First-In-Human Evaluation of [18F]Fluproxadine for Norepinephrine Transporter PET: Biodistribution, Dosimetry, and Safety
Abstract
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…
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