Selexipag

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Selexipag
Selexipag.svg
Names
IUPAC name
2-{4-[(5,6-diphenylpyrazin-2-yl)(propan-2-yl)amino]butoxy}-N-(methanesulfonyl)acetamide
Other names
ACT-293987, NS-304
Identifiers
3D model (JSmol)
ChEBI
ChEMBL
ChemSpider
ECHA InfoCard 100.237.916
KEGG
UNII
Properties
C26H32N4O4S
Molar mass 496.6 g·mol−1
Pharmacology
B01AC27 (WHO)
License data
Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa).
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Infobox references

Selexipag (brand name Uptravi) is a drug developed by Actelion for the treatment of pulmonary arterial hypertension (PAH). Selexipag and its active metabolite, ACT-333679 (or MRE-269, the free carboxylic acid), are agonists of the prostacyclin receptor, which leads to vasodilation in the pulmonary circulation.[1]

ACT-333679 or MRE-269, the active metabolite of selexipag

Contraindications[edit]

In Europe, use of selexipag together with strong inhibitors of the liver enzyme [CYP2C8], such as gemfibrozil, is contraindicated because it increases concentrations of selexipag twofold, and its active metabolite 11-fold, potentially leading to more adverse effects.[2]

History[edit]

The US FDA granted selexipag Orphan Drug status for PAH.[3] It was approved by the US FDA on 22 December 2015.[3] The expected price for the drug in the US is $160,000 to $170,000 per patient before rebates.[4]

In Europe, the drug was approved in May 2016.[5]

See also[edit]

References[edit]

  1. ^ Sitbon, O.; Morrell, N. (2012). "Pathways in pulmonary arterial hypertension: The future is here". European Respiratory Review. 21 (126): 321–327. doi:10.1183/09059180.00004812. PMID 23204120. 
  2. ^ Information des Bundesamtes für Sicherheit im Gesundheitswesen zu Uptravi (in German), Österreichisches Bundesamt für Sicherheit im Gesundheitswesen, 2017-06-07 
  3. ^ a b New Drug Approved for Rare Lung Disorder. PPN. 23 Dec 2015 Has link to GRIPHON study results
  4. ^ "Actelion sees Uptravi price of $160,000-170,000/patient". Reuters. 2016-01-05. Retrieved 2016-01-06. 
  5. ^ "Uptravi: Authorisation details". European Medicines Agency. 2016-05-12.