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Berotinib (PLB1004) is an orally bioavailable, third-generation epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI) developed by Avistone Biotechnology (Beijing Anshi Biotechnology). It is designed to irreversibly bind to and inhibit EGFR harboring sensitizing mutations (such as exon 19 deletions and L858R) as well as the T790M resistance mutation, while exhibiting selectivity over wild-type EGFR to minimize off-target toxicities. Berotinib is primarily being developed for the treatment of advanced non-small cell lung cancer (NSCLC). It is frequently studied in combination with vebreltinib (PLB1001), a c-Met inhibitor, to address dual EGFR mutation and MET amplification or overexpression, which is a common resistance mechanism to earlier-generation EGFR-TKI therapy.
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