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针对EGFR外基子20插入的小分子抑制剂的专利审查 (Ex20ins) (2019年至今)

Wenjian Zhu¹, Junping Pei¹, Xiaoyun Lu¹

¹State Key Laboratory of Bioactive Molecules and Druggability Assessment, International Cooperative Laboratory of Traditional Chinese Medicine Modernization and Innovative Drug Discovery of Chinese Ministry of Education, Guangzhou City Key Laboratory of Precision Chemical Drug Development, School of Pharmacy, Jinan University, Guangzhou, China.

Expert opinion on therapeutic patents

|December 21, 2024

概括

准表皮生长因子受体 (EGFR) 异位子20插入 (Ex20ins) 突变对于非小细胞肺癌 (NSCLC) 治疗至关重要. 本综述强调了EGFR Ex20ins抑制剂和专利的近期进展,解决治疗挑战.

科学领域:

在瘤学瘤学.
分子生物学分子生物学
药物发现药物发现药物发现

背景情况:

表皮生长因子受体 (EGFR) 激酶域突变激活信号通路,促进非小细胞肺癌 (NSCLC) 的瘤生长.
虽然许多EGFR突变对EGFR氨酸激酶抑制剂 (EGFR-TKI) 产生反应,但EGFRExon 20插入 (Ex20ins) 突变存在重大未满足的临床需求.
直接针对EGFR Ex20ins突变是NSCLC的一个有前途的治疗策略.

研究的目的:

审查EGFR Ex20ins抑制剂的临床研究.
总结一下与EGFR Ex20ins抑制剂相关的近期专利 (2019-2024年).
提供关于针对EGFR Ex20ins突变的当前景观和未来方向的概述.

主要方法:

对EGFR Ex20ins抑制剂的临床研究的文献综述.
使用Espacenet和CAS SciFinder数据库进行专利景观分析 (2019年1月 - 2024年4月).

主要成果:

越来越多的EGFR Ex20ins抑制剂正在开发中.
目前的战略重点是通过优化抑制剂和新型分子来提高疗效和克服耐药性.
新兴的方法包括向蛋白质降解剂,全抑制剂和组合疗法.

结论:

尽管取得了进展,但在向EGFR Ex20ins突变方面,诸如绕道耐药性,选择性和药物敏感性等挑战仍然存在.
对于抑制剂设计和治疗策略的持续创新至关重要.
应对这些挑战将改善EGFR Ex20ins突变的NSCLC患者的治疗结果.

关键词:

欧洲农业基金 Ex20insins 在NSCLCLC中,我们可以看到NSCLCLC.临床耐药性临床耐药性选择性的选择性小分子抑制剂小分子抑制剂

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