Comparison of three radiolabelled peptide analogues for CCK-2 receptor scintigraphy in medullary thyroid carcinoma

Purpose Cholecystokinin 2 (CCK-2) receptor overexpression has been demonstrated in a high percentage of medullary thyroid carcinomas (MTC). Analogous to somatostatin receptors, CCK-2 receptors might be viable targets for radionuclide scintigraphy and/or radionuclide therapy. Several CCK-2 receptor-b...

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Bibliographic Details
Published in:European journal of nuclear medicine and molecular imaging 2009-08, Vol.36 (8), p.1265-1272
Main Authors: Fröberg, Alida C., de Jong, Marion, Nock, Berthold A., Breeman, Wout A. P., Erion, Jack L., Maina, Theodosia, Verdijsseldonck, Marion, de Herder, Wouter W., van der Lugt, Aad, Kooij, Peter P. M., Krenning, Eric P.
Format: Article
Language:English
Subjects:
Adolescent
Adult
Aged
Amino Acid Sequence
Brain Stem Neoplasms - diagnostic imaging
Brain Stem Neoplasms - metabolism
Cancer
Cardiology
Female
Humans
Imaging
Indium Radioisotopes
Isotope Labeling
Male
Medical diagnosis
Medical imaging
Medicine
Medicine & Public Health
Middle Aged
Nuclear Medicine
Oligopeptides - chemistry
Oligopeptides - metabolism
Oligopeptides - pharmacokinetics
Oncology
Original
Original Article
Orthopedics
Peptides
Radioactivity
Radiology
Radionuclide Imaging
Receptor, Cholecystokinin B - metabolism
Spleen - metabolism
Thyroid diseases
Thyroid Neoplasms - diagnostic imaging
Thyroid Neoplasms - metabolism
Tissue Distribution
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Summary:Purpose Cholecystokinin 2 (CCK-2) receptor overexpression has been demonstrated in a high percentage of medullary thyroid carcinomas (MTC). Analogous to somatostatin receptors, CCK-2 receptors might be viable targets for radionuclide scintigraphy and/or radionuclide therapy. Several CCK-2 receptor-binding radiopeptides have been developed, and some have been carried through into clinical studies. However, these studies are mostly limited and difficult to compare. The aim of this study was to evaluate the diagnostic and therapeutic potential of three promising CCK-2 receptor-binding radiopeptides in patients with MTC. Methods 111 In-DOTA-( D )Asp-Tyr-Nle-Gly-Trp-Nle-Asp-Phe-NH 2 ( 111 In-DOTA-CCK), a CCK analogue, and the gastrin-based ligands 99m Tc-N 4 -Gly-( D )Glu-(Glu) 5 -Ala-Tyr-Gly-Trp-Met-Asp-Phe-NH 2 ( 99m Tc-demogastrin 2) and 111 In-DOTA-( D )Glu-Ala-Tyr-Gly-Trp-Met-Asp-Phe-NH 2 ( 111 In-DOTA-MG11) were each administered to the same group of six patients. Planar images made at 3–5, 7 and 24 h p.i. were used for comparison of tumour visualisation and renal uptake. Results 99m Tc-demogastrin 2 scintigraphy visualised all known lesions and new lesions in four of six patients. 111 In-DOTA-CCK and 111 In-DOTA-MG11 on the other hand missed several lesions; tumour uptake of these two radiopharmaceuticals was quite low. Comparison of retention of renal activity showed no major differences between the three radiopeptides. Conclusion 99m Tc-demogastrin 2 scintigraphy appeared most promising as a diagnostic tool in patients with MTC. Further studies are required to evaluate its value in patient management. Direct comparisons of the compounds studied strongly suggests that 111 In-DOTA-CCK and 111 In-DOTA-MG11 have less potential as imaging agents than 99m Tc-demogastrin 2. These DOTA-linked compounds are considered unlikely to be useful for radionuclide therapy because of low tumour uptake.
ISSN:1619-7070
1619-7089
DOI:10.1007/s00259-009-1098-9