文章基本信息

标题：18F-FIMP: a LAT1-specific PET probe for discrimination between tumor tissue and inflammation
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作者：Satoshi Nozaki ; Yuka Nakatani ; Aya Mawatari 等
期刊名称：Scientific Reports
电子版ISSN：2045-2322
出版年度：2019
卷号：9
期号：1
页码：1-9
DOI：10.1038/s41598-019-52270-x
出版社：Springer Nature
摘要：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, 18 F-FIMP. This probe demonstrates increased tumor specificity, compared to existing tumor-specific PET probes ( 18 F-FET, 11 C-MET, and 18 F-FDG). Evaluation of probes by in vivo PET imaging, 18 F-FIMP showed intense accumulation in LAT1-positive tumor tissues, but not in inflamed lesions, whereas intense accumulation of 18 F-FDG was observed in both tumor tissues and in inflamed lesions. Metabolite analysis showed that 18 F-FIMP was stable in liver microsomes, and mice tissues (plasma, urine, liver, pancreas, and tumor). Investigation of the protein incorporation of 18 F-FIMP showed that it was not incorporated into protein. Furthermore, the expected mean absorbed dose of 18 F-FIMP in humans was comparable or slightly higher than that of 18 F-FDG and indicated that 18 F-FIMP may be a safe PET probe for use in humans. 18 F-FIMP may provide improved specificity for tumor diagnosis, compared to 18 F-FDG, 18 F-FET, and 11 C-MET. This probe may be suitable for PET imaging for glioblastoma and the early-phase monitoring of cancer therapy outcomes.