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Lazertinib: on the Way to Its Throne

Authors
 Jiyun Lee  ;  Min Hee Hong  ;  Byoung Chul Cho 
Citation
 YONSEI MEDICAL JOURNAL, Vol.63(9) : 799-805, 2022-09 
Journal Title
YONSEI MEDICAL JOURNAL
ISSN
 0513-5796 
Issue Date
2022-09
MeSH
Antibodies, Bispecific ; Carcinoma, Non-Small-Cell Lung* ; ErbB Receptors ; Humans ; Lung Neoplasms* ; Morpholines ; Mutation ; Protein Kinase Inhibitors ; Pyrazoles ; Pyrimidines
Keywords
Lazertinib ; epidermal growth factor receptor ; non-small cell lung cancer ; targeted therapy
Abstract
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.
Files in This Item:
T202204389.pdf Download
DOI
10.3349/ymj.2022.63.9.799
Appears in Collections:
1. College of Medicine (의과대학) > Dept. of Internal Medicine (내과학교실) > 1. Journal Papers
Yonsei Authors
Cho, Byoung Chul(조병철) ORCID logo https://orcid.org/0000-0002-5562-270X
Hong, Min Hee(홍민희) ORCID logo https://orcid.org/0000-0003-3490-2195
URI
https://ir.ymlib.yonsei.ac.kr/handle/22282913/192114
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