Identification

Name
Selexipag
Accession Number
DB11362
Type
Small Molecule
Groups
Approved
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
Synonyms
Not Available
External IDs
ACT-293987 / NS-304
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
UptraviTablet, film coated200 μgOralActelion Registration Ltd2016-05-12Not applicableEu
UptraviTablet, coated600 ug/1OralActelion2015-12-21Not applicableUs
UptraviTablet200 mcgOralActelion2016-04-21Not applicableCanada
UptraviTablet, film coated600 μgOralActelion Registration Ltd2016-05-12Not applicableEu
UptraviTablet, coated1400 ug/1OralActelion2015-12-21Not applicableUs
UptraviTablet800 mcgOralActelion2016-04-21Not applicableCanada
UptraviTablet, film coated1200 μgOralActelion Registration Ltd2016-05-12Not applicableEu
UptraviTablet, film coated400 μgOralActelion Registration Ltd2016-05-12Not applicableEu
UptraviTablet, coated1200 ug/1OralActelion2015-12-21Not applicableUs
UptraviTablet1400 mcgOralActelion2016-04-21Not applicableCanada
Categories
UNII
5EXC0E384L
CAS number
475086-01-2
Weight
Average: 496.63
Monoisotopic: 496.2144267
Chemical Formula
C26H32N4O4S
InChI Key
QXWZQTURMXZVHJ-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.

TargetActionsOrganism
AProstacyclin receptor
agonist
Human
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 distribution
Not 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.

