Angiogenesis plays an essential role in tumor growth, invasion, and metastasis. Angiogenesis inhibition has been proposed as a general strategy to fight cancer. The initial pessimism about the usefulness of the antiangiogenic therapeutic approach for cancer, turned out into an increasing interest in the development of antiangiogenic compounds after the first approval of an antiangiogenic therapy in 2004. The formation of new blood vessels is a complex multi-step process, including endothelial cells activation by the angiogenic signal and their stimulation to synthesize and release degradative enzymes allowing them to migrate, proliferate and finally differentiate to give rise to capillary tubules. The discovery and pharmacological development of future generations of angiogenesis inhibitors will benefit from further advances in the understanding of the mechanisms involved in human angiogenesis. In this chapter, the different therapeutic targets for angiogenesis intervention are discussed with emphasis on the clinical developmental status of antiangiogenic drugs.