TABLE I.
Anti-angiogenic agents
| Target | Agent | Description |
|---|---|---|
| vegf ligand | Bevacizumab (Avastina) | Humanized anti-vegfa monoclonal antibody |
| Aflibercept (vegf Trapb) | Fusion protein of vegfr-1, vegfr-2, and immunoglobulin G1 Fc fragment | |
| vegf receptor | ||
| Extracellular domain | IMC-1121B | Human anti–vegfr-2 monoclonal antibody |
| Cytoplasmic domain | AEE788 | vegfr-2 and egfr inhibitor |
| Axitinib (AG-013736) | vegfr-1,2 and pdgfr inhibitor | |
| BMS-582664 | vegfr-2 and fgfr inhibitor | |
| Motesanib (AMG-706) | vegfr-1,2,3; pdgfrb; and c-Kit inhibitor | |
| OSI-930 | vegfr-2 and c-Kit inhibitor | |
| Pazopanib (GW-786034) | vegfr-2 inhibitor | |
| Tandutinib (MLN-518) | Flt-3, pdgfr, c-Kit inhibitor | |
| Vatalanib (PTK787) | vegfr-1,2,3 and pdgfrb inhibitor | |
| Sorafenib (BAY 43–9006) | b-Raf; vegfr-2,3; pdgfrb; Flt-3; and c-Kit inhibitor | |
| Sunitinib (SU11248) | vegfr-1,2; pdgfra, pdgfrb; and c-Kit inhibitor | |
| Cediranib (AZD2171) | vegfr-1,2,3; pdgfrb; and c-Kit inhibitor | |
| Vandetanib (ZD6474) | vegfr-2,3 and egfr inhibitor | |
| XL-184 | vegfr-2, Met, c-Kit, Flt-3, and Tie2 inhibitor | |
| XL-999 | vegfr-1,2,3; fgfr; pdgfr; and Flt-3 inhibitor | |
| Endogenous inhibitors | Angiostatin | Cleavage fragment of plasminogen |
| Endostatin | Cleavage fragment of collagen xviii | |
| Thrombospondin 1 | Extracellular glycoprotein | |
| Other | EMD 121974 (Cilengitidec) | αvβ3 Integrin receptor inhibitor |
| ATN-161 | αvβ1 Integrin receptor inhibitor | |
| Volociximab | αvβ1 Integrin receptor inhibitor | |
| Vitaxin | Human monoclonal antibody to αvβ3 integrin receptor | |
| AMG-386 | Angiopoietin inhibitor | |
| Thalidomide | Immunomodulatory agent | |
| AGN-745/SIRNA027 | sirna inhibiting vegfr-1 mrna | |
a
Genentech, San Francisco, CA, U.S.A.
b
Regeneron, Tarrytown, NY, U.S.A.
c
Merck and Co., Whitehouse Station, NJ, U.S.A.
vegf = vascular endothelial growth factor; vegfr = vascular endothelial growth factor receptor; egfr = epidermal growth factor receptor; pdgfr[a,b] = platelet-derived growth factor receptor [α, β]; fgfr = fibroblast growth factor receptor.