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

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References

  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.

    Article  CAS  Google Scholar 

  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.

    Article  CAS  Google Scholar 

  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.

    Article  Google Scholar 

  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.

    Article  Google Scholar 

  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.

    Article  Google Scholar 

  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.

    Article  Google Scholar 

  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.

    Article  Google Scholar 

  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.

    Article  Google Scholar 

  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.

    Article  Google Scholar 

  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.

    Google Scholar 

  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.

    Article  CAS  Google Scholar 

  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.

    Article  Google Scholar 

  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.

    Article  CAS  Google Scholar 

  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.

    Article  CAS  Google Scholar 

  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.

    Article  CAS  Google Scholar 

  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.

    Article  Google Scholar 

  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.

    Article  CAS  Google Scholar 

  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.

    Article  Google Scholar 

  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.

    Article  CAS  Google Scholar 

  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.

    Article  Google Scholar 

  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.

    Article  CAS  Google Scholar 

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Author notes

  1. Paolo Zanotti-Fregonara

    Present address: Molecular Imaging Branch, National Institute of Mental Health, Bethesda, MD, USA

Authors and Affiliations

  1. Houston Methodist Research Institute, Houston, TX, USA

    Paolo Zanotti-Fregonara, Belen Pascual, Robert C. Rostomily & Joseph C. Masdeu

  2. Invicro UK, London, UK

    Gaia Rizzo

  3. Department of Neuroimaging, Institute of Psychiatry, Psychology and Neuroscience, King’s College London, London, UK

    Mattia Veronese & Federico Turkheimer

Authors
  1. Paolo Zanotti-Fregonara
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  2. Belen Pascual
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  3. Robert C. Rostomily
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  4. Gaia Rizzo
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  5. Mattia Veronese
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  6. Joseph C. Masdeu
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  7. Federico Turkheimer
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Corresponding author

Correspondence to Paolo Zanotti-Fregonara.

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All procedures performed in studies involving human participants were in accordance with the ethical standards of the institutional research committee and with the principles of the 1964 Declaration of Helsinki and its later amendments or comparable ethical standards.

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The authors declare that they have no conflict of interest.

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Zanotti-Fregonara, P., Pascual, B., Rostomily, R.C. et al. Anatomy of 18F-GE180, a failed radioligand for the TSPO protein. Eur J Nucl Med Mol Imaging 47, 2233–2236 (2020). https://doi.org/10.1007/s00259-020-04732-y

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  • DOI: https://doi.org/10.1007/s00259-020-04732-y

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