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Communication

Simultaneous Visualization of 161Tb- and 177Lu-Labeled Somatostatin Analogues Using Dual-Isotope SPECT Imaging

1
Center for Radiopharmaceutical Sciences, Paul Scherrer Institute, 5232 Villigen-PSI, Switzerland
2
Radiochemistry, South African Nuclear Energy Corporation (Necsa), Brits 0240, South Africa
3
Institut Laue-Langevin, 38042 Grenoble, France
4
Department of Chemistry and Applied Biosciences, ETH Zurich, 8093 Zurich, Switzerland
5
Laboratory of Radiochemistry, Paul Scherrer Institute, 5232 Villigen-PSI, Switzerland
*
Author to whom correspondence should be addressed.
Academic Editor: Yann Seimbille
Pharmaceutics 2021, 13(4), 536; https://doi.org/10.3390/pharmaceutics13040536
Received: 31 January 2021 / Revised: 29 March 2021 / Accepted: 7 April 2021 / Published: 12 April 2021
(This article belongs to the Special Issue Targeted Radionuclide Therapy)
The decay of terbium-161 results in the emission of β¯-particles as well as conversion and Auger electrons, which makes terbium-161 interesting for therapeutic purposes. The aim of this study was to use dual-isotope SPECT imaging in order to demonstrate visually that terbium-161 and lutetium-177 are interchangeable without compromising the pharmacokinetic profile of the radiopharmaceutical. The 161Tb- and 177Lu-labeled somatostatin (SST) analogues DOTATOC (agonist) and DOTA-LM3 (antagonist) were tested in vitro to demonstrate equal properties regarding distribution coefficients and cell uptake into SST receptor-positive AR42J tumor cells. The radiopeptides were further investigated in AR42J tumor-bearing nude mice using the method of dual-isotope (terbium-161/lutetium-177) SPECT/CT imaging to enable the visualization of their distribution profiles in the same animal. Equal pharmacokinetic profiles were demonstrated for either of the two peptides, irrespective of whether it was labeled with terbium-161 or lutetium-177. Moreover, the visualization of the sub-organ distribution confirmed similar behavior of 161Tb- and 177Lu-labeled SST analogues. The data were verified in quantitative biodistribution studies using either type of peptide labeled with terbium-161 or lutetium-177. While the radionuclide did not have an impact on the organ distribution, this study confirmed previous data of a considerably higher tumor uptake of radiolabeled DOTA-LM3 as compared to the radiolabeled DOTATOC. View Full-Text
Keywords: terbium-161; lutetium-177; NET; antagonists; agonists; radionuclide therapy; dual-isotope SPECT terbium-161; lutetium-177; NET; antagonists; agonists; radionuclide therapy; dual-isotope SPECT
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MDPI and ACS Style

Borgna, F.; Barritt, P.; Grundler, P.V.; Talip, Z.; Cohrs, S.; Zeevaart, J.R.; Köster, U.; Schibli, R.; van der Meulen, N.P.; Müller, C. Simultaneous Visualization of 161Tb- and 177Lu-Labeled Somatostatin Analogues Using Dual-Isotope SPECT Imaging. Pharmaceutics 2021, 13, 536. https://doi.org/10.3390/pharmaceutics13040536

AMA Style

Borgna F, Barritt P, Grundler PV, Talip Z, Cohrs S, Zeevaart JR, Köster U, Schibli R, van der Meulen NP, Müller C. Simultaneous Visualization of 161Tb- and 177Lu-Labeled Somatostatin Analogues Using Dual-Isotope SPECT Imaging. Pharmaceutics. 2021; 13(4):536. https://doi.org/10.3390/pharmaceutics13040536

Chicago/Turabian Style

Borgna, Francesca, Patrick Barritt, Pascal V. Grundler, Zeynep Talip, Susan Cohrs, Jan R. Zeevaart, Ulli Köster, Roger Schibli, Nicholas P. van der Meulen, and Cristina Müller. 2021. "Simultaneous Visualization of 161Tb- and 177Lu-Labeled Somatostatin Analogues Using Dual-Isotope SPECT Imaging" Pharmaceutics 13, no. 4: 536. https://doi.org/10.3390/pharmaceutics13040536

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