Abstract: In recent years，medical molecular biology has being rapidly developed and a new era of antitumor treatment is coming with the novel concept for moleculartargeted strategies. Epidemal growth factor receptor tyrosine kinase inhibitors（EGFR-TKIs），such as gefitinib and erlotinib，have being widely used in clinic.However，the efficiency is limited because of the drug resistance or poor sensitivity in some populations with non-small cell lung cancer（NSCLC） during therapy. The review briefly summarizes the progress on mechanisms of EGFR-TKIs resistance and strategies currently being employed to overcome resistance.