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ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS › ANTINEOPLASTIC AGENTS › OTHER ANTINEOPLASTIC AGENTS › Poly (ADP-ribose) polymerase (PARP) inhibitors
rucaparib
L01XK03
Forms & Strengths
- Oral tablets: 200 mg
- Oral tablets: 250 mg
- Oral tablets: 300 mg
Adult Dosing
- Maintenance treatment of recurrent epithelial ovarian, fallopian tube, or primary peritoneal cancer: 600 mg orally twice daily
- Treatment of deleterious BRCA-mutated advanced ovarian cancer after 2 or more chemotherapies: 600 mg orally twice daily
- Castration-resistant prostate cancer with deleterious BRCA mutation: 600 mg orally twice daily with androgen deprivation therapy
Pediatric Dosing
- Safety and efficacy not established in pediatric patients
Indications
- Maintenance treatment of adult patients with recurrent epithelial ovarian, fallopian tube, or primary peritoneal cancer who are in a complete or partial response to platinum-based chemotherapy
- Treatment of adult patients with deleterious BRCA mutation-associated advanced ovarian cancer who have been treated with two or more chemotherapies
- Treatment of adult patients with deleterious BRCA mutation-associated metastatic castration-resistant prostate cancer who have received prior androgen receptor-directed therapy and a taxane-based chemotherapy
Mechanism of Action
- Inhibitor of human poly (ADP-ribose) polymerase (PARP) enzymes, including PARP1, PARP2, and PARP3
- Blocks PARP catalytic activity and traps PARP-DNA complexes, resulting in DNA damage, apoptosis, and cell death in cancer cells
- Particularly synthetic lethal in cancer cells with deficient homologous recombination repair, such as those with BRCA1 or BRCA2 mutations
Contraindications
- Hypersensitivity to rucaparib or any of its excipients
- Pregnancy and lactation due to potential for embryofetal harm
Adverse Reactions
- Common: Nausea, fatigue, vomiting, asthenia, anemia, abdominal pain, dysgeusia, constipation, decreased appetite, diarrhea, thrombocytopenia
- Serious: Myelodysplastic syndrome (MDS), acute myeloid leukemia (AML), bone marrow suppression, embryo-fetal toxicity
- Laboratory abnormalities: Increased ALT/AST, increased creatinine, decreased lymphocytes, decreased neutrophils, decreased hemoglobin
Drug Interactions
- CYP1A2 substrates: Rucaparib inhibits CYP1A2, potentially increasing concentrations of substrates such as caffeine or tizanidine
- CYP2C9, CYP2C19, and CYP3A substrates: Rucaparib is a weak-to-moderate inhibitor, use caution with sensitive substrates
- Transporter interactions: Rucaparib inhibits P-gp, BCRP, MATE1, MATE2-K, and OCT1, potentially increasing plasma levels of co-administered transporter substrates (e.g., metformin)
Curated Content: Needs Vetting Before Put to Clinical Use