1), active infections (HBV/HCV/HIV), or immunosuppressive steroid use (>10 mg/day prednisone equivalent). Live vaccines within 30 days or pregnancy also preclude enrollment.

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Administration Dosage
I-DXd will be administered as an intravenous (IV) infusion on Day 1 of each 21-day cycle (every Q3W), 8/12 mg/kg.
Related Clinical Trial
NCT Number NCT05280470  Clinical Status PHASE2
Clinical Description
A Phase 2, Multicenter, Randomized, Open-label Study of Ifinatamab Deruxtecan (I-DXd), a B7-H3 Antibody Drug Conjugate (ADC), in Subjects With Pretreated Extensive-stage Small Cell Lung Cancer (ES-SCLC) (IDeate-Lung01)
Primary Endpoint
The primary endpoint is Objective Response Rate (ORR) assessed by BICR (36 months), defined as confirmed CR (complete disappearance of lesions) or PR (≥30% reduction in lesion diameters) per RECIST 1.1. Safety is measured via treatment-emergent adverse events (TEAEs) occurring after treatment initiation.
Other Endpoint
Secondary endpoints include progression-free survival (PFS), duration of response (DoR), overall survival (OS), time to response (TTR), and disease control rate (DCR) assessed up to 36 months by BICR/investigator. Pharmacokinetic evaluations (Cmax, Tmax, Ctrough, AUC, T1/2) track I-DXd, anti-B7-H3 antibody, and MAAA-1181a levels; immunogenicity assesses treatment-emergent antidrug antibodies (ADAs).

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Experiment 5 Reporting the Activity Date of This ADC [2]
Patients Enrolled
Eligibility requires locally advanced/metastatic esophageal SCC (1L setting), controlled HIV/HBV/HCV if applicable. Exclusions: prior systemic therapy for metastatic disease, high-risk tumor invasion (aorta/respiratory tract), uncontrolled effusions, corneal disease, or prior PD- (L)1/CTLA-4 treatment. HIV+ candidates with Kaposi's sarcoma are excluded.

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Related Clinical Trial
NCT Number NCT06780111  Clinical Status PHASE1|||PHASE2
Clinical Description
A Phase 1/2 Open-Label, Umbrella Platform Design Study of Investigational Agents in Combination With Pembrolizumab (MK-3475) With or Without Chemotherapy in Participants With 1L Locally Advanced Unresectable/Metastatic Esophageal Cancer: KEYMAKER-U06 Substudy 06E
Primary Endpoint
Phase IB tracks Dose-Limiting Toxicities (DLTs) including Grade 3/4 hematologic/nonhematologic AEs (e.g., thrombocytopenia, febrile neutropenia) or treatment-related discontinuations (21-day window). Safety endpoints also cover AE incidence (28 months) and intervention discontinuation rates (25 months). Phase II measures ORR (73 months) per RECIST 1.1 via blinded central review.

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Other Endpoint
Key efficacy outcomes include Duration of Response (DOR), Progression-Free Survival (PFS), Overall Survival (OS) (all up to 73 months), and Disease Control Rate (DCR) with ≥6-month stability. Pharmacokinetics assess I-DXd parameters (Cmax/Tmax, AUC0-last/AUC-tau over 25 months), alongside antidrug antibody (ADA) development rates (73 months).
Experiment 6 Reporting the Activity Date of This ADC [3]
Patients Enrolled
Eligible participants (≥18 years) require histologically confirmed unresectable/metastatic ESCC, progression post-platinum+ICI therapy (≤1 prior line), ≥1 measurable lesion (RECIST v1.1), and ECOG 0-1. Exclusions: prior B7-H3/topoisomerase inhibitors, adenosquamous subtype, high-risk tumor invasion (aorta/respiratory tract), active brain metastases, recent thromboembolic events (6 months), or clinically significant ILD/pulmonary disease. Chronic steroids (>10 mg/day prednisone-equivalent) are excluded except for inhalers/topicals.

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Administration Dosage
Participants who are randomized to receive an intravenous infusion of I-DXd 12 mg/kg on Day 1 of every 21-day cycle (Q3W).
Related Clinical Trial
NCT Number NCT06644781  Clinical Status PHASE3
Clinical Description
A Phase 3, Multicenter, Randomized, Open-label Study of Ifinatamab Deruxtecan (I-DXd) in Subjects With Pretreated Advanced or Metastatic Esophageal Squamous Cell Carcinoma (ESCC) (IDeate-Esophageal01)
Primary Endpoint
Primary efficacy endpoints include Overall Survival (OS) and Progression-Free Survival (PFS), both measured from randomization to death or disease progression (up to 54 months) by BICR per RECIST v1.1. Secondary outcomes are Objective Response Rate (ORR), Duration of Response (DoR), and Disease Control Rate (DCR). Patient-reported outcomes assess EORTC QLQ-C30/OES18 changes, while safety tracks TEAEs, AESIs, and ADA incidence over 54 months.

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Other Endpoint
Pharmacokinetic analysis evaluates Tmax for I-DXd, anti-B7-H3 antibody, and MAAA-1181a through plasma sampling at specific timepoints (Cycle 1-4+ every 2 cycles, 21-day cycles). ADA development and treatment-emergent immunogenicity are monitored longitudinally (up to 54 months).
Experiment 7 Reporting the Activity Date of This ADC [4]
Patients Enrolled
Eligible participants require histologically confirmed Stage IV squamous NSCLC with progression post anti-PD- (L)1 + platinum therapy. HIV/HBV/HCV-infected patients may enroll with controlled viral loads. Exclusions include small cell histology, uncontrolled cardiovascular/pulmonary disease, active CNS metastases, autoimmune/ILD conditions, dual HBV/HCV infection, transplant history, or recent major surgery complications.

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Related Clinical Trial
NCT Number NCT06780098  Clinical Status PHASE2
Clinical Description
KEYMAKER-U01 Substudy 01I: A Phase 2, Randomized, Umbrella Study With Rolling Arms of Investigational Agents in Participants With Previously Treated Stage IV Squamous Non-small Cell Lung Cancer (NSCLC)
Primary Endpoint
The primary efficacy measure is Objective Response Rate (ORR) evaluated per RECIST 1.1, with CR/PR assessments by both BICR and investigators over 84 months. Safety outcomes track AE incidence (84 months) and treatment discontinuations due to AEs (60 months).
Other Endpoint
Secondary endpoints include Duration of Response (DOR), Progression-Free Survival (PFS), and Overall Survival (OS) - all assessed up to 84 months. Disease progression criteria follow RECIST 1.1, requiring ≥20% increase (+5mm absolute) in target lesions or new lesions, with BICR evaluation for DOR and PFS.
Experiment 8 Reporting the Activity Date of This ADC [5]
Patients Enrolled
Eligible participants require histologically confirmed Stage IV NSCLC (non-small cell) with no prior systemic treatment for metastatic disease. Key exclusions: small cell histology, active CNS metastases, uncontrolled autoimmune/infectious conditions, recent major surgery (<3 weeks), prior immunotherapy discontinuation due to severe irAEs, and active HBV/HCV infections unless properly controlled. Screening requirements include tumor tissue submission and completion within specified windows (35 days for Part A, 28 days for Part B).

