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.
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Gao et al. (2025) studied this question.
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