Advances in research of acquired drug-resistance of gefitinib in non-small cell lung cancer

Gefitinib, a tyrosine kinase inhibitor (TKI) of epidermal growth factor receptor (EGFR), is presently used to treat the patients previously undergoing platinum-based chemotherapy for advanced non-small cell lung cancer (NSCLC). However, acquired resistance to EGFR-targeting drugs has become a significant problem. Currently, the theory of secondary mutation of EGFR gene was widely accepted in this area. Meanwhile, some studies have shown that gefitinib resistance was related to drug transport, EGFR/Met gene amplification and the changes in signaling pathway, which indicates that this theory can not completely explain the mechanism of acquired drug-resistance. This review will summarize the mechanism of gefitinib resistance, and address the new strategies to overcome this acquired drug-resistance. DOI:10.3781/j.issn.1000-7431.2011.05.016