Cocaine is a major drug of abuse whose devastating effects have captured the attention of health officials and policy makers. Based upon the alarming health and crime-related costs associated with the use of this powerful reinforcing drug, immediate therapies are needed for the treatment of cocaine addiction. In this review, some of the small-molecule-based approaches that have been pursued in the search for such medications are highlighted. Because the pharmacological actions of cocaine stem laargely from its ability to block the dopamine transporter, many intervention strategies have focused on the dopaminergic pathway.