Antibody-drug Conjugate Information

General Information of This Antibody-drug Conjugate (ADC)
ADC ID
DRG0KYBPU
ADC Name
WO2018098269A2 conjugate 43B
Synonyms
WO2018098269A2_conjugate-43B
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Organization
Mersana Therapeutics, Inc.
Drug Status
Investigative
Indication
In total 3 Indication(s)
Breast cancer [ICD11:2C60-2C65]
Investigative
Gastric cancer [ICD11:2B72]
Investigative
Ovarian cancer [ICD11:2C73]
Investigative
Drug-to-Antibody Ratio
6.5
Antibody Name
Trastuzumab
  Antibody Info 
Antigen Name
Receptor tyrosine-protein kinase erbB-2 (ERBB2)
  Antigen Info 
Payload Name
Undisclosed
Linker Name
WO2018098269A2_conjugate 43B linker
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) 
≈ 100
%
CVCL_1603
Gastric tubular adenocarcinoma
Revealed Based on the Cell Line Data
Click To Hide/Show 5 Activity Data Related to This Level
Standard Type Value Units Cell Line Disease Model
Half Maximal Inhibitory Concentration (IC50) 
0.01
nM
CVCL_0033
Breast adenocarcinoma
Half Maximal Inhibitory Concentration (IC50) 
0.04
nM
CVCL_1603
Gastric tubular adenocarcinoma
Half Maximal Inhibitory Concentration (IC50) 
0.1
nM
CVCL_0179
Invasive breast carcinoma
Half Maximal Inhibitory Concentration (IC50) 
0.15
nM
CVCL_0031
Invasive breast carcinoma
Half Maximal Inhibitory Concentration (IC50) 
13.53
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 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 76) High HER2 expression (HER2+++)
Method Description
Female CB-17 SCID mice were inoculated subcutaneously with NCI-N87 cells (n=10 for each group). Mice inoculated subcutaneously with NCI-N87 cells (n=10 for each group) after IV administration as a single dose (1.5 mg/kg) on day 1.
In Vivo Model NCI-N87 CDX model
In Vitro Model Gastric tubular adenocarcinoma NCI-N87 cells CVCL_1603
Revealed Based on the Cell Line Data
Click To Hide/Show 5 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 0.01 nM High HER2 expression (HER2+++)
Method Description
Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
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 Inhibitory Concentration (IC50) 0.04 nM High HER2 expression (HER2+++)
Method Description
Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
In Vitro Model Gastric tubular adenocarcinoma NCI-N87 cells CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 0.10 nM High HER2 expression (HER2+++)
Method Description
Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
In Vitro Model Invasive breast carcinoma BT-474 cells CVCL_0179
Experiment 4 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 0.15 nM Negative HER2 expression (HER2-)
Method Description
Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
In Vitro Model Invasive breast carcinoma MCF-7 cells CVCL_0031
Experiment 5 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 13.53 nM Moderate HER2 expression (HER2++)
Method Description
Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
In Vitro Model Breast ductal carcinoma JIMT-1 cells CVCL_2077
References
Ref 1 Peptide-containing linkers for antibody-drug conjugates.

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