Premium
Toward 18 F‐Labeled Theranostics: A Single Agent that Can Be Labeled with 18 F, 64 Cu, or 177 Lu
Author(s) -
Lepage Mathieu L.,
Kuo HsiouTing,
Roxin Áron,
Huh Sungjoon,
Zhang Zhengxing,
Kandasamy Rajaguru,
Merkens Helen,
Kumlin Joel O.,
Limoges Alan,
Zeisler Stefan K.,
Lin KuoShyan,
Bénard François,
Perrin David M.
Publication year - 2020
Publication title -
chembiochem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.05
H-Index - 126
eISSN - 1439-7633
pISSN - 1439-4227
DOI - 10.1002/cbic.201900632
Subject(s) - biodistribution , lncap , radiochemistry , chemistry , glutamate carboxypeptidase ii , in vivo , ligand (biochemistry) , prostate cancer , nuclear medicine , cancer , in vitro , biochemistry , receptor , medicine , microbiology and biotechnology , biology
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.