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
Pathways
Not 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
Acetylsalicylic acidThe risk or severity of adverse effects can be increased when Acetylsalicylic acid is combined with Selexipag.Approved, Vet Approved
AlfuzosinAlfuzosin may increase the hypotensive activities of Selexipag.Approved, Investigational
AliskirenAliskiren may increase the hypotensive activities of Selexipag.Approved, Investigational
AloxiprinThe risk or severity of adverse effects can be increased when Aloxiprin is combined with Selexipag.Experimental
AlprenololAlprenolol may increase the hypotensive activities of Selexipag.Approved, Withdrawn
AlprostadilAlprostadil may increase the anticoagulant activities of Selexipag.Approved, Investigational
AmbrisentanSelexipag may increase the hypotensive activities of Ambrisentan.Approved, Investigational
AmifostineSelexipag may increase the hypotensive activities of Amifostine.Approved, Investigational
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
AmlodipineAmlodipine may increase the hypotensive activities of Selexipag.Approved
AmphetamineAmphetamine may increase the hypotensive activities of Selexipag.Approved, Illicit
AnagrelideAnagrelide may increase the anticoagulant activities of Selexipag.Approved
AncrodSelexipag may increase the anticoagulant activities of Ancrod.Investigational
AndrographolideAndrographolide may increase the anticoagulant activities of Selexipag.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, Investigational, Withdrawn
ArgatrobanSelexipag may increase the anticoagulant activities of Argatroban.Approved, Investigational
AtazanavirThe metabolism of Selexipag can be decreased when combined with Atazanavir.Approved, Investigational
AtenololAtenolol may increase the hypotensive activities of Selexipag.Approved
AtomoxetineThe metabolism of Selexipag can be decreased when combined with Atomoxetine.Approved
AvanafilAvanafil may increase the antihypertensive activities of Selexipag.Approved
AzelastineAzelastine may increase the anticoagulant activities of Selexipag.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
BepridilBepridil may increase the hypotensive activities of Selexipag.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
BietaserpineBietaserpine may increase the hypotensive activities of Selexipag.Experimental
BimatoprostBimatoprost may increase the hypotensive activities of Selexipag.Approved, Investigational
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.Approved, 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
BQ-123Selexipag may increase the hypotensive activities of BQ-123.Investigational
BretyliumBretylium may increase the hypotensive activities of Selexipag.Approved
BrimonidineBrimonidine may increase the antihypertensive activities of Selexipag.Approved
BrofaromineBrofaromine may increase the hypotensive activities of Selexipag.Experimental
BuflomedilBuflomedil may increase the anticoagulant activities of Selexipag.Experimental
BupranololBupranolol may increase the hypotensive activities of Selexipag.Approved
ButylphthalideButylphthalide may increase the anticoagulant activities of Selexipag.Investigational
CadralazineCadralazine may increase the hypotensive activities of Selexipag.Experimental
CafedrineSelexipag may increase the hypotensive activities of Cafedrine.Investigational
CandesartanSelexipag may increase the hypotensive activities of Candesartan.Experimental
Candesartan cilexetilCandesartan cilexetil may increase the hypotensive activities of Selexipag.Approved
CandoxatrilCandoxatril may increase the hypotensive activities of Selexipag.Experimental
CangrelorCangrelor may increase the anticoagulant activities of Selexipag.Approved
CaptoprilCaptopril may increase the hypotensive activities of Selexipag.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
CarvedilolCarvedilol may increase the hypotensive activities of Selexipag.Approved, Investigational
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, Investigational
ChlorothiazideChlorothiazide may increase the hypotensive activities of Selexipag.Approved, Vet Approved
ChlorthalidoneChlorthalidone may increase the hypotensive activities of Selexipag.Approved
CicletanineSelexipag may increase the hypotensive activities of Cicletanine.Investigational
CilazaprilCilazapril may increase the hypotensive activities of Selexipag.Approved
CilostazolCilostazol may increase the anticoagulant activities of Selexipag.Approved
Citric AcidSelexipag may increase the anticoagulant activities of Citric Acid.Approved, 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
ClonidineClonidine may increase the hypotensive activities of Selexipag.Approved
ClopidogrelClopidogrel may increase the anticoagulant activities of Selexipag.Approved, Nutraceutical
CloranololSelexipag may increase the hypotensive activities of Cloranolol.Experimental
CloricromenCloricromen may increase the anticoagulant activities of Selexipag.Experimental
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
ConivaptanThe serum concentration of Selexipag can be increased when it is combined with Conivaptan.Approved, Investigational
CrisaboroleThe metabolism of Selexipag can be decreased when combined with Crisaborole.Approved
CrizotinibThe metabolism of Selexipag can be decreased when combined with Crizotinib.Approved
CryptenamineCryptenamine may increase the hypotensive activities of Selexipag.Approved
CyclopenthiazideSelexipag may increase the hypotensive activities of Cyclopenthiazide.Experimental
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
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 Darexaban.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
DebrisoquinDebrisoquin may increase the hypotensive activities of Selexipag.Approved, Investigational
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
DelaprilSelexipag may increase the hypotensive activities of Delapril.Experimental
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
DesirudinSelexipag may increase the anticoagulant activities of Desirudin.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
DiazoxideDiazoxide may increase the hypotensive activities of Selexipag.Approved
DicoumarolSelexipag may increase the anticoagulant activities of Dicoumarol.Approved
diethylnorsperminediethylnorspermine may increase the hypotensive activities of Selexipag.Investigational
DiflunisalThe risk or severity of adverse effects can be increased when Diflunisal is combined with Selexipag.Approved
DihydralazineDihydralazine may increase the hypotensive activities of Selexipag.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
DipyridamoleDipyridamole may increase the anticoagulant activities of Selexipag.Approved
DorzolamideDorzolamide may increase the hypotensive activities of Selexipag.Approved
DoxazosinDoxazosin may increase the hypotensive activities of Selexipag.Approved
DoxycyclineThe metabolism of Selexipag can be decreased when combined with Doxycycline.Approved, Investigational, Vet Approved
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 metabolism of Selexipag can be decreased when combined with Efavirenz.Approved, Investigational
EfonidipineEfonidipine may increase the hypotensive activities of Selexipag.Approved, Investigational
