Company : Clovis Oncology Inc
Approved by : FDA, EMA, NCCN
Approval Time : Apr. 6, 2018
Direct Target : PARP1,PARP2,PARP3
Drug Type : Single-target inhibitor
Alteration : Deleterious Mutations
Indications : Rucaparib was granted approval to be used for maintenance treatment of patients with recurrent epithelial ovarian, fallopian tube, or primary peritoneal cancer who are in complete or partial response to platinum-based chemotherapy.
Mechanism Of Action :
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. Increased rucaparib-induced cytotoxicity and anti-tumor activity was observed in tumor cell lines with deficiencies in BRCA1/2 and other DNA repair genes. Rucaparib has been shown to decrease tumor growth in mouse xenograft models of human cancer with or without deficiencies in BRCA.
Dosage : The recommended dose of rucaparib is 600 mg twice daily with or without food, with treatment continued until disease progression or unacceptable toxicity. For management of adverse reactions, interruption of treatment or dose reduction should be considered. Recommended dose reductions are to 500 mg twice daily, 400 mg twice daily, and 300 mg twice daily for first, second, and third reductions, respectively.
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