Drug intelligence / Profile preview

pegylated recombinant human endostatin

Development stage
Phase 2
Lead developer
Simcere Pharmaceutical Group
Modality
Recombinant Proteins and Enzymes, Biodegradable Polymers → Polymer-based Nanoparticles → Nanoparticles → Drug Delivery Systems
Administration
Intravenous
01

Overview

Pegylated recombinant human endostatin is a modified form of the endogenous angiogenesis inhibitor, endostatin, which is a proteolytic fragment of the C-terminal region of type XVIII collagen. The drug is conjugated with polyethylene glycol (PEG) to improve its stability and pharmacokinetic properties. It acts as an angiogenesis inhibitor by inducing apoptosis in microvascular endothelial cells and inhibiting their proliferation, thereby suppressing tumor neovascularization and growth. Mechanistically, it binds to cell surface receptors such as nucleolin and integrins (notably α5β1), inhibits matrix metalloproteinases (MMPs), downregulates Wnt/β-catenin signaling, suppresses FAK/Ras/p38-MAPK/ERK pathways, reduces HIF-1α/VEGF-A expression, and induces autophagy in endothelial cells. Developed primarily for cancer therapy—especially solid tumors like non-small cell lung cancer—the pegylation enhances its clinical utility by increasing half-life and reducing renal clearance[1][2][3][4][5][6][8].

Brand names
PEG-Endostar injectionPegylated Endostar injection
Other names
polyethylene glycol recombinant endostatinM2ESM-2ESM 2ES
02

Targets

NCL (Nucleolin)MMP9 (Matrix metalloproteinase-9)MMP2 (Matrix metalloproteinase-2)ITGA5:ITGB1 (Integrin α5β1)

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