间变性淋巴瘤激酶抑制剂的最新专利审查(2018-2022)。

IF 5.4 2区 医学 Q1 CHEMISTRY, MEDICINAL Expert Opinion on Therapeutic Patents Pub Date : 2023-04-01 DOI:10.1080/13543776.2023.2216381
Deyi Ma, Mengrao Guo, Xin Zhai
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引用次数: 0

摘要

间变性淋巴瘤激酶(ALK)是胰岛素受体超家族中的一种受体酪氨酸激酶,已成为治疗多种癌症的有前途的药物靶点。截至目前,共有7种ALK抑制剂被批准用于临床癌症治疗。然而,对ALK抑制剂的耐药问题随后被报道,这导致了最近对新一代ALK抑制剂的探索。涵盖领域:本文对2018 - 2022年小分子ALK抑制剂的结构、药理数据及其作为抗癌药物的应用等专利文献进行了全面综述。此外,还详细介绍了市场上或正在临床研究中的几种潜在的ALK抑制剂。专家意见:到目前为止,还没有批准的ALK抑制剂完全没有耐药性问题,这是一个迫切需要解决的困境。通过结构修饰、多靶点抑制剂、i- 1 / 2型和ii型结合模式以及PROTAC和药物偶联物开发新的ALK抑制剂正在进行中。在过去的5年中,lorlatinib, entrectinib和恩沙替尼已经被批准,并且越来越多的关于ALK抑制剂的研究,特别是关于大环化合物的研究,已经证明了它们有希望的治疗效力。
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An updated patent review of anaplastic lymphoma kinase inhibitors (2018-2022).

Introduction: Anaplastic lymphoma kinase (ALK), a receptor tyrosine kinase in the insulin receptor superfamily, has emerged as a promising drug target for multiple cancers. Up to now, a total of seven ALK inhibitors have been approved for clinical cancer treatment. However, the issue of resistance to ALK inhibitors was subsequently reported, which led to the exploration of novel generations of ALK inhibitors recently.

Areas covered: This paper provides a comprehensive review of the patent literature from 2018 to 2022 about structures, pharmacological data of small molecular ALK inhibitors, and their utilization as anticancer agents. In addition, several potential ALK inhibitors on the market or under clinical investigations are described in detail.

Expert opinion: To date, there are no ALK inhibitors that have been approved are completely free of resistance issues, which is a plight needing urgent solution. Development of new ALK inhibitors through structure modification, multi-targeted inhibitors, type-I½ and type-II binding modes, as well as PROTAC and drug conjugates are proceeding. Over the last 5 years, lorlatinib, entrectinib, and ensartinib have been approved, and an increasing number of studies on ALK inhibitors, especially on macrocyclic compounds, have demonstrated their promising therapeutic potency.

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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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