Recently, advances in imaging technology have made possible the ability to image noninvasively specific molecular pathways in vivo that are involved in disease processes. Molecular imaging evaluates changes in cellular physiology and function rather than anatomy, which are likely to be earlier and more sensitive manifestations of disease. In addition, as newer drugs to treat disease become increasingly molecule specific, molecular imaging has become necessary to provide noninvasive determination of patients likely to benefit from treatment and early therapy response. This article reviews current and emerging molecular imaging technologies relevant to urologic surgery.