EltrombopagThe serum concentration of Selexipag can be increased when it is combined with Eltrombopag.Approved
EnalaprilEnalapril may increase the hypotensive activities of Selexipag.Approved, Vet Approved
EnalaprilatEnalaprilat may increase the hypotensive activities of Selexipag.Approved
EndralazineEndralazine may increase the hypotensive activities of Selexipag.Experimental
EnoxaparinSelexipag may increase the anticoagulant activities of Enoxaparin.Approved
EnzalutamideThe serum concentration of Selexipag can be decreased when it is combined with Enzalutamide.Approved
EpanololSelexipag may increase the hypotensive activities of Epanolol.Experimental
EpinastineEpinastine may increase the anticoagulant activities of Selexipag.Approved, Investigational
EplivanserinEplivanserin may increase the anticoagulant activities of Selexipag.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
ErythromycinThe metabolism of Selexipag can be decreased when combined with Erythromycin.Approved, Vet Approved
Ethyl biscoumacetateSelexipag may increase the anticoagulant activities of Ethyl biscoumacetate.Withdrawn
FelodipineThe metabolism of Selexipag can be decreased when combined with Felodipine.Approved, Investigational
FenoldopamFenoldopam may increase the hypotensive activities of Selexipag.Approved
Ferulic acidSelexipag may increase the anticoagulant activities of Ferulic acid.Experimental
FluconazoleThe metabolism of Selexipag can be decreased when combined with Fluconazole.Approved
FluindioneSelexipag may increase the anticoagulant activities of Fluindione.Investigational
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, Investigational, 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
GuacetisalThe risk or severity of adverse effects can be increased when Guacetisal is combined with Selexipag.Experimental
GuanabenzGuanabenz may increase the hypotensive activities of Selexipag.Approved, Investigational
GuanadrelGuanadrel may increase the hypotensive activities of Selexipag.Approved
GuanazodineSelexipag may increase the hypotensive activities of Guanazodine.Experimental
GuanethidineGuanethidine may increase the hypotensive activities of Selexipag.Approved
GuanfacineGuanfacine may increase the hypotensive activities of Selexipag.Approved, Investigational
GuanoclorSelexipag may increase the hypotensive activities of Guanoclor.Experimental
GuanoxabenzSelexipag may increase the hypotensive activities of Guanoxabenz.Experimental
GuanoxanSelexipag may increase the hypotensive activities of Guanoxan.Experimental
HarmalineHarmaline may increase the hypotensive activities of Selexipag.Experimental
Hemoglobin crosfumarilThe risk or severity of adverse effects can be increased when Hemoglobin crosfumaril is combined with Selexipag.Experimental
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
HydroflumethiazideHydroflumethiazide may increase the hypotensive activities of Selexipag.Approved, Investigational
HydroxytyrosolHydroxytyrosol may increase the anticoagulant activities of Selexipag.Investigational
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, Investigational, Withdrawn
IfetrobanIfetroban may increase the anticoagulant activities of Selexipag.Investigational
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
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
IndobufenIndobufen may increase the anticoagulant activities of Selexipag.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
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, Investigational
LapatinibThe metabolism of Selexipag can be decreased when 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
LetaxabanSelexipag may increase the anticoagulant activities of Letaxaban.Investigational
LimaprostThe risk or severity of adverse effects can be increased when Limaprost is combined with Selexipag.Approved, Investigational
LinsidomineLinsidomine may increase the anticoagulant activities of Selexipag.Experimental
LisinoprilLisinopril may increase the hypotensive activities of Selexipag.Approved, Investigational
LofexidineLofexidine may increase the hypotensive activities of Selexipag.Approved, Investigational
LopinavirThe metabolism of Selexipag can be decreased when combined with Lopinavir.Approved
LosartanThe metabolism of Selexipag can be decreased when 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, Investigational
MebanazineMebanazine may increase the hypotensive activities of Selexipag.Withdrawn
MecamylamineMecamylamine may increase the hypotensive activities of Selexipag.Approved
MelagatranSelexipag may increase the anticoagulant activities of Melagatran.Experimental
MesalazineThe risk or severity of adverse effects can be increased when Mesalazine is combined with Selexipag.Approved
MethoserpidineSelexipag may increase the hypotensive activities of Methoserpidine.Experimental
Methyl salicylateThe risk or severity of adverse effects can be increased when Methyl salicylate is combined with Selexipag.Approved, Vet Approved
MethyldopaMethyldopa may increase the hypotensive activities of Selexipag.Approved
Methylene blueMethylene blue may increase the hypotensive activities of Selexipag.Approved, 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
MetoprololMetoprolol may increase the hypotensive activities of Selexipag.Approved, Investigational
MetyrosineSelexipag may increase the hypotensive activities of Metyrosine.Approved
MibefradilMibefradil may increase the hypotensive activities of Selexipag.Investigational, Withdrawn
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
MirodenafilMirodenafil may increase the antihypertensive activities of Selexipag.Investigational
MitotaneThe serum concentration of Selexipag can be decreased when it is combined with Mitotane.Approved
MoclobemideMoclobemide may increase the hypotensive activities of Selexipag.Approved
MoexiprilMoexipril may increase the hypotensive activities of Selexipag.Approved
MolsidomineMolsidomine may increase the hypotensive activities of Selexipag.Approved, Investigational
MoxonidineMoxonidine may increase the hypotensive activities of Selexipag.Approved, Investigational
MuzolimineSelexipag may increase the hypotensive activities of Muzolimine.Experimental
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
NaftopidilNaftopidil may increase the anticoagulant activities of Selexipag.Investigational
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
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
NicardipineNicardipine may increase the hypotensive activities of Selexipag.Approved
NicorandilNicorandil may increase the hypotensive activities of Selexipag.Approved, Investigational
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, Investigational
NimesulideNimesulide may increase the anticoagulant activities of Selexipag.Approved, Investigational, Withdrawn
NimodipineNimodipine may increase the hypotensive activities of Selexipag.Approved
NisoldipineNisoldipine may increase the hypotensive activities of Selexipag.Approved
NitrendipineNitrendipine may increase the hypotensive activities of Selexipag.Approved, Investigational
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
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
