Rucaparib

Rucaparib is an inhibitor of poly (ADP-ribose) polymerase (PARP) enzymes, including PARP-1, PARP-2, and PARP-3, which play a role in DNA repair. In vitro studies have shown that rucaparib-induced cytotoxicity may involve inhibition of PARP enzymatic activity and increased formation of PARP-DNA complexes resulting in DNA damage, apoptosis, and cancer cell death.

• RUBRACA is a poly (ADP-ribose) polymerase (PARP) inhibitor indicated: Ovarian cancer for the maintenance treatment of adult patients with a deleterious BRCA mutation (germline and/or somatic)-associated recurrent epithelial ovarian, fallopian tube, or primary peritoneal cancer who are in a complete or partial response to platinum-based chemotherapy. ( 1.1 ) Prostate cancer for the treatment of adult patients with a deleterious BRCA mutation (germline and/or somatic)-associated metastatic castration-resistant prostate cancer (mCRPC) who have been treated with androgen receptor-directed therapy.ICD-10: C56.9, C61

• None. None.contraindicated

Recommended dose is 600 mg orally twice daily with or without food. ( 2.2 ) Continue treatment until disease progression or unacceptable toxicity. ( 2.2 ) For adverse reactions, consider interruption of treatment or dose reduction. ( 2.3 ) Patients receiving RUBRACA for mCRPC should also receive a gonadotropin-releasing hormone (GnRH) analog concurrently or should have had bilateral orchiectomy. ( 2.2 ) 2.1 Patient Selection Maintenance Treatment of BRCA -mutated Recurrent Ovarian Cancer Select patients for the maintenance treatment of recurrent ovarian cancer with RUBRACA based on the presence of a deleterious BRCA mutation (germline and/or somatic) [see Clinical Studies ( 14.1 )]. An FDA-approved test for the detection of deleterious germline and/or somatic BRCA mutations is not currently available. Treatment of BRCA -mutated mCRPC after Androgen Receptor-directed Therapy Select patients for the treatment of mCRPC with RUBRACA based on the presence of a deleterious BRCA mutation (germline and/or somatic) in plasma specimens [see Clinical Studies ( 14.2 )]. A negative result from a plasma specimen does not mean that the patient’s tumor is negative for BRCA mutations. Should the plasma specimen have a negative result, consider performing further genomic testing using tumor specimens as clinically indicated. Information on the FDA-approved tests for the detection of a BRCA mutation in patients with ovarian cancer or with prostate cancer is available at: http://www.fda.gov/CompanionDiagnostics.

Myelodysplastic Syndrome/Acute Myeloid Leukemia (MDS/AML): MDS/AML occurred in patients exposed to RUBRACA, and some cases were fatal. Monitor patients for hematological toxicity at baseline and monthly thereafter. Interrupt or reduce the dose based on severity of reaction. Discontinue if MDS/AML is confirmed. ( 2.3 , 5.1 ) Embryo-Fetal Toxicity: RUBRACA can cause fetal harm. Advise of the potential risk to a fetus and to use effective contraception. ( 5.2 , 8.1 , 8.3 ) 5.1 Myelodysplastic Syndrome/Acute Myeloid Leukemia Myelodysplastic Syndrome (MDS)/Acute Myeloid Leukemia (AML) occur in patients treated with RUBRACA, and are potentially fatal adverse reactions. In 2141 treated patients with ovarian and prostate cancer [see Adverse Reactions ( 6.1 )], MDS/AML occurred in 34 patients (1.6%), including those in long term follow-up. Of these, 14 occurred during treatment or during the 28-day safety follow-up (0.7%). The duration of RUBRACA treatment prior to the diagnosis of MDS/AML ranged from < 2 months to approximately 72 months. The cases were typical of secondary MDS/cancer therapy-related AML; in all cases, patients had received previous platinum-containing chemotherapy regimens and/or other DNA damaging agents. In ARIEL3, of patients with a germline and/or somatic BRCA mutation treated with RUBRACA, MDS/AML occurred in 9 out of 129 (7%) patients treated with RUBRACA and 4 out of 66 (6%) patients treated with placebo. The duration of therapy with RUBRACA in patients who developed secondary MDS/cancer therapy-related AML varied from 1.2 to 4.7 years.

