Antibody-drug Conjugate Information

General Information of This Antibody-drug Conjugate (ADC)
ADC ID
DRG0XHELN
ADC Name
CBR96-Phe-Lys-MMAE
Synonyms
CBR96 Phe Lys MMAE
   Click to Show/Hide
Drug Status
Investigative
Indication
In total 1 Indication(s)
Lung cancer [ICD11:2C25]
Investigative
Drug-to-Antibody Ratio
8
Structure
Antibody Name
Anti-Lewis-Y mAb cBR96
  Antibody Info 
Antigen Name
Lewis Y
  Antigen Info 
Payload Name
Monomethyl auristatin E
  Payload Info 
Therapeutic Target
Microtubule (MT)
  Target Info 
Linker Name
Mc-Phe-Lys-PABC
  Linker Info 
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 3 Activity Data Related to This Level
Standard Type Value Units Cell Line Disease Model
Tumor Growth Inhibition value (TGI) 
41.21
%
Karpas-299 cells
ALK-positive anaplastic large cell lymphoma
Tumor Growth Inhibition value (TGI) 
88.67
%
L2987 cells
Lung adenocarcinoma
Tumor Growth Inhibition value (TGI) 
91.6
%
L2987 cells
Lung adenocarcinoma
Revealed Based on the Cell Line Data
Click To Hide/Show 6 Activity Data Related to This Level
Standard Type Value Units Cell Line Disease Model
Half Maximal Inhibitory Concentration (IC50) 
10
ng/mL
OVCAR-3 cells
Ovarian serous adenocarcinoma
Half Maximal Inhibitory Concentration (IC50) 
13
ng/mL
SK-BR-3 cells
Breast adenocarcinoma
Half Maximal Inhibitory Concentration (IC50) 
18
ng/mL
H3396 cells
Breast carcinoma
Half Maximal Inhibitory Concentration (IC50) 
80
ng/mL
MDA-MB-435 cells
Amelanotic melanoma
Half Maximal Inhibitory Concentration (IC50) 
80
ng/mL
RCA cells
Colon carcinoma
Half Maximal Inhibitory Concentration (IC50) 
80
ng/mL
MCF-7 cells
Invasive breast carcinoma
Full List of Activity Data of This Antibody-drug Conjugate
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 3 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) 41.21% (Day 30) Negative Lewis Y expression (Lewis Y-); Positive CD30 expression (CD30+++/++)
Method Description
1 mg conjugate/kg/inj.
In Vivo Model Karpas 299 ALCL cell line xenograft model
In Vitro Model ALK-positive anaplastic large cell lymphoma Karpas-299 cells CVCL_1324
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) 88.67% (Day 40) Negative Lewis Y expression (Lewis Y-); Positive CD30 expression (CD30+++/++)
Method Description
3 mg conjugate/kg/inj.
In Vivo Model L2987 cell line xenograft model
In Vitro Model Lung adenocarcinoma L2987 cells CVCL_H586
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) 91.60% (Day 40) Negative Lewis Y expression (Lewis Y-); Positive CD30 expression (CD30+++/++)
Method Description
3 mg conjugate/kg/inj.
In Vivo Model L2987 cell line xenograft model
In Vitro Model Lung adenocarcinoma L2987 cells CVCL_H586
Revealed Based on the Cell Line Data
Click To Hide/Show 6 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [2]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 10.00 ng/mL Positive Lewis Y expression (Lewis Y+++/++; FACS analysis =2,111)
Method Description
The inhibitory activity of the mAb-Val-Cit-MMAE conjugates exhibited greater in vitrospecificity and lower in vivo toxicity was compared with corresponding hydrazone conjugatescorresponding hydrazone conjugates on H3396 cells.The cytotoxic effects of the conjugates on H3396 cells (cBR96 Ag+,cAC10 Ag-) were determined using both pulsed (2 h) and long-term(97 h) drug exposure assays.

