Lazertinib: a novel EGFR-TKI therapy for non-small cell lung cancer

Introduction: Non-small cell lung cancer (NSCLC) is the most prevalent form of lung cancer, accounting for 85% of cases worldwide. Despite advancements in treatment, many patients are diagnosed at advanced stages, and resistance to therapy, such as EGFR inhibitors, remains a significant challenge. Lazertinib, a third-generation epidermal growth factor receptor tyrosine kinase inhibitor (EGFR TKI) developed by Yuhan Corporation and Janssen Biotech, targets EGFR mutations, including T790M, which confer resistance to earlier-generation TKIs. Areas Covered: This review explores lazertinib’s development, mechanism of action, clinical efficacy, and safety profile. Preclinical studies demonstrated its superior selectivity for mutant EGFR and blood-brain barrier penetration compared to osimertinib. Clinical trials highlight its efficacy as monotherapy and in combination with amivantamab, showing improved progression-free survival and response duration in patients with advanced NSCLC. Expert Opinion: Lazertinib represents a promising advance in the treatment of EGFR-mutated NSCLC, particularly for patients with brain metastases or resistance to previous EGFR TKIs. However, emerging resistance mutations, such as C797S, underscore the need for continued innovation, including combination therapies and fourth-generation TKIs. Future research must address these challenges to optimize treatment outcomes for NSCLC patients.