Selexipag

Selexipag
Clinical data
Trade namesUptravi
Other namesACT-293987, NS-304
License data
Routes of
administration
By mouth, intravenous
Drug classprostacyclin receptor agonist
ATC code
Legal status
Legal status
Pharmacokinetic data
Bioavailability49%
Protein binding99%
MetabolismActivation by carboxylesterases, inactivation by CYP2C8 and others
MetabolitesACT-333679, the free acid (active metabolite)
Elimination half-life0.8–2.5 h (selexipag) and 6.2–13.5 h (ACT-333679)
Excretion93% faeces
Identifiers
  • 2-{4-[(5,6-Diphenylpyrazin-2-yl)(propan-2-yl)amino]butoxy}-N-(methanesulfonyl)acetamide
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
CompTox Dashboard (EPA)
ECHA InfoCard100.237.916
Chemical and physical data
FormulaC26H32N4O4S
Molar mass496.63 g·mol−1
3D model (JSmol)
  • CC(C)N(CCCCOCC(=O)NS(=O)(=O)C)C1=CN=C(C(=N1)C2=CC=CC=C2)C3=CC=CC=C3
  • InChI=1S/C26H32N4O4S/c1-20(2)30(16-10-11-17-34-19-24(31)29-35(3,32)33)23-18-27-25(21-12-6-4-7-13-21)26(28-23)22-14-8-5-9-15-22/h4-9,12-15,18,20H,10-11,16-17,19H2,1-3H3,(H,29,31)
     Y
  • Key:QXWZQTURMXZVHJ-UHFFFAOYSA-N
 NY (what is this?)  (verify)

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.

The most common side effects include headache, diarrhea, nausea and vomiting, jaw pain, myalgia (muscle pain), pain in the limbs, arthralgia (joint pain) and flushing.

It is available as a generic medication.