Key points
- Abiraterone (Zytiga) is a tablet that reduces the making of male hormone throughout the body, including in the tumour itself [1].
- It is always taken with prednisone and is used for prostate cancer that has spread [1].
- Take the tablets on an empty stomach: nothing to eat for 2 hours before and 1 hour after; food can multiply how much of the drug is absorbed [1].
- In several large studies, abiraterone helped men with prostate cancer that has spread live longer [1, 2, 3, 4].
- The main serious side effects are high blood pressure, low potassium, fluid build-up and liver damage; regular liver and potassium tests are needed [1].
What is this drug and how does it work?
For physicians
Testosterone-lowering treatments (GnRH analogue injections or removal of the testes) reduce androgen production in the testes but do not affect androgens made in the adrenal glands or the tumour itself [1]. Abiraterone acetate is converted in the body to abiraterone, which inhibits CYP17 (17α-hydroxylase/C17,20-lyase), an enzyme needed for androgen synthesis in the testes, adrenal glands and prostate tumour tissue [1].
CYP17 inhibition can increase mineralocorticoid production and cause hypertension, hypokalaemia and fluid retention; this is why abiraterone is given with low-dose prednisone [1]. It was first approved in the United States in 2011 [1].
Which cancers is it used for?
Your doctor may prescribe this drug for:
- Prostate cancer that has spread and no longer responds to hormone therapy (mCRPC) [1, 2, 3]
- High-risk prostate cancer that has spread but still responds to hormone therapy (mCSPC) [1, 4]
- Locally advanced or spread prostate cancer starting long-term hormone therapy [1, 5]
- Prostate cancer that has spread from the start (de novo) and still responds to hormone therapy [6]
Whether it suits you depends on the type and stage of your cancer and your test results. Details of each use are in the section for doctors.
For physicians
| Cancer | Setting | Key evidence |
|---|---|---|
| Metastatic castration-resistant prostate cancer (mCRPC) | After docetaxel chemotherapy; with prednisone (FDA-approved use) | COU-AA-301 [2]: median overall survival 14.8 vs 10.9 months with placebo; HR 0.646 [1] |
| Metastatic castration-resistant prostate cancer (mCRPC) | Before chemotherapy; with prednisone (FDA-approved use) | COU-AA-302 [3]: lower risk of radiographic progression (HR 0.425); at the final analysis median overall survival 34.7 vs 30.3 months (HR 0.81) [1] |
| High-risk metastatic castration-sensitive prostate cancer (mCSPC) | Newly diagnosed, with testosterone-lowering therapy and prednisone (FDA-approved use) | LATITUDE [4]: lower risk of death (HR 0.62); at the updated analysis median overall survival 53.3 vs 36.5 months (HR 0.66) [1] |
| Locally advanced or metastatic prostate cancer starting long-term hormone therapy | Abiraterone and prednisolone added to testosterone-lowering therapy | STAMPEDE: lower risk of death (HR 0.63); HR 0.61 in metastatic and 0.75 in non-metastatic disease [5]. Use in non-metastatic disease is not an FDA-labelled indication [1] |
| De novo metastatic castration-sensitive prostate cancer | Added to testosterone-lowering therapy + docetaxel (triplet therapy) | PEACE-1: in patients receiving docetaxel, lower risk of radiographic progression (HR 0.50) and death (HR 0.75) [6] |
The COU-AA-301, COU-AA-302 and LATITUDE figures come from the FDA label (including updated analyses). HR: hazard ratio; a value below 1 means a lower risk of the event with abiraterone.
How it is taken and dosing
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- Abiraterone is taken once a day as a single dose, together with prednisone tablets (once or twice a day as your doctor directs) [1].
- Take the tablets on an empty stomach: do not eat from 2 hours before until 1 hour after the dose [1]. Taking it with food makes the amount absorbed much larger and unpredictable and can increase side effects; in healthy people, one dose with a high-fat meal raised total exposure (AUC) about 10-fold [1].
- Swallow the tablets whole with water; do not crush or chew them [1].
- Keep having your testosterone-lowering injections [1].
- Missed dose: if you miss a dose of abiraterone or prednisone, take your usual dose the next day; if more than one daily dose is missed, call your doctor [1].
- Never stop abiraterone or prednisone without talking to your doctor; stopping prednisone suddenly can cause adrenal failure [1].
- Testosterone-lowering therapy: with both regimens, continue a GnRH analogue concurrently, or the patient should have had bilateral orchiectomy [1].
- Before starting: control blood pressure and correct hypokalaemia; baseline ALT, AST and bilirubin [1].
- Monitoring: ALT, AST and bilirubin every 2 weeks for the first 3 months and then monthly; blood pressure, potassium and fluid retention at least monthly; blood glucose in diabetic patients (especially with pioglitazone or repaglinide) [1].
