Fully Automated GMP-Compliant Synthesis of [ 18 F]FE-PE2I

• Published in: Pharmaceuticals (Basel, Switzerland) Vol. 14; no. 7; p. 601
• Main Authors: Bratteby, Klas, Denholt, Charlotte Lund, Lehel, Szabolcs, Petersen, Ida Nymann, Madsen, Jacob, Erlandsson, Maria, Ohlsson, Tomas, Herth, Matthias Manfred, Gillings, Nic
• Format: Journal Article
• Language: English
• Published: Switzerland MDPI AG 22.06.2021; MDPI
• Subjects: [18F]FE-PE2I; Automation; Ethanol; Experiments; Fluorides; fluorine-18; GMP; Good Manufacturing Practice; Radiation; radiochemistry; fluorine-18; [18F]FE-PE2I; automation; GMP; radiochemistry
• ISSN: 1424-8247; 1424-8247
• DOI: 10.3390/ph14070601

In the struggle to understand and accurately diagnose Parkinson's disease, radiopharmaceuticals and medical imaging techniques have played a major role. By being able to image and quantify the dopamine transporter density, noninvasive diagnostic imaging has become the gold standard. In the shift from the first generation of SPECT tracers, the fluorine-18-labeled tracer [ F]FE-PE2I has emerged as the agent of choice for many physicians. However, implementing suitable synthesis for the production of [ F]FE-PE2I has proved more challenging than expected. Through a thorough analysis of the relevant factors affecting the final radiochemical yield, we were able to implement high-yielding fully automated GMP-compliant synthesis of [ F]FE-PE2I on a Synthera + platform. By reaching RCYs up to 62%, it allowed us to isolate 25 GBq of the formulated product, and an optimized formulation resulted in the shelf life of 6 h, satisfying the increased demand for this radiopharmaceutical.