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Related Clinical Trial
NCT Number NCT04165070  Clinical Status PHASE1|||PHASE2
Clinical Description
KEYMAKER-U01 Substudy 01A: A Phase 1/2, Umbrella Study With Rolling Arms of Investigational Agents With Pembrolizumab With or Without Chemotherapy in Treatment-Naive Participants With Stage IV Non-small Cell Lung Cancer (NSCLC)
Primary Endpoint
The primary efficacy endpoint is Objective Response Rate (ORR) in Part A (24 months) per RECIST 1.1, with CR/PR assessments. Part B safety evaluates AE incidence (27 months), treatment discontinuations due to AEs, and dose-limiting toxicities (DLTs) by CTCAE 5.0 during the first 3 weeks.
Other Endpoint
Part A assesses Progression-Free Survival (PFS) using RECIST 1.1 (24 months) and AE-related outcomes. Part B includes ORR/DOR per BICR (24 months) along with pharmacokinetic parameters (Cmax/Ctrough) for investigational drugs (I-DXd, HER3-DXd, pembrolizumab) over 2 years.
Experiment 9 Reporting the Activity Date of This ADC [6]
Patients Enrolled
Eligible participants include Stage IV nonsquamous NSCLC patients (EGFR/ALK/ROS1-negative) with RECIST 1.1-measurable disease, ECOG 0-1, and adequate organ function. Exclusions cover comorbidities like uncontrolled infections, recent radiotherapy, active malignancies, CNS metastases, autoimmune/ILDs, and prior transplant/HIV/Kaposi's sarcoma, ensuring protocol safety alignment.

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Related Clinical Trial
NCT Number NCT06780085  Clinical Status PHASE2
Clinical Description
KEYMAKER-U01 Substudy 01H: A Phase 2, Randomized, Umbrella Study With Rolling Arms of Investigational Agents in Participants With Previously Treated Stage IV Nonsquamous Non-small Cell Lung Cancer (NSCLC)
Primary Endpoint
The study evaluates Objective Response Rate (ORR) per RECIST 1.1 as the primary endpoint, defined by CR or PR. Adverse events (AEs), including discontinuation rates due to AEs, are monitored as secondary safety outcomes over specified timeframes.
Other Endpoint
Key efficacy measures include Duration of Response (DOR) and Progression-Free Survival (PFS) assessed per RECIST 1.1 via BICR, alongside Overall Survival (OS). DOR spans from initial response to PD or death, while PFS tracks time to PD/death post-randomization, and OS measures survival duration.
Experiment 10 Reporting the Activity Date of This ADC [7]
Patients Enrolled
Eligible participants must have extensive-stage SCLC post-platinum therapy, archival/fresh tissue availability, and controlled HIV if applicable. Key exclusions cover active infections, uncontrolled cardiovascular/neurologic conditions, prior transplants, untreated brain metastases, recent radiotherapy, immunosuppressive therapy, and malignancies requiring active treatment within 3 years. Specific restrictions apply to Part 1, including recent anticancer therapies and corneal disease.

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Related Clinical Trial
NCT Number NCT06780137  Clinical Status PHASE1|||PHASE2
Clinical Description
A Phase 1b/2 Open-Label Clinical Study to Evaluate the Safety and Efficacy of MK-6070 and Ifinatamab Deruxtecan (I-DXd) in Participants With Relapsed/Refractory Extensive-Stage Small Cell Lung Cancer
Primary Endpoint
The primary safety outcomes include the number of participants experiencing adverse events (AEs), dose-limiting toxicities (DLTs), and discontinuations due to AEs, assessed over 44 months. Efficacy measures include Objective Response Rate (ORR) per RECIST 1.1, evaluating CR or PR rates as determined by investigator assessments.
Other Endpoint
Secondary endpoints focus on Duration of Response (DOR) and Progression-Free Survival (PFS), defined per RECIST 1.1, alongside pharmacokinetic metrics (Cmax, Tmax, AUCt, t½, steady-state parameters) for gocatamig, I-DXd, anti-B7-H3 antibody, and DXd. Anti-drug antibody (ADA) incidence is also monitored for immunogenicity assessment.
Experiment 11 Reporting the Activity Date of This ADC [8]
Patients Enrolled
Eligible participants must have DLL3-expressing malignancies: SCLC post-platinum therapy, relapsed/refractory NEPC, or other neuroendocrine tumors failing standard therapy. Key exclusions cover active CNS metastases, uncontrolled effusions, recent cardiovascular events (6 months), active hepatitis/HIV, transplants, immunosuppressive therapy (prednisone >10mg/day), interstitial lung disease, and investigational drug use within 3 weeks/5 half-lives. Autoimmune conditions and unresolved toxicities from prior treatments are prohibited.

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Related Clinical Trial
NCT Number NCT04471727  Clinical Status PHASE1|||PHASE2
Clinical Description
A Phase 1/2 Open-label, Multicenter, Dose Escalation and Dose Expansion Study of the Safety, Tolerability, and Pharmacokinetics of HPN328 Monotherapy and HPN328 With Atezolizumab or Ifinatamab Deruxtecan (I-DXd) in Patients With Advanced Cancers Associated With Expression of Delta-like Canonical Notch Ligand 3 (DLL3).
Primary Endpoint
Safety endpoints include the percentage of participants experiencing adverse events (AEs) and discontinuing due to AEs, graded per NCI CTCAE v5.0 and ASTCT criteria, monitored for up to 4 years. Dose-limiting toxicities (DLTs) following HPN328 treatment (mono/combination) are tracked alongside comprehensive pharmacokinetic parameters (Cmax, Tmax, AUCt/inf, t½, CL, Vss, AC) for gocatamig, atezolizumab, and I-DXd in serum/plasma under single dose and steady state conditions.

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Other Endpoint
Efficacy outcomes focus on tumor response using RECIST v1.1 (PCWG3-modified for NEPC), including ORR, EC-ORR (extra-cranial), BOR, PFS, EC-PFS, OS, DOR, and EC-DOR - all evaluated over 4 years. Immunogenicity is assessed via anti-drug antibody (ADA) incidence against gocatamig, atezolizumab, and I-DXd at designated timepoints. Response criteria incorporate target lesion measurements (≥30% decrease for PR, ≥20% increase for PD with 5mm threshold) and new lesion appearance.

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Experiment 12 Reporting the Activity Date of This ADC [9]
Patients Enrolled
Eligible participants must have metastatic prostate adenocarcinoma progressing on ADT with 1-2 prior ARPI therapies (PARPi allowed if indicated), stable ECOG 0-1, and bone therapy stability. Exclusions cover ILD, uncontrolled cardiovascular/metabolic conditions, prior mCRPC taxanes, active CNS metastases, steroids >10mg/day, recent radiotherapy, autoimmune/transplant history, and other malignancies requiring treatment within 3 years.

