EGFR inhibitor 57 is a novel potent, selective, allosteric fourth-generation EGFR L858R inhibitor, overcomes EGFRC797S-mediated resistance in NSCLC harboring the activating EGFRL858R mutation.
EGFR inhibitor 57 is the first allosteric EGFR inhibitor that demonstrates robust tumor regression in a mutant EGFRL858R/C797S tumor model.
EGFR inhibitor 57 is active in an H1975 EGFRL858R/T790M NSCLC xenograft model and shows superior efficacy in combination with osimertinib compared to the single agents.
