Faivre Sandrine, Demetri George, Sargent William, Raymond Eric
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.
Nat Rev Drug Discov. 2007 Sep;6(9):734-45. doi: 10.1038/nrd2380.
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.
苹果酸舒尼替尼（SU11248/索坦；辉瑞公司）是一种多靶点酪氨酸激酶抑制剂，具有强大的抗血管生成和抗肿瘤活性。在晚期肾细胞癌以及对伊马替尼（格列卫；诺华公司）难治或不耐受的胃肠道间质瘤中已证实其确切疗效，这为近期这些适应症的监管批准提供了依据。本文总结了舒尼替尼的发现与研发过程，并讨论了癌症治疗中多靶点方法的关键问题，如反应标志物和耐药性的产生，以及它们对舒尼替尼和其他多激酶抑制剂未来发展的意义。
