General Information of Drug (ID: DMAHSU0)

Drug Name
Selexipag Drug Info
Synonyms
Selexipag; NS-304; 475086-01-2; Uptravi; NS 304; ACT-293987; UNII-5EXC0E384L; Selexipag(NS-304); ACT 293987; 5EXC0E384L; 2-(4-((5,6-diphenylpyrazin-2-yl)(isopropyl)amino)butoxy)-N-(methylsulfonyl)acetamide; 2-{4-[N-(5,6-diphenylpyrazin-2-yl)-N-isopropylamino]butyloxy}-N-(methylsulfonyl)acetamide; 2-(4-((5,6-Diphenylpyrazin-2-yl)(propan-2-yl)amino)butoxy}-n-(methanesulfonyl)acetamide; Selexipag [USAN:INN]; 2-{4-[(5,6-diphenylpyrazin-2-yl)(propan-2-yl)amino]butoxy}-N-(methanesulfonyl)acetamide; Uptravi (TN)
Indication
Disease Entry ICD 11 Status REF
Pulmonary arterial hypertension BB01.0 Approved [1] , [2]
Cross-matching ID
PubChem CID
9913767
ChEBI ID
CHEBI:90844
CAS Number
CAS 475086-01-2
TTD Drug ID
DMAHSU0
INTEDE Drug ID
DR1471
ACDINA Drug ID
D00619

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
DME
Drug Status:
Approved Drug(s)
Clinical Trial Drug(s)
Discontinued Drug(s)
Drug(s) Metabolized By Cytochrome P450 2C8 (CYP2C8)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Fluorouracil DMUM7HZ Solid tumour/cancer 2A00-2F9Z Approved [5]
Estradiol DMUNTE3 Breast cancer 2C60-2C65 Approved [6]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [6]
Zidovudine DM4KI7O Human immunodeficiency virus infection 1C62 Approved [7]
Verapamil DMA7PEW Hypertension BA00-BA04 Approved [8]
Diclofenac DMPIHLS Osteoarthritis FA00-FA05 Approved [9]
Sorafenib DMS8IFC Hepatocellular carcinoma 2C12.02 Approved [10]
Quinine DMSWYF5 Malaria 1F40-1F45 Approved [6]
Mycophenolate mofetil DMPQAGE Organ transplant rejection NE84 Approved [11]
Propofol DMB4OLE Anaesthesia 9A78.6 Approved [12]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Treprostinil DMTIQF3 Pulmonary arterial hypertension BB01.0 Approved [13]
Epoprostenol DMUTYR2 Pulmonary hypertension BB01 Approved [14]
Dinoprost Tromethamine DMXQKSL Abortion JA00 Approved [15]
Misoprostol DMHVJFK Medical abortion JA00.1Z Approved [15]
LAROPIPRANT DM5FABJ Coronary heart disease BA80.Z Phase 4 [16]
Beraprost DMWL182 Pulmonary hypertension BB01 Phase 4 [17]
esuberaprost DMXLGED Gout FA25 Phase 3 [18]
Ralinepag DM7G4Y9 Pulmonary arterial hypertension BB01.0 Phase 2 [19]
Clinprost DM6E5VA Asthma CA23 Discontinued in Preregistration [20]
Ataprost DMPTG39 Asthma CA23 Discontinued in Phase 3 [21]
⏷ Show the Full List of 10 Drug(s)

Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Prostacyclin receptor (PTGIR) TTOFYT1 PI2R_HUMAN Agonist [3]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID MOA REF
Cytochrome P450 2C8 (CYP2C8) Main DME DES5XRU CP2C8_HUMAN Substrate [4]

References

1 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7552).
2 ClinicalTrials.gov (NCT01106014) Selexipag (ACT-293987) in Pulmonary Arterial Hypertension, GRIPHON Trial. U.S. National Institutes of Health.
3 Selexipag: an oral, selective prostacyclin receptor agonist for the treatment of pulmonary arterial hypertension. Eur Respir J. 2012 Oct;40(4):874-80.
4 FDA Label of Uptravi. The 2020 official website of the U.S. Food and Drug Administration.
5 Roles of cytochromes P450 1A2, 2A6, and 2C8 in 5-fluorouracil formation from tegafur, an anticancer prodrug, in human liver microsomes. Drug Metab Dispos. 2000 Dec;28(12):1457-63.
6 Role of cytochrome P450 2C8 in drug metabolism and interactions. Pharmacol Rev. 2016 Jan;68(1):168-241.
7 Summary of information on human CYP enzymes: human P450 metabolism data. Drug Metab Rev. 2002 Feb-May;34(1-2):83-448.
8 Differential expression and function of CYP2C isoforms in human intestine and liver. Pharmacogenetics. 2003 Sep;13(9):565-75.
9 Analysis of human cytochrome P450 2C8 substrate specificity using a substrate pharmacophore and site-directed mutants. Biochemistry. 2004 Dec 14;43(49):15379-92.
10 Interaction of sorafenib and cytochrome P450 isoenzymes in patients with advanced melanoma: a phase I/II pharmacokinetic interaction study. Cancer Chemother Pharmacol. 2011 Nov;68(5):1111-8.
11 PharmGKB summary: mycophenolic acid pathway. Pharmacogenet Genomics. 2014 Jan;24(1):73-9.
12 Possible involvement of multiple human cytochrome P450 isoforms in the liver metabolism of propofol. Br J Anaesth. 1998 Jun;80(6):788-95.
13 Dosing considerations in the use of intravenous prostanoids in pulmonary arterial hypertension: an experience-based review. Am Heart J. 2009 Apr;157(4):625-35.
14 Novel signaling pathways promote a paracrine wave of prostacyclin-induced vascular smooth muscle differentiation. J Mol Cell Cardiol. 2009 May;46(5):682-94.
15 Palmitoylation of the human prostacyclin receptor. Functional implications of palmitoylation and isoprenylation. J Biol Chem. 2003 Feb 28;278(9):6947-58.
16 Discovery of a potent and selective prostaglandin D2 receptor antagonist, [(3R)-4-(4-chloro-benzyl)-7-fluoro-5-(methylsulfonyl)-1,2,3,4-tetrahydroc... J Med Chem. 2007 Feb 22;50(4):794-806.
17 Prostaglandin I2 IP Receptor Agonist, Beraprost, Prevents Transient Global Cerebral Ischemia Induced Hippocampal CA1 Injury in Aging Mice. J Neurol Disord. 2014;2:1000174.
18 Specific binding of the new stable epoprostenol analogue beraprost sodium to prostacyclin receptors on human and rat platelets. Arzneimittelforschung. 1989 Apr;39(4):495-9.
19 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
20 Protective effect of a prostaglandin I2 analog, TEI-7165, on ischemic neuronal damage in gerbils. Brain Res. 1997 Sep 26;769(2):321-8.
21 Pharmacokinetics of intravenous ataprost alfadex, a new prostaglandin I2 analog in healthy volunteers. Int J Clin Pharmacol Ther Toxicol. 1993 Aug;31(8):373-5.