Identification
NameSelexipag
Accession NumberDB11362
TypeSmall Molecule
GroupsApproved
Description

Selexipag was approved by the United States FDA on December 22, 2015 for the treatment of pulmonary arterial hypertension (PAH) to delay disease progression and reduce risk of hospitalization. PAH is a relatively rare disease with usually a poor prognosis requiring more treatment options to prolong long-term outcomes. Marketed by Actelion Pharmaceuticals under brand name Uptravi, selexipag and its active metabolite, ACT-333679 (MRE-269), act as agonists of the prostacyclin receptor to increase vasodilation in the pulmonary circulation and decrease elevated pressure in the blood vessels supplying blood to the lungs.

Structure
Thumb
SynonymsNot Available
External IDs ACT-293987 / NS-304
Product Ingredients Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
UptraviTablet, film coated600 μgOralActelion Registration Ltd2016-05-12Not applicableEu
UptraviTablet, coated1400 ug/1OralActelion2015-12-21Not applicableUs
UptraviTablet, coated600 ug/1OralActelion2015-12-21Not applicableUs
UptraviTablet200 mcgOralActelion2016-04-21Not applicableCanada
UptraviTablet, film coated200 μgOralActelion Registration Ltd2016-05-12Not applicableEu
UptraviTablet800 mcgOralActelion2016-04-21Not applicableCanada
UptraviTablet, film coated400 μgOralActelion Registration Ltd2016-05-12Not applicableEu
UptraviTablet, film coated1200 μgOralActelion Registration Ltd2016-05-12Not applicableEu
UptraviTablet, coated1200 ug/1OralActelion2015-12-21Not applicableUs
UptraviTablet, coated200 ug/1OralActelion2015-12-21Not applicableUs
UptraviTablet1400 mcgOralActelion2016-04-21Not applicableCanada
UptraviTablet, film coated200 μgOralActelion Registration Ltd2016-05-12Not applicableEu
UptraviTablet, film coated800 μgOralActelion Registration Ltd2016-05-12Not applicableEu
UptraviTablet, coated1600 ug/1OralActelion2015-12-21Not applicableUs
UptraviTablet, coated800 ug/1OralActelion2015-12-21Not applicableUs
UptraviTablet400 mcgOralActelion2016-04-21Not applicableCanada
UptraviTablet1000 mcgOralActelion2016-04-21Not applicableCanada
UptraviTablet, film coated1400 μgOralActelion Registration Ltd2016-05-12Not applicableEu
UptraviTablet, coated400 ug/1OralActelion2015-12-21Not applicableUs
UptraviTablet1600 mcgOralActelion2016-04-21Not applicableCanada
UptraviTablet, film coated200 μgOralActelion Registration Ltd2016-05-12Not applicableEu
UptraviTablet, film coated1000 μgOralActelion Registration Ltd2016-05-12Not applicableEu
UptraviTablet, coated1000 ug/1OralActelion2015-12-21Not applicableUs
UptraviTablet600 mcgOralActelion2016-04-21Not applicableCanada
UptraviTablet1200 mcgOralActelion2016-04-21Not applicableCanada
UptraviTablet, film coated1600 μgOralActelion Registration Ltd2016-05-12Not applicableEu
UPTRAVI Titration PackKitActelion2015-12-21Not applicableUs
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International BrandsNot Available
Brand mixturesNot Available
Categories
UNII5EXC0E384L
CAS number475086-01-2
WeightAverage: 496.63
Monoisotopic: 496.2144267
Chemical FormulaC26H32N4O4S
InChI KeyQXWZQTURMXZVHJ-UHFFFAOYSA-N
InChI
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)
IUPAC Name
2-{4-[(5,6-diphenylpyrazin-2-yl)(propan-2-yl)amino]butoxy}-N-methanesulfonylacetamide
SMILES
CC(C)N(CCCCOCC(=O)NS(C)(=O)=O)C1=NC(C2=CC=CC=C2)=C(N=C1)C1=CC=CC=C1
Pharmacology
Indication

Selexipag is indicated for the treatment of pulmonary arterial hypertension (PAH) to delay disease progression and reduce risk of hospitalization.

Structured Indications
Pharmacodynamics

At the maximum tolerated dose of 1600 mcg twice per day, selexipag was not found to prolong the QT interval to a clinically relevant extent. Both selexipag and its metabolite caused concentration-dependent inhibition of platelet aggregation in vitro with IC50 of 5.5 µM and 0.21 µM, respectively. However, at clinically relevant concentrations, there was no effect on platelet aggregation test parameters following multiple dose administration of selexipag in healthy patients.

Mechanism of action

Selexipag is a selective prostacyclin (IP, also called PGI2) receptor agonist. The key features of pulmonary arterial hypertension include a decrease in prostacyclin and prostacyclin synthase (enzyme that helps produce prostacyclin) in the lung. Prostacyclin is a potent vasodilator with anti-proliferative, anti-inflammatory, and anti-thrombotic effects; therefore, there is strong rationale for treatment with IP receptor agonists. Selexipag is chemically distinct as it is not PGI2 or a PGI2 analogue and has high selectivity for the IP receptor. It is metabolized by carboxylesterase 1 to yield an active metabolite (ACT-333679) that is approximately 37 times more potent than selexipag. Both selexipag and its metabolite are selective for the IP receptor over other prostanoid receptors.

TargetKindPharmacological actionActionsOrganismUniProt ID
Prostacyclin receptorProteinyes
agonist
HumanP43119 details
Related Articles
Absorption

After oral administration, maximum concentrations of selexipag and its metabolite were observed to be reached at 1-3 and 3-4 hours, respectively. Absorption was impaired in the presence of food, resulting in delayed time to maximum concentration as well as ~30% lower peak plasma concentration. However, exposure was not found to be significantly affected by food.

Volume of distributionNot Available
Protein binding

Both selexipag and its active metabolite are highly protein bound, approximately 99%.

Metabolism

Selexipag yields its active metabolite by hydrolysis of the acylsulfonamide by the enzyme hepatic carboxylesterase 1. Oxidative metabolism catalyzed by CYP3A4 and CYP2C8 results in hydroxylated and dealkylated products. UGT1A3 and UGT2B7 are involved in the glucuronidation of the active metabolite. Other than active metabolite, other metabolites in circulation do not exceed 3% of the total drug-related material.

SubstrateEnzymesProduct
Selexipag
ACT-333679Details
Route of elimination

93% in feces, 12% in urine.

Half life

Selexipag's terminal half life is 0.8-2.5 hours. The active metabolite's terminal half life is 6.2-13.5 hours.

Clearance

On average, 35 L/hour.

Toxicity

A 40-70% increase in exposure was observed in subjects with severe renal impairment.

