|Other names||ACT-293987, NS-304|
|By mouth, intravenous|
|Chemical and physical data|
|Molar mass||496.63 g·mol−1|
|3D model (JSmol)|
|(what is this?)|
Selexipag, sold under the brand name Uptravi, is a medication 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. It is taken by mouth or administered intravenously.
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.
Selexipag acts on the prostacyclin receptor of lung tissue. It is selective for the prostacyclin receptor. The binding of selexipag to this receptor leads to three major effects: increased vasodilation of the arteries, decreased cell proliferation and inhibition of platelet aggregation, all beneficial in the treatment of pulmonary arterial hypertension.
The U.S. Food and Drug Administration (FDA) granted selexipag orphan drug status for PAH. It was approved by the FDA on 22 December 2015.
In Europe, the drug was approved in May 2016.
The expected price for the drug in the US is $160,000 to $170,000 per patient before rebates.