生物活性

• 描述N-desethyl sunitinib is a major and pharmacologically active metabolite of sunitinib, which is potent, ATP-competitive VEGFR, PDGFRβ and KIT inhibitor (Ki values are 2, 9, 17, 8 and 4 nM for VEGFR -1, -2, -3, PDGFRβ and KIT respectively).
• 临床研究

• NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
  NCT00372775	Non-Small Cell Lung Cancer	Phase 2	Completed	-	United States, Connecticut ... more >> Pfizer Investigational Site Norwalk, Connecticut, United States, 06856 United States, Florida Pfizer Investigational Site Cocoa Beach, Florida, United States, 32931 Pfizer Investigational Site Merritt Island, Florida, United States, 32952 Pfizer Investigational Site Titusville, Florida, United States, 32796 United States, Missouri Pfizer Investigational Site Creve Coeur, Missouri, United States, 63141 Pfizer Investigational Site St. Louis, Missouri, United States, 63110-1094 Pfizer Investigational Site St. Louis, Missouri, United States, 63110 Pfizer Investigational Site St. Peters, Missouri, United States, 63376 United States, New Jersey Pfizer Investigational Site Basking Ridge, New Jersey, United States, 07920 United States, New York Pfizer Investigational Site Commack, New York, United States, 11725 Pfizer Investigational Site New York, New York, United States, 10022 United States, Pennsylvania Pfizer Investigational Site Sayre, Pennsylvania, United States, 18840 United States, Texas Pfizer Investigational Site Austin, Texas, United States, 78705 Pfizer Investigational Site Austin, Texas, United States, 78745 Pfizer Investigational Site Austin, Texas, United States, 78758 Pfizer Investigational Site Austin, Texas, United States, 78759 Pfizer Investigational Site Round Rock, Texas, United States, 78664 France Pfizer Investigational Site Pessac, Be1 04495, France, 33604 Pfizer Investigational Site Marseille Cedex 09, France, 13009 Pfizer Investigational Site Saint-Priest en Jarez Cedex, France, 42271 Pfizer Investigational Site Toulouse cedex 9, France, 31059 Italy Pfizer Investigational Site Bologna, Italy, 40139 Pfizer Investigational Site Genova, Italy, 16132 Pfizer Investigational Site Orbassano (TO), Italy, 10043 Pfizer Investigational Site Roma, Italy, 00151 Spain Pfizer Investigational Site Madrid, Spain, 28046 Pfizer Investigational Site Valencia, Spain, 46014 Collapse <<
  NCT00499473	Adult Anaplastic Astrocytoma ... more >> Adult Diffuse Astrocytoma Adult Giant Cell Glioblastoma Adult Glioblastoma Adult Gliosarcoma Adult Mixed Glioma Adult Oligodendroglioma Adult Pineal Gland Astrocytoma Collapse <<	Phase 2	Completed	-	United States, Ohio ... more >> Ohio State University Medical Center Columbus, Ohio, United States, 43210 Collapse <<
  NCT00372775	-	-	Completed	-	-

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• 参考文献

• [1] Sun L, Liang C, et al. Discovery of 5-[5-fluoro-2-oxo-1,2- dihydroindol-(3Z)-ylidenemethyl] -2,4-dimethyl-1H-pyrrole-3-carboxylic acid (2-diethylaminoethyl)amide, a novel tyrosine kinase inhibitor targeting vascular endothelial and platelet-derived growth factor receptor tyrosine kinase. J Med Chem. 2003 Mar 27;46(7):1116-9.

  [2] Mendel DB, Laird AD, et al. In vivo antitumor activity of SU11248, a novel tyrosine kinase inhibitor targeting vascular endothelial growth factor and platelet-derived growth factor receptors: determination of a pharmacokinetic/pharmacodynamic relationship. Clin Cancer Res. 2003 Jan;9(1):327-37.