Darolutamide
Antiandrogens and androgen synthesis inhibitors
Antiandrogens and androgen synthesis inhibitorsPregnancy: contraindicated
Contraindicated in women who are or may become pregnant (EU label). Darolutamide is for men only; it can harm a fetus, and men use contraception with a partner who could conceive…
An oral androgen receptor blocker for prostate cancer, used with ongoing testosterone suppression. Taken with food.
Quick facts
- Group
- Antiandrogens and androgen synthesis inhibitors
- Target
- Androgen receptor (AR)
- Key effects
- Fatigue · Pain in the arms or legs · Rash
- Monitor
- PSA and imaging for response · Blood pressure
- ATC
- L02BB06
No doses: the clinician sets them by the current guideline.
Mechanism of action
No crystal structure with darolutamide is available. The figure shows bicalutamide, an older antiandrogen, in the same ligand-binding pocket of the human androgen receptor.
Darolutamide binds the ligand-binding domain of the androgen receptor and blocks testosterone and dihydrotestosterone. It also stops the receptor from moving into the nucleus and switching on androgen-driven genes, so prostate cancer cells stop growing. It is given together with treatment that keeps testosterone low.
- Binds the androgen receptor ligand pocket
- Blocks nuclear entry and gene activation
- Androgen-driven prostate cancer stops growing
Indications
- Non-metastatic castration-resistant prostate cancer. Prostate cancer →
- Metastatic hormone-sensitive prostate cancer, alone or with docetaxel. Prostate cancer →
Adverse effects
Common
- Fatigue
- Pain in the arms or legs
- Rash
Contraindications
- Hypersensitivity to darolutamide
- Pregnancy (EU label)
Key interactions
- St John's wort
- Can lower darolutamide levels; reviewed before starting.
- Grapefruit and its juice
- Can change darolutamide levels; avoided.
- GnRH analogues (leuprorelin, goserelin, triptorelin)
- Continued alongside: darolutamide works on top of testosterone suppression.
What is monitored
- PSA and imaging for response
- Blood pressure and cardiovascular risk factors
- Liver tests
- Rash and seizures
Administration and safety
- Oral tablets swallowed whole with food, not split, crushed or chewed.
- Testosterone-lowering treatment continues during darolutamide.
Pregnancy and breastfeeding
Contraindicated in women who are or may become pregnant (EU label). Darolutamide is for men only; it can harm a fetus, and men use contraception with a partner who could conceive during treatment and for a week after.
Nursing care
- Teach to take it with food and not to stop the GnRH analogue.
- Teach to avoid grapefruit and St John's wort.
- Teach to report chest pain, seizures, rash or blood in the urine.
- Men with a partner who could conceive use contraception during treatment and shortly after.
Pharmacokinetics
- Absorption
- Oral tablets twice a day with food.
Test yourself
Think of the answer, then tap the question to see it.
What is the target of darolutamide?
The androgen receptor (ligand-binding domain).
Which treatment must continue during darolutamide?
Testosterone suppression with a GnRH analogue or orchiectomy.
With which chemotherapy is darolutamide combined in metastatic hormone-sensitive disease?
Docetaxel.
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: Darolutamide: MedlinePlus Drug Information (MedlinePlus (U.S. National Library of Medicine), 2022); Darolutamide - NCI (National Cancer Institute, 2026); EMA: product information for darolutamide (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.