Secondary resistance of gefitinib in non-small-cell lung cancer treatment / 国际肿瘤学杂志

ABSTRACT

Gefitinib (iressa),an epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor,has antitumor activity in non-small-cell lung cancer (NSCLC).Despite the dramatic response to this inhibitor,most patients nevertheless ultimately have relapses because of the secondary resistance.In human lung adenocar-cinomas with EGFR mutation,a second-site point mutation that substitutes methionine for threonine at position 790(T790M) is associated with approximately half of cases of secondary resistance to gefitinib.Other mecha-nisras that contribute to gefitinib resistance include EGFR receptor internalization and MET gene amplification.