|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), and sold under the brand name Wakix, is a potent and selective inverse agonist of the histamine H3 receptor (Ki = 0.16 nM) which was approved for the treatment of narcolepsy in 2016. It is also currently in phase III clinical trials for the treatment of hypersomnia.
Pitolisant 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.
- Syed YY (2016). "Pitolisant: First Global Approval". Drugs. 76 (13): 1313–8. doi:10.1007/s40265-016-0620-1. PMID 27438291.
- Schlicker E, Kathmann M (2017). "Role of the Histamine H3 Receptor in the Central Nervous System". Handb Exp Pharmacol. 241: 277–299. doi:10.1007/164_2016_12. PMID 27787717.
- Calik MW (2017). "Update on the treatment of narcolepsy: clinical efficacy of pitolisant". Nat Sci Sleep. 9: 127–133. doi:10.2147/NSS.S103462. PMC 5414617. PMID 28490912.
- 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.
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