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

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Dockery LE, Gunderson CC, Moore KN

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

Onco Targets Ther. 2017 Jun 19;10:3029-3037. doi: 10.2147/OTT.S114714. eCollection 2017.

PubMed ID

28790837 [ View in PubMed

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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 CDx BRCA 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.

DrugBank Data that Cites this Article

Drugs

Rucaparib

Drug Targets

Drug	Target	Kind	Organism	Pharmacological Action	Actions
Rucaparib	Poly [ADP-ribose] polymerase 1	Protein	Humans	Yes	Inhibitor	Details
Rucaparib	Poly [ADP-ribose] polymerase 2	Protein	Humans	Yes	Inhibitor	Details
Rucaparib	Poly [ADP-ribose] polymerase 3	Protein	Humans	Yes	Inhibitor	Details

Drug Enzymes

Drug	Enzyme	Kind	Organism	Pharmacological Action	Actions
Rucaparib	Cytochrome P450 1A2	Protein	Humans	No	Substrate Inhibitor Inducer	Details

Drug Transporters

Drug	Transporter	Kind	Organism	Pharmacological Action	Actions
Rucaparib	Solute carrier family 22 member 1	Protein	Humans	No	Inhibitor	Details