What it does
Abiraterone is a medication used to treat prostate cancer by lowering hormone levels that help cancer grow.
Commonly used for: prostate cancer, hormone-sensitive prostate cancer
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Source: Pharmacy and Poisons Board · fetched 2026-01-28 20:30:05 · updated 2026-07-26 09:29:10
About this medicine
Abiraterone is a medication used to treat prostate cancer by lowering hormone levels that help cancer grow.
What it treats
- prostate cancer
- hormone-sensitive prostate cancer
How it works
It works by reducing the production of certain hormones, which can slow down or stop the growth of cancer cells.
Who it's for
This medication is for men with prostate cancer, especially those whose cancer has spread or is resistant to other treatments.
AI-assisted summary grounded in BNF data - general information only, not medical advice. Always confirm with your pharmacist or doctor.
Clinical monograph: abiraterorone
Abiraterone is an oral medication that inhibits androgen biosynthesis, primarily used in the treatment of prostate cancer. It functions by reducing the production of androgens, including testosterone and dehydroepiandrosterone (DHEA), which are known to promote the growth of prostate cancer cells. Abiraterone is often used in combination with prednisone to mitigate the effects of increased adrenal corticoids due to androgen blockade.
Indications
- Castration-resistant prostate cancer
- Metastatic prostate cancer
- Prostate cancer that has progressed following hormone therapy
Dosage
Children: Not established for paediatric use.
Adults: Refer to specific guidelines as doses may vary based on individual patient factors and treatment protocols.
Mechanism of action
Abiraterone selectively inhibits cytochrome P450 17A1 (CYP17A1), an enzyme critical in the biosynthesis of androgens. By blocking CYP17A1, abiraterone reduces the production of testosterone and other androgens from both the testes and the adrenal glands, leading to decreased androgen levels in the body, which subsequently slows the growth of androgen-dependent tumors.
Pharmacodynamics
The pharmacodynamics of abiraterone involve its ability to lower serum testosterone levels significantly, which is crucial in the management of castration-resistant prostate cancer. The reduction in circulating androgens leads to decreased stimulation of androgen receptors on prostate cancer cells, resulting in slowed tumor progression and, in some cases, regression.
Pharmacokinetics
After oral administration, abiraterone is absorbed with peak plasma concentrations typically occurring within 2 hours. It is extensively metabolized in the liver, primarily via CYP2D6 and CYP3A4 pathways, leading to multiple metabolites. The elimination half-life is approximately 12 hours, and it is excreted mainly in feces and urine. Co-administration with food can increase the bioavailability of abiraterone, hence it is recommended to take it on an empty stomach.
Contra-indications
- Hypersensitivity to abiraterone or any component of the formulation
- Severe hepatic impairment (Child-Pugh class C)
Adverse effects
- Hypertension
- Hypokalemia
- Fluid retention
- Fatigue
- Hot flushes
- Nausea
- Diarrhea
- Arthralgia
- Adrenal insufficiency
- Liver toxicity
Interactions
- CYP17 inhibitors
- CYP3A4 inducers
- CYP3A4 inhibitors
- Anticoagulants
- Corticosteroids
Precautions
- Monitor blood pressure regularly
- Assess liver function tests prior to and during treatment
- Evaluate for signs of adrenal insufficiency
- Use with caution in patients with cardiovascular disease
Pregnancy
Abiraterone is contraindicated in pregnancy due to potential harm to the fetus. Women of childbearing potential should use effective contraception during treatment.
Breast-feeding
It is not known if abiraterone is excreted in human breast milk. Caution should be exercised when administering to breastfeeding women.
Storage
Store in a cool, dry place at room temperature, away from light. Keep out of reach of children.
Formulations
- Tablets 250 mg
AI-synthesized from BNF references - general information only, not a substitute for professional medical advice or the current BNF. Verify doses with a pharmacist.