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Radiolabeled iododeoxyuridine: safety evaluation

K A Harrison1, G V Dalrymple, J Baranowska-Kortylewicz

  • 1Department of Radiology, University of Nebraska Medical Center, Omaha 68198-1045, USA.

Journal of Nuclear Medicine : Official Publication, Society of Nuclear Medicine
|April 1, 1996
PubMed
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Radiolabeled iododeoxyuridine (IUdR) shows promise as a therapeutic agent. Studies in pigs and humans indicate minimal adverse effects on normal tissues, suggesting its safety for therapeutic use.

Area of Science:

  • Oncology
  • Radiochemistry
  • Pharmacology

Background:

  • Radiolabeled iododeoxyuridine (IUdR) is being investigated for therapeutic potential.
  • Previous research focused on assessing IUdR's safety and identifying adverse effects on normal tissues.
  • The liver rapidly dehalogenates IUdR, making intravenous administration less effective.

Purpose of the Study:

  • To evaluate the safety of radiolabeled iododeoxyuridine (IUdR) as a potential therapeutic agent.
  • To assess adverse effects on normal tissues in preclinical (pigs) and clinical (human) studies.
  • To explore alternative administration routes, specifically intra-arterial and intravesicular, due to rapid dehalogenation via the intravenous route.

Main Methods:

  • Preclinical studies in farm pigs involved multiple administrations of [125I]IUdR into the aorta, carotid artery, and bladder.

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  • Pharmacokinetic and metabolite analyses were conducted using venous blood samples.
  • Histologic examination of tissues and autoradiography were performed.
  • Clinical studies in human patients with liver metastases and bladder carcinoma utilized intra-arterial and intravesicular administration of [123I]IUdR and [125I]IUdR.

    • Main Results:

    • No adverse effects on normal tissues were observed in pigs or humans.
    • Hematologic and metabolic indices remained unaltered in study subjects.
    • Intravesicular administration demonstrated minimal leakage of IUdR into the systemic circulation.

    Conclusions:

    • Radiolabeled iododeoxyuridine (IUdR) demonstrates a favorable safety profile for therapeutic applications.
    • Intra-arterial and intravesicular administration routes appear safe, with minimal impact on normal tissues.
    • IUdR is a promising candidate for targeted cancer therapies with low systemic toxicity.