betatinib

Betatinib (ES-072) is an orally bioavailable, third-generation, irreversible tyrosine kinase inhibitor (TKI) of the epidermal growth factor receptor (EGFR), developed by Essence Pharmaceutical Group. It is specifically engineered to target EGFR-sensitizing mutations, such as L858R and exon 19 deletions, as well as the T790M resistance mutation, which frequently arises in patients treated with first- or second-generation EGFR TKIs. By covalently binding to the ATP-binding site of the mutated EGFR kinase domain, betatinib inhibits downstream signaling pathways that drive tumor cell growth and survival. Notably, it exhibits high selectivity for mutated EGFR over the wild-type form, potentially reducing the incidence of off-target toxicities like skin rash and diarrhea. Betatinib is primarily under clinical investigation for the treatment of advanced or metastatic non-small cell lung cancer (NSCLC).