Antibody-drug Conjugate Information

General Information of This Antibody-drug Conjugate (ADC)
ADC ID
DRG0GKHOI
ADC Name
Her-30.0643
Synonyms
Trastuzumab-30.0643
   Click to Show/Hide
Organization
Heidelberg Pharma AG
Drug Status
Investigative
Indication
In total 2 Indication(s)
Breast cancer [ICD11:2C60-2C65]
Investigative
Ovarian cancer [ICD11:2C73]
Investigative
Drug-to-Antibody Ratio
4
Antibody Name
Trastuzumab
  Antibody Info 
Antigen Name
Receptor tyrosine-protein kinase erbB-2 (ERBB2)
  Antigen Info 
Payload Name
HDP 30.0643
  Payload Info 
Therapeutic Target
DNA-directed RNA polymerase II subunit RPB2 (POLR2B); DNA-directed RNA polymerase III subunit RPC7 (POLR3G)
  Target Info 
Linker Name
Her-30.0643 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 4 Activity Data Related to This Level
Standard Type Value Units Cell Line Disease Model
Tumor Growth Inhibition value (TGI) 
≈ 89.51
%
CVCL_2077
Breast ductal carcinoma
Tumor Growth Inhibition value (TGI) 
≈ 99.05
%
CVCL_2077
Breast ductal carcinoma
Tumor Growth Inhibition value (TGI) 
≈ 100
%
CVCL_2077
Breast ductal carcinoma
Tumor Growth Inhibition value (TGI) 
≈ 100
%
CVCL_2077
Breast ductal carcinoma
Revealed Based on the Cell Line Data
Click To Hide/Show 3 Activity Data Related to This Level
Standard Type Value Units Cell Line Disease Model
Half Maximal Effective Concentration (EC50) 
0.02
nM
CVCL_0033
Breast adenocarcinoma
Half Maximal Effective Concentration (EC50) 
0.03
nM
CVCL_0532
Ovarian serous cystadenocarcinoma
Half Maximal Effective Concentration (EC50) 
1
nM
CVCL_2077
Breast ductal carcinoma
Full List of Activity Data of This Antibody-drug Conjugate
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 4 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 89.51% (Day 17) Moderate HER2 expression (HER2++)
Method Description
Six-week old intact female NMRI nu/nu athymic mice were purchaseo and randomly divided into three groups of eight mice each. 5,000,000 JIMT-cells were injected s.c. into the flank of each mouse. The Her-30.0643 [4.4] was injected once i.v. at a doseof 30 ug/kg with respect to amanitin at day 14.
In Vivo Model JIMT-1 CDX model
In Vitro Model Breast ductal carcinoma JIMT-1 cells CVCL_2077
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 99.05% (Day 17) Moderate HER2 expression (HER2++)
Method Description
Six-week old intact female NMRI nu/nu athymic mice were purchaseo and randomly divided into three groups of eight mice each. 5,000,000 JIMT-cells were injected s.c. into the flank of each mouse. The Her-30.0643 [4.4] was injected once i.v. at a doseof 150 ug/kg with respect to amanitin at day 14.
In Vivo Model JIMT-1 CDX model
In Vitro Model Breast ductal carcinoma JIMT-1 cells CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 100.00% (Day 28) Moderate HER2 expression (HER2++)
Method Description
Six-week old intact female NMRI nu/nu athymic mice were purchaseo and randomly divided into three groups of eight mice each. 5,000,000 JIMT-cells were injected s.c. into the flank of each mouse. The Her-30.0643 [4.4] was injected once i.v. at a doseof 150 ug/kg with respect to amanitin at day 14.
In Vivo Model JIMT-1 CDX model
In Vitro Model Breast ductal carcinoma JIMT-1 cells CVCL_2077
Experiment 4 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 100.00% (Day 28) Moderate HER2 expression (HER2++)
Method Description
Six-week old intact female NMRI nu/nu athymic mice were purchaseo and randomly divided into three groups of eight mice each. 5,000,000 JIMT-cells were injected s.c. into the flank of each mouse. The Her-30.0643 [4.4] was injected once i.v. at a doseof 30 ug/kg with respect to amanitin at day 14.
In Vivo Model JIMT-1 CDX model
In Vitro Model Breast ductal carcinoma JIMT-1 cells CVCL_2077
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 [1]
Efficacy Data Half Maximal Effective Concentration (EC50) 0.02 nM High HER2 expression (HER2 +++)
Method Description
Cell viability was determined after -72 h -incubation with different concentrations of conjugates at 37°C and 5% CO2 by measurement of fixed andpermeabilized cells with an ant-BrdU-HRP antibody.
In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Effective Concentration (EC50) 0.03 nM High HER2 expression (HER2 +++)
Method Description
Cell viability was determined after -72 h -incubation with different concentrations of conjugates at 37°C and 5% CO2 by measurement of fixed andpermeabilized cells with an ant-BrdU-HRP antibody.
In Vitro Model Ovarian serous cystadenocarcinoma SK-OV-3 cells CVCL_0532
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Effective Concentration (EC50) 1.00 nM Moderate HER2 expression (HER2++)
Method Description
Cell viability was determined after -72 h -incubation with different concentrations of conjugates at 37°C and 5% CO2 by measurement of fixed andpermeabilized cells with an ant-BrdU-HRP antibody.
In Vitro Model Breast ductal carcinoma JIMT-1 cells CVCL_2077
References
Ref 1 Amatoxin derivatives.

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