"目录号: HY-14571
Cytoskeleton-
E7820 是一种血管生成抑制剂，能够抑制整合素蛋白 a2 (integrin a2) 的活性，整合素蛋白 a2 是内皮细胞中的细胞粘附分子。
Integrin
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生物活性
Description
E7820 is an angiogenesis inhibitor by suppressingintegrin a2, a cell adhesion molecule expressed on endothelial cells.
In Vitro
E7820 treatment inhibits proliferation of HUVEC induced by either bFGF and VEGF in serum-free medium with IC50values of 0.10 and 0.081 μg/mL, respectively. E7820 also inhibits both bFGF- and VEGF-driven tube formation of HUVEC in this assay. The IC50values are 0.20 and 0.24 μg/mL, respectively[3].
In Vivo
E7820 (50 mg/kg) with erlotinib has a significantly synergistic antitumor effect in three xenograft models without severe body weight loss. E7820 (50 mg/kg) and erlotinib decrease MVD and enhance apoptosis in tumor-associated endothelial cells, inhibit tumor cell proliferation and enhanced apoptosis, and enhance inhibition of cell proliferation and apoptosis through activation of both intrinsic and extrinsic apoptosis pathways in human NSCLC xenograft models[1]. E7820 shows anti-tumor activity at doses of 50, 100, and 200 mg/kg in the tumor growth and α2-integrin expression experiments[2]. E7820 (50, 100, and 200 mg/kg) inhibits tumor growth in a dose-dependent manner in all s.c. xenograft models. E7820 completely inhibits s.c. tumor growth of LoVo tumor cells and also regresses the tumor mass of KP-1 tumor cells at the dosages of both 100 and 200 mg/kg[3].
Clinical Trial
NCT00309179
Eisai Inc.
Advanced Colorectal Cancer
September 2007
Phase 2
NCT01773421
Eisai Inc.
Advanced Solid Tumors
July 8, 2011
Phase 1
NCT00078637
Eisai Inc.
Neoplasms-Lymphoma, Malignant
January 2004
Phase 1
NCT01347645
Eisai Inc.-PharmaBio Development Inc.
Colon Cancer-Rectal Cancer
October 2011
Phase 1-Phase 2
NCT01133990
Eisai Inc.-PharmaBio Development Inc.
Colorectal Cancer
April 2010
Phase 1-Phase 2
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References
[1].Ito K, et al. Enhanced anti-angiogenic effect of E7820 in combination with erlotinib in epidermal growth factor receptor-tyrosine kinase inhibitor-resistant non-small-cell lung cancer xenograft models. Cancer Sci. 2014 Aug;105(8):1023-31.
[2].Keizer RJ, et al. Evaluation of α2-integrin expression as a biomarker for tumor growth inhibition for the investigational integrin inhibitor E7820 in preclinical and clinical studies. AAPS J. 2011 Jun;13(2):230-9.
[3].Semba T, et al. An angiogenesis inhibitor E7820 shows broad-spectrum tumor growth inhibition in a xenograft model: possible value of integrin alpha2 on platelets as a biological marker. Clin Cancer Res. 2004 Feb 15;10(4):1430-8.