Abstract: Avastin is a recombinant humanized monoclonal IgG1 antibody that selectively binds to and neutralizes the biological activity of human vascular endothelial growth factor ( VEGF ). It is the first targeted agent to increase efficacy in first-line non-small cell lung cancer (NSCLC) and was approved by the U.S. Food and Drug Administration in October 2006 for use in combination with carboplatin and paclitaxel for the initial treatment of patients with NSCLC. An improvement in the objective response and a trend toward better disease-free survival and overall survival rate were observed after Avastin administration. Adverse effects, such as hypertension, proteinuria, thromboembolism, and hemorrhage, were not severe and could be well tolerated. Most patients experienced few adverse effects. The present article reviews the efficacy and safety of Avastin in patients with NSCLC.