TY - JOUR
T1 - Radiosynthesis and quality control testing of the tau imaging positron emission tomography tracer [18F]PM-PBB3 for clinical applications
AU - Kawamura, Kazunori
AU - Hashimoto, Hiroki
AU - Furutsuka, Kenji
AU - Ohkubo, Takayuki
AU - Fujishiro, Tomoya
AU - Togashi, Takahiro
AU - Arashi, Daisuke
AU - Sakai, Toshiyuki
AU - Muto, Masatoshi
AU - Ogawa, Masanao
AU - Kurihara, Yusuke
AU - Nengaki, Nobuki
AU - Takei, Makoto
AU - Nemoto, Kazuyoshi
AU - Higuchi, Makoto
AU - Zhang, Ming Rong
N1 - Publisher Copyright:
© 2020 John Wiley & Sons, Ltd.
PY - 2021/3
Y1 - 2021/3
N2 - Recently, we produced 11C-labeled 2-((1E,3E)-4-(6-(methylamino)pyridin-3-yl)buta-1,3-dienyl)benzo[d]thiazol-6-ol ([11C]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 [11C]PBB3, we further synthesized 18F-labeled 1-fluoro-3-((2-((1E,3E)-4-(6-(methylamino)pyridine-3-yl)buta-1,3-dien-1-yl)benzo[d]thiazol-6-yl)oxy)propan-2-ol ([18F]PM-PBB3). [18F]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 [18F]PM-PBB3 for clinical applications. [18F]PM-PBB3 was synthesized by direct 18F-fluorination of the tosylated derivative, followed by removal of the protecting group. [18F]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, [18F]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 [18F]PM-PBB3 injection complied with our in-house quality control and quality assurance specifications. We have accomplished >200 production runs of [18F]PM-PBB3 in our facility for various research purposes.
AB - Recently, we produced 11C-labeled 2-((1E,3E)-4-(6-(methylamino)pyridin-3-yl)buta-1,3-dienyl)benzo[d]thiazol-6-ol ([11C]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 [11C]PBB3, we further synthesized 18F-labeled 1-fluoro-3-((2-((1E,3E)-4-(6-(methylamino)pyridine-3-yl)buta-1,3-dien-1-yl)benzo[d]thiazol-6-yl)oxy)propan-2-ol ([18F]PM-PBB3). [18F]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 [18F]PM-PBB3 for clinical applications. [18F]PM-PBB3 was synthesized by direct 18F-fluorination of the tosylated derivative, followed by removal of the protecting group. [18F]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, [18F]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 [18F]PM-PBB3 injection complied with our in-house quality control and quality assurance specifications. We have accomplished >200 production runs of [18F]PM-PBB3 in our facility for various research purposes.
UR - https://www.scopus.com/pages/publications/85096651535
UR - https://www.scopus.com/pages/publications/85096651535#tab=citedBy
U2 - 10.1002/jlcr.3890
DO - 10.1002/jlcr.3890
M3 - Article
C2 - 33067819
AN - SCOPUS:85096651535
SN - 0362-4803
VL - 64
SP - 109
EP - 119
JO - Journal of Labelled Compounds and Radiopharmaceuticals
JF - Journal of Labelled Compounds and Radiopharmaceuticals
IS - 3
ER -