Table 2.
Angiogenesis Inhibitors in Various Phases of Clinical Trials
| Drug | Mechanism | Cancer |
|---|---|---|
| Phase 1 | ||
| Endostatin | Inhibits endothelial proliferation | Solid tumors |
| Angiostatin | Inhibits endothelial proliferation | Lung, breast, colon, prostate cancer |
| COL-3 | Synthetic MMP inhibitor, tetracycline derivative | – |
| SU6668 | Blocks BEGF, FGF, EGF receptor signaling | – |
| EMD-121974 | Blocks an endothelial integrin | – |
| 2-methoxy estradiol | Inhibits microtubule function | – |
| Tumstatin | Alpha-vB antagonist | Different cancers |
| Phase 2 | ||
| TNP-470 | Fumagillin analogue; inhibits endothelial proliferation | Lymphoma, leukemia |
| Squalamine | Inhibits Na/H exchanger | – |
| IL-12 | Induces IFN-gamma and IFN inducible protein-10 | – |
| Combrestatin | Apoptosis in proliferating endothelium | – |
| Penicillamine | Inhibition of endothelial cell migration | Glioblastoma |
| Phase 3 | ||
| Marimastat | Synthetic MMP inhibitor | Breast, non-small-cell lung cancer (NSCLC), pancreatic cancer |
| AG3340 | Synthetic MMP inhibitor | NSCLC, prostate |
| Neovastat | Natural MMP inhibitor | Colon, NSCLC |
| IFN-alpha | Inhibit bFGF production | – |
| Thalidomide | Not clear | Kaposi's sarcoma, prostate cancer |
| SU 5416 | Blocks VEGF receptor signaling | Kaposi's sarcoma, metastatic colon cancer |
| BAY-12-95566 | Synthetic MMP inhibitor | Lung, ovary, pancreas |