Abstract: Abstract　Sunitinib malate is one of the multi-targeted tyrosine kinase inhibitors in clinical use. It inhibits the tyrosine kinase of over 80 receptors, including the receptors of epidermal growth factor, platelet-derived growth factor, and vascular endothelial growth factor. Since 2006, it has been successfully administered to treat advanced renal cell carcinoma and imatinib-resistant or intolerant gastrointestinal stromal tumors. In addition, the mutation and overexpression of tyrosine kinase receptors are related to the oncogenesis and progression of several tumors, including lung cancer. Therefore, authors have used sunitinib to treat non-small cell lung cancer (NSCLC) using sunitinib-only regimens, continuous daily doses, or combination chemotherapy (with docetaxel or gemcitabine plus cisplatin), with a definite curative effect in NSCLC clinical trials. Trials involving combined therapy using sunitinib with gemcitabine and cisplatin for advanced NSCLC have shown that the maximum tolerated dose is as follows: intermittent oral sunitinib 37.5 mg/d once a day, (Schedule 2/1, i.e., 1 week withdrawal after a 2-week administration) with intravenous infusions of gemcitabine (1,000 mg/m2 on days 1 and 8) and cisplatin (80 mg/m2 on day 1), administered in 3-week cycles. Up to 66.7% of the patients were confirmed to achieve partial response. The adverse side effects of sunitinib that occurred during the clinical trials were generally tolerated in most of the patients, including fatigue/asthenia, pain/myalgia, nausea/vomiting, stomatitis/mucosal inflammation, and hypertension, which were mild to moderate in severity (grades 1 to 2). This suggests that sunitinib may play a more important role in the treatment of NSCLC. However, few results are currently available from related studies. Therefore, more findings from studies on sunitinib are expected, such as the various curative effects of sunitinib in different histology types and genetic mutations of NSCLC.