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Article

Evaluation of a 68Ga-Labeled DOTA-Tetrazine as a PET Alternative to 111In-SPECT Pretargeted Imaging

1
Department of Clinical Physiology, Nuclear Medicine & PET, Rigshospitalet, Blegdamsvej 9, 2100 Copenhagen, Denmark
2
Cluster for Molecular Imaging, Department of Biomedical Sciences, University of Copenhagen, Blegdamsvej 3, 2200 Copenhagen, Denmark
3
Department of Drug Design and Pharmacology, University of Copenhagen, Jagtvej 162, 2100 Copenhagen, Denmark
4
Tagworks Pharmaceuticals, Geert Grooteplein Zuid 10, 6525 GA Nijmegen, The Netherlands
5
Department of Chemistry and Chemical Biology, McMaster University, 1280 Main St West, Hamilton, ON L8S 4M1, Canada
6
Pharmaceutical Chemistry and Radiopharmacy Department, School of Pharmacy, Shahid Beheshti University of Medical Sciences, PO Box 14155–6153, Tehran, Iran
*
Authors to whom correspondence should be addressed.
Patricia E. Edem and Jesper T. Jørgensen contributed equally to this work.
Academic Editors: Anne Roivainen and Xiang-Guo Li
Molecules 2020, 25(3), 463; https://doi.org/10.3390/molecules25030463
Received: 23 December 2019 / Revised: 14 January 2020 / Accepted: 15 January 2020 / Published: 22 January 2020
(This article belongs to the Special Issue Radiopharmaceuticals for PET Imaging - Issue A)
The bioorthogonal reaction between a tetrazine and strained trans-cyclooctene (TCO) has garnered success in pretargeted imaging. This reaction was first validated in nuclear imaging using an 111In-labeled 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA)-linked bispyridyl tetrazine (Tz) ([111In]In-DOTA-PEG11-Tz) and a TCO functionalized CC49 antibody. Given the initial success of this Tz, it has been paired with TCO functionalized small molecules, diabodies, and affibodies for in vivo pretargeted studies. Furthermore, the single photon emission tomography (SPECT) radionuclide, 111In, has been replaced with the β-emitter, 177Lu and α-emitter, 212Pb, both yielding the opportunity for targeted radiotherapy. Despite use of the ‘universal chelator’, DOTA, there is yet to be an analogue suitable for positron emission tomography (PET) using a widely available radionuclide. Here, a 68Ga-labeled variant ([68Ga]Ga-DOTA-PEG11-Tz) was developed and evaluated using two different in vivo pretargeting systems (Aln-TCO and TCO-CC49). Small animal imaging and ex vivo biodistribution studies were performed and revealed target specific uptake of [68Ga]Ga-DOTA-PEG11-Tz in the bone (3.7 %ID/g, knee) in mice pretreated with Aln-TCO and tumor specific uptake (5.8 %ID/g) with TCO-CC49 in mice bearing LS174 xenografts. Given the results of this study, [68Ga]Ga-DOTA-PEG11-Tz can serve as an alternative to [111In]In-DOTA-PEG11-Tz. View Full-Text
Keywords: tetrazine ligation; PET; SPECT; gallium-68; indium-11 tetrazine ligation; PET; SPECT; gallium-68; indium-11
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MDPI and ACS Style

Edem, P.E.; Jørgensen, J.T.; Nørregaard, K.; Rossin, R.; Yazdani, A.; Valliant, J.F.; Robillard, M.; Herth, M.M.; Kjaer, A. Evaluation of a 68Ga-Labeled DOTA-Tetrazine as a PET Alternative to 111In-SPECT Pretargeted Imaging. Molecules 2020, 25, 463. https://doi.org/10.3390/molecules25030463

AMA Style

Edem PE, Jørgensen JT, Nørregaard K, Rossin R, Yazdani A, Valliant JF, Robillard M, Herth MM, Kjaer A. Evaluation of a 68Ga-Labeled DOTA-Tetrazine as a PET Alternative to 111In-SPECT Pretargeted Imaging. Molecules. 2020; 25(3):463. https://doi.org/10.3390/molecules25030463

Chicago/Turabian Style

Edem, Patricia E.; Jørgensen, Jesper T.; Nørregaard, Kamilla; Rossin, Rafaella; Yazdani, Abdolreza; Valliant, John F.; Robillard, Marc; Herth, Matthias M.; Kjaer, Andreas. 2020. "Evaluation of a 68Ga-Labeled DOTA-Tetrazine as a PET Alternative to 111In-SPECT Pretargeted Imaging" Molecules 25, no. 3: 463. https://doi.org/10.3390/molecules25030463

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