Affected organisms
  • Humans and other mammals
PathwaysNot Available
Pharmacogenomic Effects/ADRs Not Available
Interactions
Drug Interactions
DrugInteractionDrug group
7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline7,8-DICHLORO-1,2,3,4-TETRAHYDROISOQUINOLINE may increase the hypotensive activities of Selexipag.Experimental
AbciximabSelexipag may increase the anticoagulant activities of Abciximab.Approved
AbirateroneThe serum concentration of Selexipag can be increased when it is combined with Abiraterone.Approved
AcebutololAcebutolol may increase the hypotensive activities of Selexipag.Approved
AcenocoumarolSelexipag may increase the anticoagulant activities of Acenocoumarol.Approved
AcetaminophenThe serum concentration of Selexipag can be increased when it is combined with Acetaminophen.Approved
Acetylsalicylic acidThe risk or severity of adverse effects can be increased when Acetylsalicylic acid is combined with Selexipag.Approved, Vet Approved
AfatinibThe serum concentration of Selexipag can be increased when it is combined with Afatinib.Approved
AlbendazoleThe serum concentration of Selexipag can be increased when it is combined with Albendazole.Approved, Vet Approved
AldosteroneThe serum concentration of Selexipag can be decreased when it is combined with Aldosterone.Experimental
AlectinibThe serum concentration of Selexipag can be increased when it is combined with Alectinib.Approved
AlfentanilThe serum concentration of Selexipag can be increased when it is combined with Alfentanil.Approved, Illicit
AlfuzosinAlfuzosin may increase the hypotensive activities of Selexipag.Approved, Investigational
AliskirenAliskiren may increase the hypotensive activities of Selexipag.Approved, Investigational
AlprenololAlprenolol may increase the hypotensive activities of Selexipag.Approved, Withdrawn
AlprostadilAlprostadil may increase the anticoagulant activities of Selexipag.Approved, Investigational
AmantadineThe serum concentration of Selexipag can be increased when it is combined with Amantadine.Approved
AmbrisentanSelexipag may increase the hypotensive activities of Ambrisentan.Approved, Investigational
AmifostineSelexipag may increase the hypotensive activities of Amifostine.Approved, Investigational
Aminohippuric acidThe serum concentration of Selexipag can be increased when it is combined with Aminohippuric acid.Approved
Aminosalicylic AcidThe risk or severity of adverse effects can be increased when Aminosalicylic Acid is combined with Selexipag.Approved
AmiodaroneThe metabolism of Selexipag can be decreased when combined with Amiodarone.Approved, Investigational
AmitriptylineThe serum concentration of Selexipag can be increased when it is combined with Amitriptyline.Approved
AmlodipineThe serum concentration of Selexipag can be increased when it is combined with Amlodipine.Approved
AmprenavirThe serum concentration of Selexipag can be decreased when it is combined with Amprenavir.Approved
AmsacrineThe serum concentration of Selexipag can be increased when it is combined with Amsacrine.Approved
AnagrelideAnagrelide may increase the anticoagulant activities of Selexipag.Approved
AncrodSelexipag may increase the anticoagulant activities of Ancrod.Investigational
Antithrombin III humanSelexipag may increase the anticoagulant activities of Antithrombin III human.Approved
ApixabanSelexipag may increase the anticoagulant activities of Apixaban.Approved
AprepitantThe serum concentration of Selexipag can be increased when it is combined with Aprepitant.Approved, Investigational
AprotininThe therapeutic efficacy of Selexipag can be decreased when used in combination with Aprotinin.Approved, Withdrawn
ArdeparinSelexipag may increase the anticoagulant activities of Ardeparin.Approved, Withdrawn
ArgatrobanSelexipag may increase the anticoagulant activities of Argatroban.Approved, Investigational
AstemizoleThe serum concentration of Selexipag can be increased when it is combined with Astemizole.Approved, Withdrawn
AtazanavirThe metabolism of Selexipag can be decreased when combined with Atazanavir.Approved, Investigational
AtenololThe serum concentration of Selexipag can be increased when it is combined with Atenolol.Approved
AtomoxetineThe metabolism of Selexipag can be decreased when combined with Atomoxetine.Approved
AtorvastatinThe serum concentration of Selexipag can be increased when it is combined with Atorvastatin.Approved
AzelastineThe serum concentration of Selexipag can be increased when it is combined with Azelastine.Approved
AzithromycinThe serum concentration of Selexipag can be increased when it is combined with Azithromycin.Approved
BalsalazideThe risk or severity of adverse effects can be increased when Balsalazide is combined with Selexipag.Approved, Investigational
BecaplerminSelexipag may increase the anticoagulant activities of Becaplermin.Approved, Investigational
BenazeprilBenazepril may increase the hypotensive activities of Selexipag.Approved, Investigational
BendroflumethiazideBendroflumethiazide may increase the hypotensive activities of Selexipag.Approved
BenmoxinBenmoxin may increase the hypotensive activities of Selexipag.Withdrawn
BenzocaineThe serum concentration of Selexipag can be increased when it is combined with Benzocaine.Approved
BepridilThe serum concentration of Selexipag can be increased when it is combined with Bepridil.Approved, Withdrawn
BeraprostBeraprost may increase the anticoagulant activities of Selexipag.Investigational
BetaxololBetaxolol may increase the hypotensive activities of Selexipag.Approved
BethanidineBethanidine may increase the hypotensive activities of Selexipag.Approved
BexaroteneThe serum concentration of Selexipag can be decreased when it is combined with Bexarotene.Approved, Investigational
BimatoprostBimatoprost may increase the hypotensive activities of Selexipag.Approved, Investigational
BiperidenThe serum concentration of Selexipag can be increased when it is combined with Biperiden.Approved
BisoprololBisoprolol may increase the hypotensive activities of Selexipag.Approved
BivalirudinSelexipag may increase the anticoagulant activities of Bivalirudin.Approved, Investigational
BoceprevirThe metabolism of Selexipag can be decreased when combined with Boceprevir.Withdrawn
BortezomibThe metabolism of Selexipag can be decreased when combined with Bortezomib.Approved, Investigational
BosentanThe serum concentration of Selexipag can be decreased when it is combined with Bosentan.Approved, Investigational
BosutinibThe serum concentration of Selexipag can be increased when it is combined with Bosutinib.Approved
BretyliumBretylium may increase the hypotensive activities of Selexipag.Approved
BrimonidineBrimonidine may increase the hypotensive activities of Selexipag.Approved
BrimonidineBrimonidine may increase the antihypertensive activities of Selexipag.Approved
BromocriptineThe serum concentration of Selexipag can be increased when it is combined with Bromocriptine.Approved, Investigational
BupranololBupranolol may increase the hypotensive activities of Selexipag.Approved
BuprenorphineThe serum concentration of Selexipag can be increased when it is combined with Buprenorphine.Approved, Illicit, Investigational, Vet Approved
BuspironeThe serum concentration of Selexipag can be increased when it is combined with Buspirone.Approved, Investigational
ButylphthalideButylphthalide may increase the anticoagulant activities of Selexipag.Investigational
CabazitaxelThe serum concentration of Selexipag can be increased when it is combined with Cabazitaxel.Approved
CaffeineThe serum concentration of Selexipag can be increased when it is combined with Caffeine.Approved
CanagliflozinThe serum concentration of Selexipag can be increased when it is combined with Canagliflozin.Approved
CandesartanThe serum concentration of Selexipag can be increased when it is combined with Candesartan.Approved
CandoxatrilCandoxatril may increase the hypotensive activities of Selexipag.Experimental
CangrelorCangrelor may increase the anticoagulant activities of Selexipag.Approved
CaptoprilThe serum concentration of Selexipag can be increased when it is combined with Captopril.Approved
CarbamazepineThe metabolism of Selexipag can be increased when combined with Carbamazepine.Approved, Investigational
CaroxazoneCaroxazone may increase the hypotensive activities of Selexipag.Withdrawn
CarteololCarteolol may increase the hypotensive activities of Selexipag.Approved
CarvedilolThe serum concentration of Selexipag can be increased when it is combined with Carvedilol.Approved, Investigational
CaspofunginThe serum concentration of Selexipag can be increased when it is combined with Caspofungin.Approved
CelecoxibThe metabolism of Selexipag can be decreased when combined with Celecoxib.Approved, Investigational
CeliprololCeliprolol may increase the hypotensive activities of Selexipag.Approved, Investigational
CeritinibThe serum concentration of Selexipag can be increased when it is combined with Ceritinib.Approved
CertoparinSelexipag may increase the anticoagulant activities of Certoparin.Approved
ChloroquineThe serum concentration of Selexipag can be increased when it is combined with Chloroquine.Approved, Vet Approved
ChlorothiazideChlorothiazide may increase the hypotensive activities of Selexipag.Approved, Vet Approved
ChlorpromazineThe serum concentration of Selexipag can be increased when it is combined with Chlorpromazine.Approved, Vet Approved
ChlorpropamideThe serum concentration of Selexipag can be increased when it is combined with Chlorpropamide.Approved
ChlorprothixeneThe serum concentration of Selexipag can be increased when it is combined with Chlorprothixene.Approved, Withdrawn
ChlorthalidoneChlorthalidone may increase the hypotensive activities of Selexipag.Approved
CholesterolThe serum concentration of Selexipag can be increased when it is combined with Cholesterol.Experimental
Cholic AcidThe serum concentration of Selexipag can be decreased when it is combined with Cholic Acid.Approved
CilazaprilThe serum concentration of Selexipag can be increased when it is combined with Cilazapril.Approved
CilostazolCilostazol may increase the anticoagulant activities of Selexipag.Approved
CimetidineThe serum concentration of Selexipag can be decreased when it is combined with Cimetidine.Approved
CiprofloxacinThe serum concentration of Selexipag can be increased when it is combined with Ciprofloxacin.Approved, Investigational
CitalopramThe serum concentration of Selexipag can be increased when it is combined with Citalopram.Approved
Citric AcidSelexipag may increase the anticoagulant activities of Citric Acid.Nutraceutical, Vet Approved
ClarithromycinThe metabolism of Selexipag can be decreased when combined with Clarithromycin.Approved
ClemastineThe metabolism of Selexipag can be decreased when combined with Clemastine.Approved
ClofazimineThe serum concentration of Selexipag can be increased when it is combined with Clofazimine.Approved, Investigational
ClomipramineThe serum concentration of Selexipag can be increased when it is combined with Clomipramine.Approved, Vet Approved
ClonidineClonidine may increase the hypotensive activities of Selexipag.Approved
ClopidogrelThe metabolism of Selexipag can be decreased when combined with Clopidogrel.Approved, Nutraceutical
ClotrimazoleThe metabolism of Selexipag can be decreased when combined with Clotrimazole.Approved, Vet Approved
