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Bicalutamide, sold under the brand name Casodex among others, is an antiandrogen medication that is primarily used to treat prostate cancer. [10] It is typically used together with a gonadotropin-releasing hormone (GnRH) analogue or surgical removal of the testicles to treat metastatic prostate cancer (mPC).
Bicalutamide is used primarily in the treatment of early and advanced prostate cancer. [1] It is approved at a dosage of 50 mg/day as a combination therapy with a gonadotropin-releasing hormone analogue (GnRH analogue) or orchiectomy (that is, surgical or medical castration) in the treatment of stage D2 metastatic prostate cancer (mPC), [2] [3] and as a monotherapy at a dosage of 150 mg/day ...
Bicalutamide also shows a better safety profile than cyproterone acetate. When used as a high-dosage monotherapy, bicalutamide shows slightly inferior effectiveness in the treatment of prostate cancer compared to castration and GnRH analogues but a different and potentially superior tolerability and safety profile.
[9] [10] It has replaced flutamide and nilutamide as the first choice antiandrogen for prostate cancer treatment. Bicalutamide is not as hepatotoxic as flutamide and nilutamide and has a longer half-life, of 6 days in humans, that allows once a day administration at lower dosage. Bicalutamide shares the amide bond structure with flutamide.
It consists of removing the testicles, the organ where androgens are synthesized, of the cancer patient. It is the most radical treatment for ending the production of androgens. Moreover it is the easiest and least expensive one. The main disadvantage is that surgical castration is a permanent method.
In the EPC trial, in which bicalutamide monotherapy (150 mg/day) was evaluated for treatment of early prostate cancer in 8,113 men, the incidence of abnormal liver function tests at 3-year median follow-up was 3.4% for bicalutamide plus standard care (n=4,052) and 1.9% for standard care alone (n=4,061).
Bicalutamide (Casodex): Marketed for the treatment of prostate cancer and also used in the treatment of hirsutism in women, [4] as a component of hormone therapy for transgender women, [5] to delay precocious puberty in boys, [7] to prevent or alleviate priapism, [8] and for other indications.
There are no available data on hepatic bicalutamide concentrations in humans, but a rat study found that oral bicalutamide treatment resulted in 4-fold higher concentrations of the drug in the liver relative to plasma (a common finding with orally administered drugs, due to transfer through the hepatic portal system prior to reaching circulation).