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PSMA-PET radiotracers are a class of diagnostic imaging agents used in positron emission tomography (PET) to detect and stage prostate cancer. These tracers consist of a targeting ligand—typically a small molecule or peptide—that binds with high affinity to the extracellular domain of the prostate-specific membrane antigen (PSMA), also known as glutamate carboxypeptidase II (GCPII). PSMA is significantly upregulated in nearly all prostate cancer cells, particularly in high-grade, metastatic, and castrate-resistant disease. The targeting ligand is chelated or covalently bonded to a positron-emitting radioisotope, most commonly Gallium-68 ($^{68}$Ga) or Fluorine-18 ($^{18}$F). Upon intravenous administration, the tracer accumulates in PSMA-expressing tissues, allowing for precise localization of primary tumors, lymph node metastases, and distant visceral or bone lesions. This modality has demonstrated superior sensitivity and specificity compared to conventional imaging (CT and bone scan) for initial staging and the detection of biochemical recurrence.
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