Pitolisant

From Wikipedia, the free encyclopedia
Jump to navigation Jump to search
Pitolisant
Pitolisant skeletal.svg
Clinical data
Trade namesWakix
SynonymsTiprolisant; Ciproxidine; BF2.649
License data
Routes of
administration
Oral
Drug classHistamine H3 receptor inverse agonists
ATC code
Identifiers
CAS Number
PubChem CID
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
Chemical and physical data
FormulaC17H26ClNO
Molar mass295.851 g/mol g·mol−1
3D model (JSmol)
 ☒N☑Y (what is this?)  (verify)

Pitolisant (INN), also known as tiprolisant (USAN),[1] 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. [1]

It 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]

References[edit]

  1. ^ http://adisinsight.springer.com/drugs/800029451
  2. ^ 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.

External links[edit]