General Information of This Antibody-drug Conjugate (ADC)
ADC ID
DRG0TBWMT
ADC Name
EP4495597A2 39A-MMAE
Synonyms
EP4495597A2 39A-MMAE
   Click to Show/Hide
Organization
ICONIC THERAPEUTICS LLC
Drug Status
Investigative
Structure
Antibody Name
39A
 Antibody Info 
Antigen Name
Tissue factor (F3)
 Antigen Info 
Payload Name
Monomethyl auristatin E
 Payload Info 
Therapeutic Target
Microtubule (MT)
 Target Info 
Linker Name
Mc-Val-Cit-PABC
 Linker Info 
Conjugate Type
Random conjugation through reduced inter-chain cysteines.
Combination Type
Vedotin
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 lnhibition value (TGl) 
92
%
Undisclosed Undisclosed
Tumor Growth lnhibition value (TGl) 
99
%
Undisclosed Undisclosed
Tumor Growth lnhibition value (TGl) 
137
%
Undisclosed Undisclosed
Revealed Based on the Cell Line Data
Click To Hide/Show 3 Activity Data Related to This Level
Standard Type Value Units Cell Line Disease Model
Half Maximal inhibitory Concentration (lC50) 
0.04
nM
CVCL_0313
Pancreatic ductal adenocarcinoma
Half Maximal inhibitory Concentration (lC50) 
0.05
nM
CVCL_0062
Breast adenocarcinoma
Half Maximal inhibitory Concentration (lC50) 
0.08
nM
CVCL_0037
Skin squamous cell 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 lnhibition value (TGl) 92% Positive TF expression (TF+++/++)
Method Description
In the MDA-MB-231 xenograft model, the ADCs were administered on day 1 and 8 post-randomization at 2 mg/kg (qwk × 2, IV).
In Vivo Model MDA-MB-231 xenograft model
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth lnhibition value (TGl) 99% Positive TF expression (TF+++/++)
Method Description
In the MDA-MB-231 xenograft model, the ADCs were administered on day 1 and 8 post-randomization at 4 mg/kg (qwk × 2, IV).
In Vivo Model MDA-MB-231 xenograft model
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth lnhibition value (TGl) 137% Positive TF expression (TF+++/++)
Method Description
HPAF-II pancreatic carcinoma epidermoid carcinoma cell lines were implanted subcutaneously in the flank of athymic nude mice. Animals were randomized and treated with drugs (2 mg/kg, qwk × 2, IV).
In Vivo Model HPAF-II pancreatic carcinoma xenograft model
Revealed Based on the Cell Line Data
Click To Hide/Show 3 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50) 0.04 nM Positive TF expression (TF+++/++)
Method Description
The TF-specific ADCs were added to HPAF-II cells, with either a 72 h incubation or a 4 h incubation followed by removal of excess ADC and culture for another 73 h. HPAF-II cells were lysed in CTG assay reagent after treatment.
In Vitro Model Pancreatic ductal adenocarcinoma HPAF-II cells CVCL_0313
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50) 0.05 nM Positive TF expression (TF+++/++)
Method Description
The TF-specific ADCs were added to MDA-MB-231 cells, with either a 72 h incubation or a 4 h incubation followed by removal of excess ADC and culture for another 68 h. MDA-MB-231 cells were lysed in CTG assay reagent after treatment.
In Vitro Model Breast adenocarcinoma MDA-MB-231 cells CVCL_0062
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50) 0.08 nM Positive TF expression (TF+++/++)
Method Description
The TF-specific ADCs were added to A431 cells, with either a 72 h incubation or a 4 h incubation followed by removal of excess ADC and culture for another 68 h. A436cells were lysed in CTG assay reagent after treatment.
In Vitro Model Skin squamous cell carcinoma A431 cells CVCL_0037
References
Ref 1 Anti-tissue factor antibodies, antibody-drug conjugates, and related methods