阿柏西普（AVE0005）：一种通过血管内皮生长因子抑制肿瘤血管生成的替代策略。
Aflibercept (AVE0005): an alternative strategy for inhibiting tumour angiogenesis by vascular endothelial growth factors.
作者信息
Chu Quincy Siu-Chung
机构信息
University of Alberta, Cross Cancer Institute, Department of Medical Oncology, 11560 University Avenue, Edmonton, Alberta, T6G 1Z2 Canada.
出版信息
Expert Opin Biol Ther. 2009 Feb;9(2):263-71. doi: 10.1517/14712590802666397.
BACKGROUND
Aberrant angiogenesis is a landmark feature in cancer, which is important for proliferation, growth and metastasis, and is mediated by various pro-angiogenic factors. The VEGF pathway is one of the most important and best-studied angiogenic pathways. Inhibition of this pathway may provide clinical benefits to cancer patients.
OBJECTIVES
Strategies to inhibit the VEGF pathway, including antibodies to VEGF, antibodies to the extracellular domain of VEGFR-1 or VEGFR-2, decoy receptors for VEGF and tyrosine kinase inhibitors of VEGFRs, are summarized.
METHODS
This review outlines and compares the latest development of these strategies, with emphasis on aflibercept, a novel decoy fusion protein of domain 2 of VEGFR-1 and domain 3 of VEGFR-2 with the Fc fragment of IgG1.
RESULTS
Aflibercept was shown to have early clinical activity. Multiple studies are ongoing to determine the clinical benefits of aflibercept in cancer patients.
背景
异常血管生成是癌症的一个标志性特征，对肿瘤的增殖、生长和转移至关重要，且由多种促血管生成因子介导。VEGF通路是最重要且研究最深入的血管生成通路之一。抑制该通路可能为癌症患者带来临床益处。
目的
总结抑制VEGF通路的策略，包括抗VEGF抗体、抗VEGFR-1或VEGFR-2细胞外结构域抗体、VEGF诱饵受体以及VEGFRs酪氨酸激酶抑制剂。
方法
本综述概述并比较了这些策略的最新进展，重点介绍了阿柏西普，一种由VEGFR-1的第2结构域、VEGFR-2的第3结构域与IgG1的Fc片段组成的新型诱饵融合蛋白。
结果
阿柏西普已显示出早期临床活性。多项研究正在进行，以确定阿柏西普对癌症患者的临床益处。
Zotero 插件