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[64Cu]Cu-PSMA-R2 is a radiopharmaceutical diagnostic agent designed for positron emission tomography (PET) imaging of prostate cancer. It consists of the positron-emitting radioisotope copper-64 (64Cu) complexed with PSMA-R2, a small-molecule ligand that targets the prostate-specific membrane antigen (PSMA), also known as glutamate carboxypeptidase II. PSMA is a transmembrane protein that is significantly overexpressed in prostate cancer cells, particularly in metastatic and castration-resistant forms of the disease. Upon intravenous administration, [64Cu]Cu-PSMA-R2 binds with high affinity to the extracellular domain of PSMA, allowing for the visualization and localization of primary and metastatic lesions. The use of copper-64 provides a longer physical half-life (approximately 12.7 hours) compared to other common PET isotopes like gallium-68 or fluorine-18, which may facilitate delayed imaging and improve the detection of small or low-PSMA-expressing lesions. The agent is primarily being investigated by the Institut de Cancérologie de l'Ouest for the detection of biochemical recurrence in patients with prostate cancer.
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