Chao Gao , Wanning Wang , Tong Liu , Xingyu Li , Yongbo Yu , Jianhui Wu
{"title":"Annual review of EGFR inhibitors in 2024","authors":"Chao Gao , Wanning Wang , Tong Liu , Xingyu Li , Yongbo Yu , Jianhui Wu","doi":"10.1016/j.ejmech.2025.117677","DOIUrl":null,"url":null,"abstract":"<div><div>Epidermal growth factor receptor (EGFR) inhibitors play a crucial role in the treatment of EGFR mutation-driven cancers, such as non-small cell lung cancer (NSCLC). In 2024, significant breakthroughs were made in new drug development, resistance mechanisms, and combination therapy strategies. This review summarizes the key studies published in 2024, with a focus on the design strategies, structure-activity relationships (SAR), mechanisms of action, and both in vitro and in vivo activities of EGFR inhibitors. The aim is to provide new research perspectives and theoretical foundations for developing highly effective and selective inhibitors targeting diverse EGFR mutations.</div></div>","PeriodicalId":314,"journal":{"name":"European Journal of Medicinal Chemistry","volume":"292 ","pages":"Article 117677"},"PeriodicalIF":6.0000,"publicationDate":"2025-04-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"European Journal of Medicinal Chemistry","FirstCategoryId":"3","ListUrlMain":"https://www.sciencedirect.com/science/article/pii/S0223523425004428","RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q1","JCRName":"CHEMISTRY, MEDICINAL","Score":null,"Total":0}
引用次数: 0
Abstract
Epidermal growth factor receptor (EGFR) inhibitors play a crucial role in the treatment of EGFR mutation-driven cancers, such as non-small cell lung cancer (NSCLC). In 2024, significant breakthroughs were made in new drug development, resistance mechanisms, and combination therapy strategies. This review summarizes the key studies published in 2024, with a focus on the design strategies, structure-activity relationships (SAR), mechanisms of action, and both in vitro and in vivo activities of EGFR inhibitors. The aim is to provide new research perspectives and theoretical foundations for developing highly effective and selective inhibitors targeting diverse EGFR mutations.
期刊介绍:
The European Journal of Medicinal Chemistry is a global journal that publishes studies on all aspects of medicinal chemistry. It provides a medium for publication of original papers and also welcomes critical review papers.
A typical paper would report on the organic synthesis, characterization and pharmacological evaluation of compounds. Other topics of interest are drug design, QSAR, molecular modeling, drug-receptor interactions, molecular aspects of drug metabolism, prodrug synthesis and drug targeting. The journal expects manuscripts to present the rational for a study, provide insight into the design of compounds or understanding of mechanism, or clarify the targets.