Abiraterone

Abiraterone acetate is converted in vivo to abiraterone, an androgen biosynthesis inhibitor, that inhibits 17 α-hydroxylase/C17,20-lyase (CYP17). This enzyme is expressed in testicular, adrenal, and prostatic tumor tissues and is required for androgen biosynthesis.

• Abiraterone acetate tablets are indicated in combination with prednisone for the treatment of patients with Metastatic castration-resistant prostate cancer (CRPC) Metastatic high-risk castration-sensitive prostate cancer (CSPC) Abiraterone acetate tablet is a CYP17 inhibitor indicated in combination with prednisone for the treatment of patients with metastatic castration-resistant prostate cancer (CRPC). ( 1) metastatic high-risk castration-sensitive prostate cancer (CSPC).ICD-10: C61

• None.contraindicated

­ Metastatic castration-resistant prostate cancer: • Abiraterone acetate tablets 1,000 mg orally once daily with prednisone 5 mg orally twice daily. ( 2.1 ) Metastatic castration-sensitive prostate cancer: • Abiraterone acetate tablets 1,000 mg orally once daily with prednisone 5 mg orally once daily. ( 2.2 ) Patients receiving abiraterone acetate tablets should also receive a gonadotropin-releasing hormone (GnRH) analog concurrently or should have had bilateral orchiectomy. Abiraterone acetate tablets must be taken as a single dose once daily on an empty stomach. Do not eat food 2 hours before and 1 hour after taking abiraterone acetate tablets. The tablets must be swallowed whole with water. Do not crush or chew tablets.( 2.3) Dose Modification: • For patients with baseline moderate hepatic impairment (Child-Pugh Class B), reduce the abiraterone acetate tablets starting dose to 250 mg once daily. ( 2.4 ) • For patients who develop hepatotoxicity during treatment, hold abiraterone acetate tablets until recovery. Retreatment may be initiated at a reduced dose. Abiraterone acetate tablets should be discontinued if patients develop severe hepatotoxicity. ( 2.4 ) 2.1 Recommended Dose for Metastatic CRPC The recommended dose of abiraterone acetate tablets is 1,000 mg (two 500 mg tablets or four 250 mg tablets) orally once daily with prednisone 5 mg orally twice daily.

Mineralocorticoid excess: Closely monitor patients with cardiovascular disease. Control hypertension and correct hypokalemia before treatment. Monitor blood pressure, serum potassium and symptoms of fluid retention at least monthly. ( 5.1 ) Adrenocortical insufficiency: Monitor for symptoms and signs of adrenocortical insufficiency. Increased dosage of corticosteroids may be indicated before, during and after stressful situations. ( 5.2 ) Hepatotoxicity: Can be severe and fatal. Monitor liver function and modify, interrupt, or discontinue abiraterone acetate dosing as recommended. ( 5.3 ) Increased fractures and mortality in combination with radium Ra 223 dichloride: Use of abiraterone acetate plus prednisone/prednisolone in combination with radium Ra 223 dichloride is not recommended. (5.4) Embryo-Fetal Toxicity: Abiraterone acetate can cause fetal harm. Advise males with female partners of reproductive potential to use effective contraception. ( 5.5 , 8.1 , 8.3 ) Hypoglycemia: Severe hypoglycemia has been reported in patients with pre-existing diabetes who are taking medications containing thiazolidinediones (including pioglitazone) or repaglinide. Monitor blood glucose in patients with diabetes and assess if antidiabetic agent dose modifications are required. (5.6) 5.1 Hypokalemia, Fluid Retention, and Cardiovascular Adverse Reactions due to Mineralocorticoid Excess Abiraterone acetate may cause hypertension, hypokalemia, and fluid retention as a consequence of increased mineralocorticoid levels resulting from CYP17 inhibition [see Clinical Pharmacology ( 12.1 )].

