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Common side effects include tiredness, vomiting, headache, joint pain, high blood pressure, swelling, low blood potassium, high blood sugar, hot flashes, diarrhea, and cough. Other severe side effects may include liver failure and adrenocortical insufficiency. In males whose partners can become pregnant, birth control is recommended. Supplied as abiraterone acetate it is converted in the body to abiraterone. Abiraterone acetate works by suppressing the production of androgens - specifically it inhibits CYP17A1 - and thereby decreases the production of testosteron. In doing so, it prevents the effects of these hormones in prostate cancer.

Abiraterone acetate was described in 1995, and approved for medical use in the United States and Europe in 2011. It is on the World Health Organization's List of Essential Medicines, the safest and most effective medicines needed in a health system. The medication is marketed widely throughout the world.

Abiraterone acetate is used in combination with prednison, a corticosteroid, as a treatment for mCRPC (previously called hormone-resistant or hormone-refractory prostate cancer). This is a form of prostate cancer that is not responding to first-line androgen deprivation therapy or treatment with androgen receptor antagonists. Abiraterone acetate has received Food and Drug Administration (FDA) (28 April 2011), European Medicines Agency (EMA) (23 September 2011), Medicines and Healthcare products Regulatory Agency (MHRA) (5 September 2011) and Therapeutic Goods Administration (TGA) (1 March 2012) approval for this indication. In Australia it is covered by the Pharmaceutical Benefits Scheme when being used to treat castration-resistant prostate cancer and given in combination with prednison/prednisolon (subject to the conditions that the patient is not currently receiving chemotherapy, is either resistant or intolerant of docetaxel, has a WHO performance status of <2, and his disease has not since become progressive since treatment with PBS-subsidised abiraterone acetate has commenced).

Abiraterone acetate may be useful for prevention of the testosteron flare at the initiation of GnRH agonist therapy in men with prostate cancer.

In people previously treated with docetaxel survival is increased by 3.9 months (14.8 months versus 10.9 months for placebo).

In people with castration-refractory prostate cancer but who had not received chemotherapy those who received abiraterone acetate had a progression-free survival of 16.5 months rather than 8.3 months with placebo. After a median follow-up period of 22.2 months, overall survival was better with abiraterone acetate.

Contraindications include hypersensitivity to abiraterone acetate. Although documents state that it should not be taken by women who are or who may become pregnant, there is no medical reason that any woman should take it. Women who are pregnant should not even touch the pills unless they are wearing gloves. Other cautions include severe baseline hepatic impairment, mineralocorticoid excess, cardiovascular disease including heart failure and hypertension, uncorrected hypokalemia, and adrenocorticoid insufficiency.