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ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS › ANTINEOPLASTIC AGENTS › OTHER ANTINEOPLASTIC AGENTS › Poly (ADP-ribose) polymerase (PARP) inhibitors
niraparib and abiraterone
L01XK52
Forms & Strengths
- Fixed-dose combination tablets: Niraparib 50 mg / Abiraterone acetate 500 mg
- Fixed-dose combination tablets: Niraparib 100 mg / Abiraterone acetate 1000 mg
- Fixed-dose combination tablets: Niraparib 75 mg / Abiraterone acetate 500 mg
Adult Dosing
- Metastatic castration-resistant prostate cancer (mCRPC): Two 50 mg/500 mg tablets (total daily dose: 100 mg niraparib / 1000 mg abiraterone) once daily
- Alternative strength: One 100 mg/1000 mg tablet once daily
- Administer on an empty stomach at least 1 hour before or 2 hours after food
- Co-administer with prednisone or prednisolone 5 mg orally twice daily
- Continue treatment until disease progression or unacceptable toxicity
Pediatric Dosing
- Safety and efficacy have not been established in pediatric patients
- Not indicated for use in pediatric populations
Indications
- Treatment of adult patients with deleterious or suspected deleterious BRCA-mutated metastatic castration-resistant prostate cancer (mCRPC)
Mechanism of Action
- Niraparib is an inhibitor of poly (ADP-ribose) polymerase (PARP) enzymes (PARP1 and PARP2), impairing DNA repair and causing synthetic lethality in cancer cells
- Abiraterone acetate is converted in vivo to abiraterone, an androgen biosynthesis inhibitor that inhibits CYP17 (17alpha-hydroxylase/C17,20-lyase), decreasing testosterone synthesis
Contraindications
- Hypersensitivity to niraparib, abiraterone acetate, or any component of the formulation
- Pregnancy and women who may become pregnant
- Severe hepatic impairment (Child-Pugh Class C)
Adverse Reactions
- Cardiovascular: Hypertension, tachycardia, flushing
- Hematologic: Anemia, thrombocytopenia, neutropenia, leukopenia
- Gastrointestinal: Nausea, constipation, diarrhea, vomiting, dyspepsia, fatigue, asthenia
- Metabolic and Laboratory: Increased ALT, increased AST, hypokalemia, hyperglycemia, hypertriglyceridemia
- Musculoskeletal: Arthralgia, back pain, musculoskeletal pain
Drug Interactions
- Strong CYP3A4 inducers (e.g., rifampin, carbamazepine): Avoid co-administration as they decrease abiraterone exposure
- CYP2D6 substrates (e.g., metoprolol, dextromethorphan): Abiraterone inhibits CYP2D6; monitor for increased toxicity of concomitantly administered drugs
- OATP1B1 substrates: Concomitant use may increase concentrations of OATP1B1 substrates (e.g., statins)
- Drugs that prolong the QT interval: Abiraterone may cause QTc prolongation; use with caution
Curated Content: Needs Vetting Before Put to Clinical Use