重组转染(RET)激酶抑制剂的最新专利回顾(2022年至今)。

IF 4.6 2区 医学 Q1 CHEMISTRY, MEDICINAL
Expert Opinion on Therapeutic Patents Pub Date : 2025-08-01 Epub Date: 2025-06-17 DOI:10.1080/13543776.2025.2519642
Daniel Armstrong, Maha Hanafi, Brendan Frett
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引用次数: 0

摘要

在转染过程中重排(RET)是一种受体酪氨酸激酶,对细胞信号传导过程如增殖、分化和迁移至关重要。RET的改变,包括点突变和基因融合,有助于肿瘤的发生。精确肿瘤学的最新进展导致了选择性RET抑制剂的发展,其安全性和有效性都有所提高。涵盖领域:本文讨论了RET抑制剂开发的最新创新,重点是2022年至2024年发布的小分子专利。使用SciFinder和PatentScope进行全面的文献检索,检索关键词为“RET”和“RET抑制剂”。综述了新专利化合物的结构类别、靶点特征和潜在优势,特别是那些旨在克服已知抗性机制的专利化合物。专家意见:虽然选择性RET抑制剂如selpercatinib已显示出临床成功和扩大适应症,但它们的使用受到不良事件和新出现的耐药机制的限制。解决这些限制的下一代RET抑制剂代表了药物开发的关键前沿。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
An updated patent review of rearranged during transfection (RET) kinase inhibitors (2022-present).

Introduction: Rearranged during transfection (RET) is a receptor tyrosine kinase essential for cell signaling processes such as proliferation, differentiation, and migration. RET alterations, including point mutations and gene fusions, contribute to oncogenesis. Recent advances in precision oncology have led to the development of selective RET inhibitors with improved safety and efficacy profiles.

Areas covered: This review discusses recent innovations in RET inhibitor development, with a focus on small-molecule patents published from 2022 to 2024. A comprehensive literature search was conducted using SciFinder and PatentScope with the keywords 'RET' and 'RET inhibitor.' The review summarizes the structural classes, target profiles, and potential advantages of newly patented compounds, particularly those designed to overcome known resistance mechanisms.

Expert opinion: While selective RET inhibitors such as selpercatinib have shown clinical success and expanded indications, their use is limited by adverse events and emerging resistance mechanisms. Next-generation RET inhibitors that address these limitations represent a critical frontier in drug development.

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来源期刊
CiteScore
12.10
自引率
1.50%
发文量
50
审稿时长
6-12 weeks
期刊介绍: Expert Opinion on Therapeutic Patents (ISSN 1354-3776 [print], 1744-7674 [electronic]) is a MEDLINE-indexed, peer-reviewed, international journal publishing review articles on recent pharmaceutical patent claims, providing expert opinion the scope for future development, in the context of the scientific literature. The Editors welcome: Reviews covering recent patent claims on compounds or applications with therapeutic potential, including biotherapeutics and small-molecule agents with specific molecular targets; and patenting trends in a particular therapeutic area Patent Evaluations examining the aims and chemical and biological claims of individual patents Perspectives on issues relating to intellectual property The audience consists of scientists, managers and decision-makers in the pharmaceutical industry and others closely involved in R&D Sample our Bioscience journals, sign in here to start your access, Latest two full volumes FREE to you for 14 days.
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