What is "bicalutamide"

n. An oral nonsteroidal antiandrogen used in the treatment of prostate cancer and hirsutism.

Bicalutamide (brand name Casodex) is a synthetic non-steroidal antiandrogen (NSAA) that is used primarily in the treatment of prostate cancer. It is also used in the treatment of hirsutism and other androgen-dependent conditions and as a component of hormone replacement therapy for transgender women. The drug acts as a selective antagonist of the androgen receptor (AR), preventing androgens like testosterone and dihydrotestosterone (DHT) from binding to and activating the AR and exerting their biological effects. Developed and marketed by AstraZeneca, bicalutamide was approved in 1995 as a combination treatment (with a gonadotropin-releasing hormone (GnRH) analogue (e.g., leuprorelin) or surgical castration) for stage D2 metastatic prostate cancer. Since then, it has also been approved and used in some countries (though not in the United States) as a monotherapy for the treatment of an earlier stage of the disease, stage C or D1 locally advanced prostate cancer.

Since their introduction, bicalutamide and the other NSAAs have largely replaced the older, steroidal antiandrogen cyproterone acetate (CPA) in the treatment of prostate cancer. Bicalutamide was the third NSAA to be marketed, with flutamide and nilutamide preceding, and followed by enzalutamide. Relative to the earlier antiandrogens, bicalutamide has substantially reduced toxicity, and in contrast to them, is said to have an excellent and favorable safety profile. For this reason, as well as superior potency, tolerability, and pharmacokinetics, bicalutamide is preferred and has largely replaced flutamide and nilutamide in clinical practice. In accordance, bicalutamide is the most widely used antiandrogen in the treatment of prostate cancer. Between January 2007 and December 2009, it accounted for about 87.2% of NSAA prescriptions in the United States. Prior to the 2012 approval of enzalutamide, a newer and improved NSAA with even greater potency, efficacy, and effectiveness, bicalutamide was regarded as the standard-of-care antiandrogen in the treatment of the prostate cancer.

It is on the WHO Model List of Essential Medicines, the most important medications needed in a basic health system.