Automated Synthesis Modules for
            <scp>PET</scp>
            Radiochemistry

Bruton, Laura; Scott, Peter J. H.

doi:10.1002/9781119500575.ch13

Cited by 9 publications

(14 citation statements)

References 91 publications

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“…Automation is a key feature in the routine preparation of the vast majority of PET tracers for clinical use, especially when labelled with 18 F and 11 C. An automated radiosynthesis can start at high radiation levels, as operators do not need to intervene throughout the procedure and are, therefore, protected from radiation exposure. Additionally, performing the procedure on a synthetic platform ensures reproducibility, and often results in shorter production time [ 13 ]. Finally, a limiting manual intervention reduces the risk of microbiological contamination; human operators are the most likely source of contamination in a GMP laboratory [ 7 , 14 ].…”

Section: Introductionmentioning

confidence: 99%

Fully Automated, High-Dose Radiosynthesis of [18F]PARPi

et al. 2022

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[18F]PARPi is currently undergoing clinical trials as a PET tracer for many applications. However, only manual radiosynthesis was reported; this has several drawbacks, including an increased risk of contamination from the operator, and the need to limit the starting activity. The automation of the previously reported protocol for [18F]PARPi synthesis is challenging, as it requires transferring microvolumes of reagents, which many platforms cannot accommodate. We report a revised, high yield, and automated protocol for the radiosynthesis of [18F]PARPi, with final doses of over 20 GBq.

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Section: Introductionmentioning

confidence: 99%

Fully Automated, High-Dose Radiosynthesis of [18F]PARPi

et al. 2022

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“…Perhaps the most obvious application of this approach is the radiolabeling of sensitive biomolecules (such as nucleic acids and proteins) that may decompose under the conditions needed for one-step radiolabeling. ,, However, the most significant impact of this technology lies elsewhere: automation. Automated synthesis modules enable the reliable and reproducible production of radiopharmaceuticals while limiting radiation dose rates to personnel and (when needed) ensuring current good manufacturing practice (cGMP) standards. , The robustness and modularity of the CuAAC reaction make it particularly attractive for this purpose. This is especially true because highly optimized radiosyntheses have been developed for several of the 18 F-labeled synthons enumerated above, and these prosthetic groups can be used with any complementary click substrate.…”

Section: The Copper-catalyzed Azide–alkyne Cycloadditionmentioning

confidence: 99%

“…Automated synthesis modules enable the reliable and reproducible production of radiopharmaceuticals while limiting radiation dose rates to personnel and (when needed) ensuring current good manufacturing practice (cGMP) standards. 75,76 The robustness and modularity of the CuAAC reaction make it particularly attractive for this purpose. This is especially true because highly optimized radiosyntheses have been developed for several of the 18 F-labeled synthons enumerated above, and these prosthetic groups can be used with any complementary click substrate.…”

Section: ■ Introductionmentioning

confidence: 99%

Click Chemistry and Radiochemistry: An Update

Bauer,

Cornejo,

Hoang

et al. 2023

Bioconjugate Chem.

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The term "click chemistry" describes a class of organic transformations that were developed to make chemical synthesis simpler and easier, in essence allowing chemists to combine molecular subunits as if they were puzzle pieces. Over the last 25 years, the click chemistry toolbox has swelled from the canonical copper-catalyzed azide−alkyne cycloaddition to encompass an array of ligations, including bioorthogonal variants, such as the strain-promoted azide−alkyne cycloaddition and the inverse electron-demand Diels−Alder reaction. Without question, the rise of click chemistry has impacted all areas of chemical and biological science. Yet the unique traits of radiopharmaceutical chemistry have made it particularly fertile ground for this technology. In this update, we seek to provide a comprehensive guide to recent developments at the intersection of click chemistry and radiopharmaceutical chemistry and to illuminate several exciting trends in the field, including the use of emergent click transformations in radiosynthesis, the clinical translation of novel probes synthesized using click chemistry, and the advent of click-based in vivo pretargeting.

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“…The successful implementation of the radiosynthesis of PET tracers on cassette-based automation platforms is critical for translational research and future applications [14,15]. Automated radiochemistry not only enables batch-to-batch reproducibility in PET radiopharmaceutical production [16,17], which is crucial for compliance with Good Manufacturing Practice (GMP) requirements [18], but also provides radiation protection to users handling a large amount of activity [19].…”

Section: Introductionmentioning

confidence: 99%

Fully automated radiosynthesis of [¹⁸F]mG4P027 for mGluR4 imaging

et al. 2023

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Background: Fluorine-18 labeled N-(4-chloro-3-(((fluoro-18 F)methyl-d 2 )thio) phenyl)picolinamide, [ 18 F]mG4P027, is a potent positron emission tomography (PET) radiotracer for mGluR4. Our previous in vitro and in vivo evaluations have demonstrated that this tracer is promising for further translational studies. However, automated radiosynthesis process poses significant challenges that need to be addressed. Methods:The automated radiosynthesis was performed using the TRACERlab FX2N module, which comprises two distinct reactors capable of accommodating the two-step reactions. Several problem-solving strategies were employed to overcome challenges during the automation process. This included modifications to the reaction solvents, reaction conditions, use of a scavenger, drying methods, and the handling of the precursor. Results:The use of n-Bu 4 NN 3 for scavenging excess compound 1 along with an efficient drying procedure played a key role in the success of the radiosynthesis. The water was successfully removed by using a different duct to overcome the water sensitivity for the second reaction.Conclusions: Significant modifications were made to the manual process by carefully examining this process and addressing the root causes of the challenges associated with its automation. We successfully implemented automated radiosynthesis using the TRACERlab FX2N module and consequently, obtained a high-purity radiolabeled [ 18 F]mG4P027 in high yield, meeting the requirements for future human studies.

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Automated Synthesis Modules for PET Radiochemistry

Cited by 9 publications

References 91 publications

Fully Automated, High-Dose Radiosynthesis of [18F]PARPi

Fully Automated, High-Dose Radiosynthesis of [18F]PARPi

Click Chemistry and Radiochemistry: An Update

Fully automated radiosynthesis of [¹⁸F]mG4P027 for mGluR4 imaging

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Automated Synthesis Modules for PET Radiochemistry

Cited by 9 publications

References 91 publications

Fully Automated, High-Dose Radiosynthesis of [18F]PARPi

Fully Automated, High-Dose Radiosynthesis of [18F]PARPi

Click Chemistry and Radiochemistry: An Update

Fully automated radiosynthesis of [18F]mG4P027 for mGluR4 imaging

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Product

Resources

About

Fully automated radiosynthesis of [¹⁸F]mG4P027 for mGluR4 imaging