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Oral Versus Intravenous Administration of Lysine: Equal Effectiveness in Reduction of Renal Uptake of [¹¹¹In-DTPA]Octreotide

¹ Department of Nuclear Medicine, Erasmus University Medical Center, Rotterdam, The Netherlands
² Department of Clinical Genetics, Erasmus University Medical Center, Rotterdam, The Netherlands

During tumor therapy with radiolabeled somatostatin analogs, the kidneys are dose limiting. Renal uptake in patients can effectively be reduced by a 4- to 10-h intravenous infusion of a lysine/arginine solution, thereby increasing the maximum radiation dose to the tumor without renal side effects. Oral administration of amino acids could facilitate this labor-intensive procedure. Therefore, the effects of oral versus intravenous administration of D-lysine were compared in rats injected with [¹¹¹In-diethylenetriaminepentaacetic acid (DTPA)]octreotide. Methods: Rats were intravenously injected with 3 MBq/0.5 µg [¹¹¹In-DTPA]octreotide and also received D-lysine intravenously or orally in various concentrations and following various time schedules. Twenty-four hours after injection, a biodistribution study and renal ex vivo autoradiography were performed. Results: Renal uptake was reduced significantly—up to 40%—in all lysine-treated groups, without affecting the uptake in other organs. Conclusion: Renal uptake of this radiolabeled peptide can be reduced up to 40% both by oral and by intravenous administration of lysine in rats.

Key Words: peptide receptor radionuclide therapy • kidney reduction • lysine • oral administration

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