A promising novel target for anti-cancer therapy is the tumour vasculature. Both primary tumour growth and the formation of metastasis depend on the establishment of new blood vessels from preexisting ones, a process called angiogenesis. Inhibition of angiogenesis and targeting of the tumour vasculature are highly effective in controlling tumour growth. Several natural and synthetic compounds have been developed and are currently tested in pre-clinical and clinical studies. This review intends to provide an overview of agents with antiangiogenic activity and the early clinical experience with these drugs.