The following are discussed in more detail in other sections of the labeling: Hypokalemia, Fluid Retention, and Cardiovascular Adverse Reactions due to Mineralocorticoid Excess [see Warnings and Precautions ( 5.1 )]. Adrenocortical Insufficiency [see Warnings and Precautions ( 5.2 )]. Hepatotoxicity [see Warnings and Precautions ( 5.3 )]. Increased Fractures and Mortality in Combination with Radium Ra 223 Dichloride [see Warnings and Precautions (5.4) ]. ­ The most common adverse reactions (≥10%) are fatigue, arthralgia, hypertension, nausea, edema, hypokalemia, hot flush, diarrhea, vomiting, upper respiratory infection, cough, and headache. ( 6.1 ) The most common laboratory abnormalities (>20%) are anemia, elevated alkaline phosphatase, hypertriglyceridemia, lymphopenia, hypercholesterolemia, hyperglycemia, and hypokalemia. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Dr. Reddy’s Laboratories Inc., at 1-888-375-3784 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch. 6.1 Clinical Trial Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in clinical practice. Two randomized placebo-controlled, multicenter clinical trials (COU-AA-301 and COU-AA­302) enrolled patients who had metastatic CRPC in which abiraterone acetate was administered orally at a dose of 1,000 mg daily in combination with prednisone 5 mg twice daily in the active treatment arms.

• Do not use abiraterone acetate tablets in patients with baseline severe hepatic impairment (Child-Pugh Class C). ( 8.6 ) 8.1 Pregnancy Risk Summary The safety and efficacy of abiraterone acetate have not been established in females. Based on findings from animal studies and the mechanism of action, abiraterone acetate can cause fetal harm and potential loss of pregnancy. There are no human data on the use of abiraterone acetate in pregnant women. In animal reproduction studies, oral administration of abiraterone acetate to pregnant rats during organogenesis caused adverse developmental effects at maternal exposures approximately ≥ 0.03 times the human exposure (AUC) at the recommended dose (see Data). Data Animal Data In an embryo-fetal developmental toxicity study in rats, abiraterone acetate caused developmental toxicity when administered at oral doses of 10, 30 or 100 mg/kg/day throughout the period of organogenesis (gestational days 6 to 17). Findings included embryo-fetal lethality (increased post implantation loss and resorptions and decreased number of live fetuses), fetal developmental delay (skeletal effects) and urogenital effects (bilateral ureter dilation) at doses ≥10 mg/kg/day, decreased fetal ano-genital distance at ≥30 mg/kg/day, and decreased fetal body weight at 100 mg/kg/day. Doses ≥10 mg/kg/day caused maternal toxicity.

Metabolism

Following administration of abiraterone acetate, the pharmacokinetics of abiraterone have been studied in healthy subjects and in patients with metastatic CRPC. In vivo , abiraterone acetate is converted to abiraterone.

Human experience of overdose with abiraterone acetate is limited. There is no specific antidote. In the event of an overdose, stop abiraterone acetate, undertake general supportive measures, including monitoring for arrhythmias and cardiac failure and assess liver function.

• Apr 28, 2011NDANDA202379Janssen Biotech
• May 22, 2018NDANDA210308Sun Pharm
• Oct 31, 2018ANDAANDA208339Hikma
• Oct 31, 2018ANDAANDA208446Mylan
• Oct 31, 2018ANDAANDA208453Apotex
• Jan 7, 2019ANDAANDA208327Amneal Pharms
• Feb 25, 2019ANDAANDA208371Rising
• Aug 11, 2023NDANDA216793Janssen Biotech

1. 1Death6,15515%
2. 2Fatigue2,6366.5%
3. 3Prostatic Specific Antigen Increased2,0095.0%
4. 4Drug Ineffective1,9834.9%
5. 5Therapy Cessation1,5593.9%
6. 6Hot Flush1,4653.6%
7. 7Asthenia1,2973.2%
8. 8Disease Progression1,1993.0%
9. 9Hospitalisation1,0812.7%
10. 10Off Label Use1,0712.6%
11. 11Nausea1,0132.5%
12. 12Diarrhoea9662.4%
13. 13Fall9422.3%
14. 14Prostate Cancer8822.2%
15. 15Dizziness8342.1%

The 10 most recently updated of 472 ClinicalTrials.gov registrations naming Abiraterone as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

