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ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS › ENDOCRINE THERAPY › HORMONE ANTAGONISTS AND RELATED AGENTS › Other hormone antagonists and related agents
abiraterone and corticosteroids
L02BX53
Forms & Strengths
- Abiraterone acetate 500 mg tablets
- Abiraterone acetate 250 mg tablets
- Prednisone 5 mg tablets (co-administered)
- Methylprednisolone 4 mg tablets (alternative corticosteroid)
Adult Dosing
- Abiraterone acetate: 1,000 mg orally once daily on an empty stomach (no food 2 hours before and 1 hour after)
- Prednisone: 5 mg orally twice daily (metastatic castration-resistant prostate cancer)
- Prednisone: 5 mg orally once daily (metastatic castration-sensitive prostate cancer)
- Moderate hepatic impairment (Child-Pugh Class B): Reduce abiraterone dose to 250 mg once daily
Pediatric Dosing
- Not indicated for pediatric use
- Safety and efficacy in pediatric patients have not been established
Indications
- Treatment of metastatic castration-resistant prostate cancer (mCRPC) in combination with prednisone
- Treatment of metastatic high-risk castration-sensitive prostate cancer (mHSPC) in combination with prednisone
Mechanism of Action
- Abiraterone is converted in vivo to abiraterone, an androgen biosynthesis inhibitor
- Selectively inhibits cytochrome P450 17A-alpha (CYP17)
- Inhibits CYP17 enzyme complex in testicular, adrenal, and prostatic tumor tissues
- Blocks formation of testosterone precursors (dehydroepiandrosterone and androstenedione)
- Corticosteroids are co-administered to suppress ACTH drive and prevent mineralocorticoid excess
Contraindications
- Hypersensitivity to abiraterone acetate 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 (arthralgia)
- Edema
- Hot flashes
- Diarrhea
- Hypertension
- Hypokalemia
- Hepatotoxicity (elevated ALT, AST, and total bilirubin)
- Cardiac disorders (heart failure, arrhythmias)
Drug Interactions
- Strong CYP3A4 inducers (e.g., rifampin, carbamazepine): Decrease abiraterone exposure; avoid or increase dosing frequency
- Strong CYP2D6 substrates (e.g., thioridazine): Abiraterone is a CYP2D6 inhibitor; increases exposure and toxicity risk of co-administered drugs
- CYP2C8 inhibitors/inducers: May alter abiraterone systemic exposure
- Mineralocorticoid-sensitive drugs: Risk of exacerbated hypokalemia and fluid retention
Curated Content: Needs Vetting Before Put to Clinical Use