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. Author manuscript; available in PMC: 2014 Apr 17.
Published in final edited form as: Cancer Metastasis Rev. 2008 Dec;27(4):589–613. doi: 10.1007/s10555-008-9157-4
Antiangiogenic Agents
Drug Target General Mechanism of Action
AEE788 VEGFR-1 & -2, EGFR Dual inhibitor of EGFR and VEGFR
Vandetanib (ZD6474) VEGFR-2, EGFR, FGFR-1, RET Dual inhibitor of EGFR and VEGFR
Axitinib (AG-013736) VEGFR-1, -2 & -3, PDGFR-β, c-Kit Inhibits VEGFR autophosphorylation, inhibits endothelial cell proliferation and survival
Sunitinib (SU11248) VEGFR-1, -2 & -3, PDGFR-β, c-Kit Inhibits endothelial cell proliferation and survival
Recentin (AZD2171) VEGFR-1, -2 & -3, PDGFR-β, c-Kit Inhibits VEGF-induced angiogenesis in vivo
Vatalanib (PTK787/ZK222584) VEGFR-1, -2 & -3, PDGFR-β, c-Kit Inhibits endothelial cell proliferation and survival
Sorafenib (BAY 43-9006) VEGFR-2 & -3, Raf kinase, PDGFR-β, c- Inhibits tumor and endothelial cell proliferation and survival
O-(chloro-acetyl-carbamoyl) (TNP-470/AGM-1470) Kit, RET EC growth Relatively specifically cytostatically inhibits endothelial cell growth (UI 8297716)
PX-866 PI3-Kinase Inhibits PI-3-kinase pathway, cellular proliferation and survival
LY294002 PI3-Kinase Inhibits PI-3-kinase pathway, cellular proliferation and survival
Wortmannin PI3-Kinase Inhibits PI-3-kinase pathway, cellular proliferation and survival
Bevacizumab (rhuMAb VEGF) VEGF Monoclonal antibody to VEGF
Volociximab AAB1 targets AAB1, a component protein of α5β1
HuMV833 VEGF recombinant humanized IgG4k monoclonal antibody targeting VEGF
“VEGF-trap” (AVE 0005) VEGF Fusion of human IgG1 Fc to extracellular domains of VEGFR-1 and VEGFR-2; binds VEGF
IMC-1121B (anti-VEGFR-2MAb) VEGF-R2 IgG antibody targeting VEGFR-2
Endostatin α5β1, αvβ3 & αvβ5 Interferes with migration and proliferation of endothelial cell
Tumstatin αvβ3 Inhibits EC protein synthesis
Angiostatin Integrin αvβ3 Competitively binds to integrins, inhibiting interaction with matrix ligands, interfering w/cell attachment and adhesion
Neovastat MMPs Inhibition of MMPs