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Identification
NameVorapaxar
Accession NumberDB09030
TypeSmall Molecule
GroupsApproved
DescriptionVorapaxar is a tricyclic himbacine-derived selective inhibitor of protease activated receptor (PAR-1) indicated for reducing the incidence of thrombotic cardiovascular events in patients with a history of myocardial infarction (MI) or with peripheral arterial disease (PAD). By inhibiting PAR-1, a thrombin receptor expressed on platelets, vorapaxar prevents thrombin-related platelet aggregation.
Structure
Thumb
Synonyms
[(1R,3aR,4aR,6R,8aR,9S,9aS)-9-{(E)-2-[5-(3-Fluorophényl)-2-pyridinyl]vinyl}-1-méthyl-3-oxododécahydronaphto[2,3-c]furan-6-yl]carbamate d'éthyle
Carbamic acid, [(1R,3aR,4aR,6R,8aR,9S,9aS)-9-[(1E)-2-[5-(3-fluorophenyl)-2- pyridinyl]ethenyl]dodecahydro-1-methyl-3-oxonaphtho[2,3-c]furan-6-yl]-, ethyl ester
Carbamic acid, N-[(1R,3aR,4aR,6R,8aR,9S,9aS)-9-[(E)-2-[5-(3-fluorophenyl)-2-pyridinyl]ethenyl]dodecahydro-1-methyl-3-oxonaphtho[2,3-c]furan-6-yl]-, ethyl ester
Ethyl N-[(3R,3aS,4S,4aR,7R,8aR,9aR)-4-[(E)-2-[5-(3-fluorophenyl)-2-pyridyl]vinyl]-3-methyl-1-oxo-3a,4,4a,5,6,7,8,8a,9,9a-decahydro-3H-benzo[f]isobenzofuran-7-yl]carbamate
Zontivity
External Identifiers
  • MFCD16038876
  • SCH 530348
  • SCH-530348
  • SCH530348
  • ZCE93644N2
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Zontivitytablet, film coated2.08 mg/1oralMerck Sharp & Dohme Corp.2014-05-08Not applicableUs
Zontivitytablet2.5 mgoralMerck Canada IncNot applicableNot applicableCanada
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International BrandsNot Available
Brand mixturesNot Available
Salts
Name/CASStructureProperties
Vorapaxar Sulfate
ThumbNot applicableDBSALT001104
Categories
UNIIZCE93644N2
CAS number618385-01-6
WeightAverage: 492.5817
Monoisotopic: 492.242435759
Chemical FormulaC29H33FN2O4
InChI KeyInChIKey=ZBGXUVOIWDMMJE-QHNZEKIYSA-N
InChI
InChI=1S/C29H33FN2O4/c1-3-35-29(34)32-23-10-11-24-20(14-23)15-26-27(17(2)36-28(26)33)25(24)12-9-22-8-7-19(16-31-22)18-5-4-6-21(30)13-18/h4-9,12-13,16-17,20,23-27H,3,10-11,14-15H2,1-2H3,(H,32,34)/b12-9+/t17-,20+,23-,24-,25+,26-,27+/m1/s1
IUPAC Name
N-[(1R,3aR,4aR,6R,8aR,9S,9aS)-9-[(E)-2-[5-(3-fluorophenyl)pyridin-2-yl]ethenyl]-1-methyl-3-oxo-dodecahydronaphtho[2,3-c]furan-6-yl]ethoxycarboximidic acid
SMILES
[H]\C(=C(\[H])[C@]1([H])[C@]2([H])[C@@]([H])(C)OC(=O)[C@]2([H])C[C@]2([H])C[C@@]([H])(CC[C@@]12[H])N=C(O)OCC)C1=NC=C(C=C1)C1=CC(F)=CC=C1
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as naphthofurans. These are compounds containing a furan ring fused to a naphthalene moiety. Furan is a 5 membered- ring aromatic ring with four carbon and one oxygen atoms. Naphthalene is a polycyclic aromatic hydrocarbon made up of two fused benzene rings.
