Action of drug | Drug | Examples of clinical trials | Mode of action |
Direct inhibition of endothelial cells | Thalidomide | Phase III non-small-cell lung cancer | Inhibits endothelial cells directly |
 | Endostatin | Phase I solid tumour | Inhibits endothelial cells |
Inhibition of the binding of angiogenic stimuli | Humanised monoclonal anti-human VEGF (bevacizumab) | Phase II metastatic renal cell cancer; phase III with chemotherapy in untreated metastatic colorectal cancer | Monoclonal antibody to VEGF |
Inhibition of events downstream of angiogenic stimuli | SU6668 | Phase I against advanced tumours | Blocks VEGF, FGF, PDGF receptor signalling |
 | SU5416 | Phase I recurrent head and neck; phase II prostate cancer | Blocks VEGF receptor signalling |
Inhibition of matrix breakdown | Marimastat | Phase III small-cell lung cancers | Synthetic MMP inhibitor |
 | BMS-275291 | Phase II/III metastatic non-small-cell lung | Synthetic MMP inhibitor |
Inhibition of endothelial-integrin interactions | EMD121974 | Phase I in patients with HIV-related Kaposi's sarcoma | Small molecule blocker of integrin on endothelium |