An evaluation of aumolertinib for the treatment of EGFR T790M mutation-positive non-small cell lung cancer

Expert Opin Pharmacother. 2022 Apr;23(6):647-652. doi: 10.1080/14656566.2022.2050213. Epub 2022 Mar 10.

Abstract

Introduction: Epidermal growth factor receptor tyrosine kinase inhibitors (EGFR-TKIs) can significantly improve patient prognosis when used on patients with EGFR-mutant non-small cell lung cancer (NSCLC), but those patients often develop acquired resistance after 9-14 months of treatment. These resistance mechanisms are complex and diverse, with the EGFR T790M mutation being the most common. Aumolertinib is a new third-generation EGFR-TKI that is highly selective for EGFR-sensitizing mutations and EGFR T790M resistance mutation.

Areas covered: This review summarizes the mechanism of action, efficacy, and safety of aumolertinib for EGFR T790M mutation-positive NSCLC. The authors provide their expert opinions on the use of this drug, including its future prospects.

Expert opinion: Aumolertinib has shown good efficacy and safety for advanced EGFR T790M mutation-positive NSCLC patients who have progressed after EGFR-TKI treatment. It is expected to become a new treatment option, and to aid the establishment of new treatment standards. A phase III clinical study is currently underway to evaluate the suitability of aumolertinib as a first-line treatment. At present, more drug combinations and different applicable populations are being further explored. Future challenges include exploring mechanisms of aumolertinib resistance and determining its efficacy in European and American populations.

Keywords: EGFR T790M mutation; NSCLC; aumolertinib; targeted therapy.

Publication types

  • Review

MeSH terms

  • Acrylamides
  • Carcinoma, Non-Small-Cell Lung* / drug therapy
  • Carcinoma, Non-Small-Cell Lung* / genetics
  • Drug Resistance, Neoplasm / genetics
  • ErbB Receptors / genetics
  • Humans
  • Indoles
  • Lung Neoplasms* / drug therapy
  • Lung Neoplasms* / genetics
  • Mutation
  • Protein Kinase Inhibitors / pharmacology
  • Protein Kinase Inhibitors / therapeutic use
  • Pyrimidines

Substances

  • Acrylamides
  • Indoles
  • Protein Kinase Inhibitors
  • Pyrimidines
  • EGFR protein, human
  • ErbB Receptors
  • aumolertinib