Drug Groups

approved

Description

Bicalutamide is an oral non-steroidal anti-androgen for prostate cancer. It binds to the androgen receptor.

Indication

For treatment (together with surgery or LHRH analogue) of advanced prostatic cancer.

Pharmacology

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.

Affected Organisms

Biotransformation

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.

Absorption

Bicalutamide is well-absorbed following oral administration, although the absolute bioavailability is unknown.

Half Life

5.9 days

Protein Binding

96%

Clearance

* Apparent oral cl=0.32 L/h [Normal Males]

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