Preprint / Version 1

Osimertinib as a third-generation EGFR TKI in non-small cell lung cancer: selective targeting of T790M mutation and clinical advantages

##article.authors##

  • Siri Srivatsa
  • Lalita Limaye

DOI:

https://doi.org/10.58445/rars.2916

Keywords:

Epidermal Growth Factor Receptor (EGFR), Tyrosine Kinase Inhibitor (TKI), Non-Small Cell Lung Cancer (NSCLC), T790M mutation, Osimertinib

Abstract

Non-small cell lung cancer is the most common type of lung cancer, accounting for around 85% of all cases (Testa et al.). Osimertinib is a third-generation epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI) used to treat non-small cell lung cancer (NSCLC) that harbors EGFR mutations, such as the T790M mutation. T790M mutation, which is the substitution of threonine with methionine at amino acid position 790 in the EGFR protein due to a mutation in exon 20, is the most common mechanism that resists first- or second-generation TKI drugs. Approximately 50%-60% of patients receiving early-generation TKIs develop resistance (Fu et al.). Preclinical studies have shown that Osimertinib may be a favorable treatment option for patients who have developed resistance to first- or second-generation TKI drugs. This paper reviews the action and clinical advantages of third-generation TKI Osimertinib. 

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Posted

2025-08-17