EGFR Mutation and Resistance of Non–Small-Cell Lung Cancer to Gefitinib

摘要: Mutations of the epidermal growth factor receptor (EGFR) gene have been identified in specimens from patients with non-small-cell lung cancer who a response to anilinoquinazoline EGFR inhibitors. Despite dramatic responses such inhibitors, most ultimately relapse. The mechanism drug resistance is unknown. Here we report case patient EGFR-mutant, gefitinib-responsive, advanced had relapse after two years complete remission during treatment gefitinib. DNA sequence his tumor biopsy specimen at revealed presence second point mutation, resulting threonine-to-methionine amino acid change position 790 EGFR. Structural modeling and biochemical studies showed that this mutation led gefitinib resistance.