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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 ...
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]
The side effects of bicalutamide, a nonsteroidal antiandrogen (NSAA), including its frequent and rare side effects, have been well-studied and characterized. The most common side effects of bicalutamide monotherapy in men include breast tenderness, breast growth, feminization, demasculinization, and hot flashes.
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).
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[200] [201] Another early nonsteroidal antiandrogen, [202] DIMP (Ro 7–8117), which is structurally related to thalidomide [203] and is a relatively weak antiandrogen, [204] [205] was first described in 1973 and was never marketed. [206] Flutamide was followed by nilutamide in 1989. and bicalutamide in 1995. [207]
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