Rubraca

Ovarian cancer — maintenance treatment of recurrent epithelial ovarian, fallopian tube, or primary peritoneal cancer who are in complete or partial response to platinum-based chemotherapy

600 mg orally twice daily (two 300 mg tablets BID)
Take with or without food
Dose reductions: 500 mg BID → 400 mg BID → 300 mg BID
Continue until disease progression or unacceptable toxicity

Tablets: 200 mg, 250 mg, 300 mg

None listed.

• MDS/AML: Occurred in 1.3% of patients in clinical studies. Some cases were fatal. Monitor CBC at baseline and monthly. Discontinue if MDS/AML confirmed.
• Hematologic Toxicity: Anemia (44% Grade ≥3: 21%), neutropenia (18% Grade ≥3: 8%), thrombocytopenia (21% Grade ≥3: 5%). Monitor CBC at baseline, weekly for first month, then monthly for first year, then periodically.
• Hepatotoxicity: ALT/AST elevation common (34%). Monitor LFTs at baseline, every 2 weeks for first 3 months, then monthly.
• Photosensitivity: Advise patients to use sunscreen and protective clothing.
• Embryo-Fetal Toxicity

Nausea (77%), fatigue (73%), abdominal pain (46%), rash (43%), dysgeusia (39%), anemia (44%), constipation (37%), vomiting (37%), diarrhea (34%), thrombocytopenia (21%), dyspnea (21%), decreased appetite (23%)

Consult the complete prescribing information for a comprehensive list of adverse reactions and their frequencies.

Consult the complete prescribing information for drug interactions, including effects on CYP enzymes, transporters, and concomitant medications that may require dose adjustments or monitoring.

Consult the full prescribing information for pregnancy-related considerations.

Refer to prescribing information for lactation guidance.

Pediatric safety and efficacy information is detailed in the full label.

Dose modifications for organ impairment are specified in the complete prescribing information.

Rucaparib is an inhibitor of poly(ADP-ribose) polymerase (PARP) enzymes, including PARP-1, PARP-2, and PARP-3. PARP inhibition by rucaparib induces cytotoxicity via trapping of PARP-DNA complexes at sites of DNA damage, preventing DNA repair, causing DNA double-strand breaks, and exploiting synthetic lethality in tumor cells with deficient homologous recombination repair (HRR), including BRCA1/2 mutations.

Tmax: 1.9 hours. Half-life: approximately 17-19 hours. Protein binding: 70%. Metabolized by CYP2D6 and to lesser extent CYP1A2 and CYP3A4. Primarily excreted in urine (64%) and feces (28%).

Clinical efficacy and safety data supporting the approval are available in the full prescribing information and from the clinical trials listed below.

• ARIEL3 — Rucaparib maintenance vs. placebo in platinum-sensitive recurrent ovarian cancer. Phase III, n=564.
  🔬 NCT01968213 ↗ 📄 Primary Publication ↗

Rubraca has FDA-approved indications across the following cancer types covered on PipelineEvidence: