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

This paper focuses on the introduction in mild condition of fluorine-18 via a “click chemistry” copper-catalyzed azide-alkyne cycloaddition (CuAAC) radiosynthetic route. An alkyne derivative of PSMA-617, currently one of the most interesting target in prostate cancer imaging and therapy, was synthetized and radiolabelled with fluorine-18. The whole radiosynthetic procedur e was fully automated, and the final product was obtained in radiochemical good yield and purity, and proved to be stable in human plasma up to 4 h. 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 effici...
Source: Journal of Labelled Compounds and Radiopharmaceuticals - Category: Biochemistry Authors: Tags: RESEARCH ARTICLE Source Type: research