Synthesis and automated fluorine-18 radiolabeling of new PSMA-617 derivatives with a CuAAC radiosynthetic approach.

Autor: Iannone MN; Tecnomed Foundation, University of Milano-Bicocca, Milan, Italy., Stucchi S; Tecnomed Foundation, University of Milano-Bicocca, Milan, Italy., Turolla EA; Tecnomed Foundation, University of Milano-Bicocca, Milan, Italy., Beretta C; Tecnomed Foundation, University of Milano-Bicocca, Milan, Italy., Ciceri S; Department of Medical Biotechnologies and Translational Medicine, University of Milano, Milan, Italy., Chinello C; Department of Medicine and Surgery, University of Milano-Bicocca, Milan, Italy., Pagani L; Department of Medicine and Surgery, University of Milano-Bicocca, Milan, Italy., Todde S; Tecnomed Foundation, CNR-IBFM, University of Milano-Bicocca, Milan, Italy., Ferraboschi P; Department of Medical Biotechnologies and Translational Medicine, University of Milano, Milan, Italy.
Jazyk: angličtina
Zdroj: Journal of labelled compounds & radiopharmaceuticals [J Labelled Comp Radiopharm] 2022 Mar; Vol. 65 (3), pp. 48-62. Date of Electronic Publication: 2022 Jan 11.
DOI: 10.1002/jlcr.3959
Abstrakt: In the last decade, the development of new radiopharmaceuticals for the imaging and therapy of prostate cancer has been a highly active and important area of research, especially focusing on the prostate-specific membrane antigen (PSMA), an antigen which is upregulated in prostate, as well as in other tumor cells. A large variety of PSMA ligands have been radiolabeled, to date. Among the various derivatives, PSMA-617 resulted to be one of the most interesting in terms of interaction with the antigen and clinical properties, and its lutetium-177 labeled version has recently been approved by regulatory agencies for therapeutic purposes. For this reasons, the radiolabeling with fluorine-18 of a PSMA-617 derivative might be of interest. Beside other methodologies to radiolabel macromolecules with fluorine-18, the "click-chemistry" approach resulted to be very useful, and the copper-catalyzed azide-alkyne cycloaddition (CuAAC) is considered one of most efficient and reliable. This paper proposes the synthesis of a suitable precursor for the radiolabeling with fluorine-18 of a new PSMA-617 derivative. The whole radiosynthetic procedure has been fully automated, and the final product, which proved to be stable in plasma, has been obtained with radiochemical yield and purity suitable for subsequent preclinical studies.
(© 2021 John Wiley & Sons, Ltd.)
Databáze: MEDLINE
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