Pitolisant

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Pitolisant
Pitolisant skeletal.svg
Clinical data
Trade names Wakix
Synonyms Tiprolisant; Ciproxidine; BF2.649
License data
Routes of
administration
Oral
Drug class Histamine H3 receptor inverse agonists
ATC code
Identifiers
CAS Number
PubChem CID
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
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]

References[edit]

  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. 

External links[edit]