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Article

The Use of a Non-Conventional Long-Lived Gallium Radioisotope 66Ga Improves Imaging Contrast of EGFR Expression in Malignant Tumours Using DFO-ZEGFR:2377 Affibody Molecule

1
Department of Immunology, Genetics and Pathology, Uppsala University, 75185 Uppsala, Sweden
2
GE Healthcare, GEMS PET Systems, 75015 Uppsala, Sweden
3
Department of Medicinal Chemistry, Uppsala University, 75183 Uppsala, Sweden
4
Department of Medical Physics, Uppsala University Hospital, 75185 Uppsala, Sweden
5
Department of Protein Science, KTH Royal Institute of Technology, 10691 Stockholm, Sweden
6
Research Centrum for Oncotheranostics, Research School of Chemistry and Applied Biomedical Sciences, Tomsk Polytechnic University, 634050 Tomsk, Russia
*
Author to whom correspondence should be addressed.
Academic Editor: Simone U. Dalm
Pharmaceutics 2021, 13(2), 292; https://doi.org/10.3390/pharmaceutics13020292
Received: 12 January 2021 / Revised: 13 February 2021 / Accepted: 19 February 2021 / Published: 23 February 2021
Epidermal growth factor receptor (EGFR) is overexpressed in many malignancies. EGFR-targeted therapy extends survival of patients with disseminated cancers. Radionuclide molecular imaging of EGFR expression would make EGFR-directed treatment more personalized and therefore more efficient. A previous study demonstrated that affibody molecule [68Ga]Ga-DFO-ZEGFR:2377 permits specific positron-emission tomography (PET) imaging of EGFR expression in xenografts at 3 h after injection. We anticipated that imaging at 24 h after injection would provide higher contrast, but this is prevented by the short half-life of 68Ga (67.6 min). Here, we therefore tested the hypothesis that the use of the non-conventional long-lived positron emitter 66Ga (T1/2 = 9.49 h, β+ = 56.5%) would permit imaging with higher contrast. 66Ga was produced by the 66Zn(p,n)66Ga nuclear reaction and DFO-ZEGFR:2377 was efficiently labelled with 66Ga with preserved binding specificity in vitro and in vivo. At 24 h after injection, [66Ga]Ga-DFO-ZEGFR:2377 provided 3.9-fold higher tumor-to-blood ratio and 2.3-fold higher tumor-to-liver ratio than [68Ga]Ga-DFO-ZEGFR:2377 at 3 h after injection. At the same time point, [66Ga]Ga-DFO-ZEGFR:2377 provided 1.8-fold higher tumor-to-blood ratio, 3-fold higher tumor-to-liver ratio, 1.9-fold higher tumor-to-muscle ratio and 2.3-fold higher tumor-to-bone ratio than [89Zr]Zr-DFO-ZEGFR:2377. Biodistribution data were confirmed by whole body PET combined with magnetic resonance imaging (PET/MRI). The use of the positron emitter 66Ga for labelling of DFO-ZEGFR:2377 permits PET imaging of EGFR expression at 24 h after injection and improves imaging contrast. View Full-Text
Keywords: epidermal growth factor receptor; affibody molecule; PET imaging; gallium-66; ZEGFR:2377; A431 xenograft epidermal growth factor receptor; affibody molecule; PET imaging; gallium-66; ZEGFR:2377; A431 xenograft
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MDPI and ACS Style

Oroujeni, M.; Xu, T.; Gagnon, K.; Rinne, S.S.; Weis, J.; Garousi, J.; Andersson, K.G.; Löfblom, J.; Orlova, A.; Tolmachev, V. The Use of a Non-Conventional Long-Lived Gallium Radioisotope 66Ga Improves Imaging Contrast of EGFR Expression in Malignant Tumours Using DFO-ZEGFR:2377 Affibody Molecule. Pharmaceutics 2021, 13, 292. https://doi.org/10.3390/pharmaceutics13020292

AMA Style

Oroujeni M, Xu T, Gagnon K, Rinne SS, Weis J, Garousi J, Andersson KG, Löfblom J, Orlova A, Tolmachev V. The Use of a Non-Conventional Long-Lived Gallium Radioisotope 66Ga Improves Imaging Contrast of EGFR Expression in Malignant Tumours Using DFO-ZEGFR:2377 Affibody Molecule. Pharmaceutics. 2021; 13(2):292. https://doi.org/10.3390/pharmaceutics13020292

Chicago/Turabian Style

Oroujeni, Maryam, Tianqi Xu, Katherine Gagnon, Sara S. Rinne, Jan Weis, Javad Garousi, Ken G. Andersson, John Löfblom, Anna Orlova, and Vladimir Tolmachev. 2021. "The Use of a Non-Conventional Long-Lived Gallium Radioisotope 66Ga Improves Imaging Contrast of EGFR Expression in Malignant Tumours Using DFO-ZEGFR:2377 Affibody Molecule" Pharmaceutics 13, no. 2: 292. https://doi.org/10.3390/pharmaceutics13020292

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