68Ga-labelled exendin-3, a new agent for the detection of Insulinomas with PET

European Journal of Nuclear Medicine and Molecular Imaging

Volumn 37, Issue 7, 2010, Pages 1345-1355

  Brom, Maarten ^a   Oyen, Wim J G ^a   Joosten, Lieke ^a   Gotthardt, Martin ^a   Boerman, Otto C ^a  

^a RADBOUD UNIVERSITY MEDICAL CENTER   (Netherlands)

Author keywords

Exendin; GLP 1 receptor; Imaging; Insulinoma; PET; SPECT

Indexed keywords

GLUCAGON LIKE PEPTIDE 1 RECEPTOR; LYSINE 40 1,4,7,10 TETRAAZACYCLODODECANE 1,4,7,10 TETRAACETIC ACID EXENDIN 3 GA 68; LYSINE 40 1,4,7,10 TETRAAZACYCLODODECANE 1,4,7,10 TETRAACETIC ACID EXENDIN 3 IN 111; LYSINE 40 PENTETATE EXENDIN 3 IN 111; LYSINE 40 PENTETATE EXENDIN 4 IN 111; RADIOPHARMACEUTICAL AGENT; UNCLASSIFIED DRUG; 1,4,7,10 TETRAAZACYCLODODECANE 1,4,7,10 TETRAACETIC ACID; 1,4,7,10-TETRAAZACYCLODODECANE- 1,4,7,10-TETRAACETIC ACID; DIAGNOSTIC AGENT; EXENDIN 3; GALLIUM; LYSINE; PENTETIC ACID; PEPTIDE; SINGLE HETEROCYCLIC RINGS;

ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL MODEL; ANIMAL TISSUE; ARTICLE; CONTROLLED STUDY; DRUG DETERMINATION; DRUG DISTRIBUTION; DRUG DOSE ESCALATION; DRUG INHIBITION; FEMALE; IC 50; IN VITRO STUDY; IN VIVO STUDY; INSULINOMA; ISOTOPE LABELING; KIDNEY; MOUSE; NONHUMAN; PANCREAS; POSITRON EMISSION TOMOGRAPHY; PROTEIN EXPRESSION; RAT; TUMOR CELL; AMINO ACID SEQUENCE; ANIMAL; CHEMISTRY; DOSE RESPONSE; INJECTION; KINETICS; METABOLISM; METHODOLOGY; MOLECULAR GENETICS; SCINTISCANNING; TRANSPORT AT THE CELLULAR LEVEL; TUMOR CELL LINE;

AMINO ACID SEQUENCE; ANIMALS; BIOLOGICAL TRANSPORT; CELL LINE, TUMOR; DOSE-RESPONSE RELATIONSHIP, DRUG; FEMALE; GALLIUM RADIOISOTOPES; HETEROCYCLIC COMPOUNDS, 1-RING; INHIBITORY CONCENTRATION 50; INJECTIONS; INSULINOMA; KINETICS; LYSINE; MICE; MOLECULAR SEQUENCE DATA; PENTETIC ACID; PEPTIDES; POSITRON-EMISSION TOMOGRAPHY; RATS;

EID: 77954955137     PISSN: 16197070     EISSN: None     Source Type: Journal    
DOI: 10.1007/s00259-009-1363-y     Document Type: Article

References (25)