KingdomOrganic compounds
Super ClassOrganoheterocyclic compounds
ClassNaphthofurans
Sub ClassNot Available
Direct ParentNaphthofurans
Alternative Parents
Substituents
  • Naphthofuran
  • 3-phenylpyridine
  • Halobenzene
  • Fluorobenzene
  • Cyclohexylamine
  • Benzenoid
  • Pyridine
  • Gamma butyrolactone
  • Monocyclic benzene moiety
  • Aryl halide
  • Aryl fluoride
  • Heteroaromatic compound
  • Oxolane
  • Lactone
  • Carboxylic acid ester
  • Oxacycle
  • Azacycle
  • Monocarboxylic acid or derivatives
  • Carboxylic acid derivative
  • Hydrocarbon derivative
  • Organooxygen compound
  • Organonitrogen compound
  • Organofluoride
  • Organohalogen compound
  • Carbonyl group
  • Aromatic heteropolycyclic compound
Molecular FrameworkAromatic heteropolycyclic compounds
External DescriptorsNot Available
Pharmacology
IndicationVorapaxar is indicated for the reduction of thrombotic cardiovascular events in patients with a history of myocardial infarction (MI) or peripheral arterial disease (PAD). It is usually co-administered with acetylsalicylic acid (ASA) and/or clopidogrel, and should therefore be administered as an addition to these medications as it has not been studied alone.
PharmacodynamicsNot Available
Mechanism of actionVorapaxar inhibits platelet aggregation through the reversible antagonism of protease-activated receptor 1 (PAR-1), also known as thrombin receptor. PARs are a family of G-protein coupled receptors highly expressed on platelets and activated by serine protease activity of thrombin to mediate thrombotic response. By blocking PAR-1 activating, vorapaxar inhibits thrombin-induced platelet aggregation and thrombin receptor agonist peptide (TRAP)-induced platelet aggregation. Vorapaxar does not inhibit platelet aggregation induced by other agonists such as adenosine diphosphate (ADP), collagen or a thromboxane mimetic.
Related Articles
AbsorptionAfter oral administration, vorapaxar is rapidly absorbed and peak concentrations occur at a median tmax of 1 hour under faster conditions. Vorapaxar may be taken with or without food as ingestion with a high-fat meal did not result in meaningful changes in AUC. The mean absolute bioavailability is 100%.
Volume of distribution

424 L

Protein bindingVorapaxar is extensively bound (>99%) to human plasma proteins, such as human serum albumin.
Metabolism

Vorapaxar is metabolized to its major circulating metabolite, M20, and its predominant metabolite excreted into feces, M19, by CYP3A4 and CYP 2J2.

SubstrateEnzymesProduct
Vorapaxar
amine metabolite (M19)Details
Vorapaxar
monohydroxy-vorapaxar (M20)Details
Route of eliminationVorapaxar is primarily eliminated as its metabolite M19 through the feces (91.5%), and partially eliminated in the urine (8.5%).
Half lifeVorapaxar has an effective half life of 3-4 days and an apparent terminal half life of 8 days.
ClearanceNot Available
ToxicityThere is an increased risk of bleeding and intracranial hemorrhage (ICH), which is why the use of vorapaxar is contraindicated in patients with a history of stroke, trans-ischemic attack (TIA), ICH, or active pathological bleeding such as peptic ulcer. Animal studies have suggested that there is a low probability of embryo/fetal toxicities, however there are no adequate and well-controlled studies describing use in pregnant women. Vorapaxar should also be avoided during breastfeeding as it is unknown whether vorapaxar or its metabolites are excreted in human milk, however it has been shown to be actively secreted in the milk of rats.
