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In Vivo Use of a Radioiodinated Somatostatin Analogue: Dynamics, Metabolism, and Binding to Somatostatin Receptor-Positive Tumors in Man

Departments of Nuclear Medicine, Internal Medicine III, and Radiology, University Hospital Dijkzigt and Erasmus University Medical School, Rotterdam, The Netherlands
Sandoz Research Institute, Berne, Switzerland

Correspondence: For reprints contact: Willem H. Bakker, University Hospital Dijkzigt, Department of Nuclear Medicine, Dr Molewaterplein 40, 3015 GD Rotterdam, The Netherlands.

ABSTRACT

Somatostatin analogues, labeled with gamma-emitting radionuclides, are of potential value in the localization of somatostatin receptor-positive tumors with gamma camera imaging. We investigated the application in man of a radioiodinated analogue of somatostatin, ¹²³I-Tyr-3-octreotide, which has similar biologic characteristics as the native peptide. The radiopharmaceutical is cleared rapidly from the circulation (up to 85% of the dose after 10 min) mainly by the liver. Liver radioactivity is rapidly excreted into the biliary system. Until 3 hr after injection, radioactivity in the circulation is mainly in the form of ¹²³I-Tyr-3-octreotide. Thereafter, plasma samples contain increasing proportions of free iodide. Similarly, during the first hours after injection, radioactivity in the urine exists mainly in the form of the unchanged peptide. Thereafter, a progressive increase in radioiodide excretion is observed, indicating degradation of the radiopharmaceutical in vivo. Fecal excretion of radioactivity amounts to only a few percent of the dose. The calculated median effective dose equivalent is comparable with values for applications of other ¹²³I-radiopharmaceuticals (0.019 mSv/MBq).

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