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Pitolisant skeletal.svg
Clinical data
Trade namesWakix
SynonymsTiprolisant; Ciproxidine; BF2.649
License data
Routes of
Drug classHistamine H3 receptor inverse agonists
ATC code
CAS Number
PubChem CID
Chemical and physical data
Molar mass295.851 g/mol g·mol−1
3D model (JSmol)
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Pitolisant (INN), also known as tiprolisant (USAN),[1] 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.[2]


Pitolisant was developed by Jean-Charles Schwartz, Walter Schunack, and colleagues after the former discovered the H₃ receptor.[3] It was the first H₃ receptor inverse agonist to be tested in humans or introduced for clinical use.[3] 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 United States FDA in August 2019. 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.


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  2. ^ Syed, Yahiya Y. (20 July 2016). "Pitolisant: First Global Approval". Drugs. 76 (13): 1313–1318. doi:10.1007/s40265-016-0620-1.
  3. ^ a b 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.