- Molecular NameBicalutamide
- SynonymNA
- Weight430.378
- Drugbank_IDDB01128
- ACS_NO90357-06-5
- Show 3D model
- LogP (experiment)3.049
- LogP (predicted, AB/LogP v2.0)2.6
- pka12
- LogD (pH=7, predicted)2.6
- Solubility (experiment)0.005 mg/ml
- LogS (predicted, ACD/Labs)(ph=7)-5.88
- LogSw (predicted, AB/LogsW2.0)0.05
- Sw (mg/ml) (predicted, ACD/Labs)0.0
- No.of HBond Donors2
- No.of HBond Acceptors6
- No.of Rotatable Bonds7
- TPSA115.64
- StatusFDA approved
- AdministrationN/A
- PharmacologyAn oral non-steroidal anti-androgen used in the treatment of prostate cancer] and hirsutism.
- Absorption_value90.0
- Absorption (description)Bicalutamide is extensively absorbed after oral administration
- Caco_2N/A
- BioavailabilityN/A
- Protein binding96.0
- Volume of distribution (VD)N/A
- Blood/Plasma Partitioning ratio (D_blood)N/A
- MetabollsmUndergoes extensive metabolism in the liver; the active R-enantiomer is metabolised predominantly by oxidation, the inactive S-enantiomer primarily by glucuronidation.
- Half life139 h (R-enantiomer); the S-enantiomer is cleared more rapidly
- ExcretionThe drug is rapidly cleared and the metabolites are excreted in approximately equal amounts in urine and faeces. Approximately half of an administered dose is excreted in urine as the glucuronide conjugates of the drug and its metabolite, hydroxy-bicalutamide. The remainder is detected in faeces as the drug and metabolite. Bicalutamide is not removed in significant amounts by dialysis.
- Urinary Excretion1.7
- Clerance0.043 ml/min/kg (R-enantiomer).
- ToxicityHepatic failure has occurred rarely and consideration should be given to periodic liver function monitoring.
- LD50 (rat)N/A
- LD50 (mouse)N/A