Review

Nature Reviews Drug Discovery 6, 734-745 (September 2007) | doi:10.1038/nrd2380

Article series: Case Histories

Case historyMolecular basis for sunitinib efficacy and future clinical development

Sandrine Faivre1, George Demetri2, William Sargent3 & Eric Raymond1  About the authors

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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.

Author affiliations

  1. 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.
  2. Dana-Farber Cancer Institute, Center for Sarcoma and Bone Oncology, Ludwig Center at Dana-Farber/Harvard, 44 Binney Street, Shields-Warren G530, Boston, Massachusetts 02115, USA.
  3. Pfizer Inc., 235 East 42nd Street, New York 10017, USA.

Correspondence to: Eric Raymond1 Email: eric.raymond@bjn.aphp.fr

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