Pharmacological evaluation of intravenous delivery of 5-bromodeoxyuridine to patients with brain tumors

A. Russo, L. Gianni, T. J. Kinsella, R. W. Klecker, J. Jenkins, J. Rowland, E. Glatstein, J. B. Mitchell, J. Collins, C. Myers

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Previously, 5-bromodeoxyuridine (BrdUrd) has been shown to be an effective radiosensitizing agent in rapidly dividing cells. As part of a Phase I/II study to evaluate BrdUrd as a radiosensitizer in gliomas, the pharmacology was studied in eight patients. BrdUrd was infused using an i.v. route as a 12-hr constant infusion each day for as long as 14 days. BrdUrd steady-state arterial levels are described for three different infusional rates: 1.6 μmol/sq m/min (350 mg/sq m/12 hr) produced a steady state arterial level of 0.7 μM; 3.2 μmol/sq m/min (700 mg/sq m/12 hr) resulted in 2.1 μM; 5.9 μmol/sq m/min (650 mg/sq m/6 hr) showed a level of 3.9 μM. Because of myelosuppression, the highest tolerable dose for this intermittent long-term infusional therapy with BrdUrd appears to be 700 mg/sq m/12 hr. Contrary to the nonlinear pharmacokinetics of thymidine, 5-fluorouracil, and 5-fluorodeoxyuridine described previously, BrdUrd shows linear behavior in the range studied. BrdUrd still has promise as a radiosensitizer for gliomas in humans, but an alternative means of safe delivery into the carotid artery is needed. Because of an estimated 11- to 16-fold-higher local concentration, use of the intraarterial route could deliver optimum levels of BrdUrd to the tumor with minimal systemic toxicity.

Original languageEnglish
Pages (from-to)1702-1705
Number of pages4
JournalCancer Research
Issue number4
Publication statusPublished - 1984

ASJC Scopus subject areas

  • Cancer Research
  • Oncology


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