The Synthesis of 18F-FDS and Its Potential Application in Molecular Imaging

Abstract

# These authors contributed equally to this work. AbstractPurpose-2-Deoxy-2-[ 18 F]fluoro-D-glucose (FDG) is the most commonly used positron emission tomography (PET) tracer for oncological and neurological imaging, but it has limitations on detecting tumor or inflammation in brain gray matter. In this study, we describe the development of 2-deoxy-2-[ 18 F]fluorosorbitol ( 18 F-FDS) and its possible application in lesion detection around brain area.Procedures-18 F-FDS was obtained by reduction of FDG using NaBH 4 (81±4% yield in 30 min). Cell uptake/efflux experiments in cell culture and small animal PET imaging on tumor and inflammation models were performed.Results-Despite the low accumulation in cell culture, 18 F-FDS had good tumor uptake and contrast in the subcutaneous U87MG tumor model (4.54%ID/g at 30 min post-injection). Minimal uptake in the normal mouse brain facilitated good tumor contrast in both U87MG and GL-26 orthotopic tumor models. 18 F-FDS also had increased uptake in the inflamed foci of the TPAinduced acute inflammation model.Conclusions-Because of the ease of synthesis and favorable in vivo kinetics, 18 F-FDS may have potential applications in certain cases where FDG is inadequate (e.g., brain tumor).

Biodistribution and Radiation Dosimetry of the Enterobacteriaceae-Specific Imaging Probe [18F]Fluorodeoxysorbitol Determined by PET/CT in Healthy Human Volunteers

“…[ 18 F]FDS was first synthesized via reducing [ 18 F]FDG as described by Li, et al [16]. As Li, et al intended, this radiopharmaceutical was produced for brain tumor imaging since it showed no significant uptake in normal brain tissue.…”

“…[ 18 F]FDS was synthesized from [ 18 F]FDG, similar to the method previously reported [16]. Briefly, [ 18 F]FDG was firstly reduced with sodium borohydride at 45°C under N 2 bubbling for 15 min.…”

Initial Preclinical Evaluation of 18F-Fluorodeoxysorbitol PET as a Novel Functional Renal Imaging Agent

“…18 F-FDS was synthesized following a previously described procedure (9). In short, NaBH 4 (2 mg, 0.053 mmol) was added to a solution of 18 F-FDG in saline, and the resulting mixture was stirred at 35°C for 15 min.…”

“…2-deoxy-2-18 F-fluorodeoxysorbitol ( 18 F-FDS), an analog of sorbitol, can be easily synthesized via a 1-step reduction of 18 F-FDG, which is readily available (9)(10)(11). In early human studies, sorbitol urinary clearance was reported to be identical to inulin clearance (sorbitol-to-inulin clearance ratio 5 1.01) (12).…”

Validation of 2-18F-Fluorodeoxysorbitol as a Potential Radiopharmaceutical for Imaging Bacterial Infection in the Lung

“…2-18 F-fluorodeoxysorbitol ( 18 F-FDS), a positron-emitting analog of sorbitol, was first prepared by Li et al for tumor imaging but was found not to accumulate in cancer cells in vitro (300-fold lower accumulation than that of 18 F-FDG) (11). A recent study indicated that 18 F-FDS specifically accumulates in several strains of gram-negative bacteria but not gram-positive bacteria, with 1,000-fold higher uptake in Escherichia coli than in mammalian cells.…”