Antibody-drug Conjugate Information

General Information of This Antibody-drug Conjugate (ADC)
ADC ID
DRG0EZZAW
ADC Name
PEN-221
Synonyms
PEN 221; PEN221
   Click to Show/Hide
Organization
Tarveda Therapeutics, Inc.
Drug Status
Phase 1/2
Antibody Name
Undisclosed
Antigen Name
Somatostatin receptor type 2 (SSTR2)
  Antigen Info 
Payload Name
Mertansine DM1
  Payload Info 
Therapeutic Target
Microtubule (MT)
  Target Info 
Linker Name
Disulfide cleavable linker
  Linker Info 
Conjugate Type
Site-specific conjugation through the Sortase A.
Elimination
The route of elimination has not yet been fully elucidated. After IV infusion, trastuzumab emtansine has a clearance of 0.68 L/day.
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) 5.93 uM
PEN-221 plasma concentration profile following intravenous administration to non-tumor bearing mice, 2 mg/kg.
 [1]
Area Under the Concentration-Time Curve (AUC) 7.3 uM*h
PEN-221 plasma concentration profile following intravenous administration to non-tumor bearing mice, 2 mg/kg.
 [1]
Distribution
Click To Hide/Show 2 Distribution Data Related to This Level
Standard Type Value Units Description Reference
Area Under the Concentration-Time Curve (AUC) 7.3 uM*h
PEN-221 plasma concentration profile following intravenous administration to non-tumor bearing mice, 2 mg/kg.
 [1]
Volume of Distribution (Vd) 963 mL/kg
PEN-221 plasma concentration profile following intravenous administration to non-tumor bearing mice, 2 mg/kg.
 [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) 7.3 uM*h
PEN-221 plasma concentration profile following intravenous administration to non-tumor bearing mice, 2 mg/kg.
 [1]
Excretion
Click To Hide/Show 3 Excretion Data Related to This Level
Standard Type Value Units Description Reference
Area Under the Concentration-Time Curve (AUC) 7.3 uM*h
PEN-221 plasma concentration profile following intravenous administration to non-tumor bearing mice, 2 mg/kg.
 [1]
Elimination Half-Life (t1/2) 12.2 h
PEN-221 plasma concentration profile following intravenous administration to non-tumor bearing mice, 2 mg/kg.
 [1]
Clearance (CL) 2.32 mL/kg/min
PEN-221 plasma concentration profile following intravenous administration to non-tumor bearing mice, 2 mg/kg.
 [1]
References
Ref 1 Targeting the Somatostatin Receptor 2 with the Miniaturized Drug Conjugate, PEN-221: A Potent and Novel Therapeutic for the Treatment of Small Cell Lung Cancer