Androgen biosynthesis (CYP17) inhibitor Pregnancy: Not for use in women; contraindicated in women who are or may potentially be pregnant. A condom is required (with additional contraception if partner is of childbearing potential).

Abiraterone acetate

Brand names: Zytiga

Abiraterone acetate is an oral androgen-biosynthesis inhibitor used, with prednisolone or prednisone, to treat metastatic prostate cancer. It is a specialist oncology medicine given alongside androgen-deprivation therapy.

Auto-extracted from the source labelling — not yet independently clinician-verified. These values were distilled from the UK SPC (or the US label where noted) but have not had a clinician sign-off. Confirm against the current SmPC before prescribing.

Adult dose

Dose: 1,000 mg

Route: Oral

Frequency: Once daily

Four 250 mg tablets as a single daily dose, not with food (taken on an empty stomach). Given with prednisone or prednisolone: 5 mg daily for mHSPC, 10 mg daily for mCRPC. Continue medical castration with an LHRH analogue in patients not surgically castrated. For hepatotoxicity, re-treatment may be given at a reduced dose of 500 mg once daily.

Dose auto-extracted from UK Summary of Product Characteristics (SPC) via the eMC; US FDA prescribing information (openFDA / DailyMed) — cross-check; US labelling may differ from UK — not yet clinician-verified. Always confirm against the product SmPC and your local formulary before prescribing.

Contraindications

Hypersensitivity to the active substance or any excipient
Women who are or may potentially be pregnant
Severe hepatic impairment (Child-Pugh Class C)
In combination with Ra-223 (when given with prednisone/prednisolone)

Side effects

Peripheral oedema
Hypokalaemia
Hypertension
Urinary tract infection
Alanine aminotransferase and/or aspartate aminotransferase increased; hepatotoxicity
Cardiac failure, angina pectoris, atrial fibrillation, tachycardia

Interactions

Avoid concomitant strong CYP3A4 inducers; if unavoidable, increase abiraterone dosing frequency
Avoid CYP2D6 substrates with a narrow therapeutic index; consider dose reduction of the concomitant substrate

Clinical monograph

How it works

It irreversibly inhibits CYP17A1, blocking androgen synthesis in the testes, adrenal glands and tumour, thereby lowering testosterone to suppress androgen-driven prostate cancer.

Prescribing in practice

Mineralocorticoid excess from CYP17 inhibition causes fluid retention, hypertension and hypokalaemia, which is why concomitant corticosteroid cover is mandatory and must not be omitted.
Hepatotoxicity occurs and liver function must be checked before and regularly during treatment, with dose interruption if transaminases rise markedly.
It should be taken on an empty stomach, as food substantially increases absorption and exposure.

Monitoring

Monitor blood pressure, serum potassium, fluid status and liver function regularly throughout treatment.

Counselling the patient

Take the tablets on an empty stomach, well apart from food, and keep taking the prescribed steroid.
Report ankle swelling, breathlessness or marked tiredness, which may indicate fluid retention or low potassium.

Evidence & guidelines

Abiraterone is supported by major randomised trials and NICE approval demonstrating improved survival in metastatic prostate cancer.

Reference: NICE TA387/TA721; EAU; SmPC Zytiga; Drug verified in RxNorm (NLM); confirm dosing against the manufacturer SPC (eMC). Verify against your local formulary and current prescribing references before prescribing. The structured dose values shown have been reviewed by a clinician. Monograph status: clinician-reviewed (2026-07-04).

Curated clinical cross-links plus same-class fallbacks.

Calculators

Pathways