Antibody-drug Conjugate Information

General Information of This Antibody-drug Conjugate (ADC)
ADC ID
DRG0OXIMZ
ADC Name
CTX-MMAE
Synonyms
CTX-vcPABC-MMAE
   Click to Show/Hide
Drug Status
Investigative
Indication
In total 1 Indication(s)
Pancreatic cancer [ICD11:2C10]
Investigative
Drug-to-Antibody Ratio
4
Antibody Name
Cetuximab
  Antibody Info 
Antigen Name
Epidermal growth factor receptor (EGFR)
  Antigen Info 
Payload Name
Monomethyl auristatin E
  Payload Info 
Therapeutic Target
Microtubule (MT)
  Target Info 
Linker Name
PD-Val-Cit-PABC
  Linker Info 
Conjugate Type
Site-specific 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 12 Activity Data Related to This Level
Standard Type Value Units Cell Line Disease Model
Tumor Growth Inhibition value (TGI) 
≈ 12.5
%
MIA PaCa-2 cells
Pancreatic ductal adenocarcinoma
Tumor Growth Inhibition value (TGI) 
≈ 15.63
%
PANC-1 cells
Pancreatic ductal adenocarcinoma
Tumor Growth Inhibition value (TGI) 
≈ 45.63
%
PANC-1 cells
Pancreatic ductal adenocarcinoma
Tumor Growth Inhibition value (TGI) 
≈ 54.17
%
MIA PaCa-2 cells
Pancreatic ductal adenocarcinoma
Tumor Growth Inhibition value (TGI) 
≈ 87.5
%
PANC-1 cells
Pancreatic ductal adenocarcinoma
Tumor Growth Inhibition value (TGI) 
≈ 100
%
MIA PaCa-2 cells
Pancreatic ductal adenocarcinoma
Median survival time (MST) 
14
Day
MIA PaCa-2 cells
Pancreatic ductal adenocarcinoma
Median survival time (MST) 
23
Day
PANC-1 cells
Pancreatic ductal adenocarcinoma
Median survival time (MST) 
24
Day
MIA PaCa-2 cells
Pancreatic ductal adenocarcinoma
Median survival time (MST) 
30
Day
PANC-1 cells
Pancreatic ductal adenocarcinoma
Median survival time (MST) 
60
Day
MIA PaCa-2 cells
Pancreatic ductal adenocarcinoma
Median survival time (MST) 
61
Day
PANC-1 cells
Pancreatic ductal adenocarcinoma
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) 
39
pM
PANC-1 cells
Pancreatic ductal adenocarcinoma
Half Maximal Inhibitory Concentration (IC50) 
1.38
nM
MIA PaCa-2 cells
Pancreatic ductal adenocarcinoma
Full List of Activity Data of This Antibody-drug Conjugate
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 12 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 12.50% (Day 10 Positive EGFR expression (EGFR +++/++)
Method Description
CB17 SCID mice bearing subcutaneous MIA PaCa-2 (n = 4-5 pergroup) xenografts were intravenously injected with saline, CTX-MMAE (0.1 mg/kg) on day 0 and 8 of the study (indicated by vertical dashed lines).
In Vivo Model MIA PaCa-2 CDX model
In Vitro Model Pancreatic ductal adenocarcinoma MIA PaCa-2 cells CVCL_0428
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 15.63% (Day 20) Positive EGFR expression (EGFR +++/++)
Method Description
CB17 SCID mice bearing subcutaneous PANC-1 (n = 4-5 pergroup) xenografts were intravenously injected with saline, CTX-MMAE (0.1 mg/kg) on day 0 and 8 of the study (indicated by vertical dashed lines).
In Vivo Model PANC-1 CDX model
In Vitro Model Pancreatic ductal adenocarcinoma PANC-1 cells CVCL_0480
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 45.63% (Day 20) Positive EGFR expression (EGFR +++/++)
Method Description
CB17 SCID mice bearing subcutaneous PANC-1 (n = 4-5 pergroup) xenografts were intravenously injected with saline, CTX-MMAE (1 mg/kg) on day 0 and 8 of the study (indicated by vertical dashed lines).
In Vivo Model PANC-1 CDX model
In Vitro Model Pancreatic ductal adenocarcinoma PANC-1 cells CVCL_0480
Experiment 4 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 54.17% (Day 10) Positive EGFR expression (EGFR +++/++)
Method Description
CB17 SCID mice bearing subcutaneous MIA PaCa-2 (n = 4-5 pergroup) xenografts were intravenously injected with saline, CTX-MMAE (1 mg/kg) on day 0 and 8 of the study (indicated by vertical dashed lines).
In Vivo Model MIA PaCa-2 CDX model
In Vitro Model Pancreatic ductal adenocarcinoma MIA PaCa-2 cells CVCL_0428
Experiment 5 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 87.50% (Day 20) Positive EGFR expression (EGFR +++/++)
Method Description
CB17 SCID mice bearing subcutaneous PANC-1 (n = 4-5 pergroup) xenografts were intravenously injected with saline, CTX-MMAE (5 mg/kg) on day 0 and 8 of the study (indicated by vertical dashed lines).
