Apalutamide
Antiandrogens and androgen synthesis inhibitors
Antiandrogens and androgen synthesis inhibitorsPregnancy: 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.
Quick facts
- Group
- 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.
Mechanism of action
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.
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 →
- Non-metastatic castration-resistant prostate cancer. Prostate cancer →
Adverse effects
Common
- Fatigue, weakness
- Joint pain, muscle stiffness
- Rash
- Hot flushes, diarrhoea, nausea, weight loss
- Limb swelling
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.
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.
Connections
← Back to the class: 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 (MedlinePlus (U.S. National Library of Medicine), 2024); Apalutamide - NCI (National Cancer Institute, 2022); EMA: product information for apalutamide (European Medicines Agency, 2026); ATCDDD - ATC/DDD Index (WHO Collaborating Centre for Drug Statistics Methodology, 2026).
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Representative model, for educational purposes only.