PP01.11 Furmonertinib is an Oral, Irreversible, Highly Brain-Penetrant Pan-EGFR Inhibitor with Activity Against Classical and Atypical EGFR Mutations

Furmonertinib is an oral, highly brain-penetrant pan-EGFR mutant selective inhibitor that contains a trifluoroethoxypridine group, predicted to improve binding to the hydrophobic pocket within the EGFR kinase domain. A randomized Phase 3 frontline study in patients with classical EGFR mutations (exon 19 deletions [exon19del], L858R) demonstrated clinical superiority over gefitinib. Promising clinical activity was observed in patients with atypical EGFR mutations such as EGFR exon 20 insertions (exon20ins). Here we present the nonclinical data supporting broad activity across EGFR activating mutations (classical and atypical) and HER2 exon20ins, and antitumor activity in the CNS.