Following the improved understanding of the biology and pathogenesis of renal cell carcinoma (RCC), small molecule tyrosine kinase inhibitors have been introduced to target the specific pathways involved in this disease. Sunitinib maleate is an oral, highly potent, multitarget tyrosine kinase inhibitor that exhibits direct antitumor and antiangiogenic activity. Sunitinib can produce durable responses and significant tumor shrinkage in patients with RCC. In a large phase III trial conducted in treatment-naïve patients with good- and intermediate-risk metastatic RCC, sunitinib significantly improved progression-free survival, overall response rate, and health-related quality of life compared to interferon-alpha, with a trend toward improved overall survival. Following these results, sunitinib is now considered the standard first-line treatment for patients with favorable-prognosis metastatic RCC. The exact role of sunitinib in sequential treatment and its combination with other novel agents will become clearer as ongoing clinical trials and clinical experience mature.This article summarizes all the relevant results recently obtained with sunitinib in clinical trials for patients with RCC.