Affected organismsNot Available
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal AbsorptionNot AvailableNot Available
Blood Brain BarrierNot AvailableNot Available
Caco-2 permeableNot AvailableNot Available
P-glycoprotein substrateNot AvailableNot Available
P-glycoprotein inhibitor INot AvailableNot Available
P-glycoprotein inhibitor IINot AvailableNot Available
Renal organic cation transporterNot AvailableNot Available
CYP450 2C9 substrateNot AvailableNot Available
CYP450 2D6 substrateNot AvailableNot Available
CYP450 3A4 substrateNot AvailableNot Available
CYP450 1A2 substrateNot AvailableNot Available
CYP450 2C9 inhibitorNot AvailableNot Available
CYP450 2D6 inhibitorNot AvailableNot Available
CYP450 2C19 inhibitorNot AvailableNot Available
CYP450 3A4 inhibitorNot AvailableNot Available
CYP450 inhibitory promiscuityNot AvailableNot Available
Ames testNot AvailableNot Available
CarcinogenicityNot AvailableNot Available
BiodegradationNot AvailableNot Available
Rat acute toxicityNot AvailableNot applicable
hERG inhibition (predictor I)Not AvailableNot Available
hERG inhibition (predictor II)Not AvailableNot Available
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
ManufacturersNot Available
PackagersNot Available
Dosage forms
FormRouteStrength
Tabletoral2.5 mg
Tablet, film coatedoral2.08 mg/1
PricesNot Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US7235567 No2001-06-132021-06-13Us
US7304078 No2004-04-062024-04-06Us
Properties
StateSolid
Experimental Properties
PropertyValueSource
logP5.39ChEMBL
Predicted Properties
PropertyValueSource
Water Solubility0.000787 mg/mLALOGPS
logP5.2ALOGPS
logP5.82ChemAxon
logS-5.8ALOGPS
pKa (Strongest Acidic)8ChemAxon
pKa (Strongest Basic)4.32ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count5ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area81.01 Å2ChemAxon
Rotatable Bond Count6ChemAxon
Refractivity135.31 m3·mol-1ChemAxon
Polarizability54.8 Å3ChemAxon
Number of Rings5ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
SpectraNot Available
References
Synthesis ReferenceNot Available
General References
  1. Ghosal A, Lu X, Penner N, Gao L, Ramanathan R, Chowdhury SK, Kishnani NS, Alton KB: Identification of human liver cytochrome P450 enzymes involved in the metabolism of SCH 530348 (Vorapaxar), a potent oral thrombin protease-activated receptor 1 antagonist. Drug Metab Dispos. 2011 Jan;39(1):30-8. doi: 10.1124/dmd.110.035493. Epub 2010 Oct 6. [PubMed:20926621 ]
  2. Lhermusier T, Baker NC, Waksman R: Overview of the 2014 Food and Drug Administration Cardiovascular and Renal Drugs Advisory Committee meeting regarding cangrelor. Am J Cardiol. 2015 Apr 15;115(8):1154-61. doi: 10.1016/j.amjcard.2015.01.551. Epub 2015 Feb 3. [PubMed:25728646 ]
  3. Tricoci P, Huang Z, Held C, Moliterno DJ, Armstrong PW, Van de Werf F, White HD, Aylward PE, Wallentin L, Chen E, Lokhnygina Y, Pei J, Leonardi S, Rorick TL, Kilian AM, Jennings LH, Ambrosio G, Bode C, Cequier A, Cornel JH, Diaz R, Erkan A, Huber K, Hudson MP, Jiang L, Jukema JW, Lewis BS, Lincoff AM, Montalescot G, Nicolau JC, Ogawa H, Pfisterer M, Prieto JC, Ruzyllo W, Sinnaeve PR, Storey RF, Valgimigli M, Whellan DJ, Widimsky P, Strony J, Harrington RA, Mahaffey KW: Thrombin-receptor antagonist vorapaxar in acute coronary syndromes. N Engl J Med. 2012 Jan 5;366(1):20-33. doi: 10.1056/NEJMoa1109719. Epub 2011 Nov 13. [PubMed:22077816 ]
  4. Cheng JW, Colucci V, Howard PA, Nappi JM, Spinler SA: Vorapaxar in atherosclerotic disease management. Ann Pharmacother. 2015 May;49(5):599-606. doi: 10.1177/1060028015571410. Epub 2015 Feb 13. [PubMed:25680760 ]
External Links
ATC CodesB01AC26
AHFS Codes
  • 20:12.18
PDB EntriesNot Available
FDA labelDownload (651 KB)
MSDSDownload (49.5 KB)
Interactions
Drug Interactions
Drug
AbciximabThe risk or severity of adverse effects can be increased when Vorapaxar is combined with Abciximab.
AbciximabAbciximab may increase the anticoagulant activities of Vorapaxar.
AcenocoumarolThe risk or severity of adverse effects can be increased when Vorapaxar is combined with Acenocoumarol.
Acetylsalicylic acidThe risk or severity of adverse effects can be increased when Acetylsalicylic acid is combined with Vorapaxar.
AlprostadilAlprostadil may increase the anticoagulant activities of Vorapaxar.
AlprostadilVorapaxar may increase the antiplatelet activities of Alprostadil.
AlteplaseVorapaxar may increase the anticoagulant activities of Alteplase.
ALX-0081Vorapaxar may increase the anticoagulant activities of ALX-0081.
Aminosalicylic AcidThe risk or severity of adverse effects can be increased when Aminosalicylic Acid is combined with Vorapaxar.
AmiodaroneThe serum concentration of Vorapaxar can be increased when it is combined with Amiodarone.
AnagrelideAnagrelide may increase the anticoagulant activities of Vorapaxar.
AncrodThe risk or severity of adverse effects can be increased when Vorapaxar is combined with Ancrod.
AnistreplaseVorapaxar may increase the anticoagulant activities of Anistreplase.
Antithrombin III humanThe risk or severity of adverse effects can be increased when Vorapaxar is combined with Antithrombin III human.
ApixabanThe risk or severity of adverse effects can be increased when Vorapaxar is combined with Apixaban.
AprotininThe therapeutic efficacy of Vorapaxar can be decreased when used in combination with Aprotinin.
ArdeparinThe risk or severity of adverse effects can be increased when Vorapaxar is combined with Ardeparin.
ArgatrobanThe risk or severity of adverse effects can be increased when Vorapaxar is combined with Argatroban.
ArgatrobanArgatroban may increase the anticoagulant activities of Vorapaxar.
AstaxanthinVorapaxar may increase the anticoagulant activities of Astaxanthin.
AtazanavirThe serum concentration of Vorapaxar can be increased when it is combined with Atazanavir.
AzelastineAzelastine may increase the anticoagulant activities of Vorapaxar.
AzelastineVorapaxar may increase the antiplatelet activities of Azelastine.
BatroxobinVorapaxar may increase the anticoagulant activities of Batroxobin.
BecaplerminThe risk or severity of adverse effects can be increased when Vorapaxar is combined with Becaplermin.
BemiparinVorapaxar may increase the anticoagulant activities of Bemiparin.
BeraprostBeraprost may increase the anticoagulant activities of Vorapaxar.
BivalirudinThe risk or severity of adverse effects can be increased when Vorapaxar is combined with Bivalirudin.
BoceprevirThe serum concentration of Vorapaxar can be increased when it is combined with Boceprevir.
CangrelorCangrelor may increase the anticoagulant activities of Vorapaxar.
CarbamazepineThe serum concentration of Vorapaxar can be decreased when it is combined with Carbamazepine.
CeritinibThe serum concentration of Vorapaxar can be increased when it is combined with Ceritinib.
CertoparinThe risk or severity of adverse effects can be increased when Vorapaxar is combined with Certoparin.
CilostazolCilostazol may increase the anticoagulant activities of Vorapaxar.
Citric AcidThe risk or severity of adverse effects can be increased when Vorapaxar is combined with Citric Acid.
ClarithromycinThe serum concentration of Vorapaxar can be increased when it is combined with Clarithromycin.
ClopidogrelClopidogrel may increase the anticoagulant activities of Vorapaxar.
CobicistatThe serum concentration of Vorapaxar can be increased when it is combined with Cobicistat.
CollagenaseThe risk or severity of adverse effects can be increased when Vorapaxar is combined with Collagenase.
Dabigatran etexilateThe risk or severity of adverse effects can be increased when Vorapaxar is combined with Dabigatran etexilate.
DalteparinThe risk or severity of adverse effects can be increased when Vorapaxar is combined with Dalteparin.
