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SY11-1 is an investigational, fourth-generation tyrosine kinase inhibitor (TKI) targeting the epidermal growth factor receptor (EGFR). Developed by Shouyao Holdings, it is specifically engineered to overcome resistance mutations that emerge following treatment with third-generation EGFR TKIs like osimertinib, most notably the EGFR C797S mutation. SY11-1 exhibits potent activity against triple-mutant EGFR variants (e.g., Del19/T790M/C797S and L858R/T790M/C797S) while maintaining high selectivity over wild-type EGFR to minimize off-target toxicities. It is primarily being evaluated for the treatment of advanced non-small cell lung cancer (NSCLC) in patients who have progressed on prior EGFR-targeted therapies.
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