General Information of This Antibody-drug Conjugate (ADC)
ADC ID
DRG0RIJZL
ADC Name
WO2013055987A1 Tmab-101
Synonyms
WO2013055987A1 Tmab-101
   Click to Show/Hide
Organization
ADC Therapeutics SA; Genentech, Inc.
Drug Status
Investigative
Indication
In total 1 Indication(s)
Breast cancer [ICD11:2C60-2C65]
Investigative
Drug-to-Antibody Ratio
1.6
Structure
Antibody Name
Trastuzumab
 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
WO2013055987A1_Tmab-101 linker
General Information of The Activity Data Related to This ADC
Obtained from the Model Organism Data
Click To Hide/Show 4 Activity Data Related to This Level
Standard Type Value Units Animal Model (No. of PDX)
Tumor Growth Inhibition value (TGI) 
≈ 78.27
%
Breast cancer model MMTV-HER2 Fo5
Tumor Growth Inhibition value (TGI) 
≈ 86.68
%
Breast cancer model MMTV-HER2 Fo5
Tumor Growth Inhibition value (TGI) 
≈ 87.51
%
Breast cancer model MMTV-HER2 Fo5
Tumor Growth Inhibition value (TGI) 
≈ 94.92
%
Breast cancer model MMTV-HER2 Fo5
Revealed Based on the Cell Line Data
Click To Hide/Show 2 Activity Data Related to This Level
Standard Type Value Units Cell Line Disease Model
Half Maximal Inhibitory Concentration (IC50) 
22.12
ug/mL
SK-BR-3 cells
Breast adenocarcinoma
Half Maximal Inhibitory Concentration (IC50) 
> 500
ug/mL
MCF-7 cells
Invasive breast carcinoma
Full List of Activity Data of This Antibody-drug Conjugate
Obtained from the Model Organism Data
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) ≈ 78.27% (Day 11) High HER2 expression (HER2 +++)
Method Description
Before being used for an in vivo efficacy study, the MMTV-HER2 Fo5 transgenic mammary tumor was surgically transplanted into the mammary fat pad of nu/nu mice in fragments that measured approximately 2x2 mm. When tumor sreached desired volumes, the tumor-bearing mice were randomized and given a single dose by IV 1 mg/kg injection of the ADC.
In Vivo Model Breast cancer model MMTV-HER2 Fo5
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 86.68% (Day 14) High HER2 expression (HER2 +++)
Method Description
Before being used for an in vivo efficacy study, the MMTV-HER2 Fo5 transgenic mammary tumor was surgically transplanted into the mammary fat pad of nu/nu mice in fragments that measured approximately 2x2 mm. MMTV-HER2 Fo5 mammary allograft tumors inoculated into CRL nu/nu mice aftersingle,then iv 1 mg/kg ADC dosing on day 0.
In Vivo Model Breast cancer model MMTV-HER2 Fo5
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 87.51% (Day 11) High HER2 expression (HER2 +++)
Method Description
Before being used for an in vivo efficacy study, the MMTV-HER2 Fo5 transgenic mammary tumor was surgically transplanted into the mammary fat pad of nu/nu mice in fragments that measured approximately 2x2 mm. When tumor sreached desired volumes, the tumor-bearing mice were randomized and given a single dose by IV 3 mg/kg injection of the ADC.
In Vivo Model Breast cancer model MMTV-HER2 Fo5
Experiment 4 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 94.92% (Day 11) High HER2 expression (HER2 +++)
Method Description
Before being used for an in vivo efficacy study, the MMTV-HER2 Fo5 transgenic mammary tumor was surgically transplanted into the mammary fat pad of nu/nu mice in fragments that measured approximately 2x2 mm. When tumor sreached desired volumes, the tumor-bearing mice were randomized and given a single dose by IV 10 mg/kg injection of the ADC.
In Vivo Model Breast cancer model MMTV-HER2 Fo5
Revealed Based on the Cell Line Data
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 22.12 ug/mL High HER2 expression (HER2 +++)
Method Description
Certain cells are seeded at 1000-2000/well or 2000-3000/well in a 96-well plate, 50 uL/well. After one or two days, ADCs are added with "no ADC" control wells receiving medium alone. Conditions are in duplicate or triplicate After 3-5 days, 100 uL/well Cell TiterGlo ll isadded.
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) > 500 ug/mL Negative HER2 expression (HER2 -)
Method Description
Certain cells are seeded at 1000-2000/well or 2000-3000/well in a 96-well plate, 50 uL/well. After one or two days, ADCs are added with "no ADC" control wells receiving medium alone. Conditions are in duplicate or triplicate After 3-5 days, 100 uL/well Cell TiterGlo ll isadded.
In Vitro Model Invasive breast carcinoma MCF-7 cells CVCL_0031
References
Ref 1 Pyrrolobenzodiazepines and conjugates thereof; 2013-04-18.

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