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Androgen Receptor Antagonist (Second-Generation) Pregnancy: Contraindicated; male partners must use contraception during treatment and for 1 week after

Darolutamide

Brand names: Nubeqa

Adult dose

Dose: 600 mg twice daily
Route: Oral
Frequency: Twice daily with food
Max: 1200 mg/day
Licensed for non-metastatic CRPC (nmCRPC) in men with PSA doubling time 10 months or less. Also licensed in combination with docetaxel for metastatic hormone-sensitive prostate cancer (mHSPC)

Paediatric dose

Dose: Not applicable N/A/kg
Route: Oral
Frequency: Not applicable
Max: Not applicable
Not applicable

Dose adjustments

Renal

Reduce to 300 mg twice daily if eGFR under 30 or on haemodialysis

Hepatic

Reduce to 300 mg twice daily in moderate hepatic impairment; avoid in severe

Paediatric weight-based calculator

Not applicable

Clinical pearls

  • ARAMIS trial: darolutamide significantly improved metastasis-free survival in nmCRPC vs placebo (40.4 vs 18.4 months)
  • Key advantage over enzalutamide and apalutamide: low CNS penetration due to structural properties — significantly lower seizure risk; preferred in patients with seizure history or risk
  • ARASENS trial: darolutamide + docetaxel + ADT improved overall survival in mHSPC — NICE approved triplet therapy
  • No dose adjustment required for most drug interactions due to unique pharmacokinetic profile (low P-gp affinity vs enzalutamide)
  • Newer agent — patients should be aware this requires ongoing ADT continuation throughout treatment

Contraindications

  • Women of childbearing potential (teratogenic)
  • Concurrent use of combined P-gp and strong CYP3A4 inducers

Side effects

  • Fatigue (common)
  • Arthralgia
  • Rash
  • Hypertension
  • Seizure risk (significantly lower than enzalutamide — advantage in elderly or patients at seizure risk)
  • Nausea

Interactions

  • Combined P-gp and strong CYP3A4 inducers — rifampicin (significantly reduce darolutamide levels)
  • Rosuvastatin (darolutamide increases rosuvastatin exposure via BCRP/OATP inhibition — monitor for statin toxicity)

Monitoring

  • PSA
  • Testosterone (confirm castrate levels)
  • Liver function
  • Blood pressure
  • Bone metastasis imaging (if nmCRPC)

Reference: BNFc; BNF 90; NICE TA660 (Darolutamide for nmCRPC); ARAMIS Trial; ARASENS Trial; EAU Guidelines 2024. Verify against your local formulary and the latest BNF before prescribing.

Related

Curated clinical cross-links plus same-class fallbacks.