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European Journal of Nuclear Medicine and Molecular Imaging
Published in: European Journal of Nuclear Medicine and Molecular Imaging 10/2020

01-09-2020 | Letter to the Editor

Anatomy of 18F-GE180, a failed radioligand for the TSPO protein

Authors: Paolo Zanotti-Fregonara, Belen Pascual, Robert C. Rostomily, Gaia Rizzo, Mattia Veronese, Joseph C. Masdeu, Federico Turkheimer

Published in: European Journal of Nuclear Medicine and Molecular Imaging | Issue 10/2020

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Excerpt

Few translocator protein (TSPO) radioligands have been rapidly translated into human clinical research with the enthusiasm of 18F-GE180. Within two years from the publication of the first kinetic analyses in humans [1, 2], four clinical studies in patients with brain tumors [3, 4] and multiple sclerosis [5, 6], at least three case-reports [7‐9], and one editorial praising the “definitely superior” imaging qualities of 18F-GE180 [10] appeared in the literature. …
Literature
1.
Fan Z, Calsolaro V, Atkinson RA, Femminella GD, Waldman A, Buckley C, et al. Flutriciclamide (18F-GE180) PET: first-in-human PET study of novel third-generation in vivo marker of human translocator protein. J Nucl Med. 2016;57:1753–9.CrossRef
2.
Feeney C, Scott G, Raffel J, Roberts S, Coello C, Jolly A, et al. Kinetic analysis of the translocator protein positron emission tomography ligand [18F]GE-180 in the human brain. Eur J Nucl Med Mol Imaging. 2016;43:2201–10.CrossRef
3.
Albert NL, Unterrainer M, Fleischmann DF, Lindner S, Vettermann F, Brunegraf A, et al. TSPO PET for glioma imaging using the novel ligand 18F-GE-180: first results in patients with glioblastoma. Eur J Nucl Med Mol Imaging. 2017.
4.
Unterrainer M, Fleischmann DF, Diekmann C, Vomacka L, Lindner S, Vettermann F, et al. Comparison of (18)F-GE-180 and dynamic (18)F-FET PET in high grade glioma: a double-tracer pilot study. Eur J Nucl Med Mol Imaging. 2018.
5.
Unterrainer M, Mahler C, Vomacka L, Lindner S, Havla J, Brendel M, et al. TSPO PET with [(18)F]GE-180 sensitively detects focal neuroinflammation in patients with relapsing-remitting multiple sclerosis. Eur J Nucl Med Mol Imaging. 2018;45:1423–31.CrossRef
6.
Vomacka L, Albert NL, Lindner S, Unterrainer M, Mahler C, Brendel M, et al. TSPO imaging using the novel PET ligand [(18)F]GE-180: quantification approaches in patients with multiple sclerosis. EJNMMI Res. 2017;7:89.CrossRef
7.
Unterrainer M, Fleischmann DF, Lindner S, Brendel M, Rupprecht R, Tonn JC, et al. Detection of cerebrospinal fluid dissemination of recurrent glioblastoma using TSPO-PET with 18F-GE-180. Clin Nucl Med. 2018;43:518–9.CrossRef
8.
Mahler C, Unterrainer M, Muth C, Egensperger R, Vomacka L, Lindner S, et al. Imaging microglial activation in tacrolimus-associated CNS vasculitis with translocator protein PET. Neurology. 2018;91:936–7.CrossRef
9.
Schoberl F, Levin J, Remi J, Goldschagg N, Eren O, Okamura N, et al. IgLON5: a case with predominant cerebellar tau deposits and leptomeningeal inflammation. Neurology. 2018;91:180–2.CrossRef
10.
Langen KJ, Willuweit A. TSPO PET using (18)F-GE-180: a new perspective in neurooncology? Eur J Nucl Med Mol Imaging. 2017;44:2227–9.CrossRef
11.
Zanotti-Fregonara P, Veronese M, Pascual B, Rostomily RC, Turkheimer F, Masdeu JC. The validity of 18 F-GE180 as a TSPO imaging agent. Eur J Nucl Med Mol I. 2019;46:1205–7.CrossRef
12.
Sridharan S, Raffel J, Nandoskar A, Record C, Brooks DJ, Owen D, et al. Confirmation of specific binding of the 18-kDa translocator protein (TSPO) radioligand [(18)F]GE-180: a blocking study using XBD173 in multiple sclerosis normal appearing white and grey matter. Mol Imaging Biol. 2019.
13.
