PARP Inhibitors for Cancer Therapy

• Published in: Cell Vol. 169; no. 2; p. 183
• Main Authors: Lin, Ken Y., Kraus, W. Lee
• Format: Journal Article
• Language: English
• Published: United States Elsevier Inc 06-04-2017
• Subjects: Antineoplastic Agents - therapeutic use; BRCA1 Protein - genetics; BRCA2 Protein - genetics; Drug Approval; Female; Humans; Indoles - therapeutic use; Mutation; Ovarian Neoplasms - drug therapy; Ovarian Neoplasms - genetics; Poly(ADP-ribose) Polymerase Inhibitors - therapeutic use
• ISSN: 0092-8674; 1097-4172
• DOI: 10.1016/j.cell.2017.03.034

Rucaparib is an inhibitor of nuclear poly (ADP-ribose) polymerases (inhibition of PARP-1 > PARP-2 > PARP-3), following a similar drug, Olaparib. It disrupts DNA repair and replication pathways (and possibly transcription), leading to selective killing of cancer cells with BRCA1/2 mutations. Rucaparib is approved for recurrent ovarian cancers with germline or somatic mutations in BRCA1/2.
Rucaparib is an inhibitor of nuclear poly (ADP-ribose) polymerases (inhibition of PARP-1 > PARP-2 > PARP-3), following a similar drug, Olaparib. It disrupts DNA repair and replication pathways (and possibly transcription), leading to selective killing of cancer cells with BRCA1/2 mutations. Rucaparib is approved for recurrent ovarian cancers with germline or somatic mutations in BRCA1/2.