Targeted therapies against cancer have become more and more important. In particular, the inhibition of tumor angiogenesis and vascular targeting have been the focus of new treatment strategies. Numerous new substances were developed as angiogenesis inhibitors and evaluated in clinical trials for safety, tolerance, and efficacy. With positive study results, some of these molecules have already been approved for clinical use. For example, this is true for the vascular endothelial growth factor neutralizing antibody bevacizumab (BEV) in metastatic colorectal cancer, nonsmall cell lung cancer, renal cancer, and breast cancer. The tyrosine kinase (TK) inhibitors sorafenib and sunitinib have been approved for metastatic renal cancer as well as for hepatocellular carcinoma, and sunitinib has also been approved for gastrointestinal stroma tumors. In this chapter we try to give an overview of the substances currently investigated in Phase III studies and beyond with regard to antiangiogenesis in cancer therapy.