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ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS › ENDOCRINE THERAPY › HORMONE ANTAGONISTS AND RELATED AGENTS › Other hormone antagonists and related agents
abiraterone
L02BX03
Forms & Strengths
- Tablet: 250 mg
- Tablet: 500 mg
Adult Dosing
- Metastatic castration-resistant prostate cancer: 1000 mg orally once daily combined with low-dose prednisone 5 mg orally twice daily
- Metastatic high-risk castration-sensitive prostate cancer: 1000 mg orally once daily combined with prednisone 5 mg once daily
Pediatric Dosing
- Safety and efficacy in pediatric patients have not been established
Indications
- Metastatic castration-resistant prostate cancer
- Metastatic high-risk castration-sensitive prostate cancer
Mechanism of Action
- Selective inhibitor of CYP17 (17 alpha-hydroxylase/C17,20-lyase)
- Decreases testosterone production in testes, adrenal glands, and prostate tumor tissue
Contraindications
- Hypersensitivity to abiraterone or any component of the formulation
- Severe hepatic impairment (Child-Pugh Class C)
- Pregnancy or women who may become pregnant
Adverse Reactions
- Fatigue
- Joint swelling or discomfort
- Edema
- Hot flashes
- Diarrhea
- Vomiting
- Cough
- Hypertension
- Hyperglycemia
- Hypertriglyceridemia
- Elevated serum transaminases
- Hypokalemia
Drug Interactions
- Strong CYP3A4 inducers (e.g., rifampin, carbamazepine) decrease abiraterone exposure
- CYP2D6 substrates (e.g., dextromethorphan) systemic exposure increased; use with caution
- Strong CYP3A4 inhibitors may increase abiraterone concentrations
Curated Content: Needs Vetting Before Put to Clinical Use