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Rucaparib: the past, present, and future of a newly approved PARP inhibitor for ovarian cancer

Authors Dockery LE, Gunderson CC, Moore KN

Received 5 March 2017

Accepted for publication 13 May 2017

Published 19 June 2017 Volume 2017:10 Pages 3029—3037

DOI https://doi.org/10.2147/OTT.S114714

Checked for plagiarism Yes

Review by Single-blind

Peer reviewers approved by Dr Akshita Wason

Peer reviewer comments 3

Editor who approved publication: Dr Yao Dai

LE Dockery, CC Gunderson, KN Moore

Department of Obstetrics and Gynecology, Section of Gynecologic Oncology, Stephenson Cancer Center, University of Oklahoma Health Sciences Center, Oklahoma City, OK, USA

Abstract: Rucaparib camsylate (CO-338, AG-014699, PF-01367338) is a potent PARP-1, PARP-2, and PARP-3 inhibitor. Phase I and II studies demonstrated clinical efficacy in both BRCA-mutated (inclusive of germline and somatic) ovarian tumors and ovarian tumors with homologous recombination deficiency (HRD) loss of heterozygosity (LOH). Rucaparib has received the US Food and Drug Administration (FDA) approval for patients with deleterious BRCA mutation (germline and/or somatic)-associated advanced ovarian cancer who have been treated with two or more chemotherapies. There is evidence to suggest that rucaparib has clinical efficacy against ovarian tumors with high HRD-LOH. Rucaparib’s companion diagnostic FoundationFocus™ CDxBRCA test is the first FDA-approved next-generation sequencing-based companion diagnostic test designed to identify patients likely to respond to rucaparib. This article reviews the mechanisms of action, safety, approval, and indications for use of the PARP inhibitor rucaparib as well as future trials and use of rucaparib’s companion diagnostic test.

Keywords: rucaparib, PARP inhibitor, ovarian cancer, companion diagnostic, loss of heterozy­gosity

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