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Related Clinical Trial
NCT Number NCT06863272  Clinical Status PHASE1|||PHASE2
Clinical Description
MK-2400-01A Substudy: A Phase 1/2, Open-label Umbrella Substudy of MK-2400-U01 Master Protocol to Evaluate the Safety and Efficacy of Ifinatamab Deruxtecan-based Treatment Combinations or Ifinatamab Deruxtecan Alone in Participants With Metastatic Castration-resistant Prostate Cancer (mCRPC) (IDeate-Prostate02)
Primary Endpoint
Primary safety outcomes include DLTs (Grade 4 toxicities, significant Grade 3 events, treatment delays/discontinuations), AEs, and treatment discontinuations due to AEs in both efficacy (54 months) and safety lead-in phases (21 days), with PSA response rate additionally tracked in the efficacy phase. DLT criteria cover hematologic/nonhematologic toxicities, liver injuries, febrile neutropenia, and dose interruptions.

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Other Endpoint
Key efficacy measures per PCWG-modified RECIST 1.1 include ORR (CR/PR), rPFS (radiological progression/death), OS, DOR (response maintenance), TFST (subsequent therapy initiation), time to PSA progression (≥25% increase + ≥2ng/mL threshold), and TTPP (pain progression per BPI-SF/AQA), all monitored for up to 54 months with Kaplan-Meier analyses.

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Experiment 13 Reporting the Activity Date of This ADC [10]
Patients Enrolled
Eligible participants must have ECOG 0-1, measurable lesions per RECIST 1.1 (excluding irradiated sites without progression), adequate organ function, and specified advanced/metastatic cancers (e.g., HNSCC, ESCC, NSCLC, SCLC, CRPC). Key exclusions include prior B7-H3/I-DXd treatment, ADC-related toxicities, multiple malignancies (exceptions apply), uncontrolled cardiovascular/pulmonary disease, active infections, and conditions compromising safety or study integrity per investigator assessment. ESCC Cohort 4 requires progression post-platinum/ICI with &le;1 prior line of systemic therapy.

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Administration Dosage
Participants with advanced solid tumors who received I-DXd IV Q3W monotherapy during dose escalation phase. Enrollment to this phase is currently closed.
Related Clinical Trial
NCT Number NCT04145622  Clinical Status PHASE1|||PHASE2
Clinical Description
Phase I/II, Two-Part, Multicenter First-in-Human Study of Ifinatamab Deruxtecan (DS-7300a, I-DXd) in Subjects With Advanced Solid Malignant Tumors (IDeate-PanTumor01)
Primary Endpoint
The study assesses dose-limiting toxicities (DLTs) during Cycle 1 (Days 1-21) in dose escalation, monitors adverse events (AEs) through 8 treatment cycles (21 days each until progression), and evaluates the antitumor activity of ifinatamab deruxtecan (I-DXd) over the same 8-cycle period.
Other Endpoint
Pharmacokinetic analyses focus on AUClast, AUCtau, Cmax, Tmax, and Ctrough parameters during 8 treatment cycles (21-day cycles until progression), alongside anti-drug antibody (ADA) incidence tracking over the same timeframe to evaluate immunogenicity and drug exposure dynamics.
Experiment 14 Reporting the Activity Date of This ADC [11]
Patients Enrolled
Eligibility requires ECOG 0-1, measurable lesions (RECIST v1.1), progression after standard therapy, and tumor-specific criteria (e.g., prior ICI/platinum for HNSCC; &le;3 lines for endometrial cancer; HER2-low status for breast cancer). Key exclusions: prior B7-H3/I-DXd treatment, ADC-related toxicities, untreated brain metastases, inadequate washout periods. Disease-specific mandates include biopsy availability (archival/tfresh), Child-Pugh A for HCC, and targeted therapy for actionable mutations.

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Administration Dosage
Participants with recurrent or metastatic endometrial cancer who were previously treated with 1 or more systemic therapy who received an intravenous infusion of I-DXd 12 mg/kg.
Related Clinical Trial
NCT Number NCT06330064  Clinical Status PHASE2
Clinical Description
A Phase 1B/2 Pan-Tumor, Open-Label Study To Evaluate The Efficacy And Safety Of Ifinatamab Deruxtecan (I-DXd) In Subjects With Recurrent Or Metastatic Solid Tumors (IDeate-PanTumor02)
Primary Endpoint
The primary efficacy endpoint is Objective Response Rate (ORR) assessed by investigator per RECIST v1.1 (complete/partial response confirmed) until progression/death (up to 57 months). Safety outcomes include dose-limiting toxicities (Grade ≥3 non-disease-related events in Cycle 1) and treatment-emergent adverse events (TEAEs) monitored from consent until 47 days post-treatment, graded via NCI-CTCAE v5.0 in the HCC cohort.

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Other Endpoint
Secondary endpoints encompass incidence of TEAEs, serious AEs (SAEs), and adverse events of special interest (AESIs) through follow-up, alongside efficacy measures: Duration of Response (DoR), Progression-Free Survival (PFS), Disease Control Rate (DCR), and Overall Survival (OS). Pharmacokinetics (Cmax, Tmax, t1/2, Ctrough, AUC) and immunogenicity (ADA incidence) are evaluated via noncompartmental analysis during 21-day cycles up to 57 months.

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Experiment 15 Reporting the Activity Date of This ADC [12]
Related Clinical Trial
NCT Number NCT05280470  Clinical Status Phase 2
Clinical Description
A phase 2, multicenter, randomized, open-label study of DS-7300a, a B7-H3 antibody drug conjugate (ADC), in subjects with pretreated extensive-stage small cell lung cancer (ES-SCLC).
Experiment 16 Reporting the Activity Date of This ADC [13]
Related Clinical Trial
NCT Number NCT04145622  Clinical Status Phase 1/2
Clinical Description
Phase 1/2, two-part, multicenter first-in-human study of DS-7300a in subjects with advanced solid malignant tumors.
Discovered Using Patient-derived Xenograft Model
Click To Hide/Show 1 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [14]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 100% High CD276 expression (CD276+++)
Method Description
PDX studies CTG-2093, CTG-0166, CTG-0820, and CTG-1061 studies were performed by Champions Oncology, Inc. Models were established by inoculating tumor fragments derived from patients with small cell lung cancer (SCLC), nonsmall cell lung cancer (NSCLC), head and neck cancer, and bladder cancer, respectively, which were maintained in host mice, subcutaneously into female Hsd: Athymic Nude-Foxn1nu mice.Group assignment was carried out when the tumor volume reached approximately 100 to 300 mm3. The tumor-bearing mice were treated with DS-7300a or relevant controls intravenously on days 0 and 14.