CobicistatThe metabolism of Selexipag can be decreased when combined with Cobicistat.Approved
ColchicineThe serum concentration of Selexipag can be increased when it is combined with Colchicine.Approved
ColforsinThe serum concentration of Selexipag can be increased when it is combined with Colforsin.Experimental
ConivaptanThe serum concentration of Selexipag can be increased when it is combined with Conivaptan.Approved, Investigational
CrizotinibThe metabolism of Selexipag can be decreased when combined with Crizotinib.Approved
CryptenamineCryptenamine may increase the hypotensive activities of Selexipag.Approved
CyclophosphamideThe serum concentration of Selexipag can be increased when it is combined with Cyclophosphamide.Approved, Investigational
CyclosporineThe metabolism of Selexipag can be decreased when combined with Cyclosporine.Approved, Investigational, Vet Approved
CyclothiazideCyclothiazide may increase the hypotensive activities of Selexipag.Approved
Dabigatran etexilateSelexipag may increase the anticoagulant activities of Dabigatran etexilate.Approved
DabrafenibThe serum concentration of Selexipag can be decreased when it is combined with Dabrafenib.Approved
DaclatasvirThe serum concentration of Selexipag can be increased when it is combined with Daclatasvir.Approved
DactinomycinThe serum concentration of Selexipag can be increased when it is combined with Dactinomycin.Approved
DalteparinSelexipag may increase the anticoagulant activities of Dalteparin.Approved
DanaparoidSelexipag may increase the anticoagulant activities of Danaparoid.Approved, Withdrawn
DarexabanSelexipag may increase the anticoagulant activities of Ym150.Investigational
DarunavirThe metabolism of Selexipag can be decreased when combined with Darunavir.Approved
DasatinibThe serum concentration of Selexipag can be increased when it is combined with Dasatinib.Approved, Investigational
DaunorubicinThe serum concentration of Selexipag can be decreased when it is combined with Daunorubicin.Approved
DebrisoquinDebrisoquin may increase the hypotensive activities of Selexipag.Approved
DeferasiroxThe serum concentration of Selexipag can be decreased when it is combined with Deferasirox.Approved, Investigational
DefibrotideDefibrotide may increase the anticoagulant activities of Selexipag.Approved, Investigational
DelavirdineThe metabolism of Selexipag can be decreased when combined with Delavirdine.Approved
dersalazineThe risk or severity of adverse effects can be increased when dersalazine is combined with Selexipag.Investigational
DeserpidineSelexipag may increase the hypotensive activities of Deserpidine.Approved
DesipramineThe serum concentration of Selexipag can be increased when it is combined with Desipramine.Approved
DesirudinSelexipag may increase the anticoagulant activities of Desirudin.Approved
DesloratadineThe serum concentration of Selexipag can be increased when it is combined with Desloratadine.Approved, Investigational
DexamethasoneThe serum concentration of Selexipag can be decreased when it is combined with Dexamethasone.Approved, Investigational, Vet Approved
DextranSelexipag may increase the anticoagulant activities of Dextran.Approved, Vet Approved
Dextran 40Selexipag may increase the anticoagulant activities of Dextran 40.Approved
Dextran 70Selexipag may increase the anticoagulant activities of Dextran 70.Approved
Dextran 75Selexipag may increase the anticoagulant activities of Dextran 75.Approved
DextromethorphanThe serum concentration of Selexipag can be increased when it is combined with Dextromethorphan.Approved
DiazoxideDiazoxide may increase the hypotensive activities of Selexipag.Approved
DiclofenacThe serum concentration of Selexipag can be increased when it is combined with Diclofenac.Approved, Vet Approved
DicoumarolSelexipag may increase the anticoagulant activities of Dicoumarol.Approved
DiflunisalThe risk or severity of adverse effects can be increased when Diflunisal is combined with Selexipag.Approved
DigoxinThe serum concentration of Selexipag can be decreased when it is combined with Digoxin.Approved
DihydralazineSelexipag may increase the hypotensive activities of Dihydralazine.Investigational
DihydroergotamineThe metabolism of Selexipag can be decreased when combined with Dihydroergotamine.Approved
DiltiazemThe metabolism of Selexipag can be decreased when combined with Diltiazem.Approved
DipyridamoleThe serum concentration of Selexipag can be increased when it is combined with Dipyridamole.Approved
DorzolamideDorzolamide may increase the hypotensive activities of Selexipag.Approved
DoxazosinThe serum concentration of Selexipag can be increased when it is combined with Doxazosin.Approved
DoxepinThe serum concentration of Selexipag can be increased when it is combined with Doxepin.Approved
DoxorubicinThe serum concentration of Selexipag can be decreased when it is combined with Doxorubicin.Approved, Investigational
DoxycyclineThe metabolism of Selexipag can be decreased when combined with Doxycycline.Approved, Investigational, Vet Approved
DronabinolThe serum concentration of Selexipag can be increased when it is combined with Dronabinol.Approved, Illicit
DronedaroneThe metabolism of Selexipag can be decreased when combined with Dronedarone.Approved
Edetic AcidSelexipag may increase the anticoagulant activities of Edetic Acid.Approved, Vet Approved
EdoxabanSelexipag may increase the anticoagulant activities of Edoxaban.Approved
EfavirenzThe serum concentration of Selexipag can be decreased when it is combined with Efavirenz.Approved, Investigational
EfonidipineEfonidipine may increase the hypotensive activities of Selexipag.Approved
ElbasvirThe serum concentration of Selexipag can be increased when it is combined with Elbasvir.Approved
EltrombopagThe serum concentration of Selexipag can be increased when it is combined with Eltrombopag.Approved
EnalaprilThe serum concentration of Selexipag can be increased when it is combined with Enalapril.Approved, Vet Approved
EnalaprilatEnalaprilat may increase the hypotensive activities of Selexipag.Approved
EnoxaparinSelexipag may increase the anticoagulant activities of Enoxaparin.Approved
EnzalutamideThe serum concentration of Selexipag can be decreased when it is combined with Enzalutamide.Approved
EpinastineEpinastine may increase the anticoagulant activities of Selexipag.Approved, Investigational
eplivanserineeplivanserine may increase the anticoagulant activities of Selexipag.Investigational
EpoprostenolEpoprostenol may increase the anticoagulant activities of Selexipag.Approved
EprosartanEprosartan may increase the hypotensive activities of Selexipag.Approved
EptifibatideEptifibatide may increase the anticoagulant activities of Selexipag.Approved, Investigational
ErgonovineThe serum concentration of Selexipag can be increased when it is combined with Ergonovine.Approved
ErgotamineThe serum concentration of Selexipag can be increased when it is combined with Ergotamine.Approved
ErythromycinThe metabolism of Selexipag can be decreased when combined with Erythromycin.Approved, Vet Approved
Eslicarbazepine acetateThe serum concentration of Selexipag can be decreased when it is combined with Eslicarbazepine acetate.Approved
EstramustineThe serum concentration of Selexipag can be increased when it is combined with Estramustine.Approved
EstriolThe serum concentration of Selexipag can be decreased when it is combined with Estriol.Approved, Vet Approved
EstroneThe serum concentration of Selexipag can be decreased when it is combined with Estrone.Approved
Ethyl biscoumacetateSelexipag may increase the anticoagulant activities of Ethyl biscoumacetate.Withdrawn
EtoposideThe serum concentration of Selexipag can be increased when it is combined with Etoposide.Approved
EtravirineThe serum concentration of Selexipag can be decreased when it is combined with Etravirine.Approved
FelodipineThe serum concentration of Selexipag can be increased when it is combined with Felodipine.Approved, Investigational
FenoldopamFenoldopam may increase the hypotensive activities of Selexipag.Approved
FentanylThe serum concentration of Selexipag can be increased when it is combined with Fentanyl.Approved, Illicit, Investigational, Vet Approved
FexofenadineThe serum concentration of Selexipag can be increased when it is combined with Fexofenadine.Approved
FidaxomicinThe serum concentration of Selexipag can be increased when it is combined with Fidaxomicin.Approved
FluconazoleThe metabolism of Selexipag can be decreased when combined with Fluconazole.Approved
FluindioneSelexipag may increase the anticoagulant activities of Fluindione.Investigational
FluoxetineThe serum concentration of Selexipag can be increased when it is combined with Fluoxetine.Approved, Vet Approved
FlupentixolThe serum concentration of Selexipag can be increased when it is combined with Flupentixol.Approved, Withdrawn
FluphenazineThe serum concentration of Selexipag can be increased when it is combined with Fluphenazine.Approved
FlurazepamThe serum concentration of Selexipag can be increased when it is combined with Flurazepam.Approved, Illicit
FluvoxamineThe metabolism of Selexipag can be decreased when combined with Fluvoxamine.Approved, Investigational
FondaparinuxSelexipag may increase the anticoagulant activities of Fondaparinux.Investigational
Fondaparinux sodiumSelexipag may increase the anticoagulant activities of Fondaparinux sodium.Approved, Investigational
FosamprenavirThe metabolism of Selexipag can be decreased when combined with Fosamprenavir.Approved
FosaprepitantThe serum concentration of Selexipag can be increased when it is combined with Fosaprepitant.Approved
FosinoprilFosinopril may increase the hypotensive activities of Selexipag.Approved
FosphenytoinThe metabolism of Selexipag can be increased when combined with Fosphenytoin.Approved
FurazolidoneFurazolidone may increase the hypotensive activities of Selexipag.Approved, Vet Approved
Fusidic AcidThe serum concentration of Selexipag can be increased when it is combined with Fusidic Acid.Approved
GabexateSelexipag may increase the anticoagulant activities of Gabexate.Investigational
GefitinibThe serum concentration of Selexipag can be increased when it is combined with Gefitinib.Approved, Investigational
GemfibrozilThe metabolism of Selexipag can be decreased when combined with Gemfibrozil.Approved
GenisteinThe serum concentration of Selexipag can be increased when it is combined with Genistein.Investigational
GlyburideThe serum concentration of Selexipag can be increased when it is combined with Glyburide.Approved
Gramicidin DThe serum concentration of Selexipag can be increased when it is combined with Gramicidin D.Approved
GrepafloxacinThe serum concentration of Selexipag can be increased when it is combined with Grepafloxacin.Withdrawn
GuanabenzGuanabenz may increase the hypotensive activities of Selexipag.Approved
GuanadrelGuanadrel may increase the hypotensive activities of Selexipag.Approved
GuanethidineGuanethidine may increase the hypotensive activities of Selexipag.Approved
GuanfacineGuanfacine may increase the hypotensive activities of Selexipag.Approved, Investigational
HaloperidolThe serum concentration of Selexipag can be increased when it is combined with Haloperidol.Approved
HeparinSelexipag may increase the anticoagulant activities of Heparin.Approved, Investigational
HexamethoniumHexamethonium may increase the hypotensive activities of Selexipag.Experimental
