Last reviewed 2026-04-20 · How we verify

Abiraterone Acetate (abiraterone)

Abiraterone is an androgen biosynthesis inhibitor that targets CYP17 to reduce androgen production in prostate cancer cells.

Abiraterone, developed by Pfizer Inc., is an androgen biosynthesis inhibitor that targets CYP17. It is used to treat metastatic castration-resistant prostate cancer (mCRPC) and metastatic high-risk castration-sensitive prostate cancer (mHSPC). Abiraterone works by inhibiting the production of androgens, which are hormones that fuel the growth of prostate cancer cells. This is particularly useful for patients who have not responded to other treatments. Abiraterone is typically used in combination with a corticosteroid and is taken orally. It has been shown to be effective in reducing the levels of testosterone and other androgens in the body. Abiraterone has become a significant treatment option for prostate cancer patients.

At a glance

Mechanism of action

Abiraterone works by inhibiting the enzyme CYP17, which is responsible for producing androgens in the body. Androgens, such as testosterone, are hormones that fuel the growth of prostate cancer cells. By blocking the production of androgens, abiraterone can help slow the growth of prostate cancer cells. This is particularly useful for patients who have not responded to other treatments.

Approved indications

• Metastatic castration-resistant prostate cancer (mCRPC)
• Chemotherapy-naive metastatic castration-resistant prostate cancer (mCRPC)
• Metastatic high-risk castration-sensitive prostate cancer (mHSPC)

Common side effects

• Fatigue
• Arthralgia
• Hypertension
• Nausea
• Edema
• Hypokalemia
• Hot Flush
• Diarrhea
• Vomiting
• Upper Respiratory Infection
• Cough
• Headache

Drug interactions

• CYP3A4 Inducers
• CYP3A4 Inducers
• CYP2D6 Substrates
• CYP2D6 Substrates
• CYP2C8 Substrates
• Rifampin
• Ketoconazole
• Thioridazine
• Dextromethorphan
• Pioglitazone

Key clinical trials

• Docetaxel to Androgen Receptor Pathway Inhibitors in Patients With Metastatic Castration Sensitive Prostate Cancer and Suboptimal PSA Response (PHASE3)
• A Single-Arm Phase II Study of Neoadjuvant Intensified Androgen Deprivation (Leuprolide and Abiraterone Acetate) in Combination With AKT Inhibition (Capivasertib) for High-Risk Localized Prostate Cancer With PTEN Loss (PHASE2)
• A Phase I/II Study of PDS01ADC With Docetaxel and Abiraterone in Adults With Metastatic Castration Sensitive and PDS01ADC With Docetaxel in Castration Resistant Prostate Cancer (PHASE1, PHASE2)
• Multi-arm Multi-modality Therapy for Very High Risk Localized and Low Volume Metastatic Prostatic Adenocarcinoma (PHASE2)
• Exploration of Treatment Effect of Novel Hormone Therapy Combined With Local Treatment Based on PSMA PET/CT Evaluation in mHSCP Patients (PHASE2)
• A Clinical Study of Ifinatamab Deruxtecan Based Treatment Combinations or as Monotherapy to Treat Metastatic Castrate Resistant Prostate Cancer (mCRPC) (MK-2400-01A/IDeate-Prostate02) (PHASE1, PHASE2)
• A Study of Niraparib Combination Therapies for the Treatment of Metastatic Castration-Resistant Prostate Cancer (PHASE2)
• A Study of Opevesostat (MK-5684) Versus Alternative Next-generation Hormonal Agent (NHA) in Metastatic Castration-resistant Prostate Cancer (mCRPC) Post One NHA (MK-5684-004) (PHASE3)

Primary sources

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Competitive intelligence

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• Abiraterone Acetate CI brief — competitive landscape report
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