Radiation dosimetry of the translocator protein ligands [18F]PBR111 and [18F]PBR102

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dc.contributor.authorVerschuer, JDen_AU
dc.contributor.authorTowson, Jen_AU
dc.contributor.authorEberl, Sen_AU
dc.contributor.authorKatsifis, Aen_AU
dc.contributor.authorHenderson, Den_AU
dc.contributor.authorLam, Pen_AU
dc.contributor.authorWen, LFen_AU
dc.contributor.authorLoc'h, Cen_AU
dc.contributor.authorMattner, Fen_AU
dc.contributor.authorThomson, Sen_AU
dc.contributor.authorMohamed, Aen_AU
dc.contributor.authorFulham, MJen_AU
dc.date.accessioned2020-03-29T19:42:00Zen_AU
dc.date.available2020-03-29T19:42:00Zen_AU
dc.date.issued2012-07-01en_AU
dc.date.statistics2020-03-20en_AU
dc.description.abstractIntroduction The translocator protein (TSPO) ligands [18F]PBR111 and [18F]PBR102 show promise for imaging neuroinflammation. Our aim was to estimate the radiation dose to humans from primate positron emission tomography (PET) studies using these ligands and compare the results with those obtained from studies in rodents. Methods [18F]PBR111 and [18F]PBR102 PET–computed tomography studies were carried out in baboons. The cumulated activity in the selected source organs was obtained from the volume of interest time–activity curves drawn on coronal PET slices and adjusted for organ mass relative to humans. Radiation dose estimates were calculated in OLINDA/EXM Version 1.1 from baboon studies and compared with those calculated from Sprague–Dawley rat tissue concentration studies, also adjusted for relative organ mass. Results In baboons, both ligands cleared rapidly from brain, lung, kidney and spleen and more slowly from liver and heart. For [18F]PBR111, the renal excretion fraction was 6.5% and 17% for hepatobiliary excretion; for [18F]PBR102, the renal excretion was 3.0% and 15% for hepatobiliary excretion. The estimated effective dose in humans from baboon data was 0.021 mSv/MBq for each ligand, whilst from rat data, the estimates were 0.029 for [18F]PBR111 and 0.041 mSv/MBq for [18F]PBR102. Conclusion Biodistribution in a nonhuman primate model is better suited than the rat model for the calculation of dosimetry parameters when translating these ligands from preclinical to human clinical studies. Effective dose calculated from rat data was overestimated compared to nonhuman primate data. The effective dose coefficient for both these TSPO ligands determined from PET studies in baboons is similar to that for [18F]FDG. © 2012 Elsevier Inc.en_AU
dc.identifier.citationVerschuer, J. D., Towson, J., Eberl, S., Katsifis, A., Henderson, D., Lam, P., Wen, L., Loc'h, C., Mattner, F., Thomson, S., Mohamed, A., & Fulham, M. J. (2012). Radiation dosimetry of the translocator protein ligands [18F]PBR111 and [18F]PBR102. Nuclear Medicine and Biology, 39(5), 742-753. doi:10.1016/j.nucmedbio.2011.11.003en_AU
dc.identifier.govdoc8895en_AU
dc.identifier.issn0969-8051en_AU
dc.identifier.issue5en_AU
dc.identifier.journaltitleNuclear Medicine and Biologyen_AU
dc.identifier.pagination742-753en_AU
dc.identifier.urihttps://doi.org/10.1016/j.nucmedbio.2011.11.003en_AU
dc.identifier.urihttp://apo.ansto.gov.au/dspace/handle/10238/9281en_AU
dc.identifier.volume39en_AU
dc.language.isoenen_AU
dc.publisherElsevier B.V.en_AU
dc.subjectRadiation dosesen_AU
dc.subjectPositron computed tomographyen_AU
dc.subjectLigandsen_AU
dc.subjectInflammationen_AU
dc.subjectOrgansen_AU
dc.subjectRatsen_AU
dc.subjectClinical trialsen_AU
dc.subjectBaboonsen_AU
dc.titleRadiation dosimetry of the translocator protein ligands [18F]PBR111 and [18F]PBR102en_AU
dc.typeJournal Articleen_AU
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