Lazertinib

Description：Lazertinib is a 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 administration,   lazertinib specifically and irreversibly binds to and inhibits selective EGFR   mutants, which prevents EGFR mutant-mediated signaling and leads to cell   death in EGFR mutant-expressing tumor cells. Lazertinib may inhibit   programmed cell death-1 ligand 1 (PD-L1) and inflammatory cytokines in   specific cancer cells harboring certain EGFR mutations. Compared to some   other EGFR inhibitors, lazertinib may have therapeutic benefits in tumors   with T790M- or L858R-mediated drug resistance. In addition, lazertinib   penetrates the blood-brain barrier (BBB). This agent shows minimal activity   against wild-type EGFR (wtEGFR), and does not cause dose-limiting toxicities,   which occur during the use of non-selective EGFR inhibitors and inhibit   wtEGFR. EGFR, a receptor tyrosine kinase (RTK) mutated in many tumor cell   types, plays a key role in tumor cell proliferation and tumor vascularization.

Clinical Trial：Phase 1|Phase 2

Target：EGFR