[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/) › Apalutamide # Apalutamide ## Antiandrogens and androgen synthesis inhibitors? Antiandrogens and androgen synthesis inhibitors ## Pregnancy: contraindicated? Contraindicated in women who are or may become pregnant (EU label). It is for men only; it can harm a fetus, so men use condoms and contraception during treatment and for months… An oral androgen receptor blocker for prostate cancer. Watch for falls, fractures, rash and seizures; it speeds up the breakdown of other drugs. Updated Nov 12, 2026 ## Quick facts **Group** [Antiandrogens and androgen synthesis inhibitors](https://durgical.com/en/pharmacology/classes/antiandrogens-and-androgen-synthesis-inhibitors/) **Target** Androgen receptor (AR) **Key effects** Fatigue · Joint pain · Rash **Monitor** PSA and imaging for response · Skin **ATC** L02BB05 No doses: the clinician sets them by the current guideline. On this page - The basics Mechanism of action - Indications - Adverse effects - Pharmacokinetics - Memory aid - Clinical What the labels mean - Safety Contraindications - Key interactions - What is monitored - Administration and safety - Pregnancy and breastfeeding - Nursing care - Study Test yourself - Connections Connections ## Mechanism of action ◎**Androgen receptor (AR)**Apalutamide ⓘ No crystal structure with apalutamide 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 Apalutamide binds the ligand-binding domain of the androgen receptor, blocks androgens, stops the receptor entering the nucleus and prevents it binding DNA. Androgen-driven genes stay off and prostate cancer cells stop growing. It is given with ongoing testosterone suppression. - Binds the androgen receptor ligand pocket - Blocks nuclear entry and DNA binding - Prostate cancer cells stop growing ## Indications - Metastatic castration-sensitive prostate cancer. [Prostate cancer →](https://durgical.com/en/conditions/prostate-cancer/) - Non-metastatic castration-resistant prostate cancer. [Prostate cancer →](https://durgical.com/en/conditions/prostate-cancer/) ## Adverse effects ### Common - Fatigue, weakness - Joint pain, muscle stiffness - Rash - Hot flushes, diarrhoea, nausea, weight loss - Limb swelling ### Serious (rare, important) - Falls and fractures - Seizures - Ischaemic heart disease and stroke - Severe skin reactions - Lung inflammation (cough, breathlessness, fever) ## Contraindications - Hypersensitivity to apalutamide - Pregnancy (EU label) ## Key interactions **Fexofenadine and omeprazole** Apalutamide speeds their breakdown or removal and can make them less effective. **GnRH analogues (leuprorelin, goserelin, triptorelin)** Continued alongside apalutamide. ## What is monitored - PSA and imaging for response - Bone health and fall risk - Skin - Cardiovascular risk factors; seizures ## Administration and safety - Oral tablets swallowed whole; if swallowing is not possible, the manufacturer's dispersion instructions are followed. - Testosterone-lowering treatment continues. ## Pregnancy and breastfeeding Contraindicated in women who are or may become pregnant (EU label). It is for men only; it can harm a fetus, so men use condoms and contraception during treatment and for months after. ## Nursing care - Assess fall risk and bone health; teach home safety. - Teach to report rash, blisters or mouth sores. - Review the medication list: apalutamide lowers the levels of many drugs. - Condoms (and another method with a partner who could conceive) during treatment and for months after; no sperm donation. ## Pharmacokinetics **Absorption** Oral tablets once a day, with or without food; can be dispersed for feeding tubes as the instructions describe. ## Memory aid «Apalutamide: A for accidents»: falls and fractures are its signature warning. ## Test yourself Think of the answer, then tap the question to see it. ## What is the signature safety issue of apalutamide? Falls and fractures (also seizures and rash). ## Why does apalutamide interact with omeprazole and fexofenadine? It induces drug-metabolising enzymes and transporters and lowers their levels. ## What must continue alongside apalutamide? Testosterone suppression with a GnRH analogue or orchiectomy. [Add to my cards (3)](https://durgical.app/estudiar/?add=/en/pharmacology/apalutamide/) [More Pharmacology questions →](https://durgical.com/en/practice/?f=pharmacology) ## What the labels mean **Pregnancy: contraindicated** Contraindicated in women who are or may become pregnant (EU label). It is for men only; it can harm a fetus, so men use condoms and contraception during treatment and for months… ## Connections ## Related drugs 3 - [Darolutamide](https://durgical.com/en/pharmacology/darolutamide/) - [Enzalutamide](https://durgical.com/en/pharmacology/enzalutamide/) - [Abiraterone](https://durgical.com/en/pharmacology/abiraterone/) ## Related conditions 1 - [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: [Apalutamide: MedlinePlus Drug Information](https://medlineplus.gov/druginfo/meds/a618018.html) (MedlinePlus (U.S. National Library of Medicine), 2024); [Apalutamide - NCI](https://www.cancer.gov/about-cancer/treatment/drugs/apalutamide) (National Cancer Institute, 2022); [EMA: product information for apalutamide](https://www.ema.europa.eu/en/documents/product-information/erleada-epar-product-information_en.pdf) (European Medicines Agency, 2026); [ATCDDD - ATC/DDD Index](https://atcddd.fhi.no/atc_ddd_index/?code=L02BB05) (WHO Collaborating Centre for Drug Statistics Methodology, 2026). ## **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/apalutamide/ License: CC BY 4.0 (https://creativecommons.org/licenses/by/4.0/). Cite as: DurgiPedia (durgical.com), https://durgical.com/en/pharmacology/apalutamide/