DanaparoidThe risk or severity of adverse effects can be increased when Vorapaxar is combined with Danaparoid.
DarunavirThe serum concentration of Vorapaxar can be increased when it is combined with Darunavir.
DasatinibDasatinib may increase the anticoagulant activities of Vorapaxar.
DefibrotideDefibrotide may increase the anticoagulant activities of Vorapaxar.
Deoxycholic AcidThe risk or severity of adverse effects can be increased when Vorapaxar is combined with Deoxycholic Acid.
DesirudinThe risk or severity of adverse effects can be increased when Vorapaxar is combined with Desirudin.
DesmoteplaseVorapaxar may increase the anticoagulant activities of Desmoteplase.
DextranThe risk or severity of adverse effects can be increased when Vorapaxar is combined with Dextran.
Dextran 40The risk or severity of adverse effects can be increased when Vorapaxar is combined with Dextran 40.
Dextran 70The risk or severity of adverse effects can be increased when Vorapaxar is combined with Dextran 70.
Dextran 75The risk or severity of adverse effects can be increased when Vorapaxar is combined with Dextran 75.
DicoumarolThe risk or severity of adverse effects can be increased when Vorapaxar is combined with Dicoumarol.
DiflunisalThe risk or severity of adverse effects can be increased when Diflunisal is combined with Vorapaxar.
DipyridamoleDipyridamole may increase the anticoagulant activities of Vorapaxar.
DitazoleVorapaxar may increase the anticoagulant activities of Ditazole.
Drotrecogin alfaVorapaxar may increase the anticoagulant activities of Drotrecogin alfa.
Edetic AcidThe risk or severity of adverse effects can be increased when Vorapaxar is combined with Edetic Acid.
EdoxabanThe risk or severity of adverse effects can be increased when Vorapaxar is combined with Edoxaban.
EnoxaparinThe risk or severity of adverse effects can be increased when Vorapaxar is combined with Enoxaparin.
EnzalutamideThe serum concentration of Vorapaxar can be decreased when it is combined with Enzalutamide.
EpinastineEpinastine may increase the anticoagulant activities of Vorapaxar.
EpinastineVorapaxar may increase the antiplatelet activities of Epinastine.
EpoprostenolEpoprostenol may increase the anticoagulant activities of Vorapaxar.
EptifibatideEptifibatide may increase the anticoagulant activities of Vorapaxar.
Ethyl biscoumacetateThe risk or severity of adverse effects can be increased when Vorapaxar is combined with Ethyl biscoumacetate.
FibrinolysinVorapaxar may increase the anticoagulant activities of Fibrinolysin.
Fondaparinux sodiumThe risk or severity of adverse effects can be increased when Vorapaxar is combined with Fondaparinux sodium.
FosphenytoinThe serum concentration of Vorapaxar can be decreased when it is combined with Fosphenytoin.
GlucosamineGlucosamine may increase the antiplatelet activities of Vorapaxar.
HeparinThe risk or severity of adverse effects can be increased when Vorapaxar is combined with Heparin.
HirulogThe risk or severity of adverse effects can be increased when Vorapaxar is combined with Hirulog.
Ibritumomab tiuxetanThe risk or severity of adverse effects can be increased when Vorapaxar is combined with Ibritumomab tiuxetan.
IbrutinibThe risk or severity of adverse effects can be increased when Ibrutinib is combined with Vorapaxar.
IbudilastIbudilast may increase the anticoagulant activities of Vorapaxar.
IbudilastVorapaxar may increase the antiplatelet activities of Ibudilast.
Icosapent ethylIcosapent ethyl may increase the anticoagulant activities of Vorapaxar.
Icosapent ethylVorapaxar may increase the antiplatelet activities of Icosapent ethyl.
IdelalisibThe serum concentration of Vorapaxar can be increased when it is combined with Idelalisib.
IfenprodilIfenprodil may increase the anticoagulant activities of Vorapaxar.
IfenprodilVorapaxar may increase the antiplatelet activities of Ifenprodil.
IloprostIloprost may increase the anticoagulant activities of Vorapaxar.
IndinavirThe serum concentration of Vorapaxar can be increased when it is combined with Indinavir.