- Hepatotoxicity: ALT/AST above 5 times the upper limit or bilirubin above 3 times: hold; after return to baseline or AST/ALT ≤2.5 times and bilirubin ≤1.5 times, resume at 750 mg daily; on recurrence, 500 mg daily; on recurrence at 500 mg, discontinue. After restarting, liver tests at least every 2 weeks for 3 months and then monthly. ALT above 3 times with bilirubin above 2 times (without biliary obstruction or another cause): discontinue permanently [1].
- Baseline hepatic impairment: Child-Pugh B: 250 mg once daily, with liver tests weekly for the first month, every 2 weeks for the next 2 months and then monthly; if ALT/AST rises above 5 times or bilirubin above 3 times, discontinue permanently. Child-Pugh C: do not use [1].
- Renal impairment: no dose adjustment needed [1].
- Strong CYP3A4 inducers: avoid; if unavoidable, increase dosing frequency to twice daily only during co-administration (e.g., 1000 mg twice daily) [1].
For physicians
Standard dosing (FDA label)
Abiraterone + prednisone (mCRPC)
Metastatic castration-resistant prostate cancerCycle length: Daily and continuous
Metastatic castration-resistant prostate cancer
Before prescribing: Prescribing notes| Drug | Dose | Route | Schedule |
|---|---|---|---|
| Abiraterone acetate | 1000 mg once daily | Oral, fasting | Every day |
| Prednisone | 5 mg twice daily | Oral | Every day |
Dosing as per the FDA label [1].
Abiraterone + prednisone (high-risk mCSPC)
High-risk metastatic castration-sensitive prostate cancerCycle length: Daily and continuous
High-risk metastatic castration-sensitive prostate cancer
Before prescribing: Prescribing notes| Drug | Dose | Route | Schedule |
|---|---|---|---|
| Abiraterone acetate | 1000 mg once daily | Oral, fasting | Every day |
| Prednisone | 5 mg once daily | Oral | Every day |
Dosing as per the FDA label [1].
Doses follow the trial protocol, guideline or official drug label (source given in the notes of each regimen). Before prescribing, check blood counts, renal and hepatic function, drug interactions and the patient’s condition, and adjust the dose according to the drug label.
Side effects
The most common side effects:
- Tiredness, joint pain and swelling, swollen legs and constipation [1].
- Hot flushes, diarrhoea, cough and trouble sleeping [1].
- High blood pressure and low blood potassium; this is why regular blood pressure checks and blood tests are needed [1].
- In tests: anaemia and raised blood sugar and blood fats [1].
For physicians
In pooled data from placebo-controlled trials, the most common adverse reactions (≥ 10%) were fatigue, arthralgia, hypertension, nausea, oedema, hypokalaemia, hot flush, diarrhoea, vomiting, upper respiratory tract infection, cough and headache; the most common laboratory abnormalities (above 20%) were anaemia, raised alkaline phosphatase, hypertriglyceridaemia, hypercholesterolaemia, lymphopenia, hyperglycaemia and hypokalaemia [1]. The table below shows the frequency of some adverse reactions in the COU-AA-302 trial [1].
| Adverse reaction | Abiraterone + prednisone (542 patients) | Placebo + prednisone (540 patients) |
|---|---|---|
| Fatigue | 39% | 34% |
| Joint swelling or discomfort | 30% | 25% |
| Oedema | 25% | 21% |
| Constipation | 23% | 19% |
| Hot flush | 22% | 18% |
| Hypertension | 22% | 13% |
| Diarrhoea | 22% | 18% |
| Cough | 17% | 14% |
| Insomnia | 14% | 11% |
| Contusion | 13% | 9.1% |
| Upper respiratory tract infection | 13% | 8.0% |
| Dyspepsia | 11% | 5.0% |
In LATITUDE (prednisone once daily), hypertension was reported in 37% (grade 3-4 in 20%) and hypokalaemia in 20% (grade 3-4 in 10%) of patients in the abiraterone arm [1].
Serious side effects
These are less common but serious; tell your team early if you notice any sign of them:
- High blood pressure, low potassium or fluid build-up: headache, weakness and muscle cramps, palpitations or sudden swelling [1].
- Heart problems such as heart failure: shortness of breath or swollen legs [1].
- Liver damage, mostly in the first 3 months; regular liver tests are needed, and report yellow skin or eyes, dark urine or pain on the right side of the abdomen straight away [1].
- Lack of cortisol if prednisone is stopped suddenly, or during infection and stress: severe weakness, dizziness and vomiting. Do not stop prednisone on your own [1].
- A severe drop in blood sugar in people with diabetes who take certain diabetes medicines [1].
