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Molecules 2016, 21(9), 1164; doi:10.3390/molecules21091164

Evaluation of the Enantiomer Specific Biokinetics and Radiation Doses of [18F]Fluspidine—A New Tracer in Clinical Translation for Imaging of σ1 Receptors

Helmholtz-Zentrum Dresden-Rossendorf, Institute of Radiopharmaceutical Cancer Research, Department of Neuroradiopharmaceuticals, Leipzig 04318, Germany
Department of Nuclear Medicine, University Hospital Leipzig, Leipzig 04103, Germany
Division of Brain Sciences, Department of Medicine, Hammersmith Hospital Campus, Imperial College London, London SW7 2AZ, UK
Pharmaceutical and Medicinal Chemistry, University Münster, Münster 48149, Germany
Integrated Research and Treatment Center (IFB) Adiposity Diseases, University Hospital Leipzig, Leipzig 04103, Germany
Author to whom correspondence should be addressed.
Academic Editor: Zhen Cheng
Received: 28 July 2016 / Revised: 22 August 2016 / Accepted: 26 August 2016 / Published: 1 September 2016
(This article belongs to the Special Issue Molecular Imaging Probes)
View Full-Text   |   Download PDF [949 KB, uploaded 1 September 2016]   |  


The enantiomers of [18F]fluspidine, recently developed for imaging of σ1 receptors, possess distinct pharmacokinetics facilitating their use in different clinical settings. To support their translational potential, we estimated the human radiation dose of (S)-(−)-[18F]fluspidine and (R)-(+)-[18F]fluspidine from ex vivo biodistribution and PET/MRI data in mice after extrapolation to the human scale. In addition, we validated the preclinical results by performing a first-in-human PET/CT study using (S)-(−)-[18F]fluspidine. Based on the respective time-activity curves, we calculated using OLINDA the particular organ doses (ODs) and effective doses (EDs). The ED values of (S)-(−)-[18F]fluspidine and (R)-(+)-[18F]fluspidine differed significantly with image-derived values obtained in mice with 12.9 μSv/MBq and 14.0 μSv/MBq (p < 0.025), respectively. A comparable ratio was estimated from the biodistribution data. In the human study, the ED of (S)-(−)-[18F]fluspidine was calculated as 21.0 μSv/MBq. Altogether, the ED values for both [18F]fluspidine enantiomers determined from the preclinical studies are comparable with other 18F-labeled PET imaging agents. In addition, the first-in-human study confirmed that the radiation risk of (S)-(−)-[18F]fluspidine imaging is within acceptable limits. However, as already shown for other PET tracers, the actual ED of (S)-(−)-[18F]fluspidine in humans was underestimated by preclinical imaging which needs to be considered in other first-in-human studies. View Full-Text
Keywords: image based internal dosimetry; [18F]fluspidine; preclinical hybrid PET/MRI; radiation safety; σ1 receptors image based internal dosimetry; [18F]fluspidine; preclinical hybrid PET/MRI; radiation safety; σ1 receptors

This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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Kranz, M.; Sattler, B.; Wüst, N.; Deuther-Conrad, W.; Patt, M.; Meyer, P.M.; Fischer, S.; Donat, C.K.; Wünsch, B.; Hesse, S.; Steinbach, J.; Brust, P.; Sabri, O. Evaluation of the Enantiomer Specific Biokinetics and Radiation Doses of [18F]Fluspidine—A New Tracer in Clinical Translation for Imaging of σ1 Receptors. Molecules 2016, 21, 1164.

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