18 F-FIMP: a LAT1-specific PET probe for discrimination between tumor tissue and inflammation

Positron emission tomography (PET) imaging can assist in the early-phase diagnostic and therapeutic evaluation of tumors. Here, we report the radiosynthesis, small animal PET imaging, and biological evaluation of a L-type amino acid transporter 1 (LAT1)-specific PET probe, F-FIMP. This probe demonst...

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Published inScientific reports Vol. 9; no. 1; p. 15718
Main Authors Nozaki, Satoshi, Nakatani, Yuka, Mawatari, Aya, Shibata, Nina, Hume, William E, Hayashinaka, Emi, Wada, Yasuhiro, Doi, Hisashi, Watanabe, Yasuyoshi
Format Journal Article
LanguageEnglish
Published England 31.10.2019
Subjects
Animals
Arthritis, Experimental - diagnostic imaging
Arthritis, Experimental - metabolism
Cell Line
Cell Line, Tumor
Disease Models, Animal
Humans
Large Neutral Amino Acid-Transporter 1 - metabolism
Mice
Neoplasms - diagnostic imaging
Neoplasms - metabolism
Positron-Emission Tomography - methods
Proteins - metabolism
Radiopharmaceuticals - metabolism
Radiopharmaceuticals - pharmacokinetics
Tissue Distribution
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Summary:Positron emission tomography (PET) imaging can assist in the early-phase diagnostic and therapeutic evaluation of tumors. Here, we report the radiosynthesis, small animal PET imaging, and biological evaluation of a L-type amino acid transporter 1 (LAT1)-specific PET probe, F-FIMP. This probe demonstrates increased tumor specificity, compared to existing tumor-specific PET probes ( F-FET, C-MET, and F-FDG). Evaluation of probes by in vivo PET imaging, F-FIMP showed intense accumulation in LAT1-positive tumor tissues, but not in inflamed lesions, whereas intense accumulation of F-FDG was observed in both tumor tissues and in inflamed lesions. Metabolite analysis showed that F-FIMP was stable in liver microsomes, and mice tissues (plasma, urine, liver, pancreas, and tumor). Investigation of the protein incorporation of F-FIMP showed that it was not incorporated into protein. Furthermore, the expected mean absorbed dose of F-FIMP in humans was comparable or slightly higher than that of F-FDG and indicated that F-FIMP may be a safe PET probe for use in humans. F-FIMP may provide improved specificity for tumor diagnosis, compared to F-FDG, F-FET, and C-MET. This probe may be suitable for PET imaging for glioblastoma and the early-phase monitoring of cancer therapy outcomes.
ISSN:2045-2322