Abstract
Peptide receptor scintigraphy with the radioactive somatostatin analogue [111In-DTPA-D-Phe1] octreotide is a sensitive and specific technique to show in vivo the presence and abundance of somatostatin receptors on various tumors. With this technique primary tumors and metastases of neuroendocrine cancers as well as of many other cancer types can be localized. This technique is currently used to assess the possibility of peptide receptor radionuclide therapy with repeated administration of high doses of [111n-DTPA-D-Phe1]octreotide. 111 In emits Auger and conversion electrons, having a tissue penetration of 0.02–10 μm and 200–500 μm, respectively. Thirty end-stage patients with mostly neuroendocrine progressing tumors were treated with [111n-DTPA-D-Phe1] octreotide, up to a maximal cumulative patient dose of about 74 GBq, in a phase-I trial. There were no major clinical side effects after up to 2 years of treatment, except that in a few patients a transient decline in platelet counts and lymphocyte subsets occurred. Promising beneficial effects on clinical symptoms, hormone production, and tumor proliferation were found. Of the 21 patients who received a cumulative dose of more than 20 GBq, eight showed stabilization of disease and six others a reduction in tumor size. There is a tendency towards better results in patients whose tumors have a higher accumulation of the radioligand. Peptide receptor radionuclide therapy is also feasible with 111In as the radionuclide. Theoretically, depending on the homogeneity of distribution of tumor cells expressing peptide receptors and the size of the tumor, β-emitting radionuclides, e.g., 90Y, labeled to DOTA-chelated peptides may be more effective than 111In for peptide receptor radionuclide therapy. The first peptide receptor radionuclide therapy trials with [90Y-DOTA-Tyr3]octreotide started recently.
Access this chapter
Tax calculation will be finalised at checkout
Purchases are for personal use only
Preview
Unable to display preview. Download preview PDF.
References
Andersson P, Forssel-Aronsson E, Johanson V, Wangberg B, Nilsson O, Fjalling M, Ahlman H (1996) Internalization of indium-111 into human neuroendocrine tumor cells after incubation with indium-111-DTPA-D-Phe 1-octreotide. J Nucl Med 37: 2002–2006
Bakker WH, Albert R, Bruns C, Breeman WAP, Hofland LJ, Marbach P, Pless J, Pralet D, Stolz B, Koper JW, Lamberts SWJ, Visser TJ, Krenning EP (1991) [111In-DTPA-D-Phe1]- octreotide, a potential radiopharmaceutical for imaging of somatostatin receptor-positive tumors: synthesis, radiolabeling and in vitro validation. Life Sci 49:1583–1591
Bernard HF, Krenning EP, Breeman WAP, Rolleman EJ, Bakker WH, Visser TJ, Macke H, de Jong M (1997)D-lysine reduction of indium-Ill octreotide and yttrium-90 octreotide renal uptake. J Nucl Med 38:1929–1934
Breeman WA, van Hagen MP, Visser-Wisselaar HA, van der Pluijm ME, Koper JW, Setyono- Han B, Bakker WH, Kwekkeboom DJ, Hazenberg MP, Lamberts SW, Visser TJ, Krenning EP (1996) In vitro and in vivo studies of substance P receptor expression in rats with the new analog [indium-lll-DTPA-Argl] substance P. J Nucl Med 37: 108–117
de Jong M, Rolleman EJ, Bernard BF, Visser TJ, Bakker WH, Breeman WAP, Krenning EP (1996) Inhibition of renal uptake of indium-lll-DTPA-octreotide in vivo. J Nucl Med 37: 1388–1392
de Jong M, Bakker WH, Krenning EP, Breeman WAP, van der Pluijm ME, Bernard BF, Visser TJ, Jermann E, Behe M, Powell P, Macke HR (1997) Yttrium-90 and indium-111 labelling, receptor binding and biodistribution of [DOTA0, D-Phel, Tyr3]octreotide, a promising somatostatin analogue for radionuclide therapy. Eur J Nucl Med 24: 368–371
