A1 Refereed original research article in a scientific journal

64Cu- and 68Ga-Labelled [Nle14,Lys40(Ahx-NODAGA)NH2]-Exendin-4 for Pancreatic Beta Cell Imaging in Rats




SubtitleImaging Beta Cells with 64Cu- and 68Ga-Labelled NODAGA-Exendin-4

AuthorsMikkola Kirsi, Yim Cheng-Bin, Fagerholm Veronica, Ishizu Tamiko, Elomaa Viki-Veikko, Rajander Johan, Jurttila Jori, Saanijoki Tiina, Tolvanen Tuula, Tirri Marko, Gourni Eleni, Béhé Martin, Gotthardt Martin, Reubi Jean Claude, Mäcke Helmut, Roivainen Anne, Solin Olof, Nuutila Pirjo

PublisherSpringer US

Publication year2014

JournalMolecular Imaging and Biology

Journal acronymMIB

Volume16

Issue2

First page 255

Last page263

Number of pages9

ISSN1536-1632

eISSN1860-2002

DOIhttps://doi.org/10.1007/s11307-013-0691-2

Web address http://link.springer.com/article/10.1007/s11307-013-0691-2


Abstract


Purpose

Glucagon-like peptide-1 receptor (GLP-1R) is a molecular target for imaging of pancreatic beta cells. We compared the ability of [Nle14,Lys40(Ahx-NODAGA-64Cu)NH2]-exendin-4 ([64Cu]NODAGA-exendin-4) and [Nle14,Lys40(Ahx-NODAGA-68Ga)NH2]-exendin-4 ([68Ga]NODAGA-exendin-4) to detect native pancreatic islets in rodents.



Procedures

The stability, lipophilicity and affinity of the radiotracers to the GLP-1R were determined in vitro. The biodistribution of the tracers was assessed using autoradiography, ex vivo biodistribution and PET imaging. Estimates for human radiation dosimetry were calculated.



Results

We found GLP-1R-specific labelling of pancreatic islets. However, the pancreas could not be visualised in PET images. The highest uptake of the tracers was observed in the kidneys. Effective dose estimates for [64Cu]NODAGA-exendin-4 and [68Ga]NODAGA-exendin-4 were 0.144 and 0.012 mSv/MBq, respectively.



Conclusion

[64Cu]NODAGA-exendin-4 might be more effective for labelling islets than [68Ga]NODAGA-exendin-4. This is probably due to the lower specific radioactivity of [68Ga]NODAGA-exendin-4 compared to [64Cu]NODAGA-exendin-4. The radiation dose in the kidneys may limit the use of [64Cu]NODAGA-exendin-4 as a clinical tracer.



 



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