Antibody-drug Conjugate Information

General Information of This Antibody-drug Conjugate (ADC)
ADC ID
DRG0REROK
ADC Name
BGA9962
Synonyms
BGA9962
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Organization
BEIGENE, LTD. | BEIGENE SWITZERLAND GMBH
Drug Status
Investigative
Drug-to-Antibody Ratio
7.8
Structure
Antibody Name
BGA5384
  Antibody Info 
Antigen Name
Carcinoembryonic antigen-related cell adhesion molecule 5 (CEACAM5)
  Antigen Info 
Payload Name
ADC-C3 Payload
  Payload Info 
Linker Name
Linker of ADC2-58
  Linker Info 
Conjugate Type
Random conjugation through reduced inter-chain cysteines.
General Information of The Activity Data Related to This ADC
Discovered Using Patient-derived Xenograft Model
Click To Hide/Show 2 Activity Data Related to This Level
Standard Type Value Units Animal Model (No. of PDX)
Tumor Growth lnhibition value (TGl) 
106
%
Human patient-derived gastric xenograft model
Tumor Growth lnhibition value (TGl) 
107
%
Human patient-derived gastric xenograft model
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 Effective Concentration (EC50) 
0.17
nM
CVCL_1531
Lung adenocarcinoma
Half Maximal Effective Concentration (EC50) 
0.39
nM
CVCL_0434
Gastric adenocarcinoma
Half Maximal Effective Concentration (EC50) 
0.83
nM
CVCL_1384
Colon adenocarcinoma
Half Maximal Effective Concentration (EC50) 
27
nM
CVCL_0062
Breast adenocarcinoma
Full List of Activity Data of This Antibody-drug Conjugate
Discovered Using Patient-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 lnhibition value (TGl) 106% Positive CEA expression (CEA+++/++)
Method Description
Human patient-derived gastric tumors were induced on the right flank by a subcutaneous injection. When tumor volume reached approximately 200 mm3 in size, mice were randomized into 5 groups with 8, 9, and 9 animals in vehicle, BGA7650, and BGA9962 groups on Day 0, respectively. After ensuring all cohorts hadapproximately equal average tumor volumes to start, animals were intravenously administered vehicle, BGA9962 (2 mg/kg) on treatment Day 1. Animal body weight and tumor volume were measured twice weekly.

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In Vivo Model Human patient-derived gastric xenograft model
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth lnhibition value (TGl) 107% Positive CEA expression (CEA+++/++)
Method Description
Human patient-derived gastric tumors were induced on the right flank by a subcutaneous injection. When tumor volume reached approximately 200 mm3 in size, mice were randomized into 5 groups with 8, 9, and 9 animals in vehicle, BGA7650, and BGA9962 groups on Day 0, respectively. After ensuring all cohorts hadapproximately equal average tumor volumes to start, animals were intravenously administered vehicle, BGA9962 (6 mg/kg) on treatment Day 1. Animal body weight and tumor volume were measured twice weekly.

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In Vivo Model Human patient-derived gastric xenograft model
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 Effective Concentration (EC50) 0.17 nM Positive CEA expression (CEA+++/++)
Method Description
NCI-H2122 cells were plated at a density of 2000 cells per well and the next day were treated with payload compounds (5x dilution) for 6 days.
In Vitro Model Lung adenocarcinoma NCI-H2122 cells CVCL_1531
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Effective Concentration (EC50) 0.39 nM Positive CEA expression (CEA+++/++)
Method Description
MKN45 cells were plated at a density of 5000 cells per well and the next day were treated with payload compounds (5x dilution) for 6 days.
In Vitro Model Gastric adenocarcinoma MKN45 cells CVCL_0434
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Effective Concentration (EC50) 0.83 nM Positive CEA expression (CEA+++/++)
Method Description
Ls147T cells were plated at a density of 5000 cells per well and the next day were treated with payload compounds (5x dilution) for 6 days.
In Vitro Model Colon adenocarcinoma Ls147T cells CVCL_1384
Experiment 4 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Effective Concentration (EC50) 27 nM Negative CEA expression (CEA-)
Method Description
MDA-MB-231 cells were plated at a density of 2000 cells per well and the next day were treated with payload compounds (5x dilution) for 6 days.
In Vitro Model Breast adenocarcinoma MDA-MB-231 cells CVCL_0062
References
Ref 1 Anti-CEA antibody drug conjugates and methods of use