8-Hydroxy-quinolyl-glucuronide (8-HOQ-Glu) can be deglucuronidated by the beta-glucoronidase enzyme, which has an activity that is considerably high in certain kinds of cancer cell. Owing to this enzyme activity, 8-HOQ-Glu can be considered as a potential anti-cancer drug. The combination of the radiotoxicity known of 125I nuclide with the cytotoxicity of 8-hydroxy-quinoline (8-HOQ) and particularly the selective carrying of 125I into the cancer cells is the principal aim of this study. As a first step, the metabolic 8-HOQ-Glu was extracted from the urine of rabbits treated with 8-HOQ directly radioiodinated using the iodogen method. The results showed that the radioiodination was successfully realized, and its yield was found to be about 90-95%.