Rucaparib in ovarian cancer: an update on safety, efficacy and place in therapy
Author(s) -
Graziela Zibetti Dal Molin,
Kohei Omatsu,
Anil K. Sood,
Robert L. Coleman
Publication year - 2018
Publication title -
therapeutic advances in medical oncology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.272
H-Index - 49
eISSN - 1758-8359
pISSN - 1758-8340
DOI - 10.1177/1758835918778483
Subject(s) - medicine , parp inhibitor , ovarian cancer , olaparib , oncology , veliparib , ovarian carcinoma , cancer , pharmacodynamics , pharmacology , parp1 , poly adp ribose polymerase , chemotherapy , cancer research , pharmacokinetics , polymerase , biology , enzyme , biochemistry
Rucaparib is a poly (ADP-ribose) polymerase (PARP) inhibitor and potent inhibitor of PARP1, PARP2 and PARP3 enzymes. Phase II and III trials have documented that rucaparib has single-agent antitumor activity in patients with high-grade ovarian carcinoma, with both BRCA-mutated (germline and somatic) and with homologous recombination deficiency (HRD). Rucaparib as a maintenance treatment showed increased progression-free survival in patients with ovarian carcinoma who achieved a response to platinum-based chemotherapy, with an acceptable safety profile. The approval of this drug, along with the companion diagnostic FoundationFocus CDxBRCA test represents an important new therapeutic option in the treatment of ovarian cancer. This article reviews the mechanisms of action, safety, pharmacokinetics and pharmacodynamics and indications for use of rucaparib as well as future trials.
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