Selexipag

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
Selexipag
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
CAS Number
3D model (JSmol)
ChEBI
ChEMBL
ChemSpider
ECHA InfoCard 100.237.916
KEGG
PubChem CID
UNII
Properties
Chemical formula
 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

Contraindications

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]

Adverse effects

The adverse effects of selexipag are similar to those of intravenous prostacyclins used for pulmonary arterial hypertension. Common side effects include headache and jaw pain. An increased risk for hyperthyroidism has also been noted in people taking selexipag.

History

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

References
  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. 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.
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