Antibody-drug Conjugate Information

General Information of This Antibody-drug Conjugate (ADC)
ADC ID
DRG0KEGVL
ADC Name
HER2-HC-Me-SS-PBD
Synonyms
HER2-HC-A140C-Me-SS-PBD
   Click to Show/Hide
Drug Status
Investigative
Indication
In total 1 Indication(s)
Breast cancer [ICD11:2C60-2C65]
Investigative
Drug-to-Antibody Ratio
1.9-2
Antibody Name
Anti-HER2 mAb
  Antibody Info 
Antigen Name
Receptor tyrosine-protein kinase erbB-2 (ERBB2)
  Antigen Info 
Payload Name
SG2000
  Payload Info 
Therapeutic Target
Human Deoxyribonucleic acid (hDNA)
  Target Info 
Linker Name
Me-disulfide linker
  Linker Info 
Conjugate Type
Random conjugation through reduced inter-chain cysteines.
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) 
≈ 44
%
MMTV-HER2 cells
Breast cancer
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) ≈ 44.00% (Day 24) High HER2 expression (HER2+++)
Method Description
All animals were euthanized before tumors reached 3000 mm3 or showed signs of impending ulceration. Mice were dosed IV via the tail vein with ADC conjugates A1-A4. A1 and A2 were dosed at 4 mg/kg.
In Vivo Model MMTV-HER2 Fo5 CDX model (Trastuzumab resistant)
In Vitro Model Breast cancer MMTV-HER2 cells Mus musculus
References
Ref 1 Intratumoral Payload Concentration Correlates with the Activity of Antibody-Drug Conjugates. Mol Cancer Ther. 2018 Mar;17(3):677-685. doi: 10.1158/1535-7163.MCT-17-0697. Epub 2018 Jan 18.

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