Lazertinib: on the Way to Its Throne

다국어 초록 (Multilingual Abstract)

Lazertinib is an oral, irreversible, third-generation epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI) thatforms an irreversible covalent bond to the Cys797 residue in the ATP-binding site of the EGFR kinase domain and exhibits a highselectivity for sensitizing and T790M EGFR mutations. In January 2021, it was first approved for the treatment of advanced ormetastatic non-small cell lung cancer (NSCLC) patients with EGFR T790M who had previously received EGFR TKI therapy basedon LASER201, a phase I/II trial. At a recommended dose of 240 mg, lazertinib achieved an encouraging anti-tumor activity in bothextra- and intracranial lesions. With a high half-maximal inhibitory concentration for EGFR wildtype tumors, it is anticipated topose a lower risk of skin and cardiac adverse events compared to osimertinib. Lazertinib is currently being investigated as a mono-therapy in first-line treatment and in combination with amivantamab under various settings. In this review, we systematically sum-marize the preclinical and clinical data of lazertinib and discuss future perspectives on the treatment of EGFR-mutant NSCLC.

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