ItraconazoleThe serum concentration of Vorapaxar can be increased when it is combined with Itraconazole.
KetoconazoleThe serum concentration of Vorapaxar can be increased when it is combined with Ketoconazole.
LepirudinThe risk or severity of adverse effects can be increased when Vorapaxar is combined with Lepirudin.
LimaprostThe risk or severity of adverse effects can be increased when Limaprost is combined with Vorapaxar.
LopinavirThe serum concentration of Vorapaxar can be increased when it is combined with Lopinavir.
MesalazineThe risk or severity of adverse effects can be increased when Mesalazine is combined with Vorapaxar.
MilrinoneMilrinone may increase the anticoagulant activities of Vorapaxar.
MilrinoneVorapaxar may increase the antiplatelet activities of Milrinone.
MitotaneThe serum concentration of Vorapaxar can be decreased when it is combined with Mitotane.
NadroparinThe risk or severity of adverse effects can be increased when Vorapaxar is combined with Nadroparin.
NCX 4016NCX 4016 may increase the anticoagulant activities of Vorapaxar.
NefazodoneThe serum concentration of Vorapaxar can be increased when it is combined with Nefazodone.
NelfinavirThe serum concentration of Vorapaxar can be increased when it is combined with Nelfinavir.
NevirapineThe serum concentration of Vorapaxar can be decreased when it is combined with Nevirapine.
NimesulideNimesulide may increase the anticoagulant activities of Vorapaxar.
NimesulideVorapaxar may increase the antiplatelet activities of Nimesulide.
ObinutuzumabThe risk or severity of adverse effects can be increased when Vorapaxar is combined with Obinutuzumab.
Omega-3 fatty acidsOmega-3 fatty acids may increase the antiplatelet activities of Vorapaxar.
OtamixabanThe risk or severity of adverse effects can be increased when Vorapaxar is combined with Otamixaban.
ParnaparinVorapaxar may increase the anticoagulant activities of Parnaparin.
PentobarbitalThe serum concentration of Vorapaxar can be decreased when it is combined with Pentobarbital.
Pentosan PolysulfateThe risk or severity of adverse effects can be increased when Vorapaxar is combined with Pentosan Polysulfate.
PentoxifyllinePentoxifylline may increase the antiplatelet activities of Vorapaxar.
PhenindioneThe risk or severity of adverse effects can be increased when Vorapaxar is combined with Phenindione.
PhenobarbitalThe serum concentration of Vorapaxar can be decreased when it is combined with Phenobarbital.
PhenprocoumonThe risk or severity of adverse effects can be increased when Vorapaxar is combined with Phenprocoumon.
PhenytoinThe serum concentration of Vorapaxar can be decreased when it is combined with Phenytoin.
PlasminVorapaxar may increase the anticoagulant activities of Plasmin.
PosaconazoleThe serum concentration of Vorapaxar can be increased when it is combined with Posaconazole.
PrasugrelPrasugrel may increase the anticoagulant activities of Vorapaxar.
PrimidoneThe serum concentration of Vorapaxar can be decreased when it is combined with Primidone.
Protein CThe risk or severity of adverse effects can be increased when Vorapaxar is combined with Protein C.
ProtocatechualdehydeThe risk or severity of adverse effects can be increased when Vorapaxar is combined with Protocatechualdehyde.
ResveratrolResveratrol may increase the anticoagulant activities of Vorapaxar.
ResveratrolVorapaxar may increase the antiplatelet activities of Resveratrol.
ReteplaseVorapaxar may increase the anticoagulant activities of Reteplase.
ReviparinThe risk or severity of adverse effects can be increased when Vorapaxar is combined with Reviparin.
RidogrelRidogrel may increase the anticoagulant activities of Vorapaxar.
RidogrelVorapaxar may increase the antiplatelet activities of Ridogrel.
RifabutinThe serum concentration of Vorapaxar can be decreased when it is combined with Rifabutin.
RifampicinThe serum concentration of Vorapaxar can be decreased when it is combined with Rifampicin.
RifapentineThe serum concentration of Vorapaxar can be decreased when it is combined with Rifapentine.
