Antibody-drug Conjugate Information

General Information of This Antibody-drug Conjugate (ADC)
ADC ID
DRG0KHFFZ
ADC Name
PF-06263507
Synonyms
PF06263507; MMAF ADC; PF 6263507; A1-mcMMAF; A1-mafodotin
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Organization
Oxford Biomedica Plc; Pfizer Inc.
Drug Status
Terminated in phase 1
Indication
In total 3 Indication(s)
Breast cancer [ICD11:2C60-2C65]
Terminated in phase 1
Non-small cell lung cancer [ICD11:2C25]
Terminated in phase 1
Ovarian cancer [ICD11:2C73]
Terminated in phase 1
Drug-to-Antibody Ratio
4
Structure
Antibody Name
PF-06281192
  Antibody Info 
Antigen Name
Trophoblast glycoprotein (TPBG)
  Antigen Info 
Payload Name
Monomethyl auristatin F
  Payload Info 
Therapeutic Target
Microtubule (MT)
  Target Info 
Linker Name
Maleimido-caproyl
  Linker Info 
Conjugate Type
Random conjugation through reduced inter-chain cysteines.
Combination Type
McMMAF
Puchem SID
463820238 , 472419799 , 404719995
DrugMap ID
DM5KBDY
TTD ID
D03JZC
ChEBI ID
CHEMBL4297804
General Information of The Activity Data Related to This ADC
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 2 Activity Data Related to This Level
Standard Type Value Units Cell Line Disease Model
Tumor Growth Inhibition value (TGI) 
≈ 71.7
%
Lung cancer cells
Lung cancer
Tumor Growth Inhibition value (TGI) 
≈ 100
%
Lung cancer cells
Lung cancer
Full List of Activity Data of This Antibody-drug Conjugate
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 71.70% (Day 60) 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.

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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 [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 100.00% (Day 60) 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.

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In Vivo Model Lung cancer CDX model
In Vitro Model Lung cancer Lung cancer cells Homo sapiens
References
Ref 1 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.

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