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Annual review of EGFR inhibitors in 2024

Chao Gao, Wanning Wang, Tong Liu, Xingyu Li, Yongbo Yu, Jianhui Wu

2025European Journal of Medicinal Chemistry15 citationsDOIOpen Access PDF

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.

Topics & Concepts

Epidermal growth factor receptorEGFR inhibitorsIn vivoLung cancerChemistrySite of actionCancer researchPharmacologyComputational biologyReceptorMedicineOncologyBiologyInternal medicineBiochemistryGeneticsProtein Degradation and InhibitorsLung Cancer Treatments and MutationsCancer therapeutics and mechanisms
Annual review of EGFR inhibitors in 2024 | Litcius