HydracarbazineHydracarbazine may increase the hypotensive activities of Selexipag.Experimental
HydralazineHydralazine may increase the hypotensive activities of Selexipag.Approved
HydrochlorothiazideHydrochlorothiazide may increase the hypotensive activities of Selexipag.Approved, Vet Approved
HydrocortisoneThe serum concentration of Selexipag can be increased when it is combined with Hydrocortisone.Approved, Vet Approved
HydroflumethiazideHydroflumethiazide may increase the hypotensive activities of Selexipag.Approved
IbudilastIbudilast may increase the anticoagulant activities of Selexipag.Approved, Investigational
Icosapent ethylIcosapent ethyl may increase the anticoagulant activities of Selexipag.Approved, Nutraceutical
IdelalisibThe serum concentration of Selexipag can be increased when it is combined with Idelalisib.Approved
IdraparinuxSelexipag may increase the anticoagulant activities of idraparinux.Investigational
IfenprodilIfenprodil may increase the anticoagulant activities of Selexipag.Approved, Withdrawn
IloprostIloprost may increase the anticoagulant activities of Selexipag.Approved, Investigational
ImatinibThe metabolism of Selexipag can be decreased when combined with Imatinib.Approved
ImidaprilSelexipag may increase the hypotensive activities of Imidapril.Investigational
ImipramineThe serum concentration of Selexipag can be increased when it is combined with Imipramine.Approved
IndapamideIndapamide may increase the hypotensive activities of Selexipag.Approved
IndenololIndenolol may increase the hypotensive activities of Selexipag.Withdrawn
IndinavirThe metabolism of Selexipag can be decreased when combined with Indinavir.Approved
IndomethacinThe serum concentration of Selexipag can be increased when it is combined with Indomethacin.Approved, Investigational
IndoraminIndoramin may increase the hypotensive activities of Selexipag.Withdrawn
IproclozideIproclozide may increase the hypotensive activities of Selexipag.Withdrawn
IproniazidIproniazid may increase the hypotensive activities of Selexipag.Withdrawn
IrbesartanThe metabolism of Selexipag can be decreased when combined with Irbesartan.Approved, Investigational
IsavuconazoniumThe metabolism of Selexipag can be decreased when combined with Isavuconazonium.Approved, Investigational
IsocarboxazidIsocarboxazid may increase the hypotensive activities of Selexipag.Approved
IsradipineThe metabolism of Selexipag can be decreased when combined with Isradipine.Approved
ItraconazoleThe metabolism of Selexipag can be decreased when combined with Itraconazole.Approved, Investigational
IvacaftorThe serum concentration of Selexipag can be increased when it is combined with Ivacaftor.Approved
IvermectinThe serum concentration of Selexipag can be increased when it is combined with Ivermectin.Approved, Vet Approved
KetamineThe serum concentration of Selexipag can be increased when it is combined with Ketamine.Approved, Vet Approved
KetanserinKetanserin may increase the anticoagulant activities of Selexipag.Investigational
KetoconazoleThe metabolism of Selexipag can be decreased when combined with Ketoconazole.Approved, Investigational
LabetalolLabetalol may increase the hypotensive activities of Selexipag.Approved
LacidipineLacidipine may increase the hypotensive activities of Selexipag.Approved
LansoprazoleThe serum concentration of Selexipag can be increased when it is combined with Lansoprazole.Approved, Investigational
LapatinibThe serum concentration of Selexipag can be increased when it is combined with Lapatinib.Approved, Investigational
LatanoprostLatanoprost may increase the hypotensive activities of Selexipag.Approved, Investigational
LepirudinSelexipag may increase the anticoagulant activities of Lepirudin.Approved
LercanidipineLercanidipine may increase the hypotensive activities of Selexipag.Approved, Investigational
LevofloxacinThe serum concentration of Selexipag can be increased when it is combined with Levofloxacin.Approved, Investigational
LevothyroxineThe serum concentration of Selexipag can be decreased when it is combined with Levothyroxine.Approved
LidocaineThe serum concentration of Selexipag can be increased when it is combined with Lidocaine.Approved, Vet Approved
LimaprostThe risk or severity of adverse effects can be increased when Limaprost is combined with Selexipag.Approved
LiothyronineThe serum concentration of Selexipag can be decreased when it is combined with Liothyronine.Approved, Vet Approved
LiotrixThe serum concentration of Selexipag can be decreased when it is combined with Liotrix.Approved
LisinoprilThe serum concentration of Selexipag can be increased when it is combined with Lisinopril.Approved, Investigational
LofexidineLofexidine may increase the hypotensive activities of Selexipag.Approved, Investigational
LomitapideThe serum concentration of Selexipag can be increased when it is combined with Lomitapide.Approved
LoperamideThe serum concentration of Selexipag can be increased when it is combined with Loperamide.Approved
LopinavirThe metabolism of Selexipag can be decreased when combined with Lopinavir.Approved
LoratadineThe serum concentration of Selexipag can be increased when it is combined with Loratadine.Approved
LosartanThe serum concentration of Selexipag can be increased when it is combined with Losartan.Approved
LovastatinThe metabolism of Selexipag can be decreased when combined with Lovastatin.Approved, Investigational
LuliconazoleThe serum concentration of Selexipag can be increased when it is combined with Luliconazole.Approved
LumacaftorThe serum concentration of Selexipag can be increased when it is combined with Lumacaftor.Approved
MacitentanSelexipag may increase the hypotensive activities of Macitentan.Approved
ManidipineManidipine may increase the hypotensive activities of Selexipag.Approved
MaprotilineThe serum concentration of Selexipag can be increased when it is combined with Maprotiline.Approved
MebanazineMebanazine may increase the hypotensive activities of Selexipag.Withdrawn
MebendazoleThe serum concentration of Selexipag can be increased when it is combined with Mebendazole.Approved, Vet Approved
MecamylamineMecamylamine may increase the hypotensive activities of Selexipag.Approved
MefloquineThe serum concentration of Selexipag can be increased when it is combined with Mefloquine.Approved
Megestrol acetateThe serum concentration of Selexipag can be increased when it is combined with Megestrol acetate.Approved, Vet Approved
MeprobamateThe serum concentration of Selexipag can be increased when it is combined with Meprobamate.Approved, Illicit
MesalazineThe risk or severity of adverse effects can be increased when Mesalazine is combined with Selexipag.Approved
MethadoneThe serum concentration of Selexipag can be increased when it is combined with Methadone.Approved
MethyldopaMethyldopa may increase the hypotensive activities of Selexipag.Approved
Methylene blueMethylene blue may increase the hypotensive activities of Selexipag.Investigational
MethylphenidateMethylphenidate may decrease the antihypertensive activities of Selexipag.Approved, Investigational
MetipranololMetipranolol may increase the hypotensive activities of Selexipag.Approved
MetolazoneMetolazone may increase the hypotensive activities of Selexipag.Approved
MetoprololThe serum concentration of Selexipag can be increased when it is combined with Metoprolol.Approved, Investigational
MetyrosineSelexipag may increase the hypotensive activities of Metyrosine.Approved
MibefradilThe serum concentration of Selexipag can be increased when it is combined with Mibefradil.Withdrawn
MiconazoleThe serum concentration of Selexipag can be increased when it is combined with Miconazole.Approved, Investigational, Vet Approved
MidazolamThe serum concentration of Selexipag can be decreased when it is combined with Midazolam.Approved, Illicit
MifepristoneThe serum concentration of Selexipag can be increased when it is combined with Mifepristone.Approved, Investigational
MilrinoneMilrinone may increase the anticoagulant activities of Selexipag.Approved
MinaprineMinaprine may increase the hypotensive activities of Selexipag.Approved
MinoxidilMinoxidil may increase the hypotensive activities of Selexipag.Approved
MitomycinThe serum concentration of Selexipag can be increased when it is combined with Mitomycin.Approved
MitotaneThe serum concentration of Selexipag can be decreased when it is combined with Mitotane.Approved
MitoxantroneThe serum concentration of Selexipag can be decreased when it is combined with Mitoxantrone.Approved, Investigational
MoclobemideMoclobemide may increase the hypotensive activities of Selexipag.Approved
ModafinilThe serum concentration of Selexipag can be decreased when it is combined with Modafinil.Approved, Investigational
MoexiprilMoexipril may increase the hypotensive activities of Selexipag.Approved
MolsidomineMolsidomine may increase the hypotensive activities of Selexipag.Approved
MorphineThe serum concentration of Selexipag can be increased when it is combined with Morphine.Approved, Investigational
MoxonidineMoxonidine may increase the hypotensive activities of Selexipag.Approved
NadololNadolol may increase the hypotensive activities of Selexipag.Approved
NadroparinSelexipag may increase the anticoagulant activities of Nadroparin.Approved
NafamostatSelexipag may increase the anticoagulant activities of Nafamostat.Approved, Investigational
NafcillinThe serum concentration of Selexipag can be decreased when it is combined with Nafcillin.Approved
NaftopidilNaftopidil may increase the anticoagulant activities of Selexipag.Investigational
NaltrexoneThe serum concentration of Selexipag can be increased when it is combined with Naltrexone.Approved, Investigational, Vet Approved
NaringeninThe serum concentration of Selexipag can be increased when it is combined with Naringenin.Experimental
NebivololNebivolol may increase the hypotensive activities of Selexipag.Approved, Investigational
NefazodoneThe metabolism of Selexipag can be decreased when combined with Nefazodone.Approved, Withdrawn
NelfinavirThe metabolism of Selexipag can be decreased when combined with Nelfinavir.Approved
NeostigmineThe serum concentration of Selexipag can be increased when it is combined with Neostigmine.Approved, Vet Approved
NetupitantThe serum concentration of Selexipag can be increased when it is combined with Netupitant.Approved
NevirapineThe metabolism of Selexipag can be increased when combined with Nevirapine.Approved
NialamideNialamide may increase the hypotensive activities of Selexipag.Withdrawn
NicardipineThe serum concentration of Selexipag can be increased when it is combined with Nicardipine.Approved
NicorandilNicorandil may increase the hypotensive activities of Selexipag.Approved
NifedipineThe serum concentration of Selexipag can be decreased when it is combined with Nifedipine.Approved
NiguldipineNiguldipine may increase the hypotensive activities of Selexipag.Experimental
NilotinibThe metabolism of Selexipag can be decreased when combined with Nilotinib.Approved, Investigational
NilvadipineNilvadipine may increase the hypotensive activities of Selexipag.Approved
NimesulideNimesulide may increase the anticoagulant activities of Selexipag.Approved, Withdrawn
NimodipineNimodipine may increase the hypotensive activities of Selexipag.Approved
NisoldipineThe serum concentration of Selexipag can be increased when it is combined with Nisoldipine.Approved
