Antibody-drug Conjugate Information

General Information of This Antibody-drug Conjugate (ADC)
ADC ID
DRG0HCBTX
ADC Name
EDB- (κK183C-K94R-K290C)-vc-0101
Synonyms
EDB- (κK183C-K94R-K290C)-vc-0101
   Click to Show/Hide
Organization
Pfizer Inc.
Drug Status
Investigative
Drug-to-Antibody Ratio
3.8
Structure
Antibody Name
EDB- (kK183C-K94R-K290C)
  Antibody Info 
Antigen Name
Vesicle-associated membrane protein 8 (VAMP8)
  Antigen Info 
Payload Name
Auristatin 0101
  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
VC-0101
General Information of The ADMET Data Related to This ADC(2027 Update)
Absorption
Click To Hide/Show 2 Absorption Data Related to This Level
Standard Type Value Units Description Reference
Maximum Observed Concentration (Cmax) 156±30 ug/mL
The pharmacokinetics of EDB- (KK183C-K94R-K290C)-vc-0101 ADC 6mg/kg dosed cynomolgus monkeys
 [1]
Area Under the Concentration-Time Curve (AUC) 14567±3045 ug*hr/mL
The pharmacokinetics of EDB- (KK183C-K94R-K290C)-vc-0101 ADC 6mg/kg dosed cynomolgus monkeys
 [1]
Distribution
Click To Hide/Show 1 Distribution Data Related to This Level
Standard Type Value Units Description Reference
Area Under the Concentration-Time Curve (AUC) 14567±3045 ug*hr/mL
The pharmacokinetics of EDB- (KK183C-K94R-K290C)-vc-0101 ADC 6mg/kg dosed cynomolgus monkeys
 [1]
Metabolism
Click To Hide/Show 1 Metabolism Data Related to This Level
Standard Type Value Units Description Reference
Area Under the Concentration-Time Curve (AUC) 14567±3045 ug*hr/mL
The pharmacokinetics of EDB- (KK183C-K94R-K290C)-vc-0101 ADC 6mg/kg dosed cynomolgus monkeys
 [1]
Excretion
Click To Hide/Show 2 Excretion Data Related to This Level
Standard Type Value Units Description Reference
Area Under the Concentration-Time Curve (AUC) 14567±3045 ug*hr/mL
The pharmacokinetics of EDB- (KK183C-K94R-K290C)-vc-0101 ADC 6mg/kg dosed cynomolgus monkeys
 [1]
Elimination Half-Life (t1/2) 5.9±1.1 days
The pharmacokinetics of EDB- (KK183C-K94R-K290C)-vc-0101 ADC 6mg/kg dosed cynomolgus monkeys
 [1]
General Information of The Activity Data Related to This ADC
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 (lC50) 
216
ng/mL
CVCL_2759
Normal
Half Maximal inhibitory Concentration (lC50) 
15584
ng/mL
CVCL_A8EZ
Colon cancer
Full List of Activity Data of This Antibody-drug Conjugate
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 (lC50) 216 ng/mL Positive EDB expression (EDB+++/++)
Method Description
Calculated using four-parameter logistic model #203 with XLfit v4.2 (IDBS)
In Vitro Model Normal WI38-VA13 cells CVCL_2759
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50) 15584 ng/mL Negative EDB expression (EDB-)
Method Description
Calculated using four-parameter logistic model #203 with XLfit v4.2 (IDBS)
In Vitro Model Colon cancer HT29 cells CVCL_A8EZ
References
Ref 1 Anti-EDB antibodies and antibody-drug conjugates