The following serious adverse reactions are discussed elsewhere in the labeling: Myelodysplastic Syndrome/Acute Myeloid Leukemia [see Warnings and Precautions ( 5.1 )]. Most common adverse reactions (≥10%) among patients with ovarian cancer were nausea, fatigue (including asthenia), anemia, ALT/AST increased, vomiting, diarrhea, decreased appetite, thrombocytopenia, dysgeusia, neutropenia, blood creatinine increased, dyspnea, dizziness, dyspepsia, photosensitivity reaction, and leukopenia. ( 6.1 ) Most common adverse reactions (≥10%) among patients with BRCA -mutated mCRPC were fatigue/asthenia, musculoskeletal pain, nausea, anemia, decreased appetite, increased ALT/AST, constipation, diarrhea, vomiting, thrombocytopenia, dyspnea, increased blood creatinine, edema, dizziness, weight decreased, abdominal pain, dysgeusia, rash, neuropathy peripheral, urinary tract infection, cough, headache, hemorrhage, neutropenia, and photosensitivity reaction. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact pharmaand agent at 1-800-506-8501 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch . 6.1 Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice.

Lactation: Advise women not to breastfeed. ( 8.2 ) 8.1 Pregnancy Risk Summary Based on findings from animal studies and its mechanism of action, Rubraca can cause fetal harm when administered to pregnant women. There are no available data in pregnant women to inform the drug-associated risk. In an animal reproduction study, administration of rucaparib to pregnant rats during organogenesis resulted in embryo-fetal death at maternal exposures that were 0.04 times the AUC 0-24h in patients receiving the recommended dose of 600 mg twice daily [see Data] . Apprise pregnant women of the potential risk to a fetus. The background risk of major birth defects and miscarriage for the indicated population is unknown. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2% to 4% and 15% to 20%, respectively. Data Animal Data In a dose range-finding embryo-fetal development study, pregnant rats received oral doses of 50, 150, 500, or 1000 mg/kg/day of rucaparib during the period of organogenesis. Post-implantation loss (100% early resorptions) was observed in all animals at doses greater than or equal to 50 mg/kg/day (with maternal systemic exposures approximately 0.04 times the human exposure at the recommended dose based on AUC 0-24h ).

Metabolism

The AUC and C max of rucaparib demonstrated linear pharmacokinetics over a dose range from 240 mg to 840 mg twice daily (0.4 times to 1.4 times the approved recommended dosage). The mean (coefficient of variation [CV]) steady-state rucaparib C max is 1,940 ng/mL (54%) and AUC 0-12h is 16,900 h×ng/mL (54%) at the approved recommended dosage.

• Dec 19, 2016NDANDA209115Pharmaand

1. 1Fatigue2,54729%
2. 2Nausea2,25826%
3. 3Malignant Neoplasm Progression1,18414%
4. 4Decreased Appetite8029.2%
5. 5Diarrhoea7899.0%
6. 6Constipation7838.9%
7. 7Vomiting7808.9%
8. 8Asthenia6797.8%
9. 9Adverse Event5716.5%
10. 10Carbohydrate Antigen 125 Increased5696.5%
11. 11Dysgeusia5656.4%
12. 12Anaemia5536.3%
13. 13Product Dose Omission Issue5506.3%
14. 14Platelet Count Decreased5396.2%
15. 15Drug Ineffective5195.9%

The 10 most recently updated of 69 ClinicalTrials.gov registrations naming Rucaparib as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

