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European Journal of Nuclear Medicine and Molecular Imaging

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01-04-2005 | Occasional Survey

Radiolabelling DOTA-peptides with ⁶⁸Ga

Authors: Wouter A. P. Breeman, Marion de Jong, Erik de Blois, Bert F. Bernard, Mark Konijnenberg, Eric P. Krenning

Published in: European Journal of Nuclear Medicine and Molecular Imaging | Issue 4/2005

Abstract

Purpose

A new field of interest is the application of ⁶⁸Ga-labelled DOTA-conjugated peptides for positron emission tomography (PET). The commercially available or house-made generators require time-consuming and tedious handling of the eluate. Radiolabelling at high specific activities without further purification is not possible, while high specific activities are necessary for peptides that potentially display pharmacological side-effects. Here we present the practical aspects and the results of radiolabelling DOTA-peptides with a TiO₂-based commercially available ⁶⁸Ge/⁶⁸Ga generator.

Methods

Reaction kinetics and parameters influencing the incorporation of the radionuclide at the highest achievable specific activity were investigated. Since high finger doses were anticipated during handling of the high beta-energy emitter⁶⁸Ga, finger dosimetric measurements were performed during radiolabelling and in vivo administration.

Results

Fractionated elution of the generator revealed that 80% of the radioactivity was recovered in 1 ml. Bi- and trivalent ionic contaminants that compete for the incorporation of the radionuclide were below 50 nM; thus further tedious and time-consuming purification was avoided. Radiolabelling was performed at pH 3.5–4. Plastic shielding (≥7-mm wall thickness) around the syringe during administration effectively eliminated the positrons. In rats ⁶⁸GaCl₃ had slow clearance from blood, while ⁶⁸Ga-EDTA was rapidly cleared via the kidneys. Uptake of ⁶⁸Ga-DOTATOC in somatostatin receptor-positive tissues was high, with no significant difference between 1 and 4 h post injection.

Conclusion

DOTA-peptides for PET imaging can be labelled with ⁶⁸Ga up to specific activities of 1 GBq per nmol within 20 min, enabling the clinical application of peptides that display potential pharmacological side-effects.

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Title: Radiolabelling DOTA-peptides with 68Ga
Authors: Wouter A. P. Breeman
Marion de Jong
Erik de Blois
Bert F. Bernard
Mark Konijnenberg
Eric P. Krenning
Publication date: 01-04-2005
Publisher: Springer-Verlag
Published in: European Journal of Nuclear Medicine and Molecular Imaging / Issue 4/2005
Print ISSN: 1619-7070
Electronic ISSN: 1619-7089
DOI: https://doi.org/10.1007/s00259-004-1702-y

Keynote webinar | Spotlight on medication adherence

Springer Medicine

Radiolabelling DOTA-peptides with ⁶⁸Ga

Abstract

Purpose

Methods

Results

Conclusion

Keynote webinar | Spotlight on medication adherence

Springer Medicine

Abstract

Purpose

Methods

Results

Conclusion

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