[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/) › Enzalutamide [Pharmacology](https://durgical.com/en/pharmacology/) · [Antiandrogens and androgen synthesis inhibitors](https://durgical.com/en/pharmacology/classes/antiandrogens-and-androgen-synthesis-inhibitors/) # Enzalutamide A second-generation antiandrogen for prostate cancer that blocks the androgen receptor more strongly than older drugs. It can cause falls and, rarely, seizures. 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: L02BB04 ◎**Androgen receptor (AR)**Enzalutamide ⓘ No crystal structure with enzalutamide is available. The figure shows bicalutamide, an older antiandrogen, in the same ligand-binding pocket of the human androgen receptor. **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 Enzalutamide is a non-steroidal competitive androgen receptor antagonist with much higher affinity than bicalutamide. It prevents androgens from binding, reducing receptor-driven gene transcription in prostate cancer cells, and prolongs survival in castration-resistant disease. - Binds the androgen receptor with high affinity - Androgens cannot bind - Receptor-driven gene transcription falls - Prostate cancer growth slows, even when castration-resistant ## Pharmacokinetics **Absorption** Taken by mouth once a day, with or without food **Metabolism** By CYP2C8 and CYP3A4; it is itself a strong inducer of several liver enzymes **Half-life** About 6 days; steady state takes about a month ## Indications - Castration-resistant prostate cancer, metastatic or non-metastatic [Prostate cancer →](https://durgical.com/en/conditions/prostate-cancer/) - Metastatic castration-sensitive prostate cancer [Prostate cancer →](https://durgical.com/en/conditions/prostate-cancer/) ## Adverse effects ### Common - Fatigue and weakness - Hot flushes - Back and joint pain - Hypertension - Decreased appetite and diarrhoea - Dizziness and headache ### Serious (rare, important) - Seizures - Posterior reversible encephalopathy syndrome (headache, confusion, vision changes) - Falls and fractures - Chest pain or breathlessness; higher short-term mortality in older men with heart disease - Severe allergic swelling of the face, tongue or throat - Breast enlargement in men ## Contraindications - Not for use in women, especially in pregnancy ## Key interactions **Strong CYP2C8 inhibitors (gemfibrozil)** Raise enzalutamide levels. **Strong CYP3A4 inducers (rifampicin)** Lower enzalutamide levels. **Substrates of CYP3A4, CYP2C9 and CYP2C19 (for example warfarin, fentanyl, nifedipine, quinidine)** Enzalutamide induces these enzymes and lowers their levels; many combinations are avoided. ## What is monitored - Blood pressure - Neurological symptoms (seizure risk factors) - Fall and fracture risk - Cardiovascular symptoms - PSA ## Administration and safety - Oral tablet or capsule once a day, at about the same time, with or without food; swallowed whole with water, not crushed, chewed or opened. - Women who are or may be pregnant do not touch the capsules or tablets. ## Nursing care - Ask about any history of seizures, brain injury or drugs that lower the seizure threshold. - Assess fall risk and teach home safety. - Review all medicines for interactions: it lowers the levels of many drugs. - Teach to report headache with confusion or vision changes, chest pain or facial swelling. ## Pregnancy and breastfeeding Only for men; it can harm a fetus, and men use condoms with a pregnant partner and effective contraception with a partner who could become pregnant, during treatment and for 3 months after. ## Memory aid ENZAlutamide: ENhanced antagonist, but it ENZyme-induces everything else, and the brain can seize. ## Test yourself Think of the answer, then tap the question to see it. ## How does enzalutamide differ from bicalutamide at the receptor? Both are competitive androgen receptor antagonists, but enzalutamide binds with several-fold higher affinity and is effective in castration-resistant disease. ## Which neurological adverse effect requires screening for risk factors before enzalutamide? Seizures; the drug crosses the blood-brain barrier. ## Why can enzalutamide make warfarin or fentanyl less effective? It induces CYP3A4, CYP2C9 and CYP2C19, speeding the metabolism of their substrates. [Add to my cards (3)](https://durgical.app/estudiar/?add=/en/pharmacology/enzalutamide/) ## Related drugs - [Bicalutamide](https://durgical.com/en/pharmacology/bicalutamide/) - [Abiraterone](https://durgical.com/en/pharmacology/abiraterone/) ## 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: [Enzalutamide: MedlinePlus Drug Information](https://medlineplus.gov/druginfo/meds/a612033.html) (MedlinePlus (U.S. National Library of Medicine), 2025); [ATCDDD - ATC/DDD Index](https://atcddd.fhi.no/atc_ddd_index/?code=L02BB04) (WHO Collaborating Centre for Drug Statistics Methodology, 2026); Goodman & Gilman's The Pharmacological Basis of Therapeutics, 14th ed., ch. 73 (McGraw Hill, 2023). ## **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/enzalutamide/ License: CC BY 4.0 (https://creativecommons.org/licenses/by/4.0/). Cite as: DurgiPedia (durgical.com), https://durgical.com/en/pharmacology/enzalutamide/