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@ARTICLE{Krapf:1035303,
author = {Krapf, Philipp and Wicher, Thomas and Zlatopolskiy, Boris
and Ermert, Johannes and Neumaier, Bernd},
title = {{F}ully automated production of
((({S})-1-carboxy-5-(6-([18{F}]fluoro)-2-methoxynicotinamido)pentyl)carbamoyl)-l-glutamic
acid ([18{F}]{JKPSMA}-7},
journal = {Pharmaceuticals},
volume = {18},
number = {1},
issn = {1424-8247},
address = {Basel},
publisher = {MDPI},
reportid = {FZJ-2025-00361},
pages = {119 -},
year = {2025},
abstract = {The radiotracer [18F]JK-PSMA-7, a prostate cancer imaging
agent for positron emission tomography (PET), was previously
synthesized by indirect radiofluorination using an
18F-labeled active ester as a prosthetic group, which had to
be isolated and purified before it could be linked to the
pharmacologically active Lys-urea-Glu motif. Although this
procedure could be automated on two-reactor modules like the
GE TRACERLab FX2N (FXN) to afford the tracer in modest
radiochemical yields (RCY) of $18–25\%,$ it is unsuitable
for cassette-based systems with a single reactor. Methods:
To simplify implementation on an automated synthesis module,
the radiosynthesis of [18F]JK-PSMA-7 was devised as a
one-pot, two-step reaction. The new method is based on
direct (“late-stage”) radiofluorination of an
appropriate onium triflate precursor and subsequent
deprotection with ortho-phosphoric acid. It was successfully
established on the cassette-based Trasis AllInOne (AIO)
module. Results: Overall, the new protocol enabled the
production of [18F]JK-PSMA-7 in activity yields of 39 ±
$4\%(RCY$ = $58\%)$ with an overall synthesis time of about
1 h. In a single production run with an initial activity of
36-43 GBq, 13-19 GBq of [18F]JK-PSMA-7 with a radiochemical
purity of $>99\%was$ obtained. Conclusions: We have
established a highly reliable, GMP-compliant process for the
automated radiosynthesis of [18F]JK-PSMA-7 on the Trasis
AllinOne (AIO) synthesizer, ensuring consistent and
efficient production of this radioligand.},
cin = {INM-5},
ddc = {610},
cid = {I:(DE-Juel1)INM-5-20090406},
pnm = {5253 - Neuroimaging (POF4-525)},
pid = {G:(DE-HGF)POF4-5253},
typ = {PUB:(DE-HGF)16},
pubmed = {39861180},
UT = {WOS:001405742900001},
doi = {10.3390/ph18010119},
url = {https://juser.fz-juelich.de/record/1035303},
}