NitrazepamThe serum concentration of Selexipag can be increased when it is combined with Nitrazepam.Approved
NitrendipineThe serum concentration of Selexipag can be increased when it is combined with Nitrendipine.Approved
NitroaspirinThe risk or severity of adverse effects can be increased when Nitroaspirin is combined with Selexipag.Investigational
NitroprussideNitroprusside may increase the hypotensive activities of Selexipag.Approved
NorethisteroneThe serum concentration of Selexipag can be decreased when it is combined with Norethisterone.Approved
ObinutuzumabSelexipag may increase the hypotensive activities of Obinutuzumab.Approved
OctamoxinOctamoxin may increase the hypotensive activities of Selexipag.Withdrawn
OlaparibThe metabolism of Selexipag can be decreased when combined with Olaparib.Approved
OlmesartanOlmesartan may increase the hypotensive activities of Selexipag.Approved, Investigational
OlsalazineThe risk or severity of adverse effects can be increased when Olsalazine is combined with Selexipag.Approved
OmapatrilatOmapatrilat may increase the hypotensive activities of Selexipag.Investigational
OmeprazoleThe serum concentration of Selexipag can be increased when it is combined with Omeprazole.Approved, Investigational, Vet Approved
OsimertinibThe serum concentration of Selexipag can be increased when it is combined with Osimertinib.Approved
OtamixabanSelexipag may increase the anticoagulant activities of Otamixaban.Investigational
OxprenololOxprenolol may increase the hypotensive activities of Selexipag.Approved
P-NitrophenolThe serum concentration of Selexipag can be increased when it is combined with P-Nitrophenol.Experimental
PaclitaxelThe serum concentration of Selexipag can be increased when it is combined with Paclitaxel.Approved, Vet Approved
PalbociclibThe serum concentration of Selexipag can be increased when it is combined with Palbociclib.Approved
Palmitic AcidThe serum concentration of Selexipag can be increased when it is combined with Palmitic Acid.Experimental
PantoprazoleThe serum concentration of Selexipag can be increased when it is combined with Pantoprazole.Approved
PargylinePargyline may increase the hypotensive activities of Selexipag.Approved
ParoxetineThe serum concentration of Selexipag can be increased when it is combined with Paroxetine.Approved, Investigational
PenbutololPenbutolol may increase the hypotensive activities of Selexipag.Approved, Investigational
PentobarbitalThe metabolism of Selexipag can be increased when combined with Pentobarbital.Approved, Vet Approved
PentoliniumPentolinium may increase the hypotensive activities of Selexipag.Approved
Pentosan PolysulfateSelexipag may increase the anticoagulant activities of Pentosan Polysulfate.Approved
PentoxifyllinePentoxifylline may increase the hypotensive activities of Selexipag.Approved, Investigational
PerindoprilThe serum concentration of Selexipag can be increased when it is combined with Perindopril.Approved
PhenelzinePhenelzine may increase the hypotensive activities of Selexipag.Approved
PhenindioneSelexipag may increase the anticoagulant activities of Phenindione.Approved
PheniprazinePheniprazine may increase the hypotensive activities of Selexipag.Withdrawn
PhenobarbitalThe metabolism of Selexipag can be increased when combined with Phenobarbital.Approved
PhenoxybenzaminePhenoxybenzamine may increase the hypotensive activities of Selexipag.Approved
PhenoxypropazinePhenoxypropazine may increase the hypotensive activities of Selexipag.Withdrawn
PhenprocoumonSelexipag may increase the anticoagulant activities of Phenprocoumon.Approved
PhentolaminePhentolamine may increase the hypotensive activities of Selexipag.Approved
PhenytoinThe metabolism of Selexipag can be increased when combined with Phenytoin.Approved, Vet Approved
PimozideThe serum concentration of Selexipag can be increased when it is combined with Pimozide.Approved
PinacidilPinacidil may increase the hypotensive activities of Selexipag.Withdrawn
PindololPindolol may increase the hypotensive activities of Selexipag.Approved
PioglitazoneThe metabolism of Selexipag can be decreased when combined with Pioglitazone.Approved, Investigational
PirlindolePirlindole may increase the hypotensive activities of Selexipag.Approved
PivhydrazinePivhydrazine may increase the hypotensive activities of Selexipag.Withdrawn
Platelet Activating FactorThe serum concentration of Selexipag can be decreased when it is combined with Platelet Activating Factor.Experimental
PolythiazidePolythiazide may increase the hypotensive activities of Selexipag.Approved
PonatinibThe serum concentration of Selexipag can be increased when it is combined with Ponatinib.Approved
PosaconazoleThe metabolism of Selexipag can be decreased when combined with Posaconazole.Approved, Investigational, Vet Approved
PrasugrelPrasugrel may increase the anticoagulant activities of Selexipag.Approved
PravastatinThe serum concentration of Selexipag can be increased when it is combined with Pravastatin.Approved
PrazosinThe serum concentration of Selexipag can be increased when it is combined with Prazosin.Approved
PrednisoneThe serum concentration of Selexipag can be increased when it is combined with Prednisone.Approved, Vet Approved
PrimidoneThe metabolism of Selexipag can be increased when combined with Primidone.Approved, Vet Approved
ProbenecidThe serum concentration of Selexipag can be increased when it is combined with Probenecid.Approved
ProgesteroneThe serum concentration of Selexipag can be decreased when it is combined with Progesterone.Approved, Vet Approved
PromethazineThe serum concentration of Selexipag can be increased when it is combined with Promethazine.Approved
PropafenoneThe serum concentration of Selexipag can be increased when it is combined with Propafenone.Approved
PropranololThe serum concentration of Selexipag can be increased when it is combined with Propranolol.Approved, Investigational
Protein CSelexipag may increase the anticoagulant activities of Protein C.Approved
Protein S humanSelexipag may increase the anticoagulant activities of Protein S human.Approved
ProtocatechualdehydeSelexipag may increase the anticoagulant activities of Protocatechualdehyde.Approved
ProtriptylineThe serum concentration of Selexipag can be increased when it is combined with Protriptyline.Approved
QuercetinThe serum concentration of Selexipag can be increased when it is combined with Quercetin.Experimental
QuinacrineThe serum concentration of Selexipag can be increased when it is combined with Quinacrine.Approved
QuinaprilQuinapril may increase the hypotensive activities of Selexipag.Approved, Investigational
QuinidineThe serum concentration of Selexipag can be increased when it is combined with Quinidine.Approved
QuinineQuinine may increase the hypotensive activities of Selexipag.Approved
RabeprazoleThe metabolism of Selexipag can be decreased when combined with Rabeprazole.Approved, Investigational
RamatrobanRamatroban may increase the anticoagulant activities of Selexipag.Investigational
RamiprilRamipril may increase the hypotensive activities of Selexipag.Approved
RanitidineThe serum concentration of Selexipag can be increased when it is combined with Ranitidine.Approved
RanolazineThe serum concentration of Selexipag can be increased when it is combined with Ranolazine.Approved, Investigational
RasagilineRasagiline may increase the hypotensive activities of Selexipag.Approved
ReboxetineThe serum concentration of Selexipag can be increased when it is combined with Reboxetine.Approved, Investigational
RegorafenibThe serum concentration of Selexipag can be increased when it is combined with Regorafenib.Approved
RemikirenRemikiren may increase the hypotensive activities of Selexipag.Approved
RescinnamineSelexipag may increase the hypotensive activities of Rescinnamine.Approved
ReserpineThe serum concentration of Selexipag can be decreased when it is combined with Reserpine.Approved
ResveratrolResveratrol may increase the anticoagulant activities of Selexipag.Experimental, Investigational
ReviparinSelexipag may increase the anticoagulant activities of Reviparin.Approved
RidogrelRidogrel may increase the anticoagulant activities of Selexipag.Approved
RifabutinThe metabolism of Selexipag can be increased when combined with Rifabutin.Approved
RifampicinThe metabolism of Selexipag can be increased when combined with Rifampicin.Approved
RifapentineThe metabolism of Selexipag can be increased when combined with Rifapentine.Approved
RilmenidineSelexipag may increase the hypotensive activities of Rilmenidine.Investigational
RilpivirineThe serum concentration of Selexipag can be increased when it is combined with Rilpivirine.Approved
RiociguatSelexipag may increase the hypotensive activities of Riociguat.Approved
RitonavirThe metabolism of Selexipag can be decreased when combined with Ritonavir.Approved, Investigational
RituximabSelexipag may increase the hypotensive activities of Rituximab.Approved
RivaroxabanSelexipag may increase the anticoagulant activities of Rivaroxaban.Approved
RolapitantThe serum concentration of Selexipag can be increased when it is combined with Rolapitant.Approved
RosiglitazoneThe metabolism of Selexipag can be decreased when combined with Rosiglitazone.Approved, Investigational
SafrazineSafrazine may increase the hypotensive activities of Selexipag.Withdrawn
Salicylic acidThe risk or severity of adverse effects can be increased when Salicylic acid is combined with Selexipag.Approved, Vet Approved
SaprisartanSaprisartan may increase the hypotensive activities of Selexipag.Experimental
SaquinavirThe metabolism of Selexipag can be decreased when combined with Saquinavir.Approved, Investigational
ScopolamineThe serum concentration of Selexipag can be increased when it is combined with Scopolamine.Approved
SecobarbitalThe metabolism of Selexipag can be increased when combined with Secobarbital.Approved, Vet Approved
SelegilineThe serum concentration of Selexipag can be increased when it is combined with Selegiline.Approved, Investigational, Vet Approved
SertralineThe serum concentration of Selexipag can be increased when it is combined with Sertraline.Approved
SevofluraneSevoflurane may increase the anticoagulant activities of Selexipag.Approved, Vet Approved
SildenafilSildenafil may increase the antihypertensive activities of Selexipag.Approved, Investigational
SiltuximabThe serum concentration of Selexipag can be decreased when it is combined with Siltuximab.Approved
SimeprevirThe serum concentration of Selexipag can be increased when it is combined with Simeprevir.Approved
SimvastatinThe serum concentration of Selexipag can be increased when it is combined with Simvastatin.Approved
SirolimusThe serum concentration of Selexipag can be decreased when it is combined with Sirolimus.Approved, Investigational
SitaxentanSelexipag may increase the hypotensive activities of Sitaxentan.Approved, Investigational, Withdrawn
SorafenibThe serum concentration of Selexipag can be increased when it is combined with Sorafenib.Approved, Investigational
SpiraprilSpirapril may increase the hypotensive activities of Selexipag.Approved
SpironolactoneThe serum concentration of Selexipag can be increased when it is combined with Spironolactone.Approved
SRT501SRT501 may increase the anticoagulant activities of Selexipag.Investigational