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In Vivo Model Small cell lung cancer PDX model (PDX: CTG-2093)
Revealed Based on the Cell Line Data
Click To Hide/Show 4 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [14]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.36 nM
Method Description
In vivo The target specificity and species cross-reactivity of DS-7304a were assessed. Its pharmacologic activities were evaluated in several human cancer cell lines in vitro and xenograft mouse models, including patient-derived xenograft (PDX) mouse models.
In Vitro Model Endometrial adenocarcinoma MFE-280 cells CVCL_1405
Experiment 2 Reporting the Activity Date of This ADC [14]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.37 nM
Method Description
In vivo The target specificity and species cross-reactivity of DS-7303a were assessed. Its pharmacologic activities were evaluated in several human cancer cell lines in vitro and xenograft mouse models, including patient-derived xenograft (PDX) mouse models.
In Vitro Model Alveolar rhabdomyosarcoma Rh41 cells CVCL_2176
Experiment 3 Reporting the Activity Date of This ADC [14]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.55 nM
Method Description
In vivo The target specificity and species cross-reactivity of DS-7302a were assessed. Its pharmacologic activities were evaluated in several human cancer cell lines in vitro and xenograft mouse models, including patient-derived xenograft (PDX) mouse models.
In Vitro Model T acute lymphoblastic leukemia CCRF-CEM cells CVCL_0207
Experiment 4 Reporting the Activity Date of This ADC [14]
Method Description
In vivo The target specificity and species cross-reactivity of DS-7300a were assessed. Its pharmacologic activities were evaluated in several human cancer cell lines in vitro and xenograft mouse models, including patient-derived xenograft (PDX) mouse models.
In Vitro Model T acute lymphoblastic leukemia CCRF-CEM cells CVCL_0207
ZA202500415A-ADC Example 4 [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 5 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [15]
Efficacy Data Tumor Growth lnhibition value (TGl)
104.40%
Method Description
Cell line-derived xenograft models were established in male NOD SCID mice, by subcutaneous injection of 1x107 (LNCaP) tumor cells, and treatmen with 5mg/kg ADC (Q7D&#423) after tumor volume about 80-100mm3. Determined tumor volume after the experiment, measured at day 28.
In Vivo Model LNCaP prostate cancer xenograft model
Experiment 2 Reporting the Activity Date of This ADC [15]
Efficacy Data Tumor Growth lnhibition value (TGl)
108.31%
Method Description
Cell line-derived xenograft models were established in non-castrated male CB17/SCID mice, by subcutaneous injection of 1x107 (VCaP) tumor cells, and treatmen with 2.5mg/kg ADC (QW&#422) after tumor volume about 162.16mm3. Determined tumor volume after the experiment, measured at day 17.
In Vivo Model VCaP prostate cancer xenograft model
Experiment 3 Reporting the Activity Date of This ADC [15]
Efficacy Data Tumor Growth lnhibition value (TGl)
112.40%
Method Description
Cell line-derived xenograft models were established in male NOD SCID mice, by subcutaneous injection of 1x107 (LNCaP) tumor cells, and treatmen with 10mg/kg ADC (Q7D&#423) after tumor volume about 80-100mm3. Determined tumor volume after the experiment, measured at day 28.
In Vivo Model LNCaP prostate cancer xenograft model
Experiment 4 Reporting the Activity Date of This ADC [15]
Efficacy Data Tumor Growth lnhibition value (TGl)
114.03%
Method Description
Cell line-derived xenograft models were established in non-castrated male CB17/SCID mice, by subcutaneous injection of 1x107 (VCaP) tumor cells, and treatmen with 10mg/kg ADC (QW&#422) after tumor volume about 162.16mm3. Determined tumor volume after the experiment, measured at day 17.
In Vivo Model VCaP prostate cancer xenograft model
Experiment 5 Reporting the Activity Date of This ADC [15]
Efficacy Data Tumor Growth lnhibition value (TGl)
114.69%
Method Description
Cell line-derived xenograft models were established in non-castrated male CB17/SCID mice, by subcutaneous injection of 1x107 (VCaP) tumor cells, and treatmen with 5mg/kg ADC (QW&#422) after tumor volume about 162.16mm3. Determined tumor volume after the experiment, measured at day 17.
In Vivo Model VCaP prostate cancer xenograft model
Revealed Based on the Cell Line Data
Click To Hide/Show 3 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [15]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
0.154 uM
Method Description
LNCaP Cells were plated at set initial densities in 96 well flat bottom plates in the appropriate growth media. 24 hours later, dosing solutions were added at serial dilutions of each test compound spanning a concentration range of either 50 nM to 0.005 nM for the various ADCs. Cell proliferation was measured after 144 hours exposure, by CellTiter-Glo 2.0 Solution Cell Viability Assay.

   Click to Show/Hide
In Vitro Model Prostate carcinoma LNCaP cells CVCL_0395
Experiment 2 Reporting the Activity Date of This ADC [15]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
0.158 uM
Method Description
VCaP Cells were plated at set initial densities in 96 well flat bottom plates in the appropriate growth media. 24 hours later, dosing solutions were added at serial dilutions of each test compound spanning a concentration range of either 50 nM to 0.005 nM for the various ADCs. Cell proliferation was measured after 144 hours exposure, by CellTiter-Glo 2.2 Solution Cell Viability Assay.

   Click to Show/Hide
In Vitro Model Prostate carcinoma VCaP cells CVCL_2235
Experiment 3 Reporting the Activity Date of This ADC [15]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
1.345 uM
Method Description
C42 Cells were plated at set initial densities in 96 well flat bottom plates in the appropriate growth media. 24 hours later, dosing solutions were added at serial dilutions of each test compound spanning a concentration range of either 50 nM to 0.005 nM for the various ADCs. Cell proliferation was measured after 144 hours exposure, by CellTiter-Glo 2.1 Solution Cell Viability Assay.

