Toward 18F‐Labeled Theranostics: A Single Agent that Can Be Labeled with 18F, 64Cu, or 177Lu. (4th December 2019)

• Record Type: Journal Article
• Authors: Lepage, Mathieu L.; Kuo, Hsiou‐Ting; Roxin, Áron; Huh, Sungjoon; Zhang, Zhengxing; Kandasamy, Rajaguru; Merkens, Helen; Kumlin, Joel O.; Limoges, Alan; Zeisler, Stefan K.; Lin, Kuo‐Shyan; Bénard, François; Perrin, David M.
• Is Part Of: Chembiochem. Volume 21:Number 7(2020)
• Page Start: 943
• Page End: 947
• Publication Date: 2019-12-04
• Subjects: 18F labeling -- peptides -- radiotracers -- theranostics; Biochemistry -- Periodicals; Molecular biology -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1002/cbic.201900632
• Languages: English
• ISSNs: 1439-4227

Abstract

Abstract: We report a single‐molecule radiotracer that can be labeled independently with 18 F‐fluoride or radiometals ( 64 Cu, 177 Lu) in a single step. A prostate‐specific membrane antigen (PSMA)‐targeting ligand, armed with both an organotrifluoroborate and a metal‐chelator (DOTA), was designed to optionally afford 18 F‐, 64 Cu‐ or 177 Lu‐labeled products that were injected into mice bearing prostate cancer (LNCaP) xenografts. PET/CT images and ex vivo biodistribution data show high, specific tumor uptake irrespective of which radionuclide is used, thereby demonstrating a new approach to combining, in a single molecule, 18 F‐labeling capabilities for PET imaging with radiometalation for potential imaging and therapeutic applications. Abstract : Three isotopes for the price of one : A single molecular entity capable of being labeled with three different radioisotopes opens new possibilities for potential use in diagnostic PET and therapy.