CYP17 Inhibitor (Hormonal Therapy) 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, Yonsa

Abiraterone acetate is an androgen biosynthesis inhibitor used with prednisolone for metastatic prostate cancer.

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 CYP17 (17 alpha-hydroxylase/C17,20-lyase), blocking androgen synthesis in the testes, adrenal glands and tumour tissue.

Prescribing in practice

CYP17 inhibition causes mineralocorticoid excess (hypertension, hypokalaemia, fluid retention), so it is co-prescribed with a corticosteroid and these parameters are monitored.
Hepatotoxicity can occur; check liver function before and during treatment and act on significant rises.
It must be taken on an empty stomach because food markedly increases absorption and exposure.

Monitoring

Monitor blood pressure, serum potassium, fluid status and liver function, particularly during the early months of treatment.

Counselling the patient

Take on an empty stomach and do not take with food.
Do not stop the accompanying steroid tablets, and report swelling, weakness or yellowing of the skin.

Evidence & guidelines

Abiraterone improves survival in metastatic prostate cancer, demonstrated in the COU-AA-301/302 and STAMPEDE trials and recommended by NICE.

Reference: NICE TA562; COU-AA-301/302 trials; 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