Unterrainer M, Fleischmann DF, Vettermann F, Ruf V, Kaiser L, Nelwan D, et al. TSPO PET, tumour grading and molecular genetics in histologically verified glioma: a correlative (18)F-GE-180 PET study. Eur J Nucl Med Mol Imaging. 2019.
14.
Nicholas R, Brooks D, Owen D. In response to letter from Fregonara et al. 2019. Mol Imaging Biol. 2019;22(1):13–14.
15.
Visi E, Hinz R, Punter M, Majid A, Gerhard A, Herholz K. Positron emission tomography to image cerebral neuroinflammation in ischaemic stroke: a pilot study. In: Efficacy and Mechanism Evaluation, No 71. Southampton: NIHR Journals Library; 2020.
16.
Hatakeyama T, Kawai N, Nishiyama Y, Yamamoto Y, Sasakawa Y, Ichikawa T, et al. 11C-methionine (MET) and 18F-fluorothymidine (FLT) PET in patients with newly diagnosed glioma. Eur J Nucl Med Mol Imaging. 2008;35:2009–17.CrossRef
17.
Nowosielski M, DiFranco MD, Putzer D, Seiz M, Recheis W, Jacobs AH, et al. An intra-individual comparison of MRI, [18F]-FET and [18F]-FLT PET in patients with high-grade gliomas. PLoS One. 2014;9:e95830.CrossRef
18.
Albert NL, Unterrainer M, Brendel M, Kaiser L, Zweckstetter M, Cumming P, et al. In response to: the validity of (18)F-GE180 as a TSPO imaging agent. Eur J Nucl Med Mol Imaging. 2019.
19.
Owen DR, Yeo AJ, Gunn RN, Song K, Wadsworth G, Lewis A, et al. An 18-kDa translocator protein (TSPO) polymorphism explains differences in binding affinity of the PET radioligand PBR28. J Cereb Blood Flow Metab. 2012;32:1–5.CrossRef
20.
Wadsworth H, Jones PA, Chau WF, Durrant C, Fouladi N, Passmore J, et al. [(1)(8)F]GE-180: a novel fluorine-18 labelled PET tracer for imaging translocator protein 18 kDa (TSPO). Bioorg Med Chem Lett. 2012;22:1308–13.CrossRef
21.
Boutin H, Murray K, Pradillo J, Maroy R, Smigova A, Gerhard A, et al. 18F-GE-180: a novel TSPO radiotracer compared to 11C-R-PK11195 in a preclinical model of stroke. Eur J Nucl Med Mol Imaging. 2015;42:503–11.CrossRef
22.
de Groot M, Patel N, Manavaki R, Janiczek RL, Bergstrom M, Ostor A, et al. Quantifying disease activity in rheumatoid arthritis with the TSPO PET ligand (18)F-GE-180 and comparison with (18)F-FDG and DCE-MRI. EJNMMI Res. 2019;9:113.CrossRef
23.
Narayan N, Owen DR, Mandhair H, Smyth E, Carlucci F, Saleem A, et al. Translocator protein as an imaging marker of macrophage and stromal activation in rheumatoid arthritis pannus. J Nucl Med. 2018;59:1125–32.CrossRef
24.
van der Laken CJ, Elzinga EH, Kropholler MA, Molthoff CF, van der Heijden JW, Maruyama K, et al. Noninvasive imaging of macrophages in rheumatoid synovitis using 11C-(R)-PK11195 and positron emission tomography. Arthritis Rheum. 2008;58:3350–5.CrossRef
25.
Zanotti-Fregonara P, Pascual B, Rizzo G, Yu M, Pal N, Beers D, et al. Head-to-head comparison of 11C-PBR28 and 18F-GE180 for quantification of the translocator protein in the human brain. J Nucl Med. 2018;59:1260–6.CrossRef
26.
Cumming P, Burgher B, Patkar O, Breakspear M, Vasdev N, Thomas P, et al. Sifting through the surfeit of neuroinflammation tracers. J Cereb Blood Flow Metab. 2018;38:204–24.CrossRef
27.
Zanotti-Fregonara P, Zhang Y, Jenko KJ, Gladding RL, Zoghbi SS, Fujita M, et al. Synthesis and evaluation of translocator 18 kDa protein (TSPO) positron emission tomography (PET) radioligands with low binding sensitivity to human single nucleotide polymorphism rs6971. ACS Chem Neurosci. 2014;5:963–71.CrossRef
Metadata
Title
Anatomy of 18F-GE180, a failed radioligand for the TSPO protein
Authors
Paolo Zanotti-Fregonara
Belen Pascual
Robert C. Rostomily
Gaia Rizzo
Mattia Veronese
Joseph C. Masdeu
Federico Turkheimer
Publication date
01-09-2020
Publisher
Springer Berlin Heidelberg
Published in
European Journal of Nuclear Medicine and Molecular Imaging / Issue 10/2020
Print ISSN: 1619-7070
Electronic ISSN: 1619-7089
DOI
https://doi.org/10.1007/s00259-020-04732-y

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