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ABK3376 is a next-generation, highly selective, brain-penetrant **epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor** designed to target **EGFR C797S mutations** in non-small cell lung cancer (NSCLC) after resistance develops to third-generation EGFR-TKIs. It demonstrates potent and balanced inhibitory activity against EGFR L858R + C797S and Del19 + C797S mutations, while displaying high selectivity for mutant over wild-type EGFR, suggesting safer clinical use. ABK3376 efficiently penetrates the blood-brain barrier, achieving effective CNS drug exposure and holds promise for treating or preventing CNS metastasis in NSCLC. It is being developed for use as a monotherapy and in combination with third-generation EGFR inhibitors like furmonertinib. The drug is currently in phase I clinical trials for locally advanced or metastatic NSCLC[1][3][5][6][8].
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