Microfluidic continuous-flow radiosynthesis of [¹⁸F]FPEB suitable for human PET imaging

Area of Science:

• Radiochemistry
• Neuroimaging
• Pharmaceutical development

Background:

• Metabotropic glutamate receptor subtype 5 (mGluR5) plays a crucial role in neurological functions and diseases.
• Developing novel positron emission tomography (PET) radiopharmaceuticals is essential for in vivo imaging of mGluR5.
• Current synthesis methods may have limitations in efficiency and scalability for clinical applications.

Purpose of the Study:

• To synthesize fluorine-18 labeled 3-fluoro-5-[(pyridin-3-yl)ethynyl] benzonitrile ([18F]FPEB) for PET imaging of mGluR5.
• To establish a validated synthesis of [18F]FPEB using a commercial continuous-flow microfluidics device.
• To demonstrate the suitability of this microfluidic synthesis for producing a human-use PET radiopharmaceutical.

Main Methods:

• Utilized a commercial continuous-flow microfluidics device for the synthesis of [18F]FPEB.
• Employed a validated synthesis protocol for [18F]FPEB production.
• Characterized the synthesized radiopharmaceutical for quality and suitability.

Main Results:

• Successfully synthesized fluorine-18 labeled [18F]FPEB.
• Achieved synthesis using a commercial continuous-flow microfluidics system, representing a novel application for PET radiopharmaceuticals.
• Validated the synthesis process, confirming its reliability and potential for clinical translation.
• This is the first PET radiopharmaceutical suitable for human use developed with microfluidic technology.

Conclusions:

• The continuous-flow microfluidics device provides an efficient and validated method for synthesizing the mGluR5-targeting PET radiopharmaceutical [18F]FPEB.
• This technology enables the production of a human-suitable radiotracer, advancing the field of neuroimaging.
• The validated reactor-based synthesis further supports the clinical applicability of [18F]FPEB.