Enozertinib Is a Selective, Brain-Penetrant EGFR Inhibitor for Treating Non–Small Cell Lung Cancers with EGFR Exon 20 and Atypical Mutations

Preclinical and initial phase I clinical data demonstrate the potency, kinome selectivity, efficacy, and brain penetration of enozertinib in NSCLC with EGFR exon 20 insertions and atypical mutations, warranting further clinical development.