[Durgical](https://durgical.com/en/) › [DurgiPedia](https://durgical.com/en/durgipedia/) › [Pharmacology](https://durgical.com/en/pharmacology/) › [Antiandrogens and androgen synthesis inhibitors](https://durgical.com/en/pharmacology/classes/antiandrogens-and-androgen-synthesis-inhibitors/) › Bicalutamide [Pharmacology](https://durgical.com/en/pharmacology/) · [Antiandrogens and androgen synthesis inhibitors](https://durgical.com/en/pharmacology/classes/antiandrogens-and-androgen-synthesis-inhibitors/) # Bicalutamide A once-daily antiandrogen tablet for prostate cancer, given with a GnRH analogue. It can cause breast swelling and, rarely, serious liver injury. Updated 2026-11-01 - Class: [Antiandrogens and androgen synthesis inhibitors](https://durgical.com/en/pharmacology/classes/antiandrogens-and-androgen-synthesis-inhibitors/) - Receptor: Androgen receptor (AR) - ATC code: L02BB03 - WHO Model List of Essential Medicines ◎**Androgen receptor (AR)**Bicalutamide ⓘ The figure shows R-bicalutamide, the active enantiomer, in the ligand-binding domain of a human androgen receptor carrying the W741L mutation, which lets the drug fit in a crystal. **Target in 3D:** Androgen receptor (AR). PDB structure 1Z95 (RCSB PDB, public domain). [View the structure at RCSB PDB](https://www.rcsb.org/structure/1Z95) · Drag to rotate · pinch to zoom ## Mechanism of action Bicalutamide is a non-steroidal competitive antagonist of the androgen receptor. It keeps testosterone and dihydrotestosterone from binding, so the receptor does not activate androgen-driven genes in prostate cancer cells. Given with a GnRH analogue, it blocks the remaining androgen and the initial testosterone flare. - Binds the androgen receptor instead of testosterone - The receptor does not switch on androgen genes - Prostate cancer cells lose their growth signal - With a GnRH analogue it blocks the testosterone flare ## Pharmacokinetics **Absorption** Well absorbed by mouth **Metabolism** In the liver; the active R-enantiomer is metabolised slowly **Elimination** As inactive metabolites in bile and urine **Half-life** About 6 days for the active enantiomer, longer in severe liver disease ## Indications - Metastatic prostate cancer, combined with a GnRH (LHRH) analogue [Prostate cancer →](https://durgical.com/en/conditions/prostate-cancer/) ## Adverse effects ### Common - Hot flushes - Gynaecomastia and breast pain - Body pain, including back and pelvic pain - Raised liver enzymes ### Serious (rare, important) - Severe liver injury and liver failure - Interstitial lung disease - Excessive anticoagulation with warfarin - Loss of glucose control with GnRH agonists ## Contraindications - Hypersensitivity to bicalutamide - Women - Pregnancy ## Key interactions **Warfarin and other coumarin anticoagulants** Bicalutamide displaces warfarin from protein binding; INR can rise greatly; monitored closely. **CYP3A4 substrates** Bicalutamide inhibits CYP3A4 and may raise their levels. ## What is monitored - Liver tests regularly, especially in the first months - PSA - INR in patients on warfarin - Glucose with GnRH agonists ## Administration and safety - Oral tablet once a day, at the same time, with or without food. - Given together with a GnRH analogue, which is continued. ## Nursing care - Teach the signs of liver injury and when to report them. - Ask about warfarin and plan closer INR checks. - Explain breast swelling or tenderness, which can occur. - Teach that the GnRH injections continue alongside the tablet. ## Pregnancy and breastfeeding Contraindicated in pregnancy and not indicated for women; it can cause fetal harm. ## Memory aid BICALUTAMIDE keeps testosterone out of the lock: once a day, with the GnRH shot, and an eye on the liver and the INR. ## Test yourself Think of the answer, then tap the question to see it. ## Why is bicalutamide combined with a GnRH agonist at the start of prostate cancer treatment? It blocks the androgen receptor during the agonist's initial testosterone surge and also blocks the androgens that remain after castration. ## A patient on warfarin starts bicalutamide. What should be expected? The INR can rise markedly, with bleeding risk; INR is monitored closely and warfarin adjusted. ## Which serious adverse effect requires regular liver tests with bicalutamide? Hepatitis that can progress to liver failure and death. [Add to my cards (3)](https://durgical.app/estudiar/?add=/en/pharmacology/bicalutamide/) ## Related drugs - [Flutamide](https://durgical.com/en/pharmacology/flutamide/) - [Enzalutamide](https://durgical.com/en/pharmacology/enzalutamide/) - [Leuprorelin](https://durgical.com/en/pharmacology/leuprorelin/) ## Related conditions - [Prostate cancer](https://durgical.com/en/conditions/prostate-cancer/) [← Back to the class: Antiandrogens and androgen synthesis inhibitors](https://durgical.com/en/pharmacology/classes/antiandrogens-and-androgen-synthesis-inhibitors/) Educational content on how drugs work; not a prescribing guide and no substitute for a health professional's advice. No doses are given. Sources: [Bicalutamide: MedlinePlus Drug Information](https://medlineplus.gov/druginfo/meds/a697047.html) (MedlinePlus (U.S. National Library of Medicine), 2018); [DailyMed - BICALUTAMIDE tablet, film coated](https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=8b533fe4-287f-482c-b530-d9a5bf2ce40c) (DailyMed (U.S. National Library of Medicine), 2025); [ATCDDD - ATC/DDD Index](https://atcddd.fhi.no/atc_ddd_index/?code=L02BB03) (WHO Collaborating Centre for Drug Statistics Methodology, 2026); [Crystal Structure of the Androgen Receptor Ligand-binding Domain W741L Mutant Complex with R-bicalutamide](https://www.rcsb.org/structure/1Z95) (RCSB Protein Data Bank, 2005). ## **Spotted a mistake?** We are always improving for the community. Tell us what is wrong and our team will review it. Report a mistake Representative model, for educational purposes only. --- Source: https://durgical.com/en/pharmacology/bicalutamide/ License: CC BY 4.0 (https://creativecommons.org/licenses/by/4.0/). Cite as: DurgiPedia (durgical.com), https://durgical.com/en/pharmacology/bicalutamide/