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XL-184, a MET, VEGFR-2 and RET kinase inhibitor for the treatment of thyroid cancer, glioblastoma multiforme and NSCLC.XL-184,一种用于治疗甲状腺癌、多形性胶质母细胞瘤和非小细胞肺癌的MET、VEGFR-2和RET激酶抑制剂。
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本文引用的文献

1
Constitutive RET tyrosine kinase activation in hereditary medullary thyroid cancer: clinical opportunities.遗传性甲状腺髓样癌中组成性RET酪氨酸激酶激活:临床机遇
J Intern Med. 2009 Jul;266(1):114-25. doi: 10.1111/j.1365-2796.2009.02113.x.
2
Vandetanib (ZD6474), a dual inhibitor of vascular endothelial growth factor receptor (VEGFR) and epidermal growth factor receptor (EGFR) tyrosine kinases: current status and future directions.凡德他尼(ZD6474),一种血管内皮生长因子受体(VEGFR)和表皮生长因子受体(EGFR)酪氨酸激酶的双重抑制剂:现状与未来方向。
Oncologist. 2009 Apr;14(4):378-90. doi: 10.1634/theoncologist.2008-0261. Epub 2009 Apr 6.
3
Emerging therapeutic targets in non-small cell lung cancer.非小细胞肺癌中新兴的治疗靶点
Proc Am Thorac Soc. 2009 Apr 15;6(2):218-23. doi: 10.1513/pats.200808-099LC.
4
Angiogenesis in the treatment of non-small cell lung cancer.血管生成在非小细胞肺癌治疗中的应用
Proc Am Thorac Soc. 2009 Apr 15;6(2):206-17. doi: 10.1513/pats.200807-066LC.
5
Anti-VEGF therapies for malignant glioma: treatment effects and escape mechanisms.恶性胶质瘤的抗血管内皮生长因子(VEGF)治疗:治疗效果与逃逸机制
Expert Opin Ther Targets. 2009 Apr;13(4):455-68. doi: 10.1517/14728220902806444.
6
Suppression of Tie-1 in endothelial cells in vitro induces a change in the genome-wide expression profile reflecting an inflammatory function.体外抑制内皮细胞中的Tie-1会诱导全基因组表达谱发生变化,反映出一种炎症功能。
FEBS Lett. 2009 Mar 18;583(6):1023-8. doi: 10.1016/j.febslet.2009.02.027. Epub 2009 Feb 21.
7
Prognostic significance of c-Met expression in glioblastomas.c-Met表达在胶质母细胞瘤中的预后意义
Cancer. 2009 Jan 1;115(1):140-8. doi: 10.1002/cncr.23972.
8
Inhibitors of vascular endothelial growth factor in cancer.癌症中血管内皮生长因子的抑制剂
Cardiovasc Hematol Agents Med Chem. 2008 Oct;6(4):343-7. doi: 10.2174/187152508785909528.
9
Lung cancer.肺癌
N Engl J Med. 2008 Sep 25;359(13):1367-80. doi: 10.1056/NEJMra0802714.
10
Comprehensive genomic characterization defines human glioblastoma genes and core pathways.全面的基因组特征分析确定了人类胶质母细胞瘤的基因和核心通路。
Nature. 2008 Oct 23;455(7216):1061-8. doi: 10.1038/nature07385. Epub 2008 Sep 4.

XL-184,一种用于治疗甲状腺癌、多形性胶质母细胞瘤和非小细胞肺癌的MET、VEGFR-2和RET激酶抑制剂。

XL-184, a MET, VEGFR-2 and RET kinase inhibitor for the treatment of thyroid cancer, glioblastoma multiforme and NSCLC.

作者信息

Zhang Ying, Guessous Fadila, Kofman Alex, Schiff David, Abounader Roger

机构信息

University of Virginia, Department of Microbiology, PO Box 800168, Charlottesville, Virginia, 22903, USA.

出版信息

IDrugs. 2010 Feb;13(2):112-21.

PMID:20127563
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC3268517/
Abstract

XL-184 (BMS-907351), under development by Exelixis Inc and Bristol-Myers Squibb Co, is a pan-tyrosine kinase inhibitor for the potential oral treatment of medullary thyroid cancer, glioblastoma multiforme and NSCLC. The prinicipal targets of XL-184 are MET, VEGFR-2 and RET, but the drug is also reported to display inhibitory activity against KIT, FLT3 and TEK. Preclinical studies demonstrated that XL-184 potently inhibited multiple receptor tyrosine kinases in various cancer cell lines and animal xenograft models, and that the drug exhibited significant oral bioavailability and blood-brain barrier penetration. A phase I clinical trial in patients with advanced solid malignancies indicated that XL-184 accumulated dose-dependently in the plasma and had a long terminal half-life. A phase II trial in patients with progressive or recurrent glioblastoma revealed modest but promising median progression-free survival. Toxicity and side effects for the drug have generally been of low-to-moderate severity. At the time of publication, three additional trials of XL-184 were recruiting patients, including a phase I trial in combination with standard of care in patients with glioblastoma, a phase I/II trial in combination with erlotinib in patients with NSCLC, and a phase III trial in patients with medullary thyroid cancer.

摘要

XL-184(BMS-907351)由Exelixis公司和百时美施贵宝公司共同研发,是一种泛酪氨酸激酶抑制剂,有望用于口服治疗甲状腺髓样癌、多形性胶质母细胞瘤和非小细胞肺癌。XL-184的主要靶点是MET、VEGFR-2和RET,但据报道该药物对KIT、FLT3和TEK也有抑制活性。临床前研究表明,XL-184在多种癌细胞系和动物异种移植模型中能有效抑制多种受体酪氨酸激酶,且该药物具有显著的口服生物利用度和血脑屏障穿透性。一项针对晚期实体恶性肿瘤患者的I期临床试验表明,XL-184在血浆中呈剂量依赖性蓄积,且终末半衰期较长。一项针对进展性或复发性胶质母细胞瘤患者的II期试验显示,患者的中位无进展生存期虽不显著但前景乐观。该药物的毒性和副作用一般为低至中度严重程度。在撰写本文时,XL-184的另外三项试验正在招募患者,包括一项与胶质母细胞瘤患者的标准治疗联合使用的I期试验、一项与非小细胞肺癌患者的厄洛替尼联合使用的I/II期试验,以及一项针对甲状腺髓样癌患者的III期试验。