Development of F-18 radiopharmaceutical for PET imaging of infections

• Project/Area Number: 26461786
• Research Category: Grant-in-Aid for Scientific Research (C)
• Allocation Type: Multi-year Fund
• Section: 一般
• Research Field: Radiation science
• Research Institution: University of Fukui
• Principal Investigator: Martinez Miguel 福井大学, 高エネルギー医学研究センター, 特命助教 (00631491)
• Co-Investigator(Kenkyū-buntansha): 清野 泰 福井大学, 高エネルギー医学研究センター, 教授 (50305603)
• Project Period (FY): 2014-04-01 – 2017-03-31
• Project Status: Completed (Fiscal Year 2016)
• Budget Amount: ¥4,940,000 (Direct Cost: ¥3,800,000、Indirect Cost: ¥1,140,000); Fiscal Year 2016: ¥1,170,000 (Direct Cost: ¥900,000、Indirect Cost: ¥270,000); Fiscal Year 2015: ¥1,820,000 (Direct Cost: ¥1,400,000、Indirect Cost: ¥420,000); Fiscal Year 2014: ¥1,950,000 (Direct Cost: ¥1,500,000、Indirect Cost: ¥450,000)
• Keywords: PET / Infection / Inflammation / Glucosamine / Bacterial imaging agent / infection / inflammation / imaging / Glucosamine derivatives

Outline of Final Research Achievements

We had reported the radiosynthesis of 2-deoxy-2-[18F]fluoroacetamido-D-glucopyranose, which was able to distinguish infection from inflammation in animal models. Furthermore, we developed new precursors with the same efficiency of [18F]fluoride incorporation under similar radiosynthesis conditions and also developed a high-performance liquid chromatography (HPLC) method for quality control of final [18F]FAG. Final specific activity using tosylate precursor was higher than using bromo precursor. Nevertheless, final specific activity and radiosynthesis yield were lower than previous radiosynthesis procedure therefore not suitable for clinical trials. Finally, the synthesis a new UDP-N-acetylglucosamine precursor was designed and is currently ongoing.

Research Products

• [Presentation] Development of a new purification protocol for radiosynthesis of 2-deoxy-2-[18F]fluoroacetamido-D-glucopyranose. (2016)
  • Author(s): M E Martinez; A Makino; T Mori; H Okazawa; Y Kiyono.
  • Organizer: EANM-16, 29th Annual European Association of Nuclear Medicine Congress
  • Place of Presentation: Barcelona, Spain
  • Year and Date: 2016-10-15
  • Int'l Joint Research
• [Presentation] Evaluation of a new precursor for radiosynthesis of 2-deoxy-2-[18F]fluoroacetamido-D-glucopyranose. (2015)
  • Author(s): Miguel Ernesto Martinez Pozo, Yuji Tokunaga, Tetsuya Mori, Akira Makino, Hidehiko Okazawa, Yasushi Kiyono
  • Organizer: 第10回日本分子イメージング学会
  • Place of Presentation: Tokyo, Japan
  • Year and Date: 2015-05-20
• [Presentation] HPLC and HPLC-ESI-MS/MS methods for the determination of 2-acetamido-2-deoxy-D-glucopyranose analogues (2014)
  • Author(s): M E Martinez, Y Tokunaga, T Mori, A Makino, S Noriki, K Inai, H Okazawa, Y Kiyono.
  • Organizer: EANM14, 27th Annual Europe Association of Nuclear Medicine Congress
  • Place of Presentation: Gothenburg, Sweden
  • Year and Date: 2014-10-18 – 2014-10-22