Selexipag

Structural formula
General
Surname	Selexipag
other names	2- {4 - [(5,6-Diphenylpyrazin-2-yl) (propan-2-yl) amino] butoxy} - N - (methanesulfonyl) acetamide ( IUPAC ) ACT-293987 NS-304
Molecular formula	C 26 H 32 N 4 O 4 S
External identifiers / databases
CAS number 475086-01-2 EC number 809-991-1 ECHA InfoCard 100.237.916 PubChem 9913767 ChemSpider 8089417 DrugBank DB11362 Wikidata Q15424759
Drug information
Mechanism of action	selective prostacyclin (IP) receptor - agonist
properties
Molar mass	496.6 g mol −1
safety instructions
GHS hazard labeling no classification available
As far as possible and customary, SI units are used. Unless otherwise noted, the data given apply to standard conditions .

Selexipag is a medicine used to treat high blood pressure in the bloodstream of the lungs (pulmonary arterial hypertension). It is an oral selective agonist of the prostacyclin (IP) receptor and leads to vasodilation, especially in the pulmonary circulation, which leads to a reduction in blood pressure there.

The drug itself is active at the IP receptor and also has an active metabolite with a longer half-life, ACT-333679 (MRE-269), which is the free carboxylic acid.

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

Selexipag was designed by the Swiss pharmaceutical company Actelion developed and received under the trade name Uptravi in December 2015 by the US Food and Drug Administration FDA approval as an orphan drug for the treatment of pulmonary arterial hypertension. Approval in the EU followed in May 2016.

Phase III study

The approval was primarily based on the results of the "GRIPHON" study, a French multicenter, randomized, double-blind, placebo- controlled, phase III clinical study . This included 1,156 patients with idiopathic, hereditary or secondary pulmonary arterial hypertension who received individually up to 1,600 μg selexipag (or placebo) up to twice daily for a median of 70 weeks (median of placebo for 63 weeks). This showed a significant positive effect with a hazard ratio of 0.60 under Selexipag ( confidence interval 0.46–0.78). The primary endpoint was defined as death or complication from pulmonary arterial hypertension and was achieved in 27.0% with Selexipag and in 41.6% with placebo. Serious adverse effects occurred significantly more frequently and led to early discontinuation of therapy in 14.3% (7.1% with placebo). Headache (65% with Selexipag versus 33% with placebo), diarrhea (42% versus 19%), nausea (34% versus 19%), jaw pain (26% versus 6%) and vomiting (18% ) occurred particularly often . vs. 9%).

Web links

Public Assessment Report (EPAR) of the European Medicines Agency (EMA) for: Selexipag

Individual evidence

1. ↑ This substance has either not yet been classified with regard to its hazardousness or a reliable and citable source has not yet been found.
2. ↑ ^{a b} Olivier Sitbon, N. Morrell: Pathways in pulmonary arterial hypertension: The future is here . European Respiratory Review 2012, Volume 21, Edition 126, pages 321-327; doi: 10.1183 / 09059180.00004812 .
3. ^ New Drug Approved for Rare Lung Disorder. PPN. 23rd December 2015 .
4. ↑ Olivier Sitbon, Richard Channick et al .: Selexipag for the treatment of pulmonary arterial hypertension . New England Journal of Medicine 2015, Volume 373, Issue 26, December 24, 2015, Pages 2522-2533, DOI: 10.1056 / NEJMoa1503184 .