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Firazorexton (development code TAK-994) is an experimental, orally active small-molecule agonist of the orexin receptor type 2 (OX2R). Developed by Takeda, it was the first oral OX2R agonist to reach clinical trials and was designed to selectively target orexin 2 receptors with high specificity (>700-fold selectivity over orexin receptor 1). The drug aimed to address excessive daytime sleepiness and cataplexy in patients with narcolepsy type 1 by compensating for underlying orexin deficiency. Phase 2 studies demonstrated significant improvements in wakefulness and reductions in cataplexy rates compared to placebo. However, development was terminated due to hepatotoxicity observed during clinical trials[1][3][5][6].
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