For physicians
Abiraterone has no boxed warning, but the FDA label lists these warnings [1]:
- Mineralocorticoid excess (hypertension, hypokalaemia, fluid retention): in pooled data, grade 3-4 hypokalaemia occurred in 4% of patients on abiraterone vs 2% on placebo [1]. In patients who developed hypokalaemia, QT prolongation and torsades de pointes have been reported after marketing [1]. Cardiac failure occurred in 2.6% vs 0.9% [1].
- Adrenocortical insufficiency: in 0.3% of patients, especially after stopping or reducing prednisone, or with infection or stress; higher corticosteroid doses may be needed before, during and after stressful situations [1].
- Hepatotoxicity: grade 3-4 liver enzyme increases (at least 5 times normal) in 6% of patients, usually in the first 3 months; fulminant hepatitis, acute liver failure and deaths have been reported after marketing [1].
- Combination with radium-223: in the ERA-223 trial, fractures (28.6% vs 11.4%) and deaths (38.5% vs 35.5%) were more frequent with this combination; concurrent use is not recommended [1].
- Severe hypoglycaemia in diabetic patients taking pioglitazone or repaglinide [1].
- Non-infectious pneumonitis, muscle injury (including rhabdomyolysis) and anaphylactic reactions have also been reported after marketing [1].
When should I call my doctor?
Contact your doctor without delay if you have [1]:
- Dizziness, feeling faint, or a fast or irregular heartbeat
- Headache, confusion, muscle weakness or leg pain (possible low potassium or high blood pressure)
- Swelling of the legs or ankles, or shortness of breath
- Yellow skin or eyes, dark urine, or severe nausea or vomiting (possible liver damage)
- Severe weakness, nausea and vomiting or low blood pressure during an infection, stress or after stopping prednisone (possible adrenal failure)
- If you have diabetes: shaking, sweating, severe hunger or confusion (low blood sugar)
- Difficulty breathing or swallowing, swelling of the face, lips or throat, or hives
Interactions, pregnancy and precautions
- Other medicines: epilepsy medicines (phenytoin, carbamazepine, phenobarbital) and tuberculosis medicines (rifampicin, rifabutin, rifapentine) roughly halve the level of abiraterone in the blood [1]. Abiraterone also raises the blood level of some other medicines, such as the cough medicine dextromethorphan, the diabetes tablet pioglitazone and the psychiatric drug thioridazine; give your doctor a list of all your medicines [1].
- Pregnancy: men whose partner could become pregnant should use effective contraception during treatment and for 3 weeks after the last dose [1]. Women who are or may be pregnant should not touch broken or damaged tablets (or uncoated 250 mg tablets) without gloves [1]. The drug may reduce male fertility [1].
- Diabetes: people with diabetes should check their blood sugar during treatment and after stopping it [1].
- Regular tests: liver tests, potassium and blood pressure checks as your doctor plans are essential [1].
Frequently asked questions
Why do I have to take abiraterone on an empty stomach?
Food greatly and unpredictably increases how much abiraterone is absorbed and may increase side effects. That is why you should not eat from 2 hours before until 1 hour after the dose [1].
Why has prednisone been prescribed too?
Prednisone is part of the treatment and helps control the side effects of mineralocorticoid excess (high blood pressure, low potassium and fluid retention). Never stop it on your own [1].
Which tests are needed during treatment?
Liver tests are done before starting, every two weeks for the first three months and then monthly; blood pressure and potassium are also checked at least monthly [1].
What should I do if I forget a day?
Do not make up the dose; take your usual dose the next day. If you miss more than one day, call your doctor [1].
Can abiraterone be taken with chemotherapy?
Scientific evidence
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Key studies
2 itemsAbiraterone plus prednisone added to androgen deprivation therapy and docetaxel in de novo metastatic castration-sensitive prostate cancer (PEACE-1): a multicentre, open-label, randomised, phase 3 study with a 2 × 2 factorial design
Advanced and metastatic prostate cancer: ESMO Clinical Practice Guideline for diagnosis, treatment and follow-up
Related cancer types
References
6 referencesShow all references, 5 with a study cardClose the reference list
Numbers in the text, such as [1], refer to these sources. Sources with a “Study card” button are summarised in the site’s evidence library.
- 1
- 2
- 3
- 4
- 5Abiraterone for Prostate Cancer Not Previously Treated with Hormone Therapy
- 6
This page is based on reputable scientific sources and was last updated on 27 October 2026. The content of this website is for educational and informational purposes only and does not replace consultation, diagnosis or treatment by a specialist physician. Consult your treating physician about any treatment decision.
Printed from the website; the full and up-to-date version: https://drdabiri.com/en/drugs/abiraterone/