Takeda’s selective OX2R agonist oveporexton (TAK-861) gained FDA approval as Orzeyful, topping two Phase 3 trials in narcolepsy type 1. The approval makes oveporexton the first approved OX2R agonist, and Takeda framed its higher potency as enabling a low-dose approach with a favorable safety profile, including attention to liver toxicity. The FDA action followed successful clinical performance on wakefulness and cataplexy reduction endpoints, bringing a new receptor class into the narcolepsy treatment landscape. The result also highlights how dose selection and exposure management remain central for CNS drugs when safety signals require careful balancing. For competitors, the regulatory milestone shifts the competitive baseline toward OX2R-mediated pharmacology and away from older monoamine-centric strategies.