bicalutamide

Bicalutamide is a non-steroidal antiandrogen (NSAA) used primarily in the treatment of prostate cancer. It acts as a competitive antagonist of the androgen receptor, preventing testosterone and dihydrotestosterone from activating AR signaling and thereby helping to slow or halt the growth of androgen-dependent tumors.

Bicalutamide is typically used as part of androgen deprivation therapy, most often in combination with a luteinizing hormone-releasing hormone (LHRH) agonist to suppress testosterone production. It may be used as adjuvant therapy or for metastatic disease; monotherapy is less common but has been studied in selected cases. The goal is to block androgen receptor activity while reducing tumor progression.

The standard oral dose is 50 mg once daily, with higher dosing (for example, up to 150 mg daily) used in some regimens for metastatic disease. Treatment is continued as long as it is effective and tolerated, and hepatic function should be monitored because the drug is extensively metabolized in the liver. Bicalutamide has a relatively long elimination half-life, on the order of five to seven days, and its primary active metabolite is 4-hydroxybicalutamide.

Common adverse effects include hot flashes, gynecomastia and breast tenderness, decreased libido, erectile dysfunction, diarrhea, and nausea. Hepatotoxicity is a rare but serious potential adverse effect and may manifest as jaundice or elevated liver enzymes; liver function monitoring is advised. Bicalutamide is contraindicated in pregnancy and should be used with caution in patients with hepatic impairment or when taken with other hepatically cleared medications.