Nonsteroidal antiandrogen

Overview

Chemical structure of Bicalutamide

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

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

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

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

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

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.

Related Pages

• Androgen receptor
• Prostate cancer
• Testosterone
• Dihydrotestosterone
• Gonadotropin-releasing hormone