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Review
. 2023 Feb 20;26(2):135-147.
doi: 10.3779/j.issn.1009-3419.2023.102.06.

[Progress in Detection of EGFR Exon 20 Insertion Mutation and Targeted Therapies in Non-small Cell Lung Cancer]

[Article in Chinese]
Yulu Wang  1 , Tianqing Chu  2
Affiliations
Review

[Progress in Detection of EGFR Exon 20 Insertion Mutation and Targeted Therapies in Non-small Cell Lung Cancer]

[Article in Chinese]
Yulu Wang et al. Zhongguo Fei Ai Za Zhi. .

Abstract
in English, Chinese

Epidermal growth factor receptor exon 20 insertion (EGFR ex20ins) is one of the earliest driver gene activation mutations in non-small cell lung cancer (NSCLC). However, due to the unique structure of protein variation caused by this mutation, most patients with EGFR ex20ins mutation (except A763_Y764insFQEA) have poor response to the launched first/second/third generation EGFR-tyrosine kinase inhibitors (EGFR-TKIs). With the successive approval of new specific targeted drugs for EGFR ex20ins in Food and Drug Administration (FDA) and other national regulatory agencies, the development and clinical research of targeted drugs for EGFR ex20ins in China have also developed rapidly and Mobocertinib has been approved recently in China. It is worth noting that EGFR ex20ins is a variant type with strong molecular heterogeneity. How to detect it comprehensively and accurately in clinical practice, so as to enable more patients to benefit from targeted therapy, is a very important and urgent problem to be solved. This review introduces the molecular typing of EGFR ex20ins, then discusses the importance of EGFR ex20ins detection and the differences of various detection methods, and summarizes the research and development of new drugs progress of EGFR ex20ins, in order to optimize the diagnosis and treatment path of EGFR ex20ins patients by selecting accurate, rapid and appropriate detection methods, so as to improve the clinical benefits of the patients. .

【中文题目：非小细胞肺癌EGFR外显子20插入突变检测和靶向药物研究进展】 【中文摘要：表皮生长因子受体外显子20插入（epidermal growth factor receptor exon 20 insertion, EGFR ex20ins）突变是最早被发现的非小细胞肺癌（non-small cell lung cancer, NSCLC）驱动基因激活突变之一。由于这种突变引起的蛋白变异的独特结构，大多数EGFR ex20ins突变（除A763_Y764insFQEA）患者对已上市的第一、二、三代EGFR酪氨酸激酶抑制剂（EGFR-tyrosine kinase inhibitors, EGFR-TKIs）治疗应答较差。随着针对EGFR ex20ins的新型靶向药物经美国食品药品监督管理局（Food and Drug Administration, FDA）及其他国家注册部门相继获批，国内针对EGFR ex20ins的靶向药物研发迅速发展，针对EGFR ex20ins的靶向药物莫博赛替尼也于近日在国内正式获批。EGFR ex20ins是一类分子异质性很强的变异类型，如何在临床实践中全面精准地检出，让越来越多的患者从靶向治疗中获益，是一个值得关注、亟需解答的问题。本文对EGFR ex20ins的分子分型、检测的重要性及不同检测方法的差异性进行介绍，并归纳了以EGFR ex20ins为靶向的新药研发进展，以期通过选择精准、快速、合适的检测方法，优化EGFR ex20ins患者的诊疗路径，从而改善患者的临床获益。 】 【中文关键词：表皮生长因子受体外显子20插入突变；检测方法；靶向治疗；肺肿瘤】.

Keywords: Detection method; Epidermal growth factor receptor ex20ins mutation; Lung neoplasms; Target therapy.

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Figures

Fig 1
图 1. EGFR ex20ins的分子结构和分子亚型（源自于蛋白质结构数据库PDB ID 1XKK）
See this image and copyright information in PMC

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