Reviewed on 1/27/2022

What Is Abiraterone and How Does It Work?

Abiraterone is a prescription medication used to treat Prostate Cancer

  • Abiraterone is available under the following different brand names: Zytiga, Yonsa.

What Are Dosages of Abiraterone?

Adult dosage

Tablet (Zytiga)

  • 250mg
  • 500mg

Ultramicronized tablet (Yonsa)

  • 125mg

Prostate Cancer

Adult dosage

Metastatic castration-resistant prostate cancer


  • 1000mg (two 500-mg tablets or four 250-mg tablets) orally once per day with prednisone 5 mg orally every 12 hours


  • 500 mg (four 125-mg tablets) orally once per day in combination with methylprednisolone 4 mg orally twice daily

Metastatic high-risk castration-sensitive prostate cancer


  • 1000 mg (two 500-mg tablets or four 250-mg tablets) orally once per day with prednisone 5 mg orally every 12 hours

Dosage Considerations – Should be Given as Follows: 

  • See "Dosages."

What Are Side Effects Associated with Using Abiraterone?

Common side effects of Abiraterone include:

  • weakness, 
  • tiredness, 
  • feeling very hot, 
  • high blood sugar
  • increased blood pressure, 
  • swelling in the legs or feet, 
  • anemia
  • low blood potassium
  • painful urination
  • abnormal liver function tests, 
  • abnormal blood tests, 
  • joint pain or swelling, 
  • headache, 
  • nausea, 
  • vomiting, 
  • diarrhea, 
  • stuffy nose
  • sneezing, 
  • cough, and 
  • sore throat

Serious side effects of Abiraterone include:

  • hives, 
  • difficulty breathing, 
  • swelling of the face, lips, tongue, or throat, 
  • swelling in the ankles or feet, 
  • pain in the legs, 
  • fast or irregular heartbeats, 
  • lightheadedness
  • severe headache, 
  • blurred vision, 
  • pounding in your neck or ears, 
  • pain or burning while urinating, 
  • pale skin, 
  • tiredness, 
  • shortness of breath, 
  • cold hands and feet, 
  • leg cramps, 
  • constipation, 
  • irregular heartbeats, 
  • fluttering in your chest, 
  • increased thirst or urination, 
  • numbness or tingling, 
  • muscle weakness, 
  • limp feeling, 
  • stomach pain (upper right side), 
  • nausea, 
  • vomiting, 
  • dark urine, 
  • yellowing of the skin or eyes (jaundice), 
  • headache, 
  • hunger, 
  • sweating, 
  • irritability, 
  • dizziness, 
  • anxiety, and
  • shakiness

Rare side effects of Abiraterone include:

  • none 
This is not a complete list of side effects and other serious side effects or health problems may occur as a result of the use of this drug. Call your doctor for medical advice about serious side effects or adverse reactions. You may report side effects or health problems to FDA at 1-800-FDA-1088.

What Other Drugs Interact with Abiraterone?

If your medical doctor is using this medicine to treat your pain, your doctor or pharmacist may already be aware of any possible drug interactions and may be monitoring you for them. Do not start, stop, or change the dosage of any medicine before checking with your doctor, health care provider or pharmacist first.

  • Abiraterone has severe interactions with the following drugs:
    • ombitasvir/paritaprevir/ritonavir & dasabuvir (DSC) 
  • Abiraterone has serious interactions with at least 16 other drugs. 
  • Abiraterone has moderate interactions with at least 128 other drugs. 
  • Abiraterone has minor interactions with the following drugs:
    • cobicstat
    • ribociclib  

This information does not contain all possible interactions or adverse effects. Visit the RxList Drug Interaction Checker for any drug interactions. Therefore, before using this drug, tell your doctor or pharmacist of all the drugs you use. Keep a list of all your medications with you, and share the list with your doctor and pharmacist. Check with your physician if you have health questions or concerns.

What Are Warnings and Precautions for Abiraterone?


  • None

Effects of drug abuse

  • None

Short-Term Effects

  • See “What Are Side Effects Associated with Using Abiraterone?”

Long-Term Effects

  • See “What Are Side Effects Associated with Using Abiraterone?”


  • Caution in patients with a history of cardiovascular disease; safety in patients with LVEF less than 50% or NYHA Class III or IV heart failure is not established
  • Hypertension, hypokalemia, and fluid retention may result from increased mineralocorticoid due to CYP17 inhibition; control hypertension and correct hypokalemia before treatment; monitor blood pressure, serum potassium, and symptoms of fluid retention at least monthly
  • Closely monitor patients with medical conditions that might be compromised by increased blood pressure, hypokalemia, or fluid retention (e.g., heart failure, recent MI, cardiovascular disease, ventricular arrhythmia)
  • QT prolongation and Torsades de Pointes observed in patients who develop hypokalemia during postmarketing surveillance and additional clinical trials
  • Adrenocortical insufficiency reported in patients receiving abiraterone in combination with prednisone, following interruption of daily steroids and/or with concurrent infection or stress; monitor for symptoms and signs of adrenocortical insufficiency; increased corticosteroid dosage may be indicated before, during, and after stressful situations; concurrent infection or interruption of daily corticosteroids associated with adrenocortical insufficiency
  • In postmarketing experience, severe hepatic toxicity, including fulminant hepatitis, acute liver failure and deaths occurred
  • Drug plus prednisone/prednisolone not recommended for use in combination with radium 223 dichloride outside clinical trials; increased incidences of fractures (and deaths observed in patients who received drug plus prednisone/prednisolone in combination with radium Ra 223 dichloride compared to placebo in combination with drug plus prednisone/prednisolone
  • Based on animal studies and mechanism of action, may cause fetal harm and loss of pregnancy

Pregnancy and Lactation

  • Based on findings from animal studies and mechanism of action, abiraterone is contraindicated for use in pregnant women because drug can cause fetal harm and potential loss of pregnancy
  • Not indicated for use in females
  • There are no human data regarding use in pregnant women
  • In animal reproduction studies, oral administration of abiraterone acetate to pregnant rats during organogenesis caused adverse developmental effects at maternal exposures ~≥0.03 times the human exposure (AUC) at the recommended dose
  • Contraception
    • Advise males with female partners of reproductive potential to use effective contraception during treatment and for 3 weeks after the final dose of abiraterone
  • Infertility
    • Based on animal studies, may impair reproductive function and fertility in males of reproductive potential
    • Lactation: Not indicated for women
    • No information available on the presence of abiraterone acetate in human milk, or on the effects on the breastfed child or milk production
Medscape. Abiraterone.


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