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Rezivertinib is an orally available, third-generation, highly selective and irreversible epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI). It is designed to target EGFR activating mutations, including the resistance mutations T790M and L858R as well as exon 19 deletion. Rezivertinib covalently binds to mutant EGFR at the active site, inhibiting its signaling and leading to cell death in tumor cells harboring these mutations. The drug demonstrates high selectivity for mutant EGFR with minimal activity against wild-type EGFR, reducing dose-limiting toxicities associated with non-selective inhibitors. Rezivertinib has shown efficacy in patients with locally advanced or metastatic non-small cell lung cancer (NSCLC) who have progressed after prior EGFR TKI therapy and have confirmed T790M mutation. Developed by Beta Pharma (Shanghai), it provides a new treatment option for NSCLC patients with acquired resistance to earlier generation TKIs[1][2][3][4][5][6].
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