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CYP17 Inhibitor (Hormonal Therapy) Pregnancy: X

Abiraterone Acetate

Brand names: Zytiga, Yonsa

Adult dose

Dose: 1000 mg once daily (Zytiga) or 500 mg once daily (Yonsa)
Route: oral
Frequency: once daily
Max: 1000 mg/day (Zytiga); 500 mg/day (Yonsa)
Zytiga: take on empty stomach (no food ≥2h before and ≥1h after); Yonsa: take with food; must be combined with prednisolone 5 mg twice daily

Paediatric dose

Route:
Not licensed in children

Dose adjustments

Renal

No dose adjustment if eGFR >30 ml/min; caution if eGFR <30

Hepatic

Avoid in moderate-severe hepatic impairment (Child-Pugh B/C); reduce dose with mild impairment

Clinical pearls

  • Blocks androgen synthesis in adrenals, testes, and tumour — must co-prescribe prednisolone to prevent mineralocorticoid excess
  • LATITUDE trial: improved OS in newly diagnosed metastatic castration-sensitive prostate cancer
  • Monitor LFTs monthly for first 3 months, then every 3 months

Contraindications

  • Moderate/severe hepatic impairment
  • Women who are or may become pregnant

Side effects

  • Peripheral oedema
  • Hypertension
  • Hypokalaemia
  • Elevated liver enzymes
  • Hot flushes
  • Adrenal insufficiency

Interactions

  • CYP2D6 substrates (inhibits — eg. dextromethorphan)
  • Spironolactone (blocks abiraterone mechanism)
  • Strong CYP3A4 inducers (rifampicin — reduce effect)

Monitoring

  • LFTs (monthly × 3 months, then 3-monthly)
  • Blood pressure
  • Serum potassium
  • Mineralocorticoid excess signs

Reference: BNFc; BNF 86; NICE TA562; COU-AA-301/302 trials. Verify against your local formulary and the latest BNF before prescribing.

Related

Curated clinical cross-links plus same-class fallbacks.

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