Journal of Radiopharmaceuticals and Molecular Probes (대한방사성의약품학회지)

Korean Society of Radiopharmaceuticals and Molecular Probes (대한방사성의약품학회)
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Optimized production method of [18F]flortaucipir injection for imaging tau pathology in patients with Alzheimer's disease

  • Kyung Rok Nam (Division of Applied RI, Korea Institute of Radiological & Medical Sciences) ;
  • Sang Jin Han (Division of Applied RI, Korea Institute of Radiological & Medical Sciences) ;
  • Nam Hun Lee (Division of Applied RI, Korea Institute of Radiological & Medical Sciences) ;
  • Min Yong Lee (Division of Applied RI, Korea Institute of Radiological & Medical Sciences) ;
  • Youngduk Kim (New Korea Industrial Co., LTD.) ;
  • Kyo Chul Lee (Division of Applied RI, Korea Institute of Radiological & Medical Sciences) ;
  • Yong Jin Lee (Division of Applied RI, Korea Institute of Radiological & Medical Sciences) ;
  • Young Hoon Ryu (Department of Nuclear Medicine, Gangnam Severance Hospital, Yonsei University College of Medicine) ;
  • Jae Yong Choi (Division of Applied RI, Korea Institute of Radiological & Medical Sciences)
  • Received : 2020.12.11
  • Accepted : 2020.12.29
  • Published : 2020.12.31
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Abstract

Aggregated neurofibrillary tangles (NFTs) are a pathological hallmark in Alzheimer's disease (AD) and many radiopharmaceuticals targeting NFTs have been developed so far. Among these, [18F]flortaucipir (TAUVIDTM) is the first approved radiopharmaceutical in the Food and Drug Administration (FDA) to image tau pathology. In the present study, we describe the optimized radiosynthetic method for the routine production of [18F] flortaucipir using a commercialized automation module (i.e. GE TRACERlabTM FXFN pro). [18F]Flortaucipir was prepared by nucleophilic substitution from its N-tert-butoxycarbonyl protected nitro precursor, tertbutyl 7-(6-nitropyridin-3-yl)-5H-pyrido[4,3-b]indole-5-carboxylate, at 130℃ for 10 min in dimethyl sulfoxide. The mean radiochemical yield was 20 ± 4.3% (decay-corrected, n = 47) with the molar activity of 218 ± 32 GBq/µmol at the end of synthesis. The radiochemical purity was determined to be above 95%. The overall production time including quality control is approximately 100min. The final produced [18F]flortaucipir injection meets the USP criteria for quality control. Thus, this fully automated system is validated for clinical use.

Keywords

Acknowledgement

This study was supported by a grant from the Korea Institute of Radiological and Medical Sciences (KIRAMS), by the Ministry of Science and ICT (MSIT), Republic of Korea (No. 50461-2020, 50536-2020)

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