Snake venom disintegrins are the natural products that have been investigated as potent inhibitors of various integrins. Functionally, disintegrins can be divided into three groups according to their integrin selectivity and presence of specific, active motifs. This classification includes RGD-disintegrins, MLD-disintegrins, and KTS-disintegrins. RGD-disintegrins have been the most intensively investigated, and their research resulted in design and synthesis of new pharmaceutical compounds, eptifibatide and tirofiban that are currently being evaluated for the therapy of acute coronary ischaemic syndrome. MLD- and KTS-disintegrins are specific for leukocyte integrins and collagen receptors, respectively, and are being investigated in the new fields of pharmaceutical research. This review summarizes the biological activities of snake venom disintegrins, as well as discusses their potential in the study of the pharmacology of various human diseases.