Antibody-drug Conjugate Information

General Information of This Antibody-drug Conjugate (ADC)
ADC ID
DRG0IVKDI
ADC Name
Trastuzumab-alpha-amanitin conjugate 3
Synonyms
Trastuzumab alpha-amanitin conjugate 3
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Organization
Heidelberg Pharma AG
Drug Status
Investigative
Indication
In total 2 Indication(s)
Breast cancer
Investigative
.
Ovarian cancer
Investigative
.
Drug-to-Antibody Ratio
2
Antibody Name
Trastuzumab
  Antibody Info 
Antigen Name
Receptor tyrosine-protein kinase erbB-2 (HER2)
  Antigen Info 
Payload Name
Alpha-amanitin
  Payload Info 
Therapeutic Target
DNA-directed RNA polymerase II subunit RPB2 (POLR2B); DNA-directed RNA polymerase III subunit RPC7 (POLR3G)
  Target Info 
Linker Name
Trastuzumab-alpha-amanitin conjugate 3 linker
Conjugate Type
Random 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 2 Activity Data Related to This Level
Standard Type Value Units Cell Line Disease Model
Tumor Growth Inhibition value (TGI) 
≈ 71.25
%
CVCL_0532
Ovarian serous cystadenocarcinoma
Tumor Growth Inhibition value (TGI) 
≈ 85.43
%
CVCL_0532
Ovarian serous cystadenocarcinoma
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) ≈ 71.25% (Day 87) High HER2 expression (HER2 +++)
Method Description
A mouse tumor xenograft model, wherein 250,000,000 SKOV-3 ovarial carcinoma cellsare implated sub-cutaneously (s.c,) into SCID mice and allowed to grow for 10 days. After 10 days a single dose of 30 ug/kg body weight of various a-amanitin-Herceptin conjugates.
In Vivo Model SK-OV-3 CDX model
In Vitro Model Ovarian serous cystadenocarcinoma SK-OV-3 cells CVCL_0532
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 85.43% (Day 87) High HER2 expression (HER2 +++)
Method Description
A mouse tumor xenograft model, wherein 250,000,000 SKOV-3 ovarial carcinoma cellsare implated sub-cutaneously (s.c,) into SCID mice and allowed to grow for 10 days. After 10 days a single dose of 150 ug/kg body weight of various a-amanitin-Herceptin conjugates.
In Vivo Model SK-OV-3 CDX model
In Vitro Model Ovarian serous cystadenocarcinoma SK-OV-3 cells CVCL_0532
References
Ref 1 Amatoxin-armed therapeutic cell surface binding components designed for tumour therapy.