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<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>

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Olaparib research update: mechanism, structure and clinical trials

  • 期刊论文

  • 发表日期：

    2025年1月26日

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  • Hao Che,
  • Li-Wei Wang,
  • Xiang-Yang Ye,
  • Xingrui He

摘要

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.