Antibody-drug Conjugate Information

General Information of This Antibody-drug Conjugate (ADC)
ADC ID
DRG0LSAKO
ADC Name
PF-06888667
Synonyms
PF 06888667; PF06888667
   Click to Show/Hide
Drug Status
Investigative
Indication
In total 1 Indication(s)
Gastric cancer [ICD11:2B72]
Investigative
Drug-to-Antibody Ratio
4
Antibody Name
Trastuzumab
  Antibody Info 
Antigen Name
Receptor tyrosine-protein kinase erbB-2 (ERBB2)
  Antigen Info 
Payload Name
SW-163D
  Payload Info 
Therapeutic Target
Human Deoxyribonucleic acid (hDNA)
  Target Info 
Linker Name
AcLys-Val-Cit-PABC-DMAE
  Linker Info 
Conjugate Type
Site-specific conjugation conjugation through nucleophilic lysines.
General Information of The Activity Data Related to This ADC
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 1 Activity Data Related to This Level
Standard Type Value Units Cell Line Disease Model
Tumor Growth Inhibition value (TGI) 
≈ 100
%
NCI-N87 cells
Gastric tubular adenocarcinoma
Full List of Activity Data of This Antibody-drug Conjugate
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 1 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 100.00% (Day 35) High HER2 expression (HER2+++)
Method Description
Athymic mice were inoculated with HER2-positive N87 tumor cells. When tumors reached approximately 300 mm3, mice were administered PBS vehicle or the indicated ADCs at 1 mg/kg every 4 days (days 1, 5, 9, 13).
In Vivo Model NCI-N87 CDX model
In Vitro Model Gastric tubular adenocarcinoma NCI-N87 cells CVCL_1603
References
Ref 1 Natural Product Bis-Intercalator Depsipeptides as a New Class of Payloads for Antibody-Drug Conjugates. Bioconjug Chem. 2019 Jan 16;30(1):200-209. doi: 10.1021/acs.bioconjchem.8b00843. Epub 2018 Dec 13.

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