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
PalbociclibThe serum concentration of Selexipag can be increased when it is combined with Palbociclib.Approved
PargylinePargyline may increase the hypotensive activities of Selexipag.Approved
PenbutololPenbutolol may increase the hypotensive activities of Selexipag.Approved, Investigational
Pentaerythritol TetranitrateSelexipag may increase the anticoagulant activities of Pentaerythritol Tetranitrate.Approved
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
PerindoprilPerindopril may increase the hypotensive activities of Selexipag.Approved
PhenelzinePhenelzine may increase the hypotensive activities of Selexipag.Approved
PhenindioneSelexipag may increase the anticoagulant activities of Phenindione.Approved, Investigational
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, Investigational
PhentolaminePhentolamine may increase the hypotensive activities of Selexipag.Approved
PhenytoinThe metabolism of Selexipag can be increased when combined with Phenytoin.Approved, Vet Approved
PicotamidePicotamide may increase the anticoagulant activities of Selexipag.Experimental
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 FactorPlatelet Activating Factor may increase the hypotensive activities of Selexipag.Experimental
PolythiazidePolythiazide may increase the hypotensive activities of Selexipag.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
PrazosinPrazosin may increase the hypotensive activities of Selexipag.Approved
PrimidoneThe metabolism of Selexipag can be increased when combined with Primidone.Approved, Vet Approved
ProcarbazineProcarbazine may increase the hypotensive activities of Selexipag.Approved
PropranololPropranolol may increase the hypotensive activities of Selexipag.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
QuinaprilQuinapril may increase the hypotensive activities of Selexipag.Approved, Investigational
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
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
RemikirenRemikiren may increase the hypotensive activities of Selexipag.Approved
RescinnamineSelexipag may increase the hypotensive activities of Rescinnamine.Approved
ReserpineReserpine may increase the hypotensive activities of Selexipag.Approved, Investigational
ResveratrolResveratrol may increase the anticoagulant activities of Selexipag.Approved, Experimental, Investigational
ReviparinSelexipag may increase the anticoagulant activities of Reviparin.Approved, Investigational
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
RilmenidineRilmenidine may increase the hypotensive activities of Selexipag.Investigational
RiociguatSelexipag may increase the hypotensive activities of Riociguat.Approved
RituximabSelexipag may increase the hypotensive activities of Rituximab.Approved
RivaroxabanSelexipag may increase the anticoagulant activities of Rivaroxaban.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
SarpogrelateSarpogrelate may increase the anticoagulant activities of Selexipag.Investigational
SecobarbitalThe metabolism of Selexipag can be increased when combined with Secobarbital.Approved, Vet Approved
SelegilineSelegiline may increase the hypotensive activities of Selexipag.Approved, Investigational, Vet 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
SitaxentanSelexipag may increase the hypotensive activities of Sitaxentan.Approved, Investigational, Withdrawn
SpiraprilSpirapril may increase the hypotensive activities of Selexipag.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.Investigational, Nutraceutical
StiripentolThe serum concentration of Selexipag can be increased when it is combined with Stiripentol.Approved
SulfamethoxazoleThe metabolism of Selexipag can be decreased when combined with Sulfamethoxazole.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
TadalafilTadalafil may increase the antihypertensive activities of Selexipag.Approved, Investigational
TalinololSelexipag may increase the hypotensive activities of Talinolol.Investigational
TamoxifenThe metabolism of Selexipag can be decreased when combined with Tamoxifen.Approved
TelaprevirThe metabolism of Selexipag can be decreased when combined with Telaprevir.Approved, Withdrawn
TelithromycinThe metabolism of Selexipag can be decreased when combined with Telithromycin.Approved
TelmisartanTelmisartan may increase the hypotensive activities of Selexipag.Approved, Investigational
TemocaprilTemocapril may increase the hypotensive activities of Selexipag.Experimental, Investigational
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
TesmilifeneTesmilifene may increase the anticoagulant activities of Selexipag.Investigational
TetrahydropalmatineSelexipag may increase the hypotensive activities of Tetrahydropalmatine.Investigational
TheodrenalineSelexipag may increase the hypotensive activities of Theodrenaline.Investigational
TiboloneTibolone may increase the hypotensive activities of Selexipag.Approved, Investigational
TicagrelorTicagrelor may increase the anticoagulant activities of Selexipag.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
TolonidineSelexipag may increase the hypotensive activities of Tolonidine.Experimental
ToloxatoneToloxatone may increase the hypotensive activities of Selexipag.Approved
TopiroxostatThe metabolism of Selexipag can be decreased when combined with Topiroxostat.Approved, Investigational
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
TreprostinilTreprostinil may increase the hypotensive activities of Selexipag.Approved, Investigational
TrichlormethiazideTrichlormethiazide may increase the hypotensive activities of Selexipag.Approved, Vet Approved
TriflusalTriflusal may increase the anticoagulant activities of Selexipag.Approved, Investigational
TrimazosinTrimazosin may increase the hypotensive activities of Selexipag.Experimental
TrimethaphanTrimethaphan may increase the hypotensive activities of Selexipag.Approved, Investigational
TrimethoprimThe metabolism of Selexipag can be decreased when combined with Trimethoprim.Approved, Vet Approved
Trolamine salicylateThe risk or severity of adverse effects can be increased when Trolamine salicylate is combined with Selexipag.Approved
TroxerutinSelexipag may increase the anticoagulant activities of Troxerutin.Investigational
UdenafilUdenafil may increase the antihypertensive activities of Selexipag.Approved, Investigational
UnoprostoneUnoprostone may increase the hypotensive activities of Selexipag.Approved
UrapidilUrapidil may increase the hypotensive activities of Selexipag.Investigational
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
VincamineSelexipag may increase the hypotensive activities of Vincamine.Experimental
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
XipamideSelexipag may increase the hypotensive activities of Xipamide.Experimental
XylometazolineXylometazoline may increase the hypotensive activities of Selexipag.Approved
YohimbineYohimbine may decrease the antihypertensive activities of Selexipag.Approved, Vet Approved
ZiprasidoneThe metabolism of Selexipag can be decreased when combined with Ziprasidone.Approved
ZofenoprilSelexipag may increase the hypotensive activities of Zofenopril.Experimental
Food Interactions
No interactions found.

