lazertinib

Lazertinib is an oral, third-generation, irreversible epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI) used primarily in combination with amivantamab for the treatment of non-small cell lung cancer (NSCLC) that harbors specific EGFR mutations. It selectively inhibits both primary activating EGFR mutations (such as Exon 19 deletion and Exon 21 L858R substitution) and the T790M resistance mutation, while showing less activity against wild-type EGFR. Lazertinib works by irreversibly binding to the Cys797 residue in the ATP-binding site of mutant EGFR, blocking downstream signaling pathways including phosphorylation of AKT and ERK, leading to apoptosis in cancer cells. It has demonstrated significant central nervous system penetration and efficacy against brain metastases. Lazertinib was first approved in South Korea in 2021 and received FDA approval in August 2024 for use with amivantamab as a first-line therapy for metastatic or unresectable NSCLC with abnormal EGFR genes[2][5][6][8].

Brand names

LazcluzeLeclaza

Other names

lazertinib mesylate hydrate