St. John's WortThe serum concentration of Selexipag can be decreased when it is combined with St. John's Wort.Nutraceutical
StaurosporineThe serum concentration of Selexipag can be increased when it is combined with Staurosporine.Experimental
StiripentolThe serum concentration of Selexipag can be increased when it is combined with Stiripentol.Approved
StreptozocinThe serum concentration of Selexipag can be decreased when it is combined with Streptozocin.Approved
SulfamethoxazoleThe metabolism of Selexipag can be decreased when combined with Sulfamethoxazole.Approved
SulfinpyrazoneThe serum concentration of Selexipag can be increased when it is combined with Sulfinpyrazone.Approved
SulfisoxazoleThe metabolism of Selexipag can be decreased when combined with Sulfisoxazole.Approved, Vet Approved
SulodexideSelexipag may increase the anticoagulant activities of Sulodexide.Approved, Investigational
SumatriptanThe serum concentration of Selexipag can be increased when it is combined with Sumatriptan.Approved, Investigational
SunitinibThe serum concentration of Selexipag can be increased when it is combined with Sunitinib.Approved, Investigational
TacrineThe serum concentration of Selexipag can be increased when it is combined with Tacrine.Withdrawn
TacrolimusThe serum concentration of Selexipag can be decreased when it is combined with Tacrolimus.Approved, Investigational
TadalafilTadalafil may increase the antihypertensive activities of Selexipag.Approved, Investigational
TamoxifenThe serum concentration of Selexipag can be decreased when it is combined with Tamoxifen.Approved
Taurocholic AcidThe serum concentration of Selexipag can be increased when it is combined with Taurocholic Acid.Experimental
TelaprevirThe metabolism of Selexipag can be decreased when combined with Telaprevir.Withdrawn
TelithromycinThe metabolism of Selexipag can be decreased when combined with Telithromycin.Approved
TelmisartanThe serum concentration of Selexipag can be increased when it is combined with Telmisartan.Approved, Investigational
TemocaprilTemocapril may increase the hypotensive activities of Selexipag.Experimental, Investigational
TemsirolimusThe serum concentration of Selexipag can be increased when it is combined with Temsirolimus.Approved
TerazosinThe serum concentration of Selexipag can be increased when it is combined with Terazosin.Approved
TerfenadineThe serum concentration of Selexipag can be increased when it is combined with Terfenadine.Withdrawn
TeriflunomideThe serum concentration of Selexipag can be increased when it is combined with Teriflunomide.Approved
TerlipressinTerlipressin may increase the hypotensive activities of Selexipag.Approved, Investigational
TesmilifeneThe serum concentration of Selexipag can be decreased when it is combined with Tesmilifene.Investigational
TestosteroneThe serum concentration of Selexipag can be increased when it is combined with Testosterone.Approved, Investigational
TiboloneTibolone may increase the hypotensive activities of Selexipag.Approved
TicagrelorThe serum concentration of Selexipag can be increased when it is combined with Ticagrelor.Approved
TiclopidineThe metabolism of Selexipag can be decreased when combined with Ticlopidine.Approved
TicrynafenTicrynafen may increase the hypotensive activities of Selexipag.Withdrawn
TimololTimolol may increase the hypotensive activities of Selexipag.Approved
TirofibanTirofiban may increase the anticoagulant activities of Selexipag.Approved
TocilizumabThe serum concentration of Selexipag can be decreased when it is combined with Tocilizumab.Approved
TolazolineTolazoline may increase the hypotensive activities of Selexipag.Approved, Vet Approved
ToloxatoneToloxatone may increase the hypotensive activities of Selexipag.Approved
TolvaptanThe serum concentration of Selexipag can be increased when it is combined with Tolvaptan.Approved
TorasemideTorasemide may increase the hypotensive activities of Selexipag.Approved
TrandolaprilTrandolapril may increase the hypotensive activities of Selexipag.Approved
TranilastTranilast may increase the anticoagulant activities of Selexipag.Approved, Investigational
Trans-2-PhenylcyclopropylamineTrans-2-Phenylcyclopropylamine may increase the hypotensive activities of Selexipag.Experimental
TranylcypromineTranylcypromine may increase the hypotensive activities of Selexipag.Approved
TrapidilTrapidil may increase the anticoagulant activities of Selexipag.Approved
TravoprostTravoprost may increase the hypotensive activities of Selexipag.Approved
TrazodoneThe serum concentration of Selexipag can be decreased when it is combined with Trazodone.Approved, Investigational
TreprostinilTreprostinil may increase the hypotensive activities of Selexipag.Approved, Investigational
TrichlormethiazideTrichlormethiazide may increase the hypotensive activities of Selexipag.Approved, Vet Approved
TrifluoperazineThe serum concentration of Selexipag can be increased when it is combined with Trifluoperazine.Approved
TriflupromazineThe serum concentration of Selexipag can be increased when it is combined with Triflupromazine.Approved, Vet Approved
TriflusalTriflusal may increase the anticoagulant activities of Selexipag.Approved
TrimazosinTrimazosin may increase the hypotensive activities of Selexipag.Experimental
TrimethaphanTrimethaphan may increase the hypotensive activities of Selexipag.Approved
TrimethoprimThe serum concentration of Selexipag can be decreased when it is combined with Trimethoprim.Approved, Vet Approved
TrimipramineThe serum concentration of Selexipag can be increased when it is combined with Trimipramine.Approved
UdenafilUdenafil may increase the antihypertensive activities of Selexipag.Approved, Investigational
UnoprostoneUnoprostone may increase the hypotensive activities of Selexipag.Approved
ValsartanValsartan may increase the hypotensive activities of Selexipag.Approved, Investigational
VardenafilVardenafil may increase the antihypertensive activities of Selexipag.Approved
VenlafaxineThe metabolism of Selexipag can be decreased when combined with Venlafaxine.Approved
VerapamilThe metabolism of Selexipag can be decreased when combined with Verapamil.Approved
VinblastineThe serum concentration of Selexipag can be decreased when it is combined with Vinblastine.Approved
VincristineThe serum concentration of Selexipag can be decreased when it is combined with Vincristine.Approved, Investigational
VinorelbineThe serum concentration of Selexipag can be increased when it is combined with Vinorelbine.Approved, Investigational
VinpocetineSelexipag may increase the hypotensive activities of Vinpocetine.Investigational
VorapaxarVorapaxar may increase the anticoagulant activities of Selexipag.Approved
VoriconazoleThe metabolism of Selexipag can be decreased when combined with Voriconazole.Approved, Investigational
WarfarinSelexipag may increase the anticoagulant activities of Warfarin.Approved
XimelagatranSelexipag may increase the anticoagulant activities of Ximelagatran.Approved, Investigational, Withdrawn
XylometazolineXylometazoline may increase the hypotensive activities of Selexipag.Approved
YohimbineYohimbine may decrease the antihypertensive activities of Selexipag.Approved, Vet Approved
ZimelidineThe serum concentration of Selexipag can be increased when it is combined with Zimelidine.Withdrawn
ZiprasidoneThe metabolism of Selexipag can be decreased when combined with Ziprasidone.Approved
Food InteractionsNo interactions found.
References
Synthesis ReferenceNot Available
General References
  1. Sharma K: Selexipag for the treatment of pulmonary arterial hypertension. Expert Rev Respir Med. 2016 Jan;10(1):1-3. doi: 10.1586/17476348.2016.1121103. Epub 2015 Dec 7. [PubMed:26567613 ]
  2. Kaufmann P, Okubo K, Bruderer S, Mant T, Yamada T, Dingemanse J, Mukai H: Pharmacokinetics and Tolerability of the Novel Oral Prostacyclin IP Receptor Agonist Selexipag. Am J Cardiovasc Drugs. 2015 Jun;15(3):195-203. doi: 10.1007/s40256-015-0117-4. [PubMed:25850750 ]
External Links
ATC CodesB01AC27 — Selexipag
AHFS Codes
  • 48:48
PDB EntriesNot Available
FDA labelDownload (768 KB)
MSDSNot Available
Clinical Trials
Clinical Trials
PhaseStatusPurposeConditionsCount
1CompletedNot AvailableBioequivalence1
1CompletedNot AvailableCardiodynamics / Pharmacokinetics / Safety / Tolerability1
1CompletedNot AvailableHealthy Volunteers3
1CompletedOtherHealthy Volunteers1
2CompletedTreatmentRaynaud's Phenomenon Secondary to Systemic Sclerosis1
3Active Not RecruitingTreatmentPulmonary Arterial Hypertension (PAH)1
3CompletedTreatmentPulmonary Arterial Hypertension (PAH)2
3Not Yet RecruitingTreatmentPulmonary Arterial Hypertension (PAH)1
3RecruitingTreatmentPulmonary Arterial Hypertension (PAH)1
4Not Yet RecruitingOtherPulmonary Arterial Hypertension (PAH)1
Pharmacoeconomics
ManufacturersNot Available
PackagersNot Available
Dosage forms
FormRouteStrength
TabletOral1000 mcg
TabletOral1200 mcg
TabletOral1400 mcg
TabletOral1600 mcg
TabletOral200 mcg
TabletOral400 mcg
TabletOral600 mcg
TabletOral800 mcg
Tablet, coatedOral1000 ug/1
Tablet, coatedOral1200 ug/1
Tablet, coatedOral1400 ug/1
Tablet, coatedOral1600 ug/1
Tablet, coatedOral200 ug/1
Tablet, coatedOral400 ug/1
Tablet, coatedOral600 ug/1
Tablet, coatedOral800 ug/1
Tablet, film coatedOral1000 μg
Tablet, film coatedOral1200 μg
Tablet, film coatedOral1400 μg
Tablet, film coatedOral1600 μg
Tablet, film coatedOral200 μg
Tablet, film coatedOral400 μg
Tablet, film coatedOral600 μg
Tablet, film coatedOral800 μg
Kit
PricesNot Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US7205302 No2003-04-042023-04-04Us
US9173881 No2009-08-122029-08-12Us
US9284280 No2010-06-252030-06-25Us
US8791122 No2010-08-012030-08-01Us
Properties
StateSolid
Experimental PropertiesNot Available
Predicted Properties
PropertyValueSource
Water Solubility0.00434 mg/mLALOGPS
logP4.4ALOGPS
logP3.76ChemAxon
logS-5.1ALOGPS
pKa (Strongest Acidic)3.77ChemAxon
pKa (Strongest Basic)1.41ChemAxon
Physiological Charge-1ChemAxon
Hydrogen Acceptor Count7ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area101.49 Å2ChemAxon
Rotatable Bond Count11ChemAxon
Refractivity136.81 m3·mol-1ChemAxon
Polarizability54.98 Å3ChemAxon
Number of Rings3ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterNoChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleYesChemAxon
Predicted ADMET featuresNot Available
Spectra
Mass Spec (NIST)Not Available
Spectra
Spectrum TypeDescriptionSplash Key
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, NegativeNot Available
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as dialkylarylamines. These are aliphatic aromatic amines in which the amino group is linked to two aliphatic chains and one aromatic group.
KingdomOrganic compounds
Super ClassOrganic nitrogen compounds
ClassOrganonitrogen compounds
Sub ClassAmines
Direct ParentDialkylarylamines
Alternative ParentsAminopyrazines / Imidolactams / Benzene and substituted derivatives / Organosulfonic acids and derivatives / Heteroaromatic compounds / Aminosulfonyl compounds / Amino acids and derivatives / Dialkyl ethers / Azacyclic compounds / Organic oxides
SubstituentsDialkylarylamine / Aminopyrazine / Monocyclic benzene moiety / Pyrazine / Benzenoid / Imidolactam / Organic sulfonic acid or derivatives / Organosulfonic acid or derivatives / Sulfonyl / Aminosulfonyl compound
Molecular FrameworkAromatic heteromonocyclic compounds
External DescriptorsNot Available

