First-In-Human Evaluation of [18F]Fluproxadine for Norepinephrine Transporter PET
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Le résumé fourni par la source
BACKGROUND: Current norepinephrine transporter (NET) tracers used for cardiac sympathetic imaging and oncology are limited by radiosynthesis complexity, suboptimal image quality, or operational constraints. [18F]fluproxadine (formerly [18F]AF78) was developed to address these limitations by providing high NET affinity, favorable biodistribution, and an operationally straightforward radiosynthesis. We therefore conducted the first-in-human evaluation of this new class of [18F] labeled NET PET tracer to assess its safety, biodistribution, radiation dosimetry, and imaging characteristics. PATIENTS AND METHODS: In a prospective study, 4 healthy adult volunteers received [18F]fluproxadine (101.8-204.0 MBq). Dynamic whole-body PET/CT acquisitions were obtained 10 times from 1 to 232 minutes postinjection, and vital signs, laboratory tests, and adverse events were monitored. Time-activity curves were generated for major organs, including myocardium from the whole-body scans, and organ-absorbed doses and effective dose were estimated using OLINDA/EXM v2.0 from time-integrated activities. Myocardial uptake and target-to-background behavior were assessed using semiquantitative methods. Radiosynthesis performance and key operational steps were documented to assess practical scalability. RESULTS: Radiosynthesis of [18F]fluproxadine was operationally straightforward with encouraging yields and fewer specialized steps than some legacy tracers. Imaging was completed without serious adverse events. Biodistribution showed predominant renal clearance; biliary excretion was not observed within the imaging window. Highest organ doses were to the urinary bladder wall and kidneys, with additional uptake in liver, thyroid, salivary glands, and myocardium. The effective dose was 21.6±1.5 µSv/MBq. Myocardial uptake was clearly visualized on whole-body images with favorable target-to-background characteristics at delayed time points, consistent with NET biology and supporting practical cardiac imaging windows. CONCLUSIONS: [18F]fluproxadine demonstrated clear myocardial uptake, acceptable radiation dosimetry comparable to typical 18F PET agents, and an early safety profile without serious adverse events.
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Le contrôle bibliographique ouvert
DOI retrouvé dans Crossref DOI retrouvé ; titre concordant.
- Titre Crossref
- First-In-Human Evaluation of [18F]Fluproxadine for Norepinephrine Transporter PET
- Date Crossref
- 27/04/2026
- Éditeur
- Ovid Technologies (Wolters Kluwer Health)
- Type
- journal-article
Ce recoupement confirme des métadonnées liées au DOI. Il ne confirme ni la méthode ni les conclusions de l’étude, et il ne compte pas comme une seconde source scientifique indépendante.
Où se fait cette recherche
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Kobe City Medical Center General Hospital Department of Molecular Imaging Research pays non établi dans la noticeÉtablissement de santé
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National Institutes for Quantum Science and Technology pays non établi dans la noticeStructure de recherche
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Nara Medical University Department of Diagnostic and Interventional Radiology pays non établi dans la noticeUniversité ou école supérieure
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Hiroshima City University Department of Biomedical Information Sciences pays non établi dans la noticeUniversité ou école supérieure
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Ludwig-Maximilians-Universität München pays non établi dans la noticeUniversité ou école supérieure
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Okayama University pays non établi dans la noticeUniversité ou école supérieure
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University of Augsburg pays non établi dans la noticeUniversité ou école supérieure
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Universitätsklinikum Würzburg pays non établi dans la noticeÉtablissement de santé
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Ludwig-Maximilians-University of Munich Department of Nuclear Medicine pays non établi dans la noticeUniversité ou école supérieure
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Faculty of Medicine Nuclear Medicine pays non établi dans la noticeUniversité ou école supérieure
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University Hospital of Würzburg Department of Nuclear Medicine and Comprehensive Heart Failure Center (DZHI) pays non établi dans la noticeUniversité ou école supérieure
Department of Molecular Imaging Research — Kobe City Medical Center General Hospital, National Institutes for Quantum Science and Technology et Department of Diagnostic and Interventional Radiology — Nara Medical University, avec 8 autres affiliations.
Une affiliation ne permet pas de déduire la nationalité d’un auteur.