References

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
KEGG Drug
D09994
PubChem Compound
9913767
PubChem Substance
310265229
ChemSpider
8089417
ChEBI
90844
ChEMBL
CHEMBL238804
Drugs.com
Drugs.com Drug Page
Wikipedia
Selexipag
ATC Codes
B01AC27 — Selexipag
AHFS Codes
  • 48:48.00 — Vasodilating Agents
FDA label
Download (768 KB)

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
4RecruitingOtherPulmonary Arterial Hypertension (PAH)1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not 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
Prices
Not Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US7205302No2003-04-042023-04-04Us
US9173881No2009-08-122029-08-12Us
US9284280No2010-06-252030-06-25Us
US8791122No2010-08-012030-08-01Us

Properties

State
Solid
Experimental Properties
Not 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 features
Not Available

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available

Taxonomy

Description
This 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.
Kingdom
Organic compounds
Super Class
Organic nitrogen compounds
Class
Organonitrogen compounds
Sub Class
Amines
Direct Parent
Dialkylarylamines
Alternative Parents
Aminopyrazines / Imidolactams / Benzene and substituted derivatives / Organosulfonic acids and derivatives / Heteroaromatic compounds / Aminosulfonyl compounds / Dialkyl ethers / Carboxylic acids and derivatives / Azacyclic compounds / Organopnictogen compounds
show 3 more
Substituents
Dialkylarylamine / Aminopyrazine / Monocyclic benzene moiety / Pyrazine / Imidolactam / Benzenoid / Organic sulfonic acid or derivatives / Heteroaromatic compound / Organosulfonic acid or derivatives / Sulfonyl
show 14 more
Molecular Framework
Aromatic heteromonocyclic compounds
External Descriptors
Not 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 acy...
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 un...
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 react...
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, prostagland...
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), methotre...
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 November 22, 2017 12:39