Antibody-drug Conjugate Information

General Information of This Antibody-drug Conjugate (ADC)
ADC ID
DRG0TGUXX
ADC Name
huHEA125-amanitin3
Synonyms
huHEA125 Amanitin3
   Click to Show/Hide
Organization
Heidelberg Pharma AG
Drug Status
Investigative
Indication
In total 4 Indication(s)
Breast cancer [ICD11:2C60-2C65]
Investigative
Cholangiocarcinoma [ICD11:2C12]
Investigative
Colon adenocarcinoma [ICD11:2B90]
Investigative
Pancreatic ductal adenocarcinoma [ICD11:2C10]
Investigative
Drug-to-Antibody Ratio
8
Antibody Name
huHEA125
  Antibody Info 
Antigen Name
Epithelial cell adhesion molecule (EPCAM)
  Antigen Info 
Payload Name
Beta-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
huHEA125-Amanitin3 linker
Conjugate Type
Random conjugation through nucleophilic lysines.
General Information of The Activity Data Related to This ADC
Revealed Based on the Cell Line Data
Click To Hide/Show 4 Activity Data Related to This Level
Standard Type Value Units Cell Line Disease Model
Half Maximal Inhibitory Concentration (IC50) 
1-40
pM
CVCL_0218
Colon adenocarcinoma
Half Maximal Inhibitory Concentration (IC50) 
2
pM
CVCL_0031
Invasive breast carcinoma
Half Maximal Inhibitory Concentration (IC50) 
0.01-0.3
nM
CVCL_0237
Pancreatic ductal adenocarcinoma
Half Maximal Inhibitory Concentration (IC50) 
0.01-0.6
nM
CVCL_3118
Cholangiocarcinoma
Full List of Activity Data of This Antibody-drug Conjugate
Revealed Based on the Cell Line Data
Click To Hide/Show 4 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 1-40 pM Positive EPCAM expression (EPCAM+++/++)
Method Description
Cells were added in 50 ul at a density of 50,000 per ml in the experiments with ADCs and at a density of 20,000 per ml in the experiments with huHEA125-Amanitin3. Plates were incubated in a humidified atmosphere at 37°C and 5% CO2 for 72 or 96 h. At 20 h before the end of the assay, 1 uCi of H-thymidine was added.
In Vitro Model Colon adenocarcinoma COLO 205 cells CVCL_0218
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 2.00 pM Positive EPCAM expression (EPCAM+++/++)
Method Description
Cells were added in 50 ul at a density of 50,000 per ml in the experiments with ADCs and at a density of 20,000 per ml in the experiments with huHEA125-Amanitin3. Plates were incubated in a humidified atmosphere at 37°C and 5% CO2 for 72 or 96 h. At 20 h before the end of the assay, 1 uCi of H-thymidine was added.
In Vitro Model Invasive breast carcinoma MCF-7 cells CVCL_0031
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 0.01-0.3 nM Positive EPCAM expression (EPCAM+++/++)
Method Description
Cells were added in 50 ul at a density of 50,000 per ml in the experiments with ADCs and at a density of 20,000 per ml in the experiments with huHEA125-Amanitin3. Plates were incubated in a humidified atmosphere at 37°C and 5% CO2 for 72 or 96 h. At 20 h before the end of the assay, 1 uCi of H-thymidine was added.
In Vitro Model Pancreatic ductal adenocarcinoma Capan-1 cells CVCL_0237
Experiment 4 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 0.01-0.6 nM Positive EPCAM expression (EPCAM+++/++)
Method Description
Cells were added in 50 ul at a density of 50,000 per ml in the experiments with ADCs and at a density of 20,000 per ml in the experiments with huHEA125-Amanitin3. Plates were incubated in a humidified atmosphere at 37°C and 5% CO2 for 72 or 96 h. At 20 h before the end of the assay, 1 uCi of H-thymidine was added.
In Vitro Model Cholangiocarcinoma OZ cells CVCL_3118
References
Ref 1 Amatoxin-armed therapeutic cell surface binding components designed for tumour therapy.

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