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Bicalutamide is a prescription nonsteroidal androgen receptor inhibitor used with a luteinizing hormone-releasing hormone analog for Stage D2 metastatic prostate cancer. Current U.S. labeling uses a 50 mg tablet once daily in this combination regimen. Bicalutamide 150 mg daily is not approved for use alone or with other treatments.
read more about bicalutamide ...Bicalutamide competitively binds androgen receptors in target tissues and blocks the actions of testosterone and other androgens. Prostate cancer cells can depend on androgen signaling for growth. Blocking that signaling reduces androgen stimulation while the paired luteinizing hormone-releasing hormone analog lowers serum testosterone.
Bicalutamide 50 mg is approved in combination with a luteinizing hormone-releasing hormone analog for Stage D2 metastatic prostate carcinoma. It has no approved indication for women. Current labeling also states that 150 mg daily is not approved as monotherapy or in other treatment combinations.
The recommended dose is one 50 mg tablet once daily in the morning or evening together with a luteinizing hormone-releasing hormone analog. Treatment commonly starts at the same time as the hormone therapy. Dose adjustment is not required for kidney impairment or mild to moderate liver impairment under current labeling.
Severe liver injury and fatal liver failure have occurred with bicalutamide. Liver enzymes are checked before treatment, at regular intervals during the first four months, and periodically afterward. Bicalutamide can also increase bleeding risk with coumarin anticoagulants, while the paired hormone therapy can worsen glucose control. Prostate-specific antigen is followed during treatment.
Yes. Bicalutamide blocks androgen receptors and reduces androgen signaling in prostate cancer cells.
The approved 50 mg tablet regimen is taken once daily with a luteinizing hormone-releasing hormone analog.
No. The approved 50 mg regimen is used with a luteinizing hormone-releasing hormone analog.
Yes. Liver enzymes are checked before treatment, regularly during the first four months, and periodically afterward.
Bicalutamide. LiverTox. https://www.ncbi.nlm.nih.gov/books/NBK547970/. Date Accessed September 16, 2026.
Bicalutamide. MedlinePlus. https://www.medlineplus.gov/druginfo/meds/a697047.html. Date Accessed September 16, 2026.
Bicalutamide. National Cancer Institute. https://www.cancer.gov/about-cancer/treatment/drugs/bicalutamide. Date Accessed September 16, 2026.
DailyMed - BICALUTAMIDE tablet. https://www.dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=26e30155-a50b-df14-e063-6394a90a9be4. Date Accessed September 16, 2026.
Definition of Bicalutamide. NCI Dictionary of Cancer Terms. https://www.cancer.gov/publications/dictionaries/cancer-terms/def/bicalutamide. Date Accessed September 16, 2026.