WAKIX Increases Histamine in the Brain

  • The MOA of WAKIX in EDS or cataplexy in adult patients with narcolepsy is unclear; however, its efficacy could be mediated through its activity as an antagonist/inverse agonist at H3 receptors, which results in increased histamine levels in the brain

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WAKIX selectivity

  • WAKIX binds to H3 receptors with a high affinity (Ki = 1 nM)
    • No appreciable binding to other histamine receptors (H1, H2, H4 receptors; Ki ≥ 10 μM)