Pitolisant

Pitolisant, sold under the brand name Wakix, is a potent and highly selective histamine 3 (H₃) receptor antagonist/inverse agonist, representing the first commercially available medication in its class. Pitolisant enhances the activity of histaminergic neurons in the brain that function to improve a person's wakefulness and decrease the number of cataplexy attacks in people that suffer from narcolepsy.[1]

Pitolisant
Clinical data
Trade namesWakix
Other namesTiprolisant; Ciproxidine; BF2.649
AHFS/Drugs.comMonograph
MedlinePlusa619055
License data
Pregnancy
category
  • US: N (Not classified yet)
    Routes of
    administration    		Oral
    Drug classHistamine H3 receptor inverse agonists
    ATC code
    Legal status
    Legal status
    • US: ℞-only
    • In general: ℞ (Prescription only)
    Identifiers
    CAS Number
    PubChem CID
    DrugBank
    ChemSpider
    UNII
    KEGG
    ChEBI
    ChEMBL
    CompTox Dashboard (EPA)
    Chemical and physical data
    FormulaC17H26ClNO
    Molar mass295.85 g·mol−1
    3D model (JSmol)
     NY (what is this?)  (verify)

    History

    Pitolisant was developed by Jean-Charles Schwartz, Walter Schunack, and colleagues after the former discovered the H₃ receptor.[2] It was the first H₃ receptor inverse agonist to be tested in humans or introduced for clinical use.[2] It was designed and developed by Bioprojet, who has marketed the product in Europe since its approval by the European Medicines Agency in 2016.

    Pitolisant was approved by the U.S. Food and Drug Administration (FDA) in August 2019.[3] It was granted orphan designation for the treatment of narcolepsy, Fast Track designation for the treatment of excessive daytime sleepiness (EDS) and cataplexy in patients with narcolepsy, and Breakthrough Therapy designation for the treatment of cataplexy in patients with narcolepsy. Pitolisant represents the first new therapy in the U.S. in over 15 years for the treatment of both EDS and cataplexy in adult patients with narcolepsy.

    References
    1. Syed, Yahiya Y. (20 July 2016). "Pitolisant: First Global Approval". Drugs. 76 (13): 1313–1318. doi:10.1007/s40265-016-0620-1. PMID 27438291.
    2. Schwartz JC (2011). "The histamine H3 receptor: from discovery to clinical trials with pitolisant". Br. J. Pharmacol. 163 (4): 713–21. doi:10.1111/j.1476-5381.2011.01286.x. PMC 3111674. PMID 21615387.
    3. "Drug Trials Snapshots: Wakix". U.S. Food and Drug Administration (FDA). 14 August 2019. Retrieved 18 March 2020.
    • "Pitolisant". Drug Information Portal. U.S. National Library of Medicine.


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