   Click to Show/Hide
In Vitro Model Prostate carcinoma C4-2 cells CVCL_4782
SG11202408662TA ADC-C7 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 4 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [16]
Efficacy Data Half Maximal Effective Concentration (EC50)
0.007 nM
Positive B7H3 expression (B7H3+++/++)
Method Description
Adding the fresh growth-medium containing the varying concentrations of ADCs, 40ul/well into H358, H441, H1048 and MDA-MB-487.
In Vitro Model Lung small cell carcinoma, Small cell lung cancer H1048 cells CVCL_1453
Experiment 2 Reporting the Activity Date of This ADC [16]
Efficacy Data Half Maximal Effective Concentration (EC50)
0.038 nM
High B7H3 expression (B7H3 +++)
Method Description
Adding the fresh growth-medium containing the varying concentrations of ADCs, 40ul/well into H358, H441, H1048 and MDA-MB-487.
In Vitro Model Minimally invasive lung adenocarcinoma H358 cells CVCL_1559
Experiment 3 Reporting the Activity Date of This ADC [16]
Efficacy Data Half Maximal Effective Concentration (EC50)
0.894 nM
Positive B7H3 expression (B7H3+++/++)
Method Description
Adding the fresh growth-medium containing the varying concentrations of ADCs, 40ul/well into H358, H441, H1048 and MDA-MB-487.
In Vitro Model Lung papillary adenocarcinoma H441 cells CVCL_1561
Experiment 4 Reporting the Activity Date of This ADC [16]
Efficacy Data Half Maximal Effective Concentration (EC50) > 100 nM Negative B7H3 expression (B7H3-)
Method Description
Adding the fresh growth-medium containing the varying concentrations of ADCs, 40ul/well into H358, H441, H1048 and MDA-MB-487.
In Vitro Model Breast adenocarcinoma MDA-MB-453 cells CVCL_0418
SG11202408662TA ADC-C13 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 4 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [16]
Efficacy Data Half Maximal Effective Concentration (EC50)
0.01 nM
Positive B7H3 expression (B7H3+++/++)
Method Description
Adding the fresh growth-medium containing the varying concentrations of ADCs, 40ul/well into H358, H441, H1048 and MDA-MB-487.
In Vitro Model Minimally invasive lung adenocarcinoma H358 cells CVCL_1559
Experiment 2 Reporting the Activity Date of This ADC [16]
Efficacy Data Half Maximal Effective Concentration (EC50)
0.014 nM
Negative B7H3 expression (B7H3-)
Method Description
Adding the fresh growth-medium containing the varying concentrations of ADCs, 40ul/well into H358, H441, H1048 and MDA-MB-487.
In Vitro Model Lung small cell carcinoma, Small cell lung cancer H1048 cells CVCL_1453
Experiment 3 Reporting the Activity Date of This ADC [16]
Efficacy Data Half Maximal Effective Concentration (EC50)
0.861 nM
Positive B7H3 expression (B7H3+++/++)
Method Description
Adding the fresh growth-medium containing the varying concentrations of ADCs, 40ul/well into H358, H441, H1048 and MDA-MB-487.
In Vitro Model Lung papillary adenocarcinoma H441 cells CVCL_1561
Experiment 4 Reporting the Activity Date of This ADC [16]
Efficacy Data Half Maximal Effective Concentration (EC50) > 100 nM High B7H3 expression (B7H3 +++)
Method Description
Adding the fresh growth-medium containing the varying concentrations of ADCs, 40ul/well into H358, H441, H1048 and MDA-MB-487.
In Vitro Model Breast adenocarcinoma MDA-MB-453 cells CVCL_0418
SG11202408662TA ADC-C6 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 4 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [16]
Efficacy Data Half Maximal Effective Concentration (EC50)
0.013 nM
Positive B7H3 expression (B7H3+++/++)
Method Description
Adding the fresh growth-medium containing the varying concentrations of ADCs, 40ul/well into H358, H441, H1048 and MDA-MB-487.
In Vitro Model Lung small cell carcinoma, Small cell lung cancer H1048 cells CVCL_1453
Experiment 2 Reporting the Activity Date of This ADC [16]
Efficacy Data Half Maximal Effective Concentration (EC50)
0.038 nM
High B7H3 expression (B7H3 +++)
Method Description
Adding the fresh growth-medium containing the varying concentrations of ADCs, 40ul/well into H358, H441, H1048 and MDA-MB-487.
In Vitro Model Minimally invasive lung adenocarcinoma H358 cells CVCL_1559
Experiment 3 Reporting the Activity Date of This ADC [16]
Efficacy Data Half Maximal Effective Concentration (EC50)
0.5298 nM
Positive B7H3 expression (B7H3+++/++)
Method Description
Adding the fresh growth-medium containing the varying concentrations of ADCs, 40ul/well into H358, H441, H1048 and MDA-MB-487.
In Vitro Model Lung papillary adenocarcinoma H441 cells CVCL_1561
Experiment 4 Reporting the Activity Date of This ADC [16]
Efficacy Data Half Maximal Effective Concentration (EC50) > 100 nM Negative B7H3 expression (B7H3-)
Method Description
Adding the fresh growth-medium containing the varying concentrations of ADCs, 40ul/well into H358, H441, H1048 and MDA-MB-487.
In Vitro Model Breast adenocarcinoma MDA-MB-453 cells CVCL_0418
SG11202408662TA ADC-C8 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 4 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [16]
Efficacy Data Half Maximal Effective Concentration (EC50)
0.015 nM
Positive B7H3 expression (B7H3+++/++)
Method Description
Adding the fresh growth-medium containing the varying concentrations of ADCs, 40ul/well into H358, H441, H1048 and MDA-MB-487.
In Vitro Model Lung small cell carcinoma, Small cell lung cancer H1048 cells CVCL_1453
Experiment 2 Reporting the Activity Date of This ADC [16]
Efficacy Data Half Maximal Effective Concentration (EC50)
0.043 nM
High B7H3 expression (B7H3 +++)
Method Description
Adding the fresh growth-medium containing the varying concentrations of ADCs, 40ul/well into H358, H441, H1048 and MDA-MB-487.
In Vitro Model Minimally invasive lung adenocarcinoma H358 cells CVCL_1559
Experiment 3 Reporting the Activity Date of This ADC [16]
Efficacy Data Half Maximal Effective Concentration (EC50)
1.042 nM
Positive B7H3 expression (B7H3+++/++)
Method Description
Adding the fresh growth-medium containing the varying concentrations of ADCs, 40ul/well into H358, H441, H1048 and MDA-MB-487.
In Vitro Model Lung papillary adenocarcinoma H441 cells CVCL_1561
Experiment 4 Reporting the Activity Date of This ADC [16]
Efficacy Data Half Maximal Effective Concentration (EC50) > 100 nM Negative B7H3 expression (B7H3-)
Method Description
Adding the fresh growth-medium containing the varying concentrations of ADCs, 40ul/well into H358, H441, H1048 and MDA-MB-487.
In Vitro Model Breast adenocarcinoma MDA-MB-453 cells CVCL_0418
SG11202408662TA ADC-C1 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 4 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [16]
Efficacy Data Half Maximal Effective Concentration (EC50)
