Angiogenesis-targeting agents, predominantly inhibitors of vascular endothelial growth factor and its receptors, have become a mainstay in oncology practice over the last decade. The approved drugs, which include two antibodies and seven small molecule inhibitors, represent strong validation for the field of anti-angiogenesis in the treatment of cancer. In addition to ongoing clinical studies assessing new indications for these agents, novel inhibitors are undergoing clinical evaluations and combination therapies of anti-angiogenic drugs with other targeted approaches are being investigated. This chapter will review the development of the currently marketed drugs targeting VEGFR, as well as the new inhibitors currently being assessed in the clinic.