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Befotertinib is an orally available, third-generation small molecule inhibitor of the epidermal growth factor receptor (EGFR) tyrosine kinase, specifically targeting mutant forms such as T790M. It is structurally derived from osimertinib with a trifluoromethyl group substitution for improved stability and reduced gastrointestinal side effects. Befotertinib has demonstrated superior efficacy compared to icotinib in first-line treatment of EGFR mutation-positive non-small cell lung cancer (NSCLC), including patients with rare EGFR mutations such as p.G719X/p.S768I. The drug is approved in China for locally advanced or metastatic NSCLC and shows particular promise in patients with central nervous system metastases.
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