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KMID : 1145520200060020003
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Journal of Radiopharmaceuticals and Molecular Probes
2020 Volume.6 No. 2 p.3 ~ p.12
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Optimized production method of [18F]flortaucipir injection for imaging tau pathology in patients with Alzheimer’s disease
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Nam Kyung-Rok
Han Sang-Jin
Lee Nam-Hun
Lee Min-Yong
Kim Young-Duk
Lee Kyo-Chul
Lee Yong-Jin
Ryu Young-Hoon
Choi Jae-Yong
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Abstract
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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 130oC 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.
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KEYWORD
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[18F]Av-1451, tau, Alzheimer’s disease, PET, automation
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