Infection Imaging With (18)F-FDS and First-in-Human Evaluation

Abstract

Purpose: The noninvasive imaging of bacterial infections is critical in order to reduce mortality and morbidity caused by these diseases. The recently reported (18)F-FDS ((18)F-2-fluorodeoxy sorbitol) as a PET (positron emission tomography) tracer can be used to image Enterobacteriaceae-specific infections and provides a potential alternative to this problem compared with other probes for imaging infections. In this study, automatic synthesis, validation of (18)F-FDS and a first-in-human study were performed and discussed.

Methods: A multifunctional synthesis module was employed for the radiosynthesis of (18)F-FDG ((18)F-2-fluorodeoxy glucose) and (18)F-FDS starting from (18)F ion using two-pot three-step fully automated reactions. The behavior of (18)F-FDS as an in vivo imaging probe for infections was evaluated in an Escherichia coli mouse infection model. The first detailed pharmacokinetic and biodistribution parameters were obtained from healthy human volunteers.

Results: The uptake of (18)F-FDS in an E. coli mouse-myositis infection model was easily differentiated from other organs and normal muscle. Intensive lesion uptake declined after antibiotic treatment. In the pilot human study, no adverse effects due to (18)F-FDS were observed up to 24 h post-injection. The radiotracer was rapidly cleared from the circulation and excreted mainly through the urinary system.

Conclusion: We conclude that (18)F-FDS PET holds great potential for appropriate and effective for the imaging of bacterial infections in vivo. These preliminary results indicate that further clinical studies are warranted.

Trial registration: ClinicalTrials.gov NCT02450942.

Keywords: (18)F-FDS; Automated synthesis; Gram-negative bacteria; Infection; PET.