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Lazertinib: First Approval

2021/05/24 by Sohita Dhillon · 94 citations
Chemistry · Medicine · #Cancer #Cancer research #Epidermal growth factor receptor #Gefitinib #Internal medicine #Lung Cancer Research Studies #Lung Cancer Treatments and Mutations #Lung cancer #Medicine #Oncology #Pharmacology #Quinazolinone synthesis and applications #Receptor #T790M #Tyrosine kinase #Tyrosine-kinase inhibitor

paper · pdf · doi:10.1007/s40265-021-01533-x

published in Drugs 81(9), 1107-1113 (Adis, Springer Healthcare)

openalex publication_date 2021/05/24 · openalex created_date 2025/10/10 · openalex updated_date 2026/07/31

Abstract

) is an oral, third-generation, epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI) being developed by Yuhan and Janssen Biotech for the treatment of non-small cell lung cancer (NSCLC). It is a brain-penetrant, irreversible EGFR-TKI that targets the T790M mutation and activating EGFR mutations Ex19del and L858R, while sparing wild type-EGFR. In January 2021, lazertinib received its first approval for the treatment of patients with EGFR T790M mutation-positive locally advanced or metastatic NSCLC who have previously received EGFR-TKI therapy. This article summarizes the milestones in the development of lazertinib leading to this first approval.

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