All About Abiraterone Acetate

Abiraterone Acetate is a proven prostate cancer therapy. It is a type of hormone-targeted treatment available as tablets. This drug is recommended for patients with cancer of the prostate gland that has started spreading. Its common trade names include Zytiga and Abiracine.

FDA Approval History:

  • For Late-Stage Prostate Cancer: Apr 28, 2011
  • For Metastatic Prostate Cancer: Feb 8, 2018


Abiraterone Acetate is an antiandrogen and a derivative of steroidal progesterone that is used in the treatment of patients with:

  • Metastatic castration-resistant prostate cancer (CRPC).
  • Metastatic high-risk castration-sensitive prostate cancer (CSPC).


This formulation works by inhibiting the cytochrome P450 17A1 enzyme, also known as, CYP17A1. Below are the steps by which cancer cell death occurs.

  • Enzyme CYP17A1: It is an enzyme of the hydroxylase type that is encoded in humans by the CYP17A1 gene on chromosome 10.
  • Abiraterone Enters: It enters and inhibits CYP17A1 which further suppresses androgen production. This results in a decrease in the level of testosterone.
  • Cell Death: The drug not only decreases androgen production in the testes but also affects the adrenal glands and prostate tumor tissue, leading to cell death.

Side Effects

Like other specialty medicines, Abiraterone Acetate can result in certain side effects. During the therapy, some patients may experience mild to moderate reactions. However, report to your doctor if they don’t go away on their own.


Common side effects

  • Blood in urine
  • Decreased urine output
  • Fainting
  • Bladder pain
  • Headache
  • Loss of appetite
  • Mood changes
  • Irregular heartbeat
  • Bone fracture
  • Increased thirst
  • Frequent urination
  • Lower back pain
  • Dizziness
  • Bloating of the arms


Rare side effects

  • Skin darkening
  • Sweating
  • Yellow eyes
  • Shortness of breath
  • Diarrhea
  • Chest heaviness
  • Stomach pain
  • Skin rash
  • Depression
  • Weakness
  • Extreme weakness

Warnings and Precautions

  • Pregnancy
    Abiraterone Acetate may lead to severe harm to the baby inside the womb. If its use can’t be avoided during pregnancy, the patient must be made aware of the potential benefits and risks.
  • Nursing
    Note that this drug is not indicated for use in females. Its safety and efficacy in women haven’t been established. Moreover, experts are unclear about this drug’s excretion in breast milk.
  • Pediatric Use
    This medication is contraindicated for use in people aged below 18 years.
  • Geriatric Use
    As per the study reports, experts did not find any major safety differences between young and elder patients. Though, the hypersensitivity issue in certain elderly patients must not be ignored.
  • Hepatotoxicity
    Some patients may develop signs like skin rash, loss of appetite, stomach pain, and jaundice. Experts may consider these symptoms of hepatotoxicity as an indication of treatment discontinuation.


To prevent interactions, the doctor may need to know the patient’s medical history. Dose adjustments are then done to decrease the risk of side effects. Below are some suspected interactions linked to the use of this medicine.

  • Interaction with drugs
    Medications like berotralstat, anagrelide, cabozantinib, enzalutamide, leflunomide, tamoxifen, hydrocodone, pacritinib, sotalol, primidone, and levoketoconazole can interact with this drug. Other specialty medicines may also interfere with the working and efficacy.
  • Interaction with disorders
    Cardiovascular disease and hepatic dysfunction are the two main disease interactions of this medicine. These conditions can significantly change the working of Abiraterone Acetate in certain patients. It is advised to administer the drug with caution in patients with such a medical history.
  • Interaction with food
    The use of this medicine with food may increase the chance of side effects. This interaction may result in water retention, difficulty in breathing, muscle pain, and irregular heartbeat. Thus, doctors recommend taking this medicine on an empty stomach and not eating anything for at least an hour afterward.


The recommended dose strength of Abiraterone Acetate is given below. Experts advise administering this medicine orally with prednisone 5 mg (once daily).

  • Metastatic CRPC: 1,000 mg (four 250 mg tablets) orally once daily.
  • Metastatic High-risk CSPC: 1,000 mg (two 500 mg tablets) orally once daily.

In an overdose case, signs such as nausea, shortness of breath, fainting, and heart failure may occur. Reach out to your nearest health practitioner to avoid complications. Since there is no proven overdose therapy available, the doctor may give supportive care.


NOTE: Make sure to not take this medicine without a valid prescription by a qualified oncologist. Taking or selling it otherwise may lead to consequences.