Good practices for the automated production of 18F-SiFA radiopharmaceuticals

EJNMMI Radiopharmacy and Chemistry

Research Article

Carmen Wängler¹  Simon Blok²  Peter Bartenstein³  Simon Lindner³  Ralf Schirrmacher⁴  Klaus Jurkschat⁵ 

[1] Biomedical Chemistry, Clinic of Radiology and Nuclear Medicine, Medical Faculty Mannheim, Heidelberg University, Mannheim, Germany;Department of Nuclear Medicine and Molecular Imaging, University Medical Center Groningen, University of Groningen, Groningen, The Netherlands;Department of Nuclear Medicine, LMU University Hospital, LMU Munich, Munich, Germany;Department of Oncology, Division of Oncological Imaging, University of Alberta, Edmonton, AB, Canada;Fakultät für Chemie und Chemische Biologie, Technische Universität Dortmund, Dortmund, Germany;

关键词: Fluorine-18;    Silicon fluoride acceptor;    Automation;    Positron emission tomography (PET);   

DOI  :  10.1186/s41181-023-00215-1

 received in 2023-07-28, accepted in 2023-10-03,  发布年份 2023

来源: Springer

【 摘 要 】

BackgroundThe positron emitting isotope fluorine-18 (18F) possesses almost ideal physicochemical properties for the development of radiotracers for diagnostic molecular imaging employing positron emission tomography (PET). 18F in its nucleophilic anionic 18F− form is usually prepared by bombarding an enriched 18O water target with protons of various energies between 5 and 20 MeV depending on the technical specifications of the cyclotron. Large thick-target yields between 5 and 14 GBq/µA can be obtained, enough to prepare large batches of radiotracers capable to serve a considerable contingent of patients (50 + per clinical batch). The overall yield of the radiotracer however depends on the efficiency of the 18F labeling chemistry. The Silicon Fluoride Acceptor chemistry (SiFA) has introduced a convenient and highly efficient way to provide clinical peptide-based 18F-radiotracers in a kit-like procedure matching the convenience of 99mTc radiopharmaceuticals.Main bodyA radiotracer’s clinical success primarily hinges on whether its synthesis can be automated. Due to its simplicity, the SiFA chemistry, which is based on isotopic exchange (18F for 19F), does not only work in a manual setup but has been proven to be automatable, yielding large batches of 18F-radiotracers of high molar activity (Am). The production of SiFA radiotracer can be centralized and the radiopharmaceutical be distributed via the “satellite” principle, where one production facility economically serves multiple clinical application sites. Clinically validated tracers such as [18F]SiTATE and [18F]Ga-rhPSMA-7/-7.3 have been synthesized in an automated synthesis unit under good manufacturing practice conditions and used in large patient cohorts. Communication of common guidelines and practices is warranted to further the dissemination of SiFA radiopharmaceuticals and to give easy access to this technology.ConclusionThis current review highlights the most recent achievements in SiFA radiopharmaceutical automation geared towards large batch production for clinical application. Best practice advice and guidance towards a facilitated implementation of the SiFA technology into new and already operating PET tracer production facilities is provided. A brief outlook spotlights the future potential of SiFA radiochemistry within the landscape of non-canonical labeling chemistries.

【 授权许可】

CC BY   
© Springer Nature Switzerland AG 2023

【 图 表 】

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