- Molecular NameEntacapone
- SynonymEntacapona [INN-Spanish]; entacapone; Entacapone [Usan:Inn]; Entacaponum [INN-Latin]
- Weight305.29
- Drugbank_IDDB00494
- ACS_NO130929-57-6
- Show 3D model
- LogP (experiment)N/A
- LogP (predicted, AB/LogP v2.0)1.87
- pka4.5
- LogD (pH=7, predicted)0.84
- Solubility (experiment)N/A
- LogS (predicted, ACD/Labs)(ph=7)-0.76
- LogSw (predicted, AB/LogsW2.0)1.17
- Sw (mg/ml) (predicted, ACD/Labs)1.24
- No.of HBond Donors2
- No.of HBond Acceptors8
- No.of Rotatable Bonds6
- TPSA133.39
- StatusFDA approved
- AdministrationN/A
- PharmacologyA drug that functions as a catechol-O-methyl transferase (COMT) inhibitor. It is used in the treatment of Parkinson's disease.
- Absorption_valueN/A
- Absorption (description)Entacapone is rapidly absorbed from the gastro-intestinal tract
- Caco_2N/A
- Bioavailability42.0
- Protein binding98.0
- Volume of distribution (VD)0.40 L/kg
- Blood/Plasma Partitioning ratio (D_blood)N/A
- MetabollsmUndergoes extensive first pass metabolism. Entacapone is converted to its (cis)-isomer, (Z)-entacapone, the main metabolite in plasma, followed by direct glucuronidation to inactive glucuronide conjugates. Four metabolites have been observed—M3, M6, M8 and M10.
- Half life0.28 h
- ExcretionElimination is mainly via faeces (80 to 90%) and the remainder in urine as glucuronide conjugates and (Z)-isomer.
- Urinary ExcretionNegligible
- Clerance10.3 ml/min/kg
- ToxicityNo special hazard to humans, anaemia observed in repeated dose toxicity studies.
- LD50 (rat)N/A
- LD50 (mouse)N/A