Class/mechanism: PARP inhibitor. Rucaparib inhibits activity of the poly (ADP-ribose) polymerase (PARP) enzymes--including PARP-1, PARP-2, and PARP-3--and interferes with PARP-mediated DNA repair. PARP inhibitor cytotoxicity is believed to involve formation of PARP-DNA complexes, DNA damage, apotosis, and cell death. This cytotoxicity was observed to have increased cytotoxicity in cells with mutations in BRCA1, BRCA2, and other DNA repair genes.
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Diseases for which it is used
Patient drug information
History of changes in FDA indication
- 12/19/2016: Granted accelerated approval for treatment of patients with deleterious BRCA mutation (germline and/or somatic) associated advanced ovarian cancer who have been treated with two or more chemotherapies. (Based on Study 10 and ARIEL2)
- 4/6/2018: FDA approved for the maintenance treatment of recurrent epithelial ovarian, fallopian tube, or primary peritoneal cancer who are in a complete or partial response to platinum-based chemotherapy. (Indication expanded to maintenance therapy; based on ARIEL3)
- 5/15/2020: Granted accelerated approval for patients with BRCA mutation (germline and/or somatic)-associated metastatic castration-resistant prostate cancer (mCRPC) who have been treated with androgen receptor-directed therapy and a taxane-based chemotherapy. (New disease entity; based on TRITON2)
Also known as
- Code names: CO-338, AG-014699, PF-0136738
- Brand name: Rubraca