A 19F MR chemical shift imaging (CSI) technique is presented which enables selective imaging of the antineoplastic drug 5-fluorouracil (5-FU) and its major catabolite alpha-fluoro-beta-alanine (FBAL). The CSI sequence employs a chemical shift selective (CHESS) saturation pulse to suppress either the 5-FU or the FBAL resonance before the other component of the two-line 19F MR spectrum is measured. Because the transmitter frequency can always be set to the Larmor frequency of the 19F resonance to be imaged, this approach yields 5-FU and FBAL MR images free of chemical shift artifacts in read-out and slice-selection direction. In phantom experiments, selective 5-FU and FBAL images with a spatial resolution of 15 x 15 x 20 mm3 (4.5 ml) were obtained in 30 min from a model solution, whose drug and catabolite concentrations were similar to those estimated in the liver of tumor patients undergoing IV chemotherapy with 5-FU. The drug-specific MR imaging technique developed is, therefore, well-suited for the direct and noninvasive monitoring of the up-take and trapping of 5-FU in liver tumors in vivo.