Products
Bicalutamide is commercially available in the form of film-coated tablets (Casodex, generics). It has been approved in many countries since 1995.
Structure and properties
Bicalutamide (C18H14F4N2O4S, Mr = 430.37 g/mol) is a racemate, with the -enantiomer being almost exclusively responsible for the antiandrogenic effect. It exists as a white powder that is practically insoluble in water.
Effects
Bicalutamide (ATC L02BB03) is a nonsteroidal, high-affinity, and selective antiandrogen with no activity at other hormone receptors. It binds competitively to androgen receptors, preventing the effects of androgens and thereby inhibiting hormone-dependent tumor growth.
Indications
For the treatment of prostate cancer.
Dosage
According to the SmPC. The drug is taken once daily, regardless of meals. The -enantiomer has a long half-life of approximately 7 days, so one dose per day is sufficient. This is in contrast to the short-acting flutamide (Flucinom), which must be administered three times daily.
Contraindications
- Hypersensitivity
For complete precautions, see the drug label. Bicalutamide should be used with caution in patients with liver disease.
Interactions
The -enantiomer is an inhibitor of CYP3A4 and to a lesser extent of CYP2C9, CYP2C19, and CYP2D6. Corresponding interactions cannot be excluded.
Adverse effects
Very common adverse reactions include enlargement of the mammary gland, breast tenderness to touch, flushing, constipation, pelvic pain, back pain, general aches and weakness. Severe liver dysfunction and liver failure may occur. See the drug label for a complete list.
