Various integrins are thought to be intimately involved in several pathological processes, including cancers (solid tumors and metastasis), cardiovascular diseases (stroke and heart failure), inflammatory diseases (rheumatoid arthritis) and ocular pathologies. The mechanism of the involvement of integrins in these acute and chronic disease states is slowly being elucidated. Recently, various therapeutic candidates, including antibodies, cyclic peptides and peptidomimetics, have been clinically evaluated and have been shown to successfully modulate certain disease processes. This review focuses on the key role of the alpha (v) integrin (alpha (v) beta (3)) in the angiogenic processes in diseases such as cancer, restenosis following percutaneous transluminal coronary angioplasty, stroke, ocular disease and rheumatoid arthritis.