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Fluoromethylcholine is a small molecule structural analog of choline that acts as a potent, irreversible inhibitor of the gut microbial enzyme choline trimethylamine-lyase (CutC). By blocking the microbial conversion of dietary choline into trimethylamine (TMA), it effectively reduces systemic levels of trimethylamine N-oxide (TMAO), a pro-inflammatory metabolite associated with adverse cardiovascular outcomes. In preclinical research, fluoromethylcholine has demonstrated efficacy in ameliorating immune checkpoint inhibitor-associated myocarditis (ICI-M) by preventing TMAO-induced macrophage retention and subsequent CD8+ T-cell infiltration in myocardial tissue. While being investigated as a therapeutic for inflammatory and metabolic conditions, the radiolabeled form ([18F]fluoromethylcholine) is an established PET imaging tracer used to detect cancers with high phospholipid turnover, such as prostate cancer.
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