Nonsteroidal antiandrogen
Overview[edit]
Nonsteroidal antiandrogens (NSAAs) are a class of drugs that act as antagonists to the androgen receptor (AR). They are primarily used in the treatment of prostate cancer, a disease that is often driven by androgens such as testosterone and dihydrotestosterone (DHT).
Mechanism of Action[edit]
NSAAs work by binding to the androgen receptor, thereby preventing androgens from binding and activating the receptor. This inhibition of androgen receptor activation leads to a decrease in the growth of androgen-dependent tissues, such as the prostate gland.
Clinical Uses[edit]
NSAAs are mainly used in the treatment of prostate cancer. They are often used in combination with other therapies, such as gonadotropin-releasing hormone (GnRH) analogs, to achieve maximal androgen blockade. This combination is known as combined androgen blockade (CAB).
Bicalutamide[edit]
Bicalutamide is one of the most commonly used NSAAs. It is often prescribed as part of the treatment regimen for prostate cancer. Bicalutamide is usually administered orally and is well-tolerated by most patients.
Pharmacokinetics[edit]
Bicalutamide is absorbed from the gastrointestinal tract and has a long half-life, allowing for once-daily dosing. It is metabolized in the liver and excreted primarily in the urine.
Side Effects[edit]
Common side effects of bicalutamide include hot flashes, gynecomastia, and gastrointestinal disturbances. Long-term use may also lead to liver function abnormalities, which necessitates regular monitoring of liver enzymes.
