{"title":"Olaparib research update: mechanism, structure and clinical trials","authors":"Hao Che, Li-Wei Wang, Xiang-Yang Ye, Xingrui He","doi":"10.1007/s00044-025-03375-8","DOIUrl":null,"url":null,"abstract":"<div><p>Current cancer treatments are known for their low selectivity, and life-threatening toxicity. To solve these issue, various innovative approaches were applied. One of them is the inhibition of DNA repair mechanisms, which have been developed as a new hotspot for its selective inhibition and low toxicity. Notably, PARP inhibition has shown potential for effective targeted cancer therapy. Olaparib, the first FDA-approved PARP inhibitor, has been available for nearly a decade, demonstrating superior efficacy in treating breast and ovarian cancers. This article reviews the latest mechanistic studies, structural modifications, and clinical trials of Olaparib.</p></div>","PeriodicalId":699,"journal":{"name":"Medicinal Chemistry Research","volume":"34 3","pages":"535 - 548"},"PeriodicalIF":3.1000,"publicationDate":"2025-01-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"Medicinal Chemistry Research","FirstCategoryId":"3","ListUrlMain":"https://link.springer.com/article/10.1007/s00044-025-03375-8","RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q3","JCRName":"CHEMISTRY, MEDICINAL","Score":null,"Total":0}
引用次数: 0
Abstract
Current cancer treatments are known for their low selectivity, and life-threatening toxicity. To solve these issue, various innovative approaches were applied. One of them is the inhibition of DNA repair mechanisms, which have been developed as a new hotspot for its selective inhibition and low toxicity. Notably, PARP inhibition has shown potential for effective targeted cancer therapy. Olaparib, the first FDA-approved PARP inhibitor, has been available for nearly a decade, demonstrating superior efficacy in treating breast and ovarian cancers. This article reviews the latest mechanistic studies, structural modifications, and clinical trials of Olaparib.
期刊介绍：
Medicinal Chemistry Research (MCRE) publishes papers on a wide range of topics, favoring research with significant, new, and up-to-date information. Although the journal has a demanding peer review process, MCRE still boasts rapid publication, due in part, to the length of the submissions. The journal publishes significant research on various topics, many of which emphasize the structure-activity relationships of molecular biology.
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