Duncan JR, Stephenson MT, Wu HP, Anderson CJ (1997) Indium-111-diethylene-triamine- pentaacetic acid-octreotide is delivered in vivo to pancreatic, tumor cell, renal, and hepatocyte lysosomes. Cancer Res 57: 659–671
Fjalling M, Andersson P, Forssell-Aronsson E, Gretarsdottir J, Johansson V, Tisell LE, Wangberg B, Nilsson O, Berg G, Michanek A, Lindstedt G, Ahlman H (1996) Systemic radionuclide therapy using indium-111-DTPA-D-Phel-octreotide in midgut carcinoid syndrome. J Nucl Med 37: 1519–1521
Gibril F, Reynolds JC, Doppman JL, Chen CC, Venzon DJ, Termanini B, Weber HC, Stewart CA, Jensen RT (1996) Somatostatin receptor scintigraphy: its sensitivity compared with that of other imaging methods in detecting primary and metastatic gastrinomas. Ann Intern Med 125: 26–34
Krenning EP, Bakker WH, Kooij PPM, Breeman WAP, Oei HY, de Jong M, Reubi JC, Visser TJ, Bruns C, Kwekkeboom DJ, Reijs AEM, van Hagen PM, Koper JW, Lamberts SWJ (1992) Somatostatin receptor scintigraphy with [mIn DTPA-D-Phe1]octreotide in man: metabolism, dosimetry and comparison with [123I-Tyr3]octreotide. J Nucl Med 33: 652–658
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, Hofland LJ, Koper JW, Lamberts SWJ (1993) Somatostatin receptor scintigraphy with [111 In-DTPA-D-Phe1]-and [123I-Tyr3]-octreotide: the Rotterdam experience with more than 1000 patients. Eur J Nucl Med 20: 716–731
Krenning EP, Kooij PPM, Bakker WH, Breeman WAP, Postema PTE, Kwekkeboom DJ, Oei HY, de Jong M, Visser TJ, Reijs AEM, Lamberts SWJ (1994) Radiotherapy with a radiolabeled somatostatin analogue, [111-In-DTPA-D-Phe1]-octreotide. A case history. Ann NY Acad Sci 733: 496–506
Krenning EP, Kwekkeboom DJ, Pauwels S, Kvols LK, Reubi J-C (1995) Somatostatin receptor scintigraphy. In: Freeman LM (ed) Nuclear medicine annual. Raven, New York, pp 1–50
Krinning EP, Kooij PPM, Pauwels S, Breeman WAP, Postema PTE, de Herder WW, Valkema R, Kwekkeboom DJ (1996) Somatostatin receptor: scintigraphy and radionuclide therapy. Digestion 57 [Suppl]: 57–61
Otte A, Jermann E, Behe M, Goetze M, Bucher HC, Roser HW, Heppeler A, Mueller-Brand J, Maecke H. (1997) Dotatoc: a powerful new tool for receptor-mediated radionuclide therapy. Eur J Nucl Med 24: 792–795
Otte A, Mueller-Brand J, Delias S, Nitzsche EU, Hermann R, Maecke HR (1998) Yttrium-90- labelled somatostatin analogue for cancer treatment. Lancet 351: 417–418
Termanini B, Gibril F, Reynolds JC, Doppman JL, Chen CC, Stewart CA, Sutliff VE, Jensen RT (1997) Value of somatostatin receptor scintigraphy: a prospective study in gastrinoma of its effect on clinical management. Gastroenterology 112: 335–347
Virgolini I, Raderer M, Kurtaran, Angelberger P, Banyai S, Yang Q, Li S, Banyai M, Pidlich J, Niederle B, Scheithauer W, Valent P (1994) Vasoactive intestinal peptide receptor imaging for the localization of intestinal adenocarcinomas and endocrine tumors. N Engl J Med 331: 1116–1121
Author information
Authors and Affiliations
Editor information
Editors and Affiliations
Rights and permissions
Copyright information
© 2000 Springer-Verlag Berlin · Heidelberg
About this paper
Cite this paper
Krenning, E.P. et al. (2000). The Role of Radioactive Somatostatin and Its Analogues in the Control of Tumor Growth. In: Höffken, K., Kath, R. (eds) Peptides in Oncology III. Recent Results in Cancer Research, vol 153. Springer, Berlin, Heidelberg. https://doi.org/10.1007/978-3-642-59587-5_1
Download citation
DOI: https://doi.org/10.1007/978-3-642-59587-5_1
Publisher Name: Springer, Berlin, Heidelberg
Print ISBN: 978-3-642-64038-4
Online ISBN: 978-3-642-59587-5
eBook Packages: Springer Book Archive