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Nat Rev Drug Discov. 2007 Sep;6(9):734-45.

Molecular basis for sunitinib efficacy and future clinical development.

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Service Inter-Hospitalier de Cancérologie (SIHC) Beaujon-Bichat and RayLab, Hôpital Beaujon, APHP and Denis Diderot University, 100 Boulevard du Général Leclerc, 92118 Clichy Cedex, France.


Sunitinib malate (SU11248/Sutent; Pfizer) is a multitargeted tyrosine kinase inhibitor that has potent anti-angiogenic and antitumour activities. Definitive efficacy has been demonstrated in advanced renal cell carcinoma and in gastrointestinal stromal tumours that are refractory or intolerant to imatinib (Gleevec; Novartis), which has provided the basis for the recent regulatory approvals for these indications. This article summarizes the discovery and development of sunitinib, and discusses key issues for the multitargeted approach in cancer treatment, such as markers of response and development of resistance, and their significance for the future development of sunitinib and other multikinase inhibitors.

[Indexed for MEDLINE]

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