Table 2

Examples of angiogenesis inhibitors in clinical trials

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

FGF, fibroblast growth factor; MMP, matrix metalloproteinase; PDGF, platelet-derived growth factor; VEGF, vascular endothelial growth factor.

Paleolog Arthritis Res 2002 4(Suppl 3):S81   doi:10.1186/ar575