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
agonist
General Function:
Guanyl-nucleotide exchange factor activity
Specific Function:
Receptor for prostacyclin (prostaglandin I2 or PGI2). The activity of this receptor is mediated by G(s) proteins which activate adenylate cyclase.
Gene Name:
PTGIR
Uniprot ID:
P43119
Uniprot Name:
Prostacyclin receptor
Molecular Weight:
40955.485 Da
References
  1. Kaufmann P, Okubo K, Bruderer S, Mant T, Yamada T, Dingemanse J, Mukai H: Pharmacokinetics and Tolerability of the Novel Oral Prostacyclin IP Receptor Agonist Selexipag. Am J Cardiovasc Drugs. 2015 Jun;15(3):195-203. doi: 10.1007/s40256-015-0117-4. [PubMed:25850750 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
no
Actions
substrate
General Function:
Triglyceride lipase activity
Specific Function:
Involved in the detoxification of xenobiotics and in the activation of ester and amide prodrugs. Hydrolyzes aromatic and aliphatic esters, but has no catalytic activity toward amides or a fatty acyl-CoA ester. Hydrolyzes the methyl ester group of cocaine to form benzoylecgonine. Catalyzes the transesterification of cocaine to form cocaethylene. Displays fatty acid ethyl ester synthase activity,...
Gene Name:
CES1
Uniprot ID:
P23141
Uniprot Name:
Liver carboxylesterase 1
Molecular Weight:
62520.62 Da
Kind
Protein
Organism
Human
Pharmacological action
no
Actions
substrate
General Function:
Steroid hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. In the epoxidation of arachidonic acid it generates only 14,15- and 11,12-cis-epoxyeicosatrienoic acids. It is the principal enzyme...
Gene Name:
CYP2C8
Uniprot ID:
P10632
Uniprot Name:
Cytochrome P450 2C8
Molecular Weight:
55824.275 Da
Kind
Protein
Organism
Human
Pharmacological action
no
Actions
substrate
General Function:
Vitamin d3 25-hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation reactions (e.g. caffeine 8-oxidation, omeprazole sulphoxidation, midazolam 1'-hydroxylation and midazolam 4-hydroxylation) of structurally unrelated compounds, including steroids, fatty acids, and xenobiot...
Gene Name:
CYP3A4
Uniprot ID:
P08684
Uniprot Name:
Cytochrome P450 3A4
Molecular Weight:
57342.67 Da

