A Preclinical Comparative Study of 68Ga-Labeled DOTA, NOTA and HBED-CC Chelated PSMA-targeted Radiotracers

Prostate cancer is the leading cancer in the U.S. population and the second leading cause of cancer death in men. Therapy for locally advanced disease remains contentious and an increasing number of disparate options are available. We have been engaged in the development of new, high-sensitivity, low molecular weight imaging agents for prostate cancer using the prostate-specific membrane antigen (PSMA) as a target. PSMA is a marker for androgen-independent disease that is also expressed on solid (nonprostate) tumor neovasculature. Previously, the inventors synthesized a variety of PSMA inhibitors that selectively image prostate tumors in experimental models. The inventors also previously reported two PSMA-targeted,radiotracers conjugated to a PSMA-targeting moiety. In this study, this group directly compares in vivo pharmacokinetics and tumor targeting ability of our previous lead radiotracer to a new radiotracer, which is currently in imaging clinical trials for prostate cancer agent.

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