Lazertinib: A Selective EGFR Mutant Inhibitor to Treat Non-Small Cell Lung Cancer

Abstract: One of the leading causes of death related to cancer worldwide is non-small cell lung cancer (NSCLC). Epidermal growth factor receptor (EGFR) mutations are one of the most important therapeutic targets. Lazertinib is an irreversible EGFR tyrosine kinase inhibitor (TKI) that is selectively active against EGFR mutations and the T790M resistance mutation, but not against wild-type EGFR. In this paper, we have evaluated the significant role of lazertinib in the treatment of NSCLC, compared with agents, such as osimertinib. We have analyzed the pharmacological benefits, clinical trial evidence, and interactions with the central nervous system (CNS), as well as its active role in first-line therapy beyond acquired resistance. The early-phase results are promising, but queries regarding resistance mechanisms and treatment protocols remain. We have conducted a detailed investigation of lazertinib’s therapeutic properties, its role in combination therapies, and its potential to improve treatment outcomes in EGFR-mutant NSCLC. We aimed to highlight both the opportunities and clinical uncertainties associated with lazertinib in cancer care.

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Publication Details

Journal
Anti-Cancer Agents in Medicinal Chemistry
Published
2026-07-23
DOI
https://doi.org/10.2174/0118715206446336251226053220
Primary Topic
Lung Cancer Treatments and Mutations
Type
article
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article

Lazertinib: A Selective EGFR Mutant Inhibitor to Treat Non-Small Cell Lung Cancer

Surya K. De, Hyma Mandapaka
Anti-Cancer Agents in Medicinal Chemistry
Lung Cancer Treatments and Mutations
article

Lazertinib: A Selective EGFR Mutant Inhibitor to Treat Non-Small Cell Lung Cancer

Surya K. De, Hyma Mandapaka
article en

Abstract

Abstract: One of the leading causes of death related to cancer worldwide is non-small cell lung cancer (NSCLC). Epidermal growth factor receptor (EGFR) mutations are one of the most important therapeutic targets. Lazertinib is an irreversible EGFR tyrosine kinase inhibitor (TKI) that is selectively active against EGFR mutations and the T790M resistance mutation, but not against wild-type EGFR. In this paper, we have evaluated the significant role of lazertinib in the treatment of NSCLC, compared with agents, such as osimertinib. We have analyzed the pharmacological benefits, clinical trial evidence, and interactions with the central nervous system (CNS), as well as its active role in first-line therapy beyond acquired resistance. The early-phase results are promising, but queries regarding resistance mechanisms and treatment protocols remain. We have conducted a detailed investigation of lazertinib’s therapeutic properties, its role in combination therapies, and its potential to improve treatment outcomes in EGFR-mutant NSCLC. We aimed to highlight both the opportunities and clinical uncertainties associated with lazertinib in cancer care.

Anti-Cancer Agents in Medicinal ChemistryVol. 26
Wichita State University (US)
Good health and well-being
Openalex Percentile: Top 9%
Lung Cancer Treatments and Mutations
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