Drug intelligence / Profile preview

recombinant human endostatin

Development stage
Phase 4
Lead developer
Simcere Pharmaceutical Group
Modality
Recombinant Proteins and Enzymes
Administration
Intravenous, Intratumoral, Intravitreal, Intrapleural
01

Overview

Recombinant human endostatin is a genetically engineered form of the endogenous protein endostatin, which is a 20 kDa C-terminal fragment derived from type XVIII collagen. It functions as a broad-spectrum angiogenesis inhibitor by inducing apoptosis in microvascular endothelial cells and inhibiting their proliferation and migration. The primary mechanism involves inhibition of vascular endothelial growth factor (VEGF) signaling, particularly through VEGF receptor 2 (KDR/Flk1), leading to reduced tumor neovascularization and growth. Additional mechanisms include blocking activation of extracellular signal-regulated kinases (ERK), p38 mitogen activated protein kinase (MAPK), focal adhesion kinase, E-selectin activity, and matrix metalloproteinases 2, 9, and 13. Recombinant human endostatin has been approved in China since 2006 for non-small cell lung cancer under the brand name Endostar and continues to be investigated for other malignancies[1][2][3][4][8].

Brand names
Endostar
Other names
endostatinrecombinant human endostatinantiangiogenic agentcollagen alpha-1(XVIII) chain fragment
02

Targets

αVβ1 (Integrin alpha-V beta-1)MMP2 (Matrix metalloproteinase-2)NCL (Nucleolin)ERKRK (Ribokinase)αVβ3 (Integrin αVβ3)ITGA5:ITGB1 (Integrin α5β1)VEGFR2 (Vascular endothelial growth factor receptor 2)ITGAV (Integrin αV)αVβ5 (Integrin αVβ5)

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