This review summarizes the attempts of drug targeting in the field of magnetic resonance imaging. Although the field is young and most work is performed in nonspecific lanthanide chelates, it is obvious that target selectivity and receptor and/or antigen specificity is the most important issue if functional magnetic resonance imaging is to establish itself in the next decade. Recent advances in biochemical engineering and magnetic resonance research have made targeting of diagnostic drugs a credible alternative to conventional drug use in magnetic resonance imaging.