Design, Synthesis, and Preclinical Evaluation of Prostate-Specific Membrane Antigen Targeted 99mTc-Radioimaging Agents
May 2009
in “
Molecular Pharmaceutics
”
TLDR Researchers developed promising agents for prostate cancer imaging, with the best one showing high potential for clinical use.
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.