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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 is a diarylpropionamide while flutamide is a monoarylpropionamide and nilutamide is a hydantoin. [256] Bicalutamide and flutamide, though not nilutamide, can also be classified as toluidides. [248] All three of the compounds share a common 3-trifluoromethyl aniline moiety. [257]
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 ...
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 ...
Pharmacology of bicalutamide; Template:Plasma levels and binding potential of flutamide and bicalutamide during first week; Template:Published case reports of bicalutamide-associated liver injury; Template:Published case reports of bicalutamide-associated lung toxicity
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.
The pharmacology of cyproterone ... CPA is a much more potent antiandrogen than nonsteroidal antiandrogens like flutamide and bicalutamide in gonadally intact ...
The affinity of nilutamide for the AR is about 1 to 4% of that of testosterone and is similar to that of bicalutamide and 2-hydroxyflutamide. [69] [70] [71] Similarly to 2-hydroxyflutamide, but unlike bicalutamide, nilutamide is able to weakly activate the AR at high concentrations. [70] It does not inhibit 5α-reductase. [72]