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Pitolisant skeletal.svg
Clinical data
Trade names Wakix
Synonyms Tiprolisant; Ciproxidine; BF2.649
License data
Routes of
Drug class Histamine H3 receptor inverse agonists
ATC code
CAS Number
PubChem CID
Chemical and physical data
Formula C17H26ClNO
Molar mass 295.851 g/mol
3D model (JSmol)
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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.[1][2][3][4] It is also currently in phase III clinical trials for the treatment of hypersomnia.[1]

Pitolisant was developed by Jean-Charles Schwartz, Walter Schunack, and colleagues after the former discovered the H3 receptor.[5] It was the first H3 receptor inverse agonist to be tested in humans or introduced for clinical use.[5]


  1. ^ a b http://adisinsight.springer.com/drugs/800029451
  2. ^ Syed YY (2016). "Pitolisant: First Global Approval". Drugs. 76 (13): 1313–8. doi:10.1007/s40265-016-0620-1. PMID 27438291. 
  3. ^ 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. 
  4. ^ 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 5414617Freely accessible. PMID 28490912. 
  5. ^ 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 3111674Freely accessible. PMID 21615387. 

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