Abstract： Recent progress in molecular biology has enabled us to better understand the molecular mechanism underlying pathogenesis of human malignancy including lung cancer, the advent of therapies based on mechanisms that target critical molecular pathways of tumors has evoked considerable interest. The therapeutic index is high, and optimally effective treatment can be achieved at a dose below the maximal tolerated dose,giving us a better understanding of the human lung cancer. This review focuses on the advance of targeted therapy for the first-line, second-line treatment or the maintenance treatment of non-small cell lung cancer.