The dependence of tumor growth and metastasis on blood vessels makes tumor angiogenesis a rational target for cancer therapy. One of the key mediators of angiogenesis is vascular endothelial growth factor (VEGF), which is an appealing target for anticancer therapy. The development of anti-VEGF/VEGFR agents and the latest clinical data are reviewed, including bevacizumab as a monoclonal antibody to VEGF, sunitinib and sorafenib as VEGFR tyrosine kinase inhibitors, and IMC-1C11 as VEGFR monoclonal antibody.