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新型多靶点酪氨酸激酶抑制剂苏尼替尼的研究进展 被引量:1

Sunitinib: a novel multitargeted receptor tyrosine kinase inhibitor
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摘要 苏尼替尼是一种新型的多靶点酪氨酸激酶抑制剂。临床前研究及临床研究证实该药对多种实体肿瘤有明显的抗肿瘤活性,包括肾细胞癌、胃肠道间质瘤、神经内分泌肿瘤、肉瘤、甲状腺癌、黑色素瘤、乳腺癌、结直肠癌和非小细胞肺癌,尤其是对晚期肾细胞癌和伊马替尼耐受的胃肠道间质瘤的治疗取得显著的疗效。药物不良反应主要为轻度的乏力、恶心和血小板减少。现就该药近年来的研究进展作一简要的介绍。 Sunitinb is a novel multitargeted receptor tyrosine kinase inhibitor. The preclinical and clinic trials have demonstrated that sunitinib owns potent antitumor effects in many solid tumors, including renal cell carcinoma, gastrointestinal stromal tumour, neuroendocrine tumor, sarcoma, carcinoma of thyroid, melanoma, breast carcinoma, colorectal cancer and nonsmall-cell lung cancer, especially in the therapy of advanced renal cell carcinoma and imatinib resistant gastrointestinal stromal tumour. The main adverse reactions include hypodynamia, nausea and thrombocytopenia. This paper reviews R&D progresses of sunitinib.
出处 《中国新药杂志》 CAS CSCD 北大核心 2007年第1期91-94,共4页 Chinese Journal of New Drugs
关键词 苏尼替尼 酪氨酸激酶抑制剂 肾细胞癌 胃肠道间质瘤 sunitinib tyrosine kinase inhibitor renal cell carcinoma gastrointestinal stromal tumour
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  • 1LI S,CHRIS L,SHERI S,et al.Discovery of 5-[5-fluoro-2-oxo1,2-dihydroindol-(3Z) -ylidenemethyl] -2,4-dimethyl-1 H-pyrrole-3-carboxylic acid (2-diethylaminoethyl) amide,a novel tyrosine kinase inhibitor targeting vascular endothelial and platelet-derived growth factor receptor tyrosine kinase[J].J Med Chem,2003,46(7):1116-1119.
  • 2MEDNEL DB,LAIRD AD,SMOLICH RD,et al.Development of SU5416,a selective small molecule inhibitor of VEGF receptor tyrosine kinase activity,as an antiangiogenesis agent[J].Anticancer Drug Des,2000,15(1):29 -41.
  • 3LAIRD AD,VAJKECZY P,SHAWVER LK,et al.SU6668 is a potent antiangiogenic and antitumor agent that induces regression of established tumors[J].Cancer Res,2000,60(15):4152-4160.
  • 4LAIRD AD,CHRISTENSEN JG,LI G,et al.SU6668 inhibitsFlk-1/KDR and PDGFRbeta in vivo,resulting in rapid apoptosis of tumor vasculature and tumor regression in mice[J].FASEB J,2002,16 (7):681-690.
  • 5POFAPOVA O,LAIRD A,NANNINI M,et al.Mechanism of action and biomarker studies of SU11248,a selective inhibitor of split kinase domain receptor tyrosine kinases (including VEGF receptors,PDGF receptors,c-Kit,and Flt3)[J].Eur J Cancer,2002,38(Suppl):S61.
  • 6O'FARREL AM,ABRAMS TJ,YUEN HA,et al.SU11248 is a novel FLT3 tyrosine kinase inhibitor with potent activity in vitro and in vivo[J].Blood,2003,101 (9):3597 -3605.
  • 7ABRAMS TJ,LEE LB,MURRAY LJ,et al.SU11248 inhibits kit and platelet-derived growth factor receptorβ in preclinical models of human small cell lung cancer[J].Mol Cancer Ther,2003,2(5):471 -478.
  • 8FAIVRE S,DELBALDO C,VERA K,et al.Safety,pharmacokinetic,and antitumor activity of SU11248,a novel oral multitarget tyrosine kinase inhibitor,in patients with cancer[J].J Clin Oncol,2006,24(1):25 -35.
  • 9Pfizer.Sutent Prescribing Information[EB/OL].[2006-08 -26].http://www.fda.gov/cder/foi/label/2006/021968lbl.pdf.
  • 10MENDEL DB,LAIRD AD,XIN XH,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/pharmaeodynamic relationship[J].Clin Cancer Res,2003,9 (1):327-337.

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