Benefits from pharmacological and pharmacokinetic properties of sunitinib for clinical development.

Importance Of The Field: In the last 10 years, oncology has been greatly modified by the introduction of new drugs especially designed for molecular targets. Sunitinib belongs to the category of new drugs that inhibit multityrosine kinase receptors involved in the key steps of tumorigenesis and angiogenesis.

Areas Covered In This Review: This article reviews the pharmacological and clinical aspects of sunitinib. Literature search was conducted in PubMed, and articles selected for relevance to pharmacology or clinical efficacy up to March 2010.

What The Reader Will Gain: Pharmacology of sunitinib, data regarding clinical efficacy, and challenges to overcome resistance and improve outcomes of patients.

Take Home Message: Sunitinib is an oral small molecule that displays mainly antiangiogenic properties and also direct antitumoral effects. Being well tolerated, this small molecule is now an essential treatment of advanced renal cell carcinoma and gastrointestinal stromal tumors refractory or intolerant to imatinib, two localizations associated with a poor prognosis. Future developments include the extension of the indications of sunitinib in pancreatic neuroendocrine tumors, the evaluation of combinations with conventional cytotoxic and other targeted drugs and the development of strategy to overcome resistance to sunitinib.