Abstract
In vitro octreotide receptor binding of [111In-DOTA0,d-Phe1,Tyr3]octreotide (111In-DOTATOC) and the in vivo metabolism of90Y or111In-labelled DOTATOC were investigated in rats in comparison with [111In-DTPA0]octreotide [111In-DTPAOC).111In-DOTATOC was found to have an affinity similar to octreotide itself for the octreotide receptor in rat cerebral cortex microsomes. Twenty-four hours after injection of90Y or111In-labelled DOTATOC, uptake of radioactivity in the octreotide receptor-expressing tissues pancreas, pituitary, adrenals and tumour was a factor of 2–6 that after injection of111In-DTPAOC. Uptake of labelled DOTATOC in pituitary, pancreas, adrenals and tumour was almost completely blocked by pretreatment with 0.5 mg unlabelled octreotide, indicating specific binding to the octreotide receptors. These findings strongly indicate that90Y-DOTATOC is a promising radiopharmaceutical for radiotherapy and that111In-DOTATOC is of potential value for diagnosis of patients with octreotide receptor-positive lesions, such as most neuroendocrine tumours.
Similar content being viewed by others
References
Krenning EP, Kwekkeboom DJ, Bakker WH, Breeman WAP, Kooij PPM, Oei HY, Van Hagen M, Postema PTE, De Jong M, Reubi JC, Visser TJ, Reijs AEM, Holland LJ, Koper JW, Lamberts SWJ. Somatostatin receptor scintigraphy with [111In-DTPA-d-Phe1]- and [123I-Tyr3]-octreotide: the Rotterdam experience with more than 1000 patients.Eur J Nucl Med 1993; 20: 716–731.
Krenning EP, Kooij PPM, Pauwels S, Breeman WAP, Postema PTE, De Herder WW, Valkema R, Kwekkeboom DJ. Somatostatin receptor scintigraphy and radionuclide therapy.Digestion 1996; 57: 57–61.
Stolz B, Smith-Jones PM, Albert R, Tolcsvai L, Briner U, Ruser B, Mäcke H, Weckbecker G, Bruns C. Somatostatin analogues for somatostatin-receptor-mediated radiotherapy of cancer.Digestion 1996; 57: 17–21.
Rowlinson G, Snook D, Stewart S, Epenetos AA. Intravenous EDTA to reduce bone uptake of Y-90 following Y-90 labeled antibody administration.Br J Cancer 1989; 59: 322.
Jowsey J, Rowland RE, Marshall JH. The deposition of the rare earths in bone.Radiat Res 1958; 8: 490–501.
Bakker WH, Albert R, Bruns C, Breeman WAP, Holland LJ, Marbach P, Pless J, Pralet D, Stolz B, Koper JW, Lamberts SWJ, Visser TJ, Krenning EP. [111In-DTPA-d-Phe1]octreotide, a potential radiopharmaceutical for imaging of somatostatin receptor-positive tumours: synthesis, radiolabelling and in vitro validation.Life Sci 1991; 49: 1583–1591.
Bruns C, Died MM, Palacios JM, Pless J. Identification and characterization of somatostatin receptors in neonatal rat long bones.Biochem J 1990; 265: 39–44.
Author information
Authors and Affiliations
Rights and permissions
About this article
Cite this article
de Jong, M., Bakker, W.H., Krenning, E.P. et al. Yttrium-90 and indium-111 labelling, receptor binding and biodistribution of [DOTA0,d-Phe1,Tyr3]octreotide, a promising somatostatin analogue for radionuclide therapy. Eur J Nucl Med 24, 368–371 (1997). https://doi.org/10.1007/BF00881807
Received:
Revised:
Issue Date:
DOI: https://doi.org/10.1007/BF00881807