Brands, Medical Use, Clinical Data
Brands / Synonyms
Bicalutamide; Bicalutamide [Usan:Ban:Inn]; Casodex; Casodex
For treatment (together with surgery or LHRH analogue) of advanced prostatic cancer.
Bicalutamide is an antineoplastic hormonal agent primarily used in the treatment of prostate cancer. Bicalutamide is a pure, nonsteroidal anti-androgen with affinity for androgen receptors (but not for progestogen, estrogen, or glucocorticoid receptors). Consequently, Bicalutamide blocks the action of androgens of adrenal and testicular origin which stimulate the growth of normal and malignant prostatic tissue. Prostate cancer is mostly androgen-dependent and can be treated with surgical or chemical castration. To date, antiandrogen monotherapy has not consistently been shown to be equivalent to castration.
Mechanism of Action
Bicalutamide competes with androgen for the binding of androgen receptors, consequently blocking the action of androgens of adrenal and testicular origin which stimulate the growth of normal and malignant prostatic tissue.
Bicalutamide is well-absorbed following oral administration, although the absolute bioavailability is unknown.
Biotrnasformation / Drug Metabolism
Bicalutamide undergoes stereo specific metabolism. The S (inactive) isomer is metabolized primarily by glucuronidation. The R (active) isomer also undergoes glucuronidation but is predominantly oxidized to an inactive metabolite followed by glucuronidation.
CASODEX is contraindicated in any patient who has shown a hypersensitivity reaction to the drug or any of the
CASODEX is not indicated in women. Further, CASODEX is contraindicated in women who are or may become pregnant. If
this drug is used during pregnancy, or if the patient becomes pregnant while taking this drug, the patient should be
apprised of the potential hazard to the fetus. CASODEX may cause fetal harm when administered to pregnant women. The
male offspring of rats receiving doses of 10mg/kg/day (plasma drug concentrations in rats equal to approximately 2/3
human therapeutic concentrations*) and above were observed to have reduced anogenital distance and hypospadias in
reproductive toxicology studies. These pharmacological effects have been observed with other antiandrogens. No other
teratogenic effects were observed in rabbits receiving doses up to 200mg/kg/day (approximately 1/3 human therapeutic
concentrations*) or rats receiving doses up to 250 mg/kg/day (approximately 2 times human therapeutic
*Based on a maximum dose of 50 mg/day of bicalutamide for an average 70 kg patient.
In vitro studies have shown CASODEX can displace coumarin anticoagulants, such as warfarin, from their
protein-binding sites. It is recommended that if CASODEX is started in patients already receiving coumarin
anticoagulants, prothrombin times should be closely monitored and adjustment of the anticoagulant dose may be