Fully Automated Production of (((<i>S</i>)-1-Carboxy-5-(6-([<sup>18</sup>F]fluoro)-2-methoxynicotinamido)pentyl)carbamoyl)-<span style="font-variant: small-caps">l</span>-glutamic Acid ([<sup>18</sup>F]JK-PSMA-7)
<b>Background:</b> The radiotracer [<sup>18</sup>F]JK-PSMA-7, a prostate cancer imaging agent for positron emission tomography (PET), was previously synthesized by indirect radiofluorination using an <sup>18</sup>F-labeled active ester as a prosthetic group, which...
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| Main Authors: | , , , , |
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| Format: | Article |
| Language: | English |
| Published: |
MDPI AG
2025-01-01
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| Series: | Pharmaceuticals |
| Subjects: | |
| Online Access: | https://www.mdpi.com/1424-8247/18/1/119 |
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| Summary: | <b>Background:</b> The radiotracer [<sup>18</sup>F]JK-PSMA-7, a prostate cancer imaging agent for positron emission tomography (PET), was previously synthesized by indirect radiofluorination using an <sup>18</sup>F-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. <b>Methods:</b> To simplify implementation on an automated synthesis module, the radiosynthesis of [<sup>18</sup>F]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 <i>ortho</i>-phosphoric acid. It was successfully established on the cassette-based Trasis AllInOne (AIO) module. <b>Results:</b> Overall, the new protocol enabled the production of [<sup>18</sup>F]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 [<sup>18</sup>F]JK-PSMA-7 with a radiochemical purity of >99% was obtained. <b>Conclusions:</b> We have established a highly reliable, GMP-compliant process for the automated radiosynthesis of [<sup>18</sup>F]JK-PSMA-7 on the Trasis AllinOne (AIO) synthesizer, ensuring consistent and efficient production of this radioligand. |
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| ISSN: | 1424-8247 |