Recent Advances in the Clinical Translation of Silicon Fluoride Acceptor (SiFA) 18F-Radiopharmaceuticals

Lexi Gower-Fry; Travis Kronemann; Andreas Dorian; Yinglan Pu; Carolin Jaworski; Carmen Wängler; Peter Bartenstein; Leonie Beyer; Simon Lindner; Klaus Jurkschat; Björn Wängler; Justin J Bailey; Ralf Schirrmacher

doi:10.3390/ph14070701

Recent Advances in the Clinical Translation of Silicon Fluoride Acceptor (SiFA) ¹⁸F-Radiopharmaceuticals

Pharmaceuticals (Basel). 2021 Jul 20;14(7):701. doi: 10.3390/ph14070701.

Affiliations

¹ Department of Oncology, Division of Oncological Imaging, University of Alberta, Edmonton, AB T6G 1Z2, Canada.
² Biomedical Chemistry, Department of Clinical Radiology and Nuclear Medicine, Medical Faculty Mannheim of Heidelberg University, Theodor-Kutzer-Ufer 1-3, 68167 Mannheim, Germany.
³ Department of Nuclear Medicine, University Hospital, LMU Munich, Marchioninistraße 15, 81377 Munich, Germany.
⁴ Fakultät für Chemie und Chemische Biologie, Technische Universität Dortmund, 44227 Dortmund, Germany.
⁵ Molecular Imaging and Radiochemistry, Department of Clinical Radiology and Nuclear Medicine, Medical Faculty Mannheim of Heidelberg University, Theodor-Kutzer-Ufer 1-3, 68167 Mannheim, Germany.

Abstract

The incorporation of silicon fluoride acceptor (SiFA) moieties into a variety of molecules, such as peptides, proteins and biologically relevant small molecules, has improved the generation of ¹⁸F-radiopharmaceuticals for medical imaging. The efficient isotopic exchange radiofluorination process, in combination with the enhanced [¹⁸F]SiFA in vivo stability, make it a suitable strategy for fluorine-18 incorporation. This review will highlight the clinical applicability of [¹⁸F]SiFA-labeled compounds and discuss the significant radiotracers currently in clinical use.

Keywords: fluorine-18; positron emission tomography (PET); radiochemistry; silicon fluoride acceptor (SiFA).

Publication types

Review