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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 .
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).
A dosage of bicalutamide of 2 mg/kg (or about 40 to 60 mg in boys that are 20 to 30 kg or 45 to 65 lbs) once daily is recommended for use in male peripheral precocious puberty. [149] Bicalutamide is used to block the actions of androgens in the condition, while the aromatase inhibitor is used to decrease levels of estrogens. [148]
Common (1–10%) General and psychiatric disorders • Asthenia • Decreased libido • Erectile dysfunction • Hot flashes: Skin and subcutaneous tissue disorders • Decreased body hair: Hepato-biliary disorders • Elevated liver enzymes [b] Uncommon (0.1–1%) Immune system disorders and hypersensitivity reactions • Angioedema • Hives
Footnotes: a = Phase III studies of combined androgen blockade (bicalutamide or flutamide + GnRH agonist) in men with advanced prostate cancer. b = Incidence >5% regardless of causality . c = 250 mg three times per day at 8-hour intervals.
[1] [67] Relative to 150 mg/day bicalutamide, levels of (R)-bicalutamide are about 15% higher at a dosage of 200 mg/day and about 50% higher at a dosage of 300 mg/day. [67] In contrast to ( R )-bicalutamide, the inactive enantiomer ( S )-bicalutamide is much more rapidly absorbed (as well as cleared from circulation).
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The core side effects of NSAAs such as gynecomastia, sexual dysfunction, and hot flashes occur at similar rates with the different drugs. [48] [49] Conversely, bicalutamide is associated with a significantly lower rate of diarrhea compared to flutamide.