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The Fate of 5-Bromodeoxyuridine, 5-Bromodeoxycytidine, and 5-Iododeoxycytidine in Man^*

Joseph P. Kriss, Yosh Maruyama, Lucie A. Tung, Sheila B. Bond and László Révész

( Departments of Medicine and Radiology, Stanford University School of Medicine, Stanford, California)

The fate of 5-bromodeoxyuridine (BUdR), 5-bromodeoxycytidine (BCdR), and 5-iododeoxycytidine (ICdR) in man has been studied with the use of BUdR-Br⁸², BCdR-Br⁸², and ICdR-I¹³¹. Following its intravenous injection BUdR rapidly disappeared from the blood, in part owing to its degradation associated with the liberation of bromide. BCdR disappeared equally rapidly and was degraded to BUdR, bromouracil (BU), and bromide. Bromocytosine was not identified as a degradation product. One hour after the injection of either BUdR-Br⁸² or BCdR-Br⁸², approximately 60 per cent of the Br⁸² activity was estimated to be in intracellular or intralumenal sites. After either intra-arterial or intravenous injection ICdR was rapidly degraded to iododeoxyuridine (IUdR), iodouracil (IU), and iodide. About 80 per cent or more of the iodine in the compound was recovered in the urine within 72 hours. Nearly all the urinary iodine was in the form of iodide; small amounts of ICdR, IUdR, and IU were also identified.

In three cases, following injection of ICdR-I¹³¹ into the internal carotid artery homolateral to a brain tumor, brain scanning revealed I¹³¹ in the region of the tumor but also rather diffusely distributed in the corresponding cerebral hemisphere. In two other cases, given an intravenous injection of ICdR-I¹³¹, I¹³¹ was found localized in an intracerebral metastasis and in a hepatoma, respectively. Regardless of the route of administration of ICdR-I¹³¹, the pattern of distribution of I¹³¹ activity over the various organs of the body differed markedly from case to case. Stomach, colon, vertebral column, and liver were among the organs showing evidence of localization of radioactivity. The diagnostic use of radioactive halogenated nucleosides in the selection of patients with cancer who may be candidates for combined treatment with x-radiation and nonradioactive BUdR or BCdR is discussed.

^* Supported by grants CY-4096 and C-6135 from the National Cancer Institute. National Institutes of Health, U.S. Public Health Service, Bethesda, Md.

Advanced Fellow in Academic Radiology of the James Picker Foundation.

On leave from the Instittue for Tumor Biology, Karolinska Institutet, Stockholm, Sweden.

Received 8/27/62.