Lazertinib: on the Way to Its Throne

Jiyun Lee, Min Hee Hong, Byoung Chul Cho

Research output: Contribution to journalReview articlepeer-review


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

Original languageEnglish
Pages (from-to)799-805
Number of pages7
JournalYonsei medical journal
Issue number9
Publication statusPublished - 2022 Sept 1

Bibliographical note

Funding Information:
Received: April 6, 2022 Revised: June 26, 2022 Accepted: July 29, 2022 Published online: August 18, 2022 Corresponding author: Byoung Chul Cho, MD, PhD, Lung Cancer Center, Division of Medical Oncology, Department of Internal Medicine, Yonsei Cancer Center, Yonsei University College of Medicine, 50-1 Yonsei-ro, Seodaemun-gu, Seoul 03722, Korea. Tel: 82-2-2228-0880, Fax: 82-2-2227-8070, E-mail: •Byoung Chul Cho reports grants from Novartis, Bayer, AstraZeneca, MOGAM Institute, Dong-A ST, Champions Oncology, Janssen, Yuhan, Ono, Dizal Pharma, MSD, AbbVie, Medpacto, GI Innovation, Eli Lilly, Blueprint Medicines, and Interpark Bio Convergence Corp.; personal fees from Novartis, AstraZeneca, Boehringer-Ingelheim, Roche, BMS, Ono, Yuhan, Pfizer, Eli Lilly, Janssen, Takeda, MSD, Med-pacto, Blueprint Medicines, TheraCanVac Inc, Gencurix Inc, Bridgebio Therapeutics, Kanaph Therapeutics Inc, Cyrus Therapeutics, Interpark Bio Convergence Corp., Guardant Health, Joseah BIO, and Champions Oncology; and other support from DAAN Biotherapeutics outside the submitted work. The remaining authors declare no conflicts of interest.

Publisher Copyright:
© 2022, Yonsei University College of Medicine.

All Science Journal Classification (ASJC) codes

  • Medicine(all)


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