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[F-18]FAU is a radiolabeled nucleoside analog, specifically 1-(2'-deoxy-2'-fluoro-beta-D-arabinofuranosyl) uracil, developed as a positron emission tomography (PET) imaging agent and investigated as a potential antineoplastic therapy. It functions as a DNA synthesis inhibitor by serving as a substrate for cellular enzymes; it is phosphorylated by thymidine kinase and methylated by thymidylate synthase, eventually becoming incorporated into the DNA of proliferating cells. This mechanism allows for the visualization of tumor activity and cellular proliferation. Clinical evaluation in a first-in-human study demonstrated significant retention in breast tumors and lymph node metastases with minimal bone marrow toxicity, suggesting its potential utility as both a diagnostic tool and an unlabeled therapeutic agent, although its imaging contrast may be limited for some clinical applications.
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