1. Modlin IM, Tang LH. Approaches to the diagnosis of gut neuroendocrine tumors: the last word (today). Gastroenterology 1997;112:583-90.
2. Krenning EP, Kwekkeboom DJ, Bakker WH, Breeman WA, Kooij PP, Oei HY, et al. 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;20:716-31.
3. Joseph K, Stapp J, Reinecke J, Skamel HJ, Hoffken H, Benning R, et al. Receptor scintigraphy using 111In-pentetreotide in endocrine gastroenteropancreatic tumors. Nuklearmedizin 1993;32:299-305. (Pubitemid 24021454)
4. Abboud B, Boujaoude J. Occult sporadic insulinoma: localization and surgical strategy. World J Gastroenterol 2008;14:657-65.
5. Jackson JE. Angiography and arterial stimulation venous sampling in the localization of pancreatic neuroendocrine tumours. Best Pract Res Clin Endocrinol Metab 2005;19:229-39.
6. Reubi JC, Waser B. Concomitant expression of several peptide receptors in neuroendocrine tumours: molecular basis for in vivo multireceptor tumour targeting. Eur J Nucl Med Mol Imaging 2003;30:781-93.
7. Gotthardt M, Fischer M, Naeher I, Holz JB, Jungclas H, Fritsch HW, et al. Use of the incretin hormone glucagon-like peptide-1 (GLP-1) for the detection of insulinomas: initial experimental results. Eur J Nucl Med Mol Imaging 2002;29:597-606.
8. Singh G, Eng J, Raufman JP. Use of 125I-[Y39]exendin-4 to characterize exendin receptors on dispersed pancreatic acini and gastric chief cells from guinea pig. Regul Pept 1994;53:47-59.
9. Hassan M, Eskilsson A, Nilsson C, Jonsson C, Jacobsson H, Refai E, et al. In vivo dynamic distribution of 131I-glucagon-like peptide-1 (7-36) amide in the rat studied by gamma camera. Nucl Med Biol 1999;26:413-20.
10. Gotthardt M, Boermann OC, Behr TM, Behe MP, Oyen WJ. Development and clinical application of peptide-based radio-pharmaceuticals. Curr Pharm Des 2004;10:2951-63.
11. Goke R, Larsen PJ, Mikkelsen JD, Sheikh SP. Distribution of GLP-1 binding sites in the rat brain: evidence that exendin-4 is a ligand of brain GLP-1 binding sites. Eur J Neurosci 1995;7:2294-300.
12. Wild D, Behe M, Wicki A, Storch D, Waser B, Gotthardt M, et al. [Lys40 (Ahx-DTPA-111In) NH2]exendin-4, a very promising ligand for glucagon-like peptide-1 (GLP-1) receptor targeting. J Nucl Med 2006;47:2025-33.
13. Gotthardt M, Lalyko G, van Eerd-Vismale J, Keil B, Schurrat T, Hower M, et al. A new technique for in vivo imaging of specific GLP-1 binding sites: first results in small rodents. Regul Pept 2006;137:162-7.
14. Wicki A, Wild D, Storch D, Seemayer C, Gotthardt M, Behe M, et al. [Lys40 (Ahx-DTPA-111In) NH2]-Exendin-4 is a highly efficient radiotherapeutic for glucagon-like peptide-1 receptor-targeted therapy for insulinoma. Clin Cancer Res 2007;13:3696-705.
15. Wild D, Macke H, Christ E, Gloor B, Reubi JC. Glucagon-like peptide 1-receptor scans to localize occult insulinomas. N Engl J Med 2008;359:766-8.
16. Asfari M, Janjic D, Meda P, Li G, Halban PA, Wollheim CB. Establishment of 2-mercaptoethanol-dependent differentiated insulin-secreting cell lines. Endocrinology 1992;130:167-78.
17. Laverman P, Roosenburg S, Gotthardt M, Park J, Oyen WJ, de Jong M, et al. Targeting of a CCK (2) receptor splice variant with (111) In-labelled cholecystokinin-8 (CCK8) and (111) In-labelled minigastrin. Eur J Nucl Med Mol Imaging 2008;35:386-92.
18. Kauhanen S, Seppanen M, Minn H, Gullichsen R, Salonen A, Alanen K, et al. Fluorine-18-L-dihydroxyphenylalanine (18F-DOPA) positron emission tomography as a tool to localize an insulinoma or beta-cell hyperplasia in adult patients. J Clin Endocrinol Metab 2007;92:1237-44.
19. Buchmann I, Henze M, Engelbrecht S, Eisenhut M, Runz A, Schafer M, et al. Comparison of 68Ga-DOTATOC PET and 111In-DTPAOC (Octreoscan) SPECT in patients with neuroendocrine tumours. Eur J Nucl Med Mol Imaging 2007;34:1617-26.
20. Kowalski J, Henze M, Schuhmacher J, Macke HR, Hofmann M, Haberkorn U. Evaluation of positron emission tomography imaging using [68Ga]-DOTA-D Phe (1)-Tyr (3)-octreotide in comparison to [111In]-DTPAOC SPECT. First results in patients with neuroendocrine tumors. Mol Imaging Biol 2003;5:42-8.
21. van Dalen JA, Visser EP, Laverman P, Vogel WV, Oyen W J G, Corstens F H M, et al. Effect of the positron range on the spatial resolution of a new generation pre-clinical PET using fluorine-18, gallium-68, zirconium-89 and iodine-124. Eur J Nucl Med Mol Imaging 2007;34: S228-S.
22. Reubi JC, Schar JC, Waser B, Wenger S, Heppeler A, Schmitt JS, et al. Affinity profiles for human somatostatin receptor subtypes SST1-SST5 of somatostatin radiotracers selected for scintigraphic and radiotherapeutic use. Eur J Nucl Med 2000;27:273-82.
23. Antunes P, Ginj M, Zhang H, Waser B, Baum RP, Reubi JC, et al. Are radiogallium-labelled DOTA-conjugated somatostatin ana-logues superior to those labelled with other radiometals? Eur J Nucl Med Mol Imaging 2007;34:982-93.
24. Breeman WA, de Jong M, de Blois E, Bernard BF, Konijnenberg M, Krenning EP. Radiolabelling DOTA-peptides with 68Ga. Eur J Nucl Med Mol Imaging 2005;32:478-85.
25. Brom M, Baumeister P, Melis M, Laverman P, Joosten L, Behe M, et al. Determination of the beta-cell mass by SPECT imaging with In-111-DTPA-Exendin-3 in rats. J Nucl Med 2009;50(Suppl 2):147.