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First evaluation of PET-based human biodistribution and radiation dosimetry of 11C-BU99008, a tracer for imaging the imidazoline2 binding site

Authors
  • Venkataraman, Ashwin V.1, 2
  • Keat, Nicholas3
  • Myers, James F.1
  • Turton, Samuel1
  • Mick, Inge1
  • Gunn, Roger N.3, 2
  • Rabiner, Eugenii A.3
  • Passchier, Jan3
  • Parker, Christine A.1, 4
  • Tyacke, Robin J.1
  • Nutt, David J.1
  • 1 Imperial College London, Neuropsychopharmacology Unit, Centre for Psychiatry, Division of Brain Sciences, 5th Floor Burlington Danes Building, Hammersmith Hospital campus, 160 Du Cane Road, London, W12 0NN, UK , London (United Kingdom)
  • 2 Restorative Neurosciences, Imperial College London, Burlington Danes Building, Hammersmith Hospital campus, 160 Du Cane Road, London, W12 0NN, UK , London (United Kingdom)
  • 3 Hammersmith Hospital, Imanova Limited, Imperial College London, Burlington Danes Building, Du Cane Road, London, W12 0NN, UK , London (United Kingdom)
  • 4 Experimental Medicine Imaging, GlaxoSmithKline Research & Development Limited, Gunnels Wood Road, Stevenage, SG1 2NY, UK , Stevenage (United Kingdom)
Type
Published Article
Journal
EJNMMI Research
Publisher
Springer (Biomed Central Ltd.)
Publication Date
Jul 30, 2018
Volume
8
Issue
1
Identifiers
DOI: 10.1186/s13550-018-0429-x
Source
Springer Nature
Keywords
License
Green

Abstract

BackgroundWe measured whole body distribution of 11C-BU99008, a new PET biomarker for non-invasive identification of the imidazoline2 binding site. The purpose of this phase I study was to evaluate the biodistribution and radiation dosimetry of 11C-BU99008 in healthy human subjects.MethodsA single bolus injection of 11C-BU99008 (296 ± 10.5 MBq) was administered to four healthy subjects who underwent whole-body PET/CT over 120 min from the cranial vertex to the mid-thigh. Volumes of interest were drawn around visually identifiable source organs to generate time-activity curves (TAC). Residence times were determined from time-activity curves. Absorbed doses to individual organs and the whole body effective dose were calculated using OLINDA/EXM 1.1 for each subject.ResultsThe highest measured activity concentration was in the kidney and spleen. The longest residence time was in the muscle at 0.100 ± 0.023 h, followed by the liver at 0.067 ± 0.015 h and lungs at 0.052 ± 0.010 h. The highest mean organ absorbed dose was within the heart wall (0.028 ± 0.002 mGy/MBq), followed by the kidneys (0.026 ± 0.005 mGy/MBq). The critical organ was the heart wall. The total mean effective dose averaged over subjects was estimated to be 0.0056 ± 0.0004 mSv/MBq for an injection of 11C-BU99008.ConclusionsThe biodistribution of 11C-BU99008 has been shown here for the first time in humans. Our dosimetry data showed the total mean effective dose over all subjects was 0.0056 ± 0.0004 mSv/MBq, which would result in a total effective dose of 1.96 mSv for a typical injection of 350 MBq of 11C-BU99008. The effective dose is not appreciably different from those obtained with other 11C tracers.

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