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recombinant human endostatin (National Cancer Institute)
- Development stage
- Unknown
- Lead developer
- Simcere Pharmaceutical Group
- Modality
- Recombinant Proteins and Enzymes
- Administration
- Intravenous
01
Overview
Recombinant human endostatin (rh-endostatin) is a biologic anti-angiogenic agent derived from a 20-kDa C-terminal fragment of collagen XVIII. It functions as an endogenous inhibitor of angiogenesis by interfering with the proliferation and migration of endothelial cells. Specifically, it blocks vascular endothelial growth factor (VEGF) from binding to its receptors on endothelial cells and inhibits the formation of new blood vessels (tube formation). The National Cancer Institute (NCI) evaluated this specific recombinant form, which includes a histidine-tag for purification and is expressed in Escherichia coli, in Phase I clinical trials for patients with advanced solid tumors. While a modified version (Endostar) is approved in China, the NCI-sponsored version was primarily investigated for its safety and surrogate markers of activity in the United States.
- Other names
- recombinant human endostatinendostatin
02
Targets
ITGA5:ITGB1 (Integrin α5β1)CAV1 (Caveolin-1)HS (Heparan sulfate)VEGFR2 (Vascular endothelial growth factor receptor 2)αVβ3 (Integrin αVβ3)VEGFR-1 (Vascular endothelial growth factor receptor 1)VEGFR3 (Vascular endothelial growth factor receptor 3)αVβ5 (Integrin αVβ5)
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