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Comparison of ¹¹¹In-DOTA-Tyr³-Octreotide and ¹¹¹In-DTPA-Octreotide in the Same Patients: Biodistribution, Kinetics, Organ and Tumor Uptake

Departments of Nuclear Medicine and Internal Medicine III, University Hospital Dijkzigt, Rotterdam, The Netherlands
Department of Nuclear Medicine, Kantonspital Basel, Basel, Switzerland

Correspondence: For correspondence or reprints contact: Dik J. Kwekkeboom, MD, University Hospital Dijkzigt, Department of Nuclear Medicine, 40 Dr. Molewaterplein, 3015 GD Rotterdam, The Netherlands.

ABSTRACT

Scintigraphy with [¹¹¹In-diethylenetriamine pentaacetic acid⁰-D-Phe¹]-octreotide (DTPAOC) is used to demonstrate neuroendocrine and other somatostatin-receptor-positive tumors. Despite encouraging results, this ¹¹¹In-labeled compound is not well suited for peptide-receptor-mediated radiotherapy of somatostatin-receptor-positive tumors. Another somatostatin analog, [1,4,7,10-tetraazacyclododecane-N,N',N'',N'''-tetraacetic acid⁰, D-Phe¹, Tyr³]-octreotide (DOTATOC), can be labeled with the ß-emitter ⁹⁰Y in a stable manner. Methods: We compared the distribution, kinetics and dosimetry of ¹¹¹In-DTPAOC and ¹¹¹In-DOTATOC in eight patients to predict the outcomes of these parameters in patients who will be treated with ⁹⁰Y-DOTATOC. Results: Serum radioactivity levels for the radiopharmaceuticals did not differ significantly 2–24 h after injection (P > 0.05). Up to 2 h postinjection they were slightly, but significantly, lower after administration of ¹¹¹In-DOTATOC (P < 0.01 at most time points). The percentage of peptide-bound radioactivity in serum did not differ after administration of either compound. Urinary excretion was significantly lower after administration of ¹¹¹In-DOTATOC (^P < 0.01). The visualization of known somatostatin-receptor-positive organs and tumors was clearer after administration of ¹¹¹In-DOTATOC than after administration of ¹¹¹In-DTPAOC. This was confirmed by significantly higher calculated uptakes in the pituitary gland and spleen. The uptake in the tumor sites did not differ significantly (P > 0.05), although in three of the four patients in whom tumor uptake could be calculated, it was higher after administration of ¹¹¹In-DOTATOC. Conclusion: The distribution and excretion pattern of ¹¹¹In-DOTATOC resembles that of ¹¹¹In-DTPAOC, and the uptake in somatostatin-receptor-positive organs and most tumors is higher for ¹¹¹In-DOTATOC. If ⁹⁰Y-DOTATOC shows an uptake pattern similar to ¹¹¹In-DOTATOC, it is a promising radiopharmaceutical for peptide-receptor-mediated radiotherapy in patients with somatostatin-receptor-positive tumors.

Key Words: somatostatin • somatostatin receptor • [1,4,7,10-tetraazacyclododecane-N,N',N'',N'''-tetraacetic acid⁰, D-Phe¹, Tyr³]-octreotide • ¹¹¹In-diethylenetriamine pentaacetic acid⁰-D-Phe¹-octreotide • scintigraphy

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