Abstract: Lung cancer is malignant tumor with the highest morbidity and mortality rates.Non-small cell lung cancer(NSCLC) occurs in over 85%of all lung cancer cases.Chemotherapy is the current primary treatment choice for recurrent and metastatic NSCLC. However, chemotherapy has reached a plateau in terms of short- and long-term response rates.Since the 1990s, intensified studies on molecular-targeted therapy have played an important role in NSCLC.At present, monoclonal antibodies(cetuximab) and small molecular tyrosine kinase inhibitors(erlotinib or gefitinib) for epidermal growth factor receptor(EGFR), inhibitors for vascular endothelial growth factor(VEGF), monoclonal antibody(bevacizumab), and ALK positive mutations(Crizotinib) comprise the first-line treatment regimen for NSCLC.The efficacy of small molecule tyrosine kinase inhibitors is unambiguously excellent in patients with EGFR mutations—better than that of first-line chemotherapy—achieving a response rate of 60%or higher and extending patients' progression-free survival to 10 months.Therefore, the present study introduces clinical studies of the above-mentioned drugs used as first-line targeted therapy for advanced NSCLC.