Title: Niraparib (Zejula), A Small Molecule, PARP1/2 Inhibitor for Treating Breast, Ovarian, and Pancreatic Cancers
Abstract: Chapter 12 Niraparib (Zejula), A Small Molecule, PARP1/2 Inhibitor for Treating Breast, Ovarian, and Pancreatic Cancers Raymond Ng, Raymond NgSearch for more papers by this author Raymond Ng, Raymond NgSearch for more papers by this author Book Editor(s):Jie Jack Li, Jie Jack LiSearch for more papers by this author First published: 22 September 2022 https://doi.org/10.1002/9781119847281.ch12 AboutPDFPDF ToolsRequest permissionExport citationAdd to favoritesTrack citation ShareShare Summary Poly(ADP-ribose) polymerases (PARPs) are a family of 17 proteins involved in posttranslational modification of proteins. Although PARP1 was first discovered in 1966, it took another 50 years before a PARP inhibitor was shown to be the first cancer drug to exploit synthetic lethality. PARP1 and PARP2 are nuclear proteins that contain both a DNA binding domain and a catalytic domain. A hallmark of high grade serous ovarian cancer is a defective DNA damage response, of which PARP inhibitors can exploit through synthetic lethality. Interestingly, talazoparib has the highest PARP trapping potency, followed by niraparib, rucaparib, olaparib, and veliparib. Niraparib and other PARPi represent a new class of oncology drugs that exploit synthetic lethality. As the third US Food and Drug Administration-approved PARP inhibitor, niraparib was a significant improvement over olaparib and rucaparib since it was approved for patients without a germline or somatic BRCA mutation with single daily dosing. Current Drug Synthesis, 1st Edition RelatedInformation
Publication Year: 2022
Publication Date: 2022-09-22
Language: en
Type: other
Indexed In: ['crossref']
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Cited By Count: 1
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