Indications
Bicalutamide is specifically indicated for use in combination with a luteinizing hormone-releasing hormone (LHRH) agonist to treat Stage D2 metastatic carcinoma of the prostate.
Pharmacodynamics
Bicalutamide functions as an antineoplastic hormonal agent primarily utilized in the management of prostate cancer. It is a pure, nonsteroidal anti-androgen with a strong affinity for androgen receptors, while showing no affinity for progestogen, estrogen, or glucocorticoid receptors. By blocking the action of androgens originating from both adrenal and testicular sources, Bicalutamide inhibits the growth of normal and malignant prostatic tissue, which is largely androgen-dependent. Although prostate cancer can be addressed through surgical or chemical castration, antiandrogen monotherapy has not consistently demonstrated equivalent efficacy to castration.
Absorption
Following oral administration, Bicalutamide is well-absorbed, though its absolute bioavailability remains unspecified.
Metabolism
Bicalutamide undergoes stereospecific metabolism. The S (inactive) isomer is primarily metabolized through glucuronidation. In contrast, the R (active) isomer is predominantly oxidized into an inactive metabolite, followed by glucuronidation.
Mechanism of Action
Bicalutamide functions by competitively inhibiting the binding of androgens to androgen receptors. This action effectively obstructs the influence of adrenal and testicular androgens, which are known to promote the proliferation of both normal and malignant prostatic tissue.
