64Cu-labeled inhibitors of prostate-specific membrane antigen for PET imaging of prostate cancer

Sangeeta Ray Banerjee, Mrudula Pullambhatla, Catherine A. Foss, Sridhar Nimmagadda, Riccardo Ferdani, Carolyn J. Anderson, Ronnie C. Mease, Martin G. Pomper

Research output: Contribution to journalArticlepeer-review

76 Scopus citations


Prostate-specific membrane antigen (PSMA) is a well-recognized target for identification and therapy of a variety of cancers. Here we report five 64Cu-labeled inhibitors of PSMA, [64Cu]3-7, which are based on the lysine-glutamate urea scaffold and utilize a variety of macrocyclic chelators, namely NOTA(3), PCTA(4), Oxo-DO3A(5), CB-TE2A(6), and DOTA(7), in an effort to determine which provides the most suitable pharmacokinetics for in vivo PET imaging. [64Cu]3-7 were prepared in high radiochemical yield (60-90%) and purity (>95%). Positron emission tomography (PET) imaging studies of [64Cu]3-7 revealed specific accumulation in PSMA-expressing xenografts (PSMA+ PC3 PIP) relative to isogenic control tumor (PSMA- PC3 flu) and background tissue. The favorable kinetics and high image contrast provided by CB-TE2A chelated [64Cu]6 suggest it as the most promising among the candidates tested. That could be due to the higher stability of [64Cu]CB-TE2A as compared with [64Cu]NOTA, [ 64Cu]PCTA, [64Cu]Oxo-DO3A, and [64Cu]DOTA chelates in vivo.

Original languageEnglish (US)
Pages (from-to)2657-2669
Number of pages13
JournalJournal of medicinal chemistry
Issue number6
StatePublished - Mar 27 2014

ASJC Scopus subject areas

  • Molecular Medicine
  • Drug Discovery


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