Home > Publications database > Fully automated production of (((S)-1-carboxy-5-(6-([18F]fluoro)-2-methoxynicotinamido)pentyl)carbamoyl)-l-glutamic acid ([18F]JKPSMA-7 > print

001     1035303
005     20250310131244.0
024 7 _ |a 10.3390/ph18010119
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100 1 _ |a Krapf, Philipp
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245 _ _ |a Fully automated production of (((S)-1-carboxy-5-(6-([18F]fluoro)-2-methoxynicotinamido)pentyl)carbamoyl)-l-glutamic acid ([18F]JKPSMA-7
260 _ _ |a Basel
|c 2025
|b MDPI
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520 _ _ |a 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.
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700 1 _ |a Wicher, Thomas
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700 1 _ |a Zlatopolskiy, Boris
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700 1 _ |a Ermert, Johannes
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700 1 _ |a Neumaier, Bernd
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|e Corresponding author
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773 _ _ |a 10.3390/ph18010119
|g Vol. 18, no. 1, p. 119 -
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|t Pharmaceuticals
|v 18
|y 2025
|x 1424-8247
856 4 _ |u https://juser.fz-juelich.de/record/1035303/files/Invoice_MDPI_pharmaceuticals-3358454_1083.03EUR.pdf
856 4 _ |y OpenAccess
|u https://juser.fz-juelich.de/record/1035303/files/pharmaceuticals-18-00119.pdf
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