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68Ga-DOTA-AE105 is a diagnostic radiopharmaceutical used as a positron emission tomography (PET) imaging agent to detect the expression of the urokinase-type plasminogen activator receptor (uPAR). The agent consists of the high-affinity uPAR antagonist peptide AE105, conjugated to the chelator DOTA and radiolabeled with Gallium-68 (68Ga). uPAR is a cell surface receptor that plays a critical role in extracellular matrix degradation, facilitating cancer cell invasion and metastasis, and its overexpression is associated with poor prognosis in various malignancies, including glioblastoma, breast, and prostate cancers. Developed primarily by researchers at the University of Copenhagen and Rigshospitalet, 68Ga-DOTA-AE105 has been evaluated in Phase 1 and Phase 2 clinical trials for tumor imaging. Preclinical comparisons have noted that while effective, the DOTA-chelated version may exhibit lower in vivo stability and tumor uptake compared to NODAGA-chelated or Copper-64 labeled analogs.
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