Fully Automated Production of (((S)-1-Carboxy-5-(6-([18F]fluoro)-2-methoxynicotinamido)pentyl)carbamoyl)-l-glutamic Acid ([18F]JK-PSMA-7)

• DOI: 10.3390/ph18010119
• Publication Date: 2025-01-17T15:27:58Z
• Authors: Philipp Krapf; Thomas Wicher; Boris D. Zlatopol...; Johannes Ermert; Bernd Neumaier
• Keywords: RS1-441; Pharmacy and materia medica; Trasis AllInOne (AIO) module; R; Medicine; 610; positron emission tomography (PET); prostate cancer imaging; radiofluorination; [¹⁸F]JK-PSMA-7; Article; info:eu-repo/classification/ddc/610; automation

Background: 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 prosthetic group, which had to be isolated and purified before it could linked the pharmacologically Lys-urea-Glu motif. Although this procedure automated on two-reactor modules like GE TRACERLab FX2N (FXN) afford tracer in modest radiochemical yields (RCY) of 18-25%, is unsuitable cassette-based systems with single reactor. Methods: To simplify implementation synthesis module, radiosynthesis [18F]JK-PSMA-7 devised one-pot, two-step reaction. new method based direct ("late-stage") appropriate onium triflate precursor subsequent deprotection ortho-phosphoric acid. It successfully established Trasis AllInOne (AIO) module. Results: Overall, protocol enabled production activity 39 ± 4% (RCY = 58%) overall time about 1 h. In run initial 36-43 GBq, 13-19 GBq purity >99% obtained. Conclusions: We have highly reliable, GMP-compliant process AllinOne synthesizer, ensuring consistent efficient radioligand.