Table 1.
Anti-angiogenic agents and their mechanism of action.
| Multi-kinase inhibitors (targets and IC-50 in nM) | |||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|
| VEGFR-1 | VEGFR-2 | VEGFR-3 | PDGFRα | PDGFRβ | c-Kit | RET | RAF | FLT3 | FGFR-1 | ||
| Anlotinib (4) | 26.9 | 0.2 | 0.7 | – | 115.0 | 14.8 | – | – | 6.4 | 11.7 | |
| Axitinib (5) | 0.1 | 0.2 | 0.1–0.3 | 5.0 | 1.6 | 1.7 | >1,000 | – | >1,000 | – | |
| Cediranib (6) | 1.2 | – | – | 36.0 | 5.0 | 2.0 | – | – | 5.0 | – | |
| Pazopanib (7) | 10.0 | 30.0 | 47.0 | 71.0 | 84.0 | 74.0 | >1,000 | – | >1,000 | 80.0 | |
| Regorafenib (8) | 13.0 | 4.2 | 46.0 | 22.0 | 7.0 | 1.5 | 2.5 | – | |||
| Sorafenib | – | 90.0 | 20.0 | 50.0–60.0 | 50.0–60.0 | 68.0 | 100.0–150.0 | 5.0–10.0 | 46.0 | 64.0 | |
| Sunitinib | 10.0 | 10.0 | 10.0 | 5.0–10.0 | 10.0 | 13.0 | 100–200 | – | 1–10 | 437.0 | |
| Tivozanib (9) | 30.0 | 6.5 | 15.0 | 40.0 | 49.0 | 78.0 | – | – | – | 530.0 | |
| Other agents | |||||||||||
| Aflibercept | It is a recombinant fusion protein that traps VEGF-A, VEGF-B and PlGF | ||||||||||
| Angiotensin | It is a protein that regulates vasoconstriction and blood pressure. | ||||||||||
| Bevacizumab | It is a recombinant humanized monoclonal antibody that bocks VEGF-A. | ||||||||||
| Ombrabulin | It is a synthetic analogue of combrestatin A4 that acts as vascular-disrupting agent since it binds the colchicine binding site of endothelial cell tubulin and then induce apoptosis of endothelial cells and blood vessels collapse. | ||||||||||