0.022 nM
High B7H3 expression (B7H3 +++)
Method Description
Adding the fresh growth-medium containing the varying concentrations of ADCs, 40ul/well into H358, H441, H1048 and MDA-MB-487.
In Vitro Model Minimally invasive lung adenocarcinoma H358 cells CVCL_1559
Experiment 2 Reporting the Activity Date of This ADC [16]
Efficacy Data Half Maximal Effective Concentration (EC50)
0.034 nM
Positive B7H3 expression (B7H3+++/++)
Method Description
Adding the fresh growth-medium containing the varying concentrations of ADCs, 40ul/well into H358, H441, H1048 and MDA-MB-487.
In Vitro Model Lung small cell carcinoma, Small cell lung cancer H1048 cells CVCL_1453
Experiment 3 Reporting the Activity Date of This ADC [16]
Efficacy Data Half Maximal Effective Concentration (EC50)
2.201 nM
Positive B7H3 expression (B7H3+++/++)
Method Description
Adding the fresh growth-medium containing the varying concentrations of ADCs, 40ul/well into H358, H441, H1048 and MDA-MB-487.
In Vitro Model Lung papillary adenocarcinoma H441 cells CVCL_1561
Experiment 4 Reporting the Activity Date of This ADC [16]
Efficacy Data Half Maximal Effective Concentration (EC50) > 100 nM Negative B7H3 expression (B7H3-)
Method Description
Adding the fresh growth-medium containing the varying concentrations of ADCs, 40ul/well into H358, H441, H1048 and MDA-MB-487.
In Vitro Model Breast adenocarcinoma MDA-MB-453 cells CVCL_0418
SG11202408662TA ADC-C9 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 4 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [16]
Efficacy Data Half Maximal Effective Concentration (EC50)
0.024 nM
Negative B7H3 expression (B7H3-)
Method Description
Adding the fresh growth-medium containing the varying concentrations of ADCs, 40ul/well into H358, H441, H1048 and MDA-MB-487.
In Vitro Model Lung small cell carcinoma, Small cell lung cancer H1048 cells CVCL_1453
Experiment 2 Reporting the Activity Date of This ADC [16]
Efficacy Data Half Maximal Effective Concentration (EC50)
0.033 nM
Positive B7H3 expression (B7H3+++/++)
Method Description
Adding the fresh growth-medium containing the varying concentrations of ADCs, 40ul/well into H358, H441, H1048 and MDA-MB-487.
In Vitro Model Minimally invasive lung adenocarcinoma H358 cells CVCL_1559
Experiment 3 Reporting the Activity Date of This ADC [16]
Efficacy Data Half Maximal Effective Concentration (EC50)
1.647 nM
Positive B7H3 expression (B7H3+++/++)
Method Description
Adding the fresh growth-medium containing the varying concentrations of ADCs, 40ul/well into H358, H441, H1048 and MDA-MB-487.
In Vitro Model Lung papillary adenocarcinoma H441 cells CVCL_1561
Experiment 4 Reporting the Activity Date of This ADC [16]
Efficacy Data Half Maximal Effective Concentration (EC50) > 100 nM High B7H3 expression (B7H3 +++)
Method Description
Adding the fresh growth-medium containing the varying concentrations of ADCs, 40ul/well into H358, H441, H1048 and MDA-MB-487.
In Vitro Model Breast adenocarcinoma MDA-MB-453 cells CVCL_0418
SG11202408662TA ADC-C10 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 4 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [16]
Efficacy Data Half Maximal Effective Concentration (EC50)
0.025 nM
Positive B7H3 expression (B7H3+++/++)
Method Description
Adding the fresh growth-medium containing the varying concentrations of ADCs, 40ul/well into H358, H441, H1048 and MDA-MB-487.
In Vitro Model Minimally invasive lung adenocarcinoma H358 cells CVCL_1559
Experiment 2 Reporting the Activity Date of This ADC [16]
Efficacy Data Half Maximal Effective Concentration (EC50)
0.029 nM
Negative B7H3 expression (B7H3-)
Method Description
Adding the fresh growth-medium containing the varying concentrations of ADCs, 40ul/well into H358, H441, H1048 and MDA-MB-487.
In Vitro Model Lung small cell carcinoma, Small cell lung cancer H1048 cells CVCL_1453
Experiment 3 Reporting the Activity Date of This ADC [16]
Efficacy Data Half Maximal Effective Concentration (EC50)
1.073 nM
Positive B7H3 expression (B7H3+++/++)
Method Description
Adding the fresh growth-medium containing the varying concentrations of ADCs, 40ul/well into H358, H441, H1048 and MDA-MB-487.
In Vitro Model Lung papillary adenocarcinoma H441 cells CVCL_1561
Experiment 4 Reporting the Activity Date of This ADC [16]
Efficacy Data Half Maximal Effective Concentration (EC50)
22 nM
High B7H3 expression (B7H3 +++)
Method Description
Adding the fresh growth-medium containing the varying concentrations of ADCs, 40ul/well into H358, H441, H1048 and MDA-MB-487.
In Vitro Model Breast adenocarcinoma MDA-MB-453 cells CVCL_0418
SG11202408662TA ADC-C11 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 4 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [16]
Efficacy Data Half Maximal Effective Concentration (EC50)
0.025 nM
Negative B7H3 expression (B7H3-)
Method Description
Adding the fresh growth-medium containing the varying concentrations of ADCs, 40ul/well into H358, H441, H1048 and MDA-MB-487.
In Vitro Model Lung small cell carcinoma, Small cell lung cancer H1048 cells CVCL_1453
Experiment 2 Reporting the Activity Date of This ADC [16]
Efficacy Data Half Maximal Effective Concentration (EC50)
0.027 nM
Positive B7H3 expression (B7H3+++/++)
Method Description
Adding the fresh growth-medium containing the varying concentrations of ADCs, 40ul/well into H358, H441, H1048 and MDA-MB-487.
In Vitro Model Minimally invasive lung adenocarcinoma H358 cells CVCL_1559
Experiment 3 Reporting the Activity Date of This ADC [16]
Efficacy Data Half Maximal Effective Concentration (EC50)
1.234 nM
Positive B7H3 expression (B7H3+++/++)
Method Description
Adding the fresh growth-medium containing the varying concentrations of ADCs, 40ul/well into H358, H441, H1048 and MDA-MB-487.
In Vitro Model Lung papillary adenocarcinoma H441 cells CVCL_1561
Experiment 4 Reporting the Activity Date of This ADC [16]
Efficacy Data Half Maximal Effective Concentration (EC50) > 100 nM High B7H3 expression (B7H3 +++)
Method Description
Adding the fresh growth-medium containing the varying concentrations of ADCs, 40ul/well into H358, H441, H1048 and MDA-MB-487.
In Vitro Model Breast adenocarcinoma MDA-MB-453 cells CVCL_0418
SG11202408662TA ADC-C12 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 4 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [16]
Efficacy Data Half Maximal Effective Concentration (EC50)
0.029 nM
Positive B7H3 expression (B7H3+++/++)
Method Description
Adding the fresh growth-medium containing the varying concentrations of ADCs, 40ul/well into H358, H441, H1048 and MDA-MB-487.
In Vitro Model Minimally invasive lung adenocarcinoma H358 cells CVCL_1559
