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Radiosynthesis and quality control testing of the tau imaging positron emission tomography tracer [ 18 F]PM‐PBB3 for clinical applications
Author(s) -
Kawamura Kazunori,
Hashimoto Hiroki,
Furutsuka Kenji,
Ohkubo Takayuki,
Fujishiro Tomoya,
Togashi Takahiro,
Arashi Daisuke,
Sakai Toshiyuki,
Muto Masatoshi,
Ogawa Masanao,
Kurihara Yusuke,
Nengaki Nobuki,
Takei Makoto,
Nemoto Kazuyoshi,
Higuchi Makoto,
Zhang MingRong
Publication year - 2021
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/jlcr.3890
Subject(s) - radiosynthesis , chemistry , positron emission tomography , radiochemistry , in vivo , tracer , nuclear medicine , nuclear physics , physics , medicine , microbiology and biotechnology , biology
Recently, we produced 11 C‐labeled 2‐((1 E ,3 E )‐4‐(6‐(methylamino)pyridin‐3‐yl)buta‐1,3‐dienyl)benzo[ d ]thiazol‐6‐ol ([ 11 C]PBB3) as a clinically useful positron emission tomography (PET) tracer for in vivo imaging of tau pathologies in the human brain. To overcome the limitations (i.e., rapid in vivo metabolism and short half‐life) of [ 11 C]PBB3, we further synthesized 18 F‐labeled 1‐fluoro‐3‐((2‐((1 E ,3 E )‐4‐(6‐(methylamino)pyridine‐3‐yl)buta‐1,3‐dien‐1‐yl)benzo[ d ]thiazol‐6‐yl)oxy)propan‐2‐ol ([ 18 F]PM‐PBB3). [ 18 F]PM‐PBB3 is also a useful tau PET tracer for imaging tau pathologies. In this study, we developed a routine radiosynthesis and quality control testing of [ 18 F]PM‐PBB3 for clinical applications. [ 18 F]PM‐PBB3 was synthesized by direct 18 F‐fluorination of the tosylated derivative, followed by removal of the protecting group. [ 18 F]PM‐PBB3 was obtained with sufficient radioactivity (25 ± 6.0% of the nondecay‐corrected radiochemical yield at the end of synthesis, EOS), radiochemical purity (98 ± 0.6%), and molar activity (350 ± 94 GBq/μmol at EOS; n = 53). Moreover, [ 18 F]PM‐PBB3 consistently retained >95% of radiochemical purity for 60 min without undergoing photoisomerization using a new UV‐cutoff light (yellow light) fixed in the hot cell to monitor the synthesis. All the results of the quality control testing for the [ 18 F]PM‐PBB3 injection complied with our in‐house quality control and quality assurance specifications. We have accomplished >200 production runs of [ 18 F]PM‐PBB3 in our facility for various research purposes.