• RISK-ADAPT Protocol in Metastatic Hormone-Sensitive Prostate Cancer (mHSPC)
  Not yet recruiting · Phase 2 · Interventional · 108 enrolled · Georgetown University
  NCT07645326updated 2026-06-12
• A Study of Xaluritamig Plus Abiraterone Versus Investigator's Choice in Participants With Chemotherapy-naïve Metastatic Castration-resistant Prostate Cancer
  Recruiting · Phase 3 · Interventional · 750 enrolled · Amgen
  NCT07213674updated 2026-06-12
• A Study of Tinengotinib (TT-00420) in Combination With Standard Treatments in People With Prostate Cancer
  Recruiting · Phase 1 · Phase 2 · Interventional · 50 enrolled · Memorial Sloan Kettering Cancer Center
  NCT06457919updated 2026-06-11
• A Study of BL-B01D1 Combination Therapy in Patients With Metastatic Castration-resistant Prostate Cancer
  Not yet recruiting · Phase 2 · Phase 3 · Interventional · 180 enrolled · Sichuan Baili Pharmaceutical Co., Ltd.
  NCT07641855updated 2026-06-11
• A Study of HRS-5041 Tablets Combined With Antitumor Therapy in Subjects With Advanced Prostate Cancer
  Recruiting · Phase 1 · Phase 2 · Interventional · 100 enrolled · Jiangsu HengRui Medicine Co., Ltd.
  NCT06568094updated 2026-06-10
• Docetaxel to Androgen Receptor Pathway Inhibitors in Patients With Metastatic Castration Sensitive Prostate Cancer and Suboptimal PSA Response
  Recruiting · Phase 3 · Interventional · 830 enrolled · Canadian Cancer Trials Group
  NCT06592924updated 2026-06-10
• Pharmacogenomics IND Commercial SNP Clinical Study - Abiraterone and Single Nucleotide Polymorphisms
  Active not recruiting · Phase 2 · Phase 3 · Interventional · 600 enrolled · Han Xu, M.D., Ph.D., FAPCR, Sponsor-Investigator, IRB Chair
  NCT03348670updated 2026-06-10
• Study Comparing AAA817+ARPI Versus Standard of Care in Adult Participants With PSMA-positive mCRPC
  Recruiting · Phase 3 · Interventional · 940 enrolled · Novartis Pharmaceuticals
  NCT06855277updated 2026-06-10
• An Open-label Study of JSB462 (Luxdegalutamide) in Combination With Abiraterone in Adult Male Patients With Metastatic Hormone-sensitive Prostate Cancer (mHSPC)
  Recruiting · Phase 2 · Interventional · 150 enrolled · Novartis Pharmaceuticals
  NCT06991556updated 2026-06-10
• TulmiSTAR-02: A Phase I/II Open-label Study of Tulmimetostat in Combination With Darolutamide vs. Darolutamide, and Tulmimetostat With Abiraterone in Patients With Metastatic Hormone-sensitive Prostate Cancer (mHSPC)
  Recruiting · Phase 1 · Phase 2 · Interventional · 181 enrolled · Novartis Pharmaceuticals
  NCT07190300updated 2026-06-09

Frequently asked questions

How does Abiraterone work?

Abiraterone acetate is converted in vivo to abiraterone, an androgen biosynthesis inhibitor, that inhibits 17 α-hydroxylase/C17,20-lyase (CYP17). This enzyme is expressed in testicular, adrenal, and prostatic tumor tissues and is required for androgen biosynthesis.

What is Abiraterone used for?

According to FDA labeling, Abiraterone carries indications including: Abiraterone acetate tablets are indicated in combination with prednisone for the treatment of patients with Metastatic castration-resistant prostate cancer (CRPC) Metastatic high-risk castration-sensitive prostate cancer (CSPC) Abiraterone acetate tablet is a CYP17 inhibitor indicated in combination with prednisone for the treatment of patients with metastatic castration-resistant prostate cancer (CRPC). ( 1) metastatic high-risk castration-sensitive prostate cancer (CSPC).. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.

What class of drug is Abiraterone?

Abiraterone is classified as Other hormone antagonists and related agents, Cytochrome P450 17A1 Inhibitor, Cytochrome P450 17A1 Inhibitors, Cytochrome P450 2C8 Inhibitors, Cytochrome P450 2D6 Inhibitors.

What are the brand names for Abiraterone?

Abiraterone is marketed under brand names including Abirtega, Akeega, Yonsa, Zytiga.

What are the contraindications for Abiraterone?

Abiraterone labeling lists contraindications including: None.. Always consult the full prescribing information and a clinician.