Experiment 2 Reporting the Activity Date of This ADC [16]
Efficacy Data Half Maximal Effective Concentration (EC50)
0.034 nM
Negative B7H3 expression (B7H3-)
Method Description
Adding the fresh growth-medium containing the varying concentrations of ADCs, 40ul/well into H358, H441, H1048 and MDA-MB-487.
In Vitro Model Lung small cell carcinoma, Small cell lung cancer H1048 cells CVCL_1453
Experiment 3 Reporting the Activity Date of This ADC [16]
Efficacy Data Half Maximal Effective Concentration (EC50)
1.094 nM
Positive B7H3 expression (B7H3+++/++)
Method Description
Adding the fresh growth-medium containing the varying concentrations of ADCs, 40ul/well into H358, H441, H1048 and MDA-MB-487.
In Vitro Model Lung papillary adenocarcinoma H441 cells CVCL_1561
Experiment 4 Reporting the Activity Date of This ADC [16]
Efficacy Data Half Maximal Effective Concentration (EC50) > 100 nM High B7H3 expression (B7H3 +++)
Method Description
Adding the fresh growth-medium containing the varying concentrations of ADCs, 40ul/well into H358, H441, H1048 and MDA-MB-487.
In Vitro Model Breast adenocarcinoma MDA-MB-453 cells CVCL_0418
SG11202408662TA ADC-C14 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 4 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [16]
Efficacy Data Half Maximal Effective Concentration (EC50)
0.033 nM
Positive B7H3 expression (B7H3+++/++)
Method Description
Adding the fresh growth-medium containing the varying concentrations of ADCs, 40ul/well into H358, H441, H1048 and MDA-MB-487.
In Vitro Model Minimally invasive lung adenocarcinoma H358 cells CVCL_1559
Experiment 2 Reporting the Activity Date of This ADC [16]
Efficacy Data Half Maximal Effective Concentration (EC50)
0.056 nM
Negative B7H3 expression (B7H3-)
Method Description
Adding the fresh growth-medium containing the varying concentrations of ADCs, 40ul/well into H358, H441, H1048 and MDA-MB-487.
In Vitro Model Lung small cell carcinoma, Small cell lung cancer H1048 cells CVCL_1453
Experiment 3 Reporting the Activity Date of This ADC [16]
Efficacy Data Half Maximal Effective Concentration (EC50)
0.511 nM
Positive B7H3 expression (B7H3+++/++)
Method Description
Adding the fresh growth-medium containing the varying concentrations of ADCs, 40ul/well into H358, H441, H1048 and MDA-MB-487.
In Vitro Model Lung papillary adenocarcinoma H441 cells CVCL_1561
Experiment 4 Reporting the Activity Date of This ADC [16]
Efficacy Data Half Maximal Effective Concentration (EC50) > 100 nM High B7H3 expression (B7H3 +++)
Method Description
Adding the fresh growth-medium containing the varying concentrations of ADCs, 40ul/well into H358, H441, H1048 and MDA-MB-487.
In Vitro Model Breast adenocarcinoma MDA-MB-453 cells CVCL_0418
WO2024165045A1 ADC-B [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [17]
Efficacy Data Half Maximal Effective Concentration (EC50)
0.5 nM
Low B7H3 expression (B7H3+)
Method Description
Cells were seeded (NCI-1650 or MDA-MB-453 (2E3/well) or Capan-1 (4E3/well)) into 3D 96-well plates (Corning: 4520), 80 ul/well, and incubated at 37 °C, 5% CO2, overnight.
In Vitro Model Pancreatic ductal adenocarcinoma Capan-1 cells CVCL_0237
Experiment 2 Reporting the Activity Date of This ADC [17]
Efficacy Data Half Maximal Effective Concentration (EC50)
3.9 nM
High B7H3 expression (B7H3 +++)
Method Description
Cells were seeded (NCI-1650 or MDA-MB-453 (2E3/well) or Capan-1 (4E3/well)) into 3D 96-well plates (Corning: 4520), 80 ul/well, and incubated at 37 °C, 5% CO2, overnight.
In Vitro Model Lung adenocarcinoma NCI-H1650 cells CVCL_1483
CN119317630A ADC-C14 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 3 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [18]
Efficacy Data Half Maximal Effective Concentration (EC50)
64 nM
Method Description
Distribute the cell lines H358 (1E3/well), to 3D-96-well plates (Corning: 4520), with 80 ul/well. Incubate overnight at 37°C and 5% CO2. Detect the cell viability of H358, H441, H1048 and MDA-MB-453 cells using 3D reagent (Promega, G9683).
In Vitro Model Minimally invasive lung adenocarcinoma H358 cells CVCL_1559
Experiment 2 Reporting the Activity Date of This ADC [18]
Efficacy Data Half Maximal Effective Concentration (EC50)
100 nM
Method Description
Distribute the cell lines H441 (1E3/well) to 3D-96-well plates (Corning: 4520), with 80 ul/well. Incubate overnight at 37°C and 5% CO2. Detect the cell viability of H358, H441, H1048 and MDA-MB-453 cells using 3D reagent (Promega, G9683).
In Vitro Model Lung papillary adenocarcinoma H441 cells CVCL_1561
Experiment 3 Reporting the Activity Date of This ADC [18]
Efficacy Data Half Maximal Effective Concentration (EC50)
100 nM
Method Description
Distribute the cell lines H1048 (1E3/well) to 3D-96-well plates (Corning: 4520), with 80 ul/well. Incubate overnight at 37°C and 5% CO2. Detect the cell viability of H358, H441, H1048 and MDA-MB-453 cells using 3D reagent (Promega, G9683).
In Vitro Model Lung small cell carcinoma, Small cell lung cancer H1048 cells CVCL_1453
CN119317630A ADC-C10 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 3 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [18]
Efficacy Data Half Maximal Effective Concentration (EC50)
66 nM
Method Description
Distribute the cell lines H358 (1E3/well), to 3D-96-well plates (Corning: 4520), with 80 ul/well. Incubate overnight at 37°C and 5% CO2. Detect the cell viability of H358, H441, H1048 and MDA-MB-453 cells using 3D reagent (Promega, G9683).
In Vitro Model Minimally invasive lung adenocarcinoma H358 cells CVCL_1559
Experiment 2 Reporting the Activity Date of This ADC [18]
Efficacy Data Half Maximal Effective Concentration (EC50)
96 nM
Method Description
Distribute the cell lines H1048 (1E3/well) to 3D-96-well plates (Corning: 4520), with 80 ul/well. Incubate overnight at 37°C and 5% CO2. Detect the cell viability of H358, H441, H1048 and MDA-MB-453 cells using 3D reagent (Promega, G9683).
In Vitro Model Lung small cell carcinoma, Small cell lung cancer H1048 cells CVCL_1453
Experiment 3 Reporting the Activity Date of This ADC [18]
Efficacy Data Half Maximal Effective Concentration (EC50)
100 nM
Method Description
Distribute the cell lines H441 (1E3/well) to 3D-96-well plates (Corning: 4520), with 80 ul/well. Incubate overnight at 37°C and 5% CO2. Detect the cell viability of H358, H441, H1048 and MDA-MB-453 cells using 3D reagent (Promega, G9683).
In Vitro Model Lung papillary adenocarcinoma H441 cells CVCL_1561
CN119317630A ADC-C1 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 3 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [18]
Efficacy Data Half Maximal Effective Concentration (EC50)
