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 signaling 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 the tyrosine kinase activity of VEGF receptors in clinical trials. These will be discussed in this review.