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[18F]F-H3RESCA-WWH347 is a novel radiopharmaceutical PET tracer developed for the molecular imaging of cancers that overexpress the gastrin-releasing peptide receptor (GRPR), most notably prostate cancer. The molecule consists of a high-affinity GRPR antagonist peptide, WWH347, conjugated to a restrained complexing agent (RESCA) chelator. This specific chelator was engineered to facilitate the rapid and stable incorporation of the aluminum-fluoride-18 ([18F]AlF) complex under mild conditions, which is advantageous for maintaining the integrity of peptide-based vectors. As a GRPR antagonist, the tracer binds to the receptor on the cell surface without triggering internalization, often resulting in superior imaging characteristics such as high tumor uptake and rapid background clearance compared to agonist-based tracers. It is currently being evaluated in early-phase clinical trials to improve the detection and staging of GRPR-positive malignancies.
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