Radiation dosimetry of the 18 kDa translocator protein ligand [18F]PBR111 in humans

Article Article scientifique Article Radiation dosimetry of the 18 kDa translocator protein ligand [18F]PBR111 in humans eng 2025-03-29 2025-05 author Tournier Benjamin 705309 Département de psychiatrie (PSYAT) author Mansouri Zahra 402439 Département de radiologie et informatique médicale (RADIO) author Salimi Yazdan 0000-0002-1233-9576 943941 Département de radiologie et informatique médicale (RADIO) author Ceyzeriat Kelly 910236 Centre d'imagerie bio-médicale (CIBM) author Mathoux Grégory 404256 author Richard Lepouriel Hélène 0000-0002-0778-3728 797416 Département de psychiatrie (PSYAT) author Zullino Daniele Fabio 649976 Département de psychiatrie (PSYAT) author Bois Frédéric 861168 author Zaidi Habib 0000-0001-7559-5297 98447 Département de radiologie et informatique médicale (RADIO) author Garibotto Valentina 0000-0003-2422-698X 704817 Département de radiologie et informatique médicale (RADIO) author Tsartsalis Stergios 0000-0002-6565-6313 782369 Département de psychiatrie (PSYAT) author Millet Philippe 0000-0002-5803-0478 668343 Département de psychiatrie (PSYAT) 109011 10.1016/j.nucmedbio.2025.109011 40179687 0969-8051 https://www.sciencedirect.com/science/article/pii/S0969805125000204 Purpose: The 18 kDa translocator protein (TSPO) is a mitochondrial protein that becomes overexpressed during neuroinflammatory conditions, such as in Alzheimer's disease or multiple sclerosis. TSPO is of interest because it serves as a marker for microglial and astrocytic activity, measurable via in vivo positron emission tomography (PET) molecular imaging. [18F]PBR111 is a second-generation TSPO PET radioligand with high signal specificity but a sensitivity to TSPO polymorphism, in comparison with first-generation ligands. This study focused on the biodistribution and dosimetry of [18F]PBR111 in healthy humans. Method: Six volunteers (three males, three females) were administered approximately 200 MBq of [18F]PBR111. Organs such as the lungs and liver showed the highest initial radioactivity level, while the bone marrow and bladder accumulated activity over time, likely reflecting ligand defluorination and elimination. Results: Dosimetry findings revealed a total effective dose of 16.17 μSv/MBq, equivalent to 3.04 mSv per examination. Compared to animal models, human dosimetry showed lower radiation exposure, highlighting discrepancies in predictive models. Organ-specific dose comparisons with other TSPO ligands ([18F]PBR06, [18F]FEPPA, [18F]FEDAA1106) revealed similar distribution patterns. This study underscores the clinical viability of [18F]PBR111 for TSPO imaging, providing critical data for optimizing its safe use in research and clinical settings. Conclusion: The findings support its potential for studying neuroinflammatory and systemic diseases. The trial registration number is <a href="http://clinicaltrials.gov/show/NCT06398392" rel="noopener noreferrer" target="_blank">NCT06398392</a>. PBR Radiation dose TSPO Dewey 616.89 Dewey 616.0757 Hôpitaux Universitaires de Genève 10-2018-I Swiss National Science Foundation Molecular Imaging of Neuroinflammation in Bipolar Disorder: a Translational Validation of the TSPO Quantification Methodology 184713 CH Projects 60 Département de psychiatrie 225 62 Département de radiologie et informatique médicale 227 false 1221 Neuroimagerie moléculaire en psychiatrie 983 287 Imagerie Médicale (TEP et TEMP) 542 1222 Laboratoire de neuroimagerie et de traceurs moléculaires innovants 984 496 Abus de substances 834 Nuclear medicine and biology 144-145 f9a57f40-fb49-4daf-b388-2d463c83f7c0 Article (Accepted version) Public NUCMEDBIO-Accepted.pdf 2820210 application/pdf Restricted 2026-06-01 e2313a8780029ba5fabd1ea85c84311ec08d54ff01a5fc624bca7a165633a299 e3801bc5-4828-46d4-aa17-71cba67e441c Article (Published version) Restricted 1-s2.0-S0969805125000204-main.pdf 2956448 application/pdf 040d8da5a5d3cccd30533b1014d9e35a7eab6f65f780e2ef7b353efda806e0cf ff893bad-6e16-48fa-85c7-e42761d50515 Supplemental data Restricted 1-s2.0-S0969805125000204-mmc1-1.docx 1258176 application/vnd.openxmlformats-officedocument.wordprocessingml.document 28a4f2b8a805b2f121c794b2df37e813db7491dbb69071808a55a90d51cc9e0c openAccess Faculté de médecine / Section de médecine clinique / Département de psychiatrie Faculté de médecine / Section de médecine clinique / Département de radiologie et informatique médicale

Title	Published in	Year	Views	Downloads

Radiation dosimetry of the 18 kDa translocator protein ligand [¹⁸F]PBR111 in humans	Nuclear medicine and biology	2025	78	21
[⁶⁸Ga]Ga-PSMA-11 in prostate cancer: a comprehensive review	American journal of nuclear medicine and molecular imaging	2020	206	231

Archive ouverte UNIGE

Bois, Frédéric