|Synonyms||Tiprolisant; Ciproxidine; BF2.649|
|Drug class||Histamine H3 receptor inverse agonists|
|Chemical and physical data|
|Molar mass||295.851 g/mol g·mol−1|
|3D model (JSmol)|
|(what is this?)|
Pitolisant (INN), also known as tiprolisant (USAN), is a medication in the United States that was approved by the 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, a first-in-class medication, is a potent and highly selective Histamine 3 (H₃) receptor antagonist/inverse agonist; it enhances the activity of histaminergic neurons in the brain that function to improve a patient’s wakefulness and inhibit attacks of cataplexy. 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 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.
The NDA (New Drug Submission) submission is based on results from the clinical development program in narcolepsy, which included over 300 patients, some of whom were treated for up to five years. It also included safety data in over 1500 patients across multiple patient populations. 
It was developed by Jean-Charles Schwartz, Walter Schunack, and colleagues after the former discovered the H₃ receptor. It was the first H₃ receptor inverse agonist to be tested in humans or introduced for clinical use.
|This drug article relating to the nervous system is a stub. You can help Wikipedia by expanding it.|