In Vivo Model PANC-1 CDX model
In Vitro Model Pancreatic ductal adenocarcinoma PANC-1 cells CVCL_0480
Experiment 6 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 100.00% (Day 10) Positive EGFR expression (EGFR +++/++)
Method Description
CB17 SCID mice bearing subcutaneous MIA PaCa-2 (n = 4-5 pergroup) xenografts were intravenously injected with saline, CTX-MMAE (5 mg/kg) on day 0 and 8 of the study (indicated by vertical dashed lines).
In Vivo Model MIA PaCa-2 CDX model
In Vitro Model Pancreatic ductal adenocarcinoma MIA PaCa-2 cells CVCL_0428
Experiment 7 Reporting the Activity Date of This ADC [1]
Efficacy Data Median survival time (MST) 14 Day Positive EGFR expression (EGFR +++/++)
Method Description
CB17 SCID mice bearing subcutaneous MIA PaCa-2 (n = 4-5 pergroup) xenografts were intravenously injected with saline, CTX-MMAE (0.1 mg/kg) on day 0 and 8 of the study (indicated by vertical dashed lines).
In Vivo Model MIA PaCa-2 CDX model
In Vitro Model Pancreatic ductal adenocarcinoma MIA PaCa-2 cells CVCL_0428
Experiment 8 Reporting the Activity Date of This ADC [1]
Efficacy Data Median survival time (MST) 23 Day Positive EGFR expression (EGFR +++/++)
Method Description
CB17 SCID mice bearing subcutaneous PANC-1 (n = 4-5 pergroup) xenografts were intravenously injected with saline, CTX-MMAE (0.1 mg/kg) on day 0 and 8 of the study (indicated by vertical dashed lines).
In Vivo Model PANC-1 CDX model
In Vitro Model Pancreatic ductal adenocarcinoma PANC-1 cells CVCL_0480
Experiment 9 Reporting the Activity Date of This ADC [1]
Efficacy Data Median survival time (MST) 24 Day Positive EGFR expression (EGFR +++/++)
Method Description
CB17 SCID mice bearing subcutaneous MIA PaCa-2 (n = 4-5 pergroup) xenografts were intravenously injected with saline, CTX-MMAE (1 mg/kg) on day 0 and 8 of the study (indicated by vertical dashed lines).
In Vivo Model MIA PaCa-2 CDX model
In Vitro Model Pancreatic ductal adenocarcinoma MIA PaCa-2 cells CVCL_0428
Experiment 10 Reporting the Activity Date of This ADC [1]
Efficacy Data Median survival time (MST) 30 Day Positive EGFR expression (EGFR +++/++)
Method Description
CB17 SCID mice bearing subcutaneous PANC-1 (n = 4-5 pergroup) xenografts were intravenously injected with saline, CTX-MMAE (1 mg/kg) on day 0 and 8 of the study (indicated by vertical dashed lines).
In Vivo Model PANC-1 CDX model
In Vitro Model Pancreatic ductal adenocarcinoma PANC-1 cells CVCL_0480
Experiment 11 Reporting the Activity Date of This ADC [1]
Efficacy Data Median survival time (MST) 60 Day Positive EGFR expression (EGFR +++/++)
Method Description
CB17 SCID mice bearing subcutaneous MIA PaCa-2 (n = 4-5 pergroup) xenografts were intravenously injected with saline, CTX-MMAE (5 mg/kg) on day 0 and 8 of the study (indicated by vertical dashed lines).
In Vivo Model MIA PaCa-2 CDX model
In Vitro Model Pancreatic ductal adenocarcinoma MIA PaCa-2 cells CVCL_0428
Experiment 12 Reporting the Activity Date of This ADC [1]
Efficacy Data Median survival time (MST) 61 Day Positive EGFR expression (EGFR +++/++)
Method Description
CB17 SCID mice bearing subcutaneous PANC-1 (n = 4-5 pergroup) xenografts were intravenously injected with saline, CTX-MMAE (5 mg/kg) on day 0 and 8 of the study (indicated by vertical dashed lines).
In Vivo Model PANC-1 CDX model
In Vitro Model Pancreatic ductal adenocarcinoma PANC-1 cells CVCL_0480
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) 39.00 pM Positive EGFR expression (EGFR +++/++)
Method Description
MIA PaCa-2 and PANC-1 cells were seeded at 1000 and 1500 per well, respectively, in a 96-well plate and left to adhere overnight. Cells were treated with a 5-fold dilution series of CTX-MMAE or CTX ranging from 0.000256 to 500 nM for 96 h.
In Vitro Model Pancreatic ductal adenocarcinoma PANC-1 cells CVCL_0480
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 1.38 nM Positive EGFR expression (EGFR +++/++)
Method Description
MIA PaCa-2 and PANC-1 cells were seeded at 1000 and 1500 per well, respectively, in a 96-well plate and left to adhere overnight. Cells were treated with a 5-fold dilution series of CTX-MMAE or CTX ranging from 0.000256 to 500 nM for 96 h.
In Vitro Model Pancreatic ductal adenocarcinoma MIA PaCa-2 cells CVCL_0428
References
Ref 1 Two engineered site-specific antibody-drug conjugates, HLmD4 and HLvM4, have potent therapeutic activity in two DLL4-positive tumour xenograft models. Am J Cancer Res. 2020 Aug 1;10(8):2387-2408. eCollection 2020.

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