TABLE 4 | Three types of angiogenesis inhibitors
From the following article:
Angiogenesis: an organizing principle for drug discovery?
Judah Folkman
Nature Reviews Drug Discovery 6, 273-286 (April 2007)
doi:10.1038/nrd2115
| Mechanism | Drug | Action |
|---|---|---|
| Type 1 | ||
| Blocks one main angiogenic protein | Avastin (Avastin; Genentech) Blocks | VEGF |
| VEGF Trap (Regeneron Pharmaceuticals) | Blocks VEGF | |
| Type II | ||
| Blocks two or three main angiogenic proteins | Sutent (Sutent; Pfizer) | Downregulates VEGF receptor 2, PDGF receptor, cKIT receptor |
| Tarceva (Tarceva; Genentech, OSI Pharmaceuticals, Roche) | Downregulates VEGF production, bFGF production, TGF by tumour cell | |
| Type III | ||
| Blocks a broad range of angiogenic regulators | Endostatin | Downregulates VEGF, bFGF, bFGF receptor, HIF1, EGF receptor, ID1, neuropilin Upregulates thrombospondin 1, maspin, HIF1, TIMP2 |
| Caplostatin | Broad anti-angiogenic and anticancer spectrum | |
| bFGF, basic fibroblast growth factor; EGF, epidermal growth factor; HIF1, hypoxia-inducible factor 1; ID1, inhibitor of DNA binding 1, dominant negative helix-loop-helix protein; PDGF, platelet-derived growth factor; TIMP2, tissue inhibitor of metalloproteinase 2; TGF, transforming growth factor-; VEGF, vascular endothelial growth factor. | ||
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