Design, Synthesis, and Preclinical Evaluation of Prostate-Specific Membrane Antigen Targeted 99mTc-Radioimaging Agents

    April 2009 in “ Molecular Pharmaceutics ”
    Sumith A. Kularatne, Zhigang Zhou, Jun J. Yang, Carol Beth Post, Philip S. Low
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    Studysummary This study reports that three synthesized PSMA-targeted radioimaging agents demonstrated high affinity and specific localization to prostate cancer tumors in a mouse model, highlighting their potential for cancer detection and monitoring.
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    In 2009, researchers developed and evaluated a series of prostate-specific membrane antigen (PSMA)-targeted 99mTc-radioimaging agents for prostate cancer detection. They synthesized six agents, with three showing low nanomolar affinity for PSMA-expressing LNCaP cells and selective localization to LNCaP tumor xenografts in mice. The most promising agent demonstrated 12.4% injected dose per gram of tumor tissue at 4 hours post-injection with high tumor-to-muscle ratios, indicating its potential for clinical imaging applications. The study concluded that these agents, particularly the most effective compound, could be promising for PSMA-targeted radioimaging of prostate cancer.
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