lazertinib mesylate hydrate

The hydrated mesylate salt form of lazertinib, an orally available third-generation, selective inhibitor of certain forms of the epidermal growth factor receptor (EGFR) with activating mutations, including the resistance mutation T790M, exon 19 deletions (Del19), and the L858R mutation, with potential antineoplastic activity. Upon oral administration, lazertinib specifically and irreversibly binds to and inhibits selective EGFR mutants, specifically EGFR exon 19 deletions and exon 21 L858R substitution mutations. This prevents EGFR mutant-mediated signaling and leads to cell death in EGFR mutant-expressing tumor cells. In addition, lazertinib penetrates the blood-brain barrier (BBB). As this agent shows minimal activity against wild-type EGFR (wtEGFR), systemic toxicity is minimal as compared to non-selective EGFR inhibitors. EGFR, a receptor tyrosine kinase (RTK) mutated in many tumor cell types, plays a key role in tumor cell proliferation and tumor vascularization.