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Pharmacokinetics and biodistribution of radiolabelled idoxifene: prospects for the use of PET in the evaluation of a novel antioestrogen for cancer therapy.

Abstract
With a view to evaluating the role of PET imaging in the development of new anticancer drugs, we are investigating the novel antioestrogen pyrrolidino-4-iodotamoxifen (idoxifene). [125I]idoxifene and [131I]idoxifene have been produced in no-carrier-added form using a tributyl stannylated precursor, and the bio-distribution and dynamic behaviour of the compound investigated using syngeneic transplantable mammary tumours in the rat. Our findings support the use of PET imaging with 124I to study the clinical pharmacology of idoxifene. Factors other than hormone receptor levels appear to influence tumour uptake and therefore, possibly the biological effects of this compound.
AuthorsH Young, P Carnochan, M Trivedi, G A Potter, S A Eccles, B P Haynes, M Jarman, R J Ott
JournalNuclear medicine and biology (Nucl Med Biol) Vol. 22 Issue 4 Pg. 405-11 (May 1995) ISSN: 0969-8051 [Print] United States
PMID7550016 (Publication Type: Comparative Study, Journal Article, Research Support, Non-U.S. Gov't)
Chemical References
  • Estrogen Antagonists
  • Iodine Radioisotopes
  • Organotechnetium Compounds
  • Oximes
  • Receptors, Estrogen
  • Tamoxifen
  • Technetium Tc 99m Exametazime
  • idoxifene
  • Estradiol
Topics
  • Animals
  • Estradiol (pharmacology)
  • Estrogen Antagonists (pharmacokinetics, therapeutic use)
  • Female
  • Iodine Radioisotopes (pharmacokinetics)
  • Isotope Labeling
  • Liver (drug effects, metabolism)
  • Mammary Neoplasms, Experimental (diagnostic imaging, metabolism)
  • Muscle, Skeletal (drug effects, metabolism)
  • Organotechnetium Compounds (pharmacokinetics)
  • Ovariectomy
  • Oximes (pharmacokinetics)
  • Rats
  • Rats, Inbred Strains
  • Receptors, Estrogen (metabolism)
  • Tamoxifen (analogs & derivatives, chemical synthesis, pharmacokinetics, pharmacology)
  • Technetium Tc 99m Exametazime
  • Tissue Distribution
  • Tomography, Emission-Computed
  • Uterus (drug effects, metabolism)

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