Transporters

Kind
Protein
Organism
Human
Pharmacological action
no
Actions
substrate
General Function:
Sodium-independent organic anion transmembrane transporter activity
Specific Function:
Mediates the Na(+)-independent uptake of organic anions such as pravastatin, taurocholate, methotrexate, dehydroepiandrosterone sulfate, 17-beta-glucuronosyl estradiol, estrone sulfate, prostaglandin E2, thromboxane B2, leukotriene C3, leukotriene E4, thyroxine and triiodothyronine. Involved in the clearance of bile acids and organic anions from the liver.
Gene Name:
SLCO1B1
Uniprot ID:
Q9Y6L6
Uniprot Name:
Solute carrier organic anion transporter family member 1B1
Molecular Weight:
76447.99 Da
Kind
Protein
Organism
Human
Pharmacological action
no
Actions
substrate
General Function:
Sodium-independent organic anion transmembrane transporter activity
Specific Function:
Mediates the Na(+)-independent uptake of organic anions such as 17-beta-glucuronosyl estradiol, taurocholate, triiodothyronine (T3), leukotriene C4, dehydroepiandrosterone sulfate (DHEAS), methotrexate and sulfobromophthalein (BSP). Involved in the clearance of bile acids and organic anions from the liver.
Gene Name:
SLCO1B3
Uniprot ID:
Q9NPD5
Uniprot Name:
Solute carrier organic anion transporter family member 1B3
Molecular Weight:
77402.175 Da
Kind
Protein
Organism
Human
Pharmacological action
no
Actions
substrate
General Function:
Xenobiotic-transporting atpase activity
Specific Function:
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
Gene Name:
ABCB1
Uniprot ID:
P08183
Uniprot Name:
Multidrug resistance protein 1
Molecular Weight:
141477.255 Da
Drug created on December 23, 2015 11:28 / Updated on September 01, 2017 12:08