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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 ...
As such, bicalutamide is a selective reproductive teratogen in males, and may have the potential to produce undervirilization/sexually ambiguous genitalia in male fetuses. [60] [61] Due to its teratogenic capacity, contraception should be used in women taking bicalutamide who are fertile and sexually active. [65]
Bicalutamide is a diarylpropionamide while flutamide is a monoarylpropionamide and nilutamide is a hydantoin. [255] Bicalutamide and flutamide, though not nilutamide, can also be classified as toluidides. [247] All three of the compounds share a common 3-trifluoromethyl aniline moiety. [256]
However, bicalutamide is the most potent of the three, with the highest affinity for the AR [23] [24] and the longest elimination half-life, [10] and is the safest, least toxic, and best-tolerated. [25] For these reasons, bicalutamide has largely replaced flutamide and nilutamide in clinical use, [26] and is by far the most widely used first ...
The pharmacology of bicalutamide is the study of the pharmacodynamic and pharmacokinetic properties of the nonsteroidal antiandrogen (NSAA) bicalutamide.In terms of pharmacodynamics, bicalutamide acts as a selective antagonist of the androgen receptor (AR), the biological target of androgens like testosterone and dihydrotestosterone (DHT).
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.
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There is tentative evidence for flutamide in women; however, it is associated with relatively high rates of liver problems and strong recommendations have been made against its use. [14] [35] Like spironolactone, flutamide is typically only used by women. [36] Bicalutamide is another option for the treatment of female pattern hair loss.