72 nM
Method Description
Distribute the cell lines H358 (1E3/well), to 3D-96-well plates (Corning: 4520), with 80 ul/well. Incubate overnight at 37°C and 5% CO2. Detect the cell viability of H358, H441, H1048 and MDA-MB-453 cells using 3D reagent (Promega, G9683).
In Vitro Model Minimally invasive lung adenocarcinoma H358 cells CVCL_1559
Experiment 2 Reporting the Activity Date of This ADC [18]
Efficacy Data Half Maximal Effective Concentration (EC50)
96 nM
Method Description
Distribute the cell lines H1048 (1E3/well) to 3D-96-well plates (Corning: 4520), with 80 ul/well. Incubate overnight at 37°C and 5% CO2. Detect the cell viability of H358, H441, H1048 and MDA-MB-453 cells using 3D reagent (Promega, G9683).
In Vitro Model Lung small cell carcinoma, Small cell lung cancer H1048 cells CVCL_1453
Experiment 3 Reporting the Activity Date of This ADC [18]
Efficacy Data Half Maximal Effective Concentration (EC50)
100 nM
Method Description
Distribute the cell lines H441 (1E3/well) to 3D-96-well plates (Corning: 4520), with 80 ul/well. Incubate overnight at 37°C and 5% CO2. Detect the cell viability of H358, H441, H1048 and MDA-MB-453 cells using 3D reagent (Promega, G9683).
In Vitro Model Lung papillary adenocarcinoma H441 cells CVCL_1561
CN119317630A ADC-C11 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 3 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [18]
Efficacy Data Half Maximal Effective Concentration (EC50)
72 nM
Method Description
Distribute the cell lines H358 (1E3/well), to 3D-96-well plates (Corning: 4520), with 80 ul/well. Incubate overnight at 37°C and 5% CO2. Detect the cell viability of H358, H441, H1048 and MDA-MB-453 cells using 3D reagent (Promega, G9683).
In Vitro Model Minimally invasive lung adenocarcinoma H358 cells CVCL_1559
Experiment 2 Reporting the Activity Date of This ADC [18]
Efficacy Data Half Maximal Effective Concentration (EC50)
94 nM
Method Description
Distribute the cell lines H1048 (1E3/well) to 3D-96-well plates (Corning: 4520), with 80 ul/well. Incubate overnight at 37°C and 5% CO2. Detect the cell viability of H358, H441, H1048 and MDA-MB-453 cells using 3D reagent (Promega, G9683).
In Vitro Model Lung small cell carcinoma, Small cell lung cancer H1048 cells CVCL_1453
Experiment 3 Reporting the Activity Date of This ADC [18]
Efficacy Data Half Maximal Effective Concentration (EC50)
100 nM
Method Description
Distribute the cell lines H441 (1E3/well) to 3D-96-well plates (Corning: 4520), with 80 ul/well. Incubate overnight at 37°C and 5% CO2. Detect the cell viability of H358, H441, H1048 and MDA-MB-453 cells using 3D reagent (Promega, G9683).
In Vitro Model Lung papillary adenocarcinoma H441 cells CVCL_1561
CN119317630A ADC-C13 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 3 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [18]
Efficacy Data Half Maximal Effective Concentration (EC50)
73 nM
Method Description
Distribute the cell lines H358 (1E3/well), to 3D-96-well plates (Corning: 4520), with 80 ul/well. Incubate overnight at 37°C and 5% CO2. Detect the cell viability of H358, H441, H1048 and MDA-MB-453 cells using 3D reagent (Promega, G9683).
In Vitro Model Minimally invasive lung adenocarcinoma H358 cells CVCL_1559
Experiment 2 Reporting the Activity Date of This ADC [18]
Efficacy Data Half Maximal Effective Concentration (EC50)
95 nM
Method Description
Distribute the cell lines H1048 (1E3/well) to 3D-96-well plates (Corning: 4520), with 80 ul/well. Incubate overnight at 37°C and 5% CO2. Detect the cell viability of H358, H441, H1048 and MDA-MB-453 cells using 3D reagent (Promega, G9683).
In Vitro Model Lung small cell carcinoma, Small cell lung cancer H1048 cells CVCL_1453
Experiment 3 Reporting the Activity Date of This ADC [18]
Efficacy Data Half Maximal Effective Concentration (EC50)
100 nM
Method Description
Distribute the cell lines H441 (1E3/well) to 3D-96-well plates (Corning: 4520), with 80 ul/well. Incubate overnight at 37°C and 5% CO2. Detect the cell viability of H358, H441, H1048 and MDA-MB-453 cells using 3D reagent (Promega, G9683).
In Vitro Model Lung papillary adenocarcinoma H441 cells CVCL_1561
References
Ref 1 Ifinatamab Deruxtecan (I-DXd) in Subjects With Pretreated Extensive-Stage Small Cell Lung Cancer (ES-SCLC)
Ref 2 Substudy 06E: Umbrella Study of Combination Therapies in Esophageal Cancer (MK-3475-06E/KEYMAKER-U06)
Ref 3 A Study of Ifinatamab Deruxtecan in Subjects With Pretreated Advanced or Metastatic Esophageal Squamous Cell Carcinoma (ESCC) (IDeate-Esophageal01)
Ref 4 Substudy 01I: A Study of Investigational Agents in Participants With Previously Treated Stage IV Squamous Non-small Cell Lung Cancer (NSCLC) (MK-3475-01I/KEYMAKER-U01I)
Ref 5 KEYMAKER-U01 Substudy 01A: Efficacy and Safety Study of Pembrolizumab (MK-3475) With or Without Chemotherapy When Used With Investigational Agents in Treatment-na&iuml;ve Participants With Stage IV Non-small Cell Lung Cancer (NSCLC) (MK-3475-01A/KEYMAKER-U01A)
Ref 6 A Study of Investigational Agents in Participants With Previously Treated Stage IV Nonsquamous Non-small Cell Lung Cancer (NSCLC) (MK-3475-01H/KEYMAKER-U01)
Ref 7 A Study to Evaluate the Safety and Efficacy of Gocatamig (MK-6070) and Ifinatamab Deruxtecan (I-DXd) in Participants With Relapsed/Refractory Extensive-Stage Small Cell Lung Cancer (MK-6070-002)
Ref 8 A Study in Participants With Advanced Cancers Associated With Expression of DLL3 (MK-6070-001/HPN328-4001)
Ref 9 A Clinical Study of Ifinatamab Deruxtecan Based Treatment Combinations or as Monotherapy to Treat Metastatic Castrate Resistant Prostate Cancer (mCRPC) (MK-2400-01A/IDeate-Prostate02)
Ref 10 Study of Ifinatamab Deruxtecan (DS-7300a, I-DXd) in Participants With Advanced Solid Malignant Tumors
Ref 11 A Study To Evaluate The Efficacy And Safety Of Ifinatamab Deruxtecan (I-DXd) In Subjects With Recurrent Or Metastatic Solid Tumors (IDeate-PanTumor02)
Ref 12 A Phase 2, Multicenter, Randomized, Open-label Study of DS-7300a, a B7-H3 Antibody Drug Conjugate (ADC), in Subjects With Pretreated Extensive-stage Small Cell Lung Cancer (ES-SCLC), NCT05280470
Ref 13 Phase I/II, Two-Part, Multicenter First-in-Human Study of DS-7300a in Subjects With Advanced Solid Malignant Tumors, NCT04145622
Ref 14 DS-7300a, a DNA Topoisomerase I Inhibitor, DXd-Based Antibody-Drug Conjugate Targeting B7-H3, Exerts Potent Antitumor Activities in Preclinical Models. Mol Cancer Ther. 2022 Apr 1;21(4):635-646.
Ref 15 Antibody drug conjugate comprising NMT inhibitor and its use
Ref 16 Antibody drug conjugates
Ref 17 Self-stabilizing linker conjugates
Ref 18 Antibody-drug complexes