• Pan Tumor Rollover Study
  Recruiting · Phase 2 · Interventional · 1,500 enrolled · Bristol-Myers Squibb
  NCT03899155updated 2026-06-03
• Microdevice In Ovarian, Fallopian Tube, And Peritoneal Cancer
  Recruiting · Phase 1 · Interventional · 20 enrolled · Brigham and Women's Hospital
  NCT04701645updated 2026-05-18
• A Study in Patients Previously Enrolled in a Genentech and/or F. Hoffmann-La Roche Ltd Sponsored Atezolizumab Study
  Active not recruiting · Phase 3 · Interventional · 1,000 enrolled · Hoffmann-La Roche
  NCT03768063updated 2026-04-28
• The EndoBARR Trial (Endometrial Bevacizumab, Atezolizumab, Rucaparib)
  Completed · Phase 2 · Interventional · 30 enrolled · Medical College of Wisconsin
  NCT03694262updated 2026-04-13
• A Phase II Study Of Nivolumab/ Bevacizumab/Rucaparib
  Active not recruiting · Phase 2 · Interventional · 72 enrolled · Dana-Farber Cancer Institute
  NCT02873962updated 2026-04-01
• Rucaparib vs Placebo Maintenance Therapy in Metastatic and Recurrent Endometrial Cancer
  Completed · Phase 2 · Interventional · 79 enrolled · University of Colorado, Denver
  NCT03617679updated 2026-03-24
• A Real-world Study of Characteristics, Treatment Patterns, and Clinical Outcomes Among Lutetium-177 Vipivotide Tetraxetan Treated Patients
  Completed · Observational · 1,247 enrolled · Novartis Pharmaceuticals
  NCT07477756updated 2026-03-19
• Analysis of the Clinical Experience With Rucaparib in the Rucaparib Access Program (RAP) in Spain - A GEICO Study
  Completed · Observational · 51 enrolled · Grupo Español de Investigación en Cáncer de Ovario
  NCT04539327updated 2026-03-18
• Rucaparib and Pembrolizumab for Maintenance Therapy in Stage IV Non-Squamous Non-Small Cell Lung Cancer
  Terminated · Phase 1 · Phase 2 · Interventional · 25 enrolled · University of Michigan Rogel Cancer Center
  NCT03559049updated 2026-02-12
• A Clinical Study Evaluating The Benefit of Adding Rucaparib to Enzalutamide for Men With Metastatic Prostate Cancer That Has Become Resistant To Testosterone-Deprivation Therapy
  Active not recruiting · Phase 3 · Interventional · 61 enrolled · Alliance for Clinical Trials in Oncology
  NCT04455750updated 2026-02-05

Frequently asked questions

How does Rucaparib work?

Rucaparib is an inhibitor of poly (ADP-ribose) polymerase (PARP) enzymes, including PARP-1, PARP-2, and PARP-3, which play a role in DNA repair. In vitro studies have shown that rucaparib-induced cytotoxicity may involve inhibition of PARP enzymatic activity and increased formation of PARP-DNA complexes resulting in DNA damage, apoptosis, and cancer cell death.

What is Rucaparib used for?

According to FDA labeling, Rucaparib carries indications including: RUBRACA is a poly (ADP-ribose) polymerase (PARP) inhibitor indicated: Ovarian cancer for the maintenance treatment of adult patients with a deleterious BRCA mutation (germline and/or somatic)-associated recurrent epithelial ovarian, fallopian tube, or primary peritoneal cancer who are in a complete or partial response to platinum-based chemotherapy. ( 1.1 ) Prostate cancer for the treatment of adult patients with a deleterious BRCA mutation (germline and/or somatic)-associated metastatic castration-resistant prostate cancer (mCRPC) who have been treated with androgen receptor-directed therapy.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.

What class of drug is Rucaparib?

Rucaparib is classified as Poly (ADP-ribose) polymerase (PARP) inhibitors, Poly(ADP-Ribose) Polymerase Inhibitor, Poly(ADP-Ribose) Polymerase Inhibitors, Cellular Growth Phase Reduction, Decreased DNA Integrity, Decreased Reverse Transcription to DNA.

What are the brand names for Rucaparib?

Rucaparib is marketed under brand names including Rubraca.

What are the contraindications for Rucaparib?

Rucaparib labeling lists contraindications including: None. None.. Always consult the full prescribing information and a clinician.