|Other names||ACT-293987, NS-304|
|Chemical and physical data|
|Molar mass||496.63 g·mol−1|
|3D model (JSmol)|
|(what is this?)|
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.
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.
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.
In Europe, the drug was approved in May 2016.
Society and culture
- Epoprostenol, another name for prostacyclin
- Analogues of prostacyclin:
- Sitbon O, Morrell N (December 2012). "Pathways in pulmonary arterial hypertension: the future is here". European Respiratory Review. 21 (126): 321–7. doi:10.1183/09059180.00004812. PMID 23204120.
- Information des Bundesamtes für Sicherheit im Gesundheitswesen zu Uptravi (in German), Österreichisches Bundesamt für Sicherheit im Gesundheitswesen, 2017-06-07
- New Drug Approved for Rare Lung Disorder. PPN. 23 Dec 2015 Has link to GRIPHON study results
- "Uptravi: Authorisation details". European Medicines Agency. 2016-05-12.
- "Actelion sees Uptravi price of $160,000-170,000/patient". Reuters. 2016-01-05. Retrieved 2016-01-06.
- "Selexipag". Drug Information Portal. U.S. National Library of Medicine.