Fully automated radiosynthesis of [¹⁸F]FCPPC for imaging microglia with PET

Area of Science:

• Neuroscience
• Radiochemistry
• Medical Imaging

Background:

• Colony-stimulating factor 1 receptor (CSF1R) is a key marker for microglia in the human brain, making it a potential target for neuroinflammation imaging.
• [11C]CPPC is a radiotracer for CSF1R, but its fluorine-18 labeled analog, [18F]FCPPC, had low yields with manual synthesis.
• Efficient and reliable production of [18F]FCPPC is crucial for its clinical application in microglia PET imaging.

Purpose of the Study:

• To develop and validate a fully automated radiosynthesis of the fluorine-18 labeled radiotracer [18F]FCPPC.
• To optimize the production of [18F]FCPPC for high radiochemical yield and purity.
• To establish [18F]FCPPC as a viable tool for human microglia PET imaging.

Main Methods:

• Automated radiosynthesis of [18F]FCPPC was performed using a Synthra RNplus research module.
• The synthesis process was optimized for speed and efficiency, aiming for a total synthesis time under 1 hour.
• Quality control tests were conducted to ensure the radiochemical purity and suitability of the final product for imaging.

Main Results:

• The automated radiosynthesis yielded [18F]FCPPC in a decay-corrected radiochemical yield of 26.8 ± 0.1% (n=3) within 50 minutes.
• Radiochemical purities consistently exceeded 99%.
• The synthesized [18F]FCPPC met all predefined quality control release criteria.

Conclusions:

• The first fully automated radiosynthesis of [18F]FCPPC has been successfully established.
• This automated method provides a reliable and efficient way to produce [18F]FCPPC for clinical use.
• [18F]FCPPC is a promising radiopharmaceutical for non-invasive imaging of microglia density and neuroinflammation in humans.