   Click to Show/Hide
In Vitro Model Ovarian serous adenocarcinoma OVCAR-3 cells CVCL_0465
Experiment 2 Reporting the Activity Date of This ADC [2]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 13.00 ng/mL Positive Lewis Y expression (Lewis Y+++/++; FACS analysis =3,500)
Method Description
The inhibitory activity of the mAb-Val-Cit-MMAE conjugates exhibited greater in vitrospecificity and lower in vivo toxicity was compared with corresponding hydrazone conjugatescorresponding hydrazone conjugates on H3396 cells.The cytotoxic effects of the conjugates on H3396 cells (cBR96 Ag+,cAC10 Ag-) were determined using both pulsed (2 h) and long-term(97 h) drug exposure assays.

   Click to Show/Hide
In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC [2]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 18.00 ng/mL Positive Lewis Y expression (Lewis Y+++/++; FACS analysis =755)
Method Description
The inhibitory activity of the mAb-Val-Cit-MMAE conjugates exhibited greater in vitrospecificity and lower in vivo toxicity was compared with corresponding hydrazone conjugatescorresponding hydrazone conjugates on H3396 cells.The cytotoxic effects of the conjugates on H3396 cells (cBR96 Ag+,cAC10 Ag-) were determined using both pulsed (2 h) and long-term(97 h) drug exposure assays.

   Click to Show/Hide
In Vitro Model Breast carcinoma H3396 cells CVCL_D348
Experiment 4 Reporting the Activity Date of This ADC [2]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 80.00 ng/mL Positive Lewis Y expression (Lewis Y+++/++; FACS analysis =922)
Method Description
The inhibitory activity of the mAb-Val-Cit-MMAE conjugates exhibited greater in vitrospecificity and lower in vivo toxicity was compared with corresponding hydrazone conjugatescorresponding hydrazone conjugates on H3396 cells.The cytotoxic effects of the conjugates on H3396 cells (cBR96 Ag+,cAC10 Ag-) were determined using both pulsed (2 h) and long-term(97 h) drug exposure assays.

   Click to Show/Hide
In Vitro Model Amelanotic melanoma MDA-MB-435 cells CVCL_0417
Experiment 5 Reporting the Activity Date of This ADC [2]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 80.00 ng/mL Positive Lewis Y expression (Lewis Y+++/++; FACS analysis =600)
Method Description
The inhibitory activity of the mAb-Val-Cit-MMAE conjugates exhibited greater in vitrospecificity and lower in vivo toxicity was compared with corresponding hydrazone conjugatescorresponding hydrazone conjugates on H3396 cells.The cytotoxic effects of the conjugates on H3396 cells (cBR96 Ag+,cAC10 Ag-) were determined using both pulsed (2 h) and long-term(97 h) drug exposure assays.

   Click to Show/Hide
In Vitro Model Colon carcinoma RCA cells CVCL_R735
Experiment 6 Reporting the Activity Date of This ADC [2]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 80.00 ng/mL Positive Lewis Y expression (Lewis Y+++/++; FACS analysis =645)
Method Description
The inhibitory activity of the mAb-Val-Cit-MMAE conjugates exhibited greater in vitrospecificity and lower in vivo toxicity was compared with corresponding hydrazone conjugatescorresponding hydrazone conjugates on H3396 cells.The cytotoxic effects of the conjugates on H3396 cells (cBR96 Ag+,cAC10 Ag-) were determined using both pulsed (2 h) and long-term(97 h) drug exposure assays.

   Click to Show/Hide
In Vitro Model Invasive breast carcinoma MCF-7 cells CVCL_0031
References
Ref 1 Protease-activated drug development. Theranostics. 2012;2(2):156-78.
Ref 2 An antibody-drug conjugate that targets tissue factor exhibits potent therapeutic activity against a broad range of solid tumors. Cancer Res. 2014 Feb 15;74(4):1214-26.

If you find any error in data or bug in web service, please kindly report it to Dr. Shen et al.