Novel small-molecule inhibitors of the vascular endothelial growth factor receptor.

Sustained angiogenesis is one of the hallmarks of carcinogenesis. Vascular endothelial growth factor (VEGF) is a critical molecule mediating pro-angiogenic signals against which a number of therapeutic approaches have been designed. The 2 predominant approaches to inhibiting VEGF signalling are the use of monoclonal antibodies to block the receptor or ligand and small molecule receptor kinase inhibitors. There are several small-molecule inhibitors of tyrosine kinase activity of VEGF receptors in clinical trials. These are discussed in this review.