RitonavirThe serum concentration of Vorapaxar can be increased when it is combined with Ritonavir.
RivaroxabanThe risk or severity of adverse effects can be increased when Vorapaxar is combined with Rivaroxaban.
RosiglitazoneVorapaxar may increase the anticoagulant activities of Rosiglitazone.
Salicylic acidThe risk or severity of adverse effects can be increased when Salicylic acid is combined with Vorapaxar.
SaquinavirThe serum concentration of Vorapaxar can be increased when it is combined with Saquinavir.
SCH-530348SCH-530348 may increase the anticoagulant activities of Vorapaxar.
SCH-530348Vorapaxar may increase the antiplatelet activities of SCH-530348.
SelexipagVorapaxar may increase the anticoagulant activities of Selexipag.
SevofluraneSevoflurane may increase the anticoagulant activities of Vorapaxar.
SevofluraneVorapaxar may increase the antiplatelet activities of Sevoflurane.
SRT501SRT501 may increase the anticoagulant activities of Vorapaxar.
SRT501Vorapaxar may increase the antiplatelet activities of SRT501.
St. John's WortThe serum concentration of Vorapaxar can be decreased when it is combined with St. John's Wort.
StreptokinaseVorapaxar may increase the anticoagulant activities of Streptokinase.
SulodexideThe risk or severity of adverse effects can be increased when Vorapaxar is combined with Sulodexide.
TelaprevirThe serum concentration of Vorapaxar can be increased when it is combined with Telaprevir.
TelithromycinThe serum concentration of Vorapaxar can be increased when it is combined with Telithromycin.
TenecteplaseVorapaxar may increase the anticoagulant activities of Tenecteplase.
TesmilifeneTesmilifene may increase the anticoagulant activities of Vorapaxar.
TesmilifeneVorapaxar may increase the antiplatelet activities of Tesmilifene.
TicagrelorVorapaxar may increase the anticoagulant activities of Ticagrelor.
TiclopidineTiclopidine may increase the anticoagulant activities of Vorapaxar.
TinzaparinVorapaxar may increase the anticoagulant activities of Tinzaparin.
TipranavirTipranavir may increase the antiplatelet activities of Vorapaxar.
TirofibanTirofiban may increase the anticoagulant activities of Vorapaxar.
TositumomabThe risk or severity of adverse effects can be increased when Vorapaxar is combined with Tositumomab.
TranilastTranilast may increase the anticoagulant activities of Vorapaxar.
TranilastVorapaxar may increase the antiplatelet activities of Tranilast.
TrapidilTrapidil may increase the anticoagulant activities of Vorapaxar.
TrapidilVorapaxar may increase the antiplatelet activities of Trapidil.
TreprostinilVorapaxar may increase the anticoagulant activities of Treprostinil.
TreprostinilTreprostinil may increase the antiplatelet activities of Vorapaxar.
TriflusalTriflusal may increase the anticoagulant activities of Vorapaxar.
UrokinaseVorapaxar may increase the anticoagulant activities of Urokinase.
Vitamin EVitamin E may increase the antiplatelet activities of Vorapaxar.
VoriconazoleThe serum concentration of Vorapaxar can be increased when it is combined with Voriconazole.
WarfarinThe risk or severity of adverse effects can be increased when Vorapaxar is combined with Warfarin.
XimelagatranThe risk or severity of adverse effects can be increased when Vorapaxar is combined with Ximelagatran.
Food InteractionsNot Available

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
antagonist
General Function:
Thrombin receptor activity
Specific Function:
High affinity receptor for activated thrombin coupled to G proteins that stimulate phosphoinositide hydrolysis. May play a role in platelets activation and in vascular development.
Gene Name:
F2R
Uniprot ID:
P25116
Molecular Weight:
47439.83 Da
References
  1. Bonaca MP, Morrow DA: SCH 530348: a novel oral thrombin receptor antagonist. Future Cardiol. 2009 Sep;5(5):435-42. doi: 10.2217/fca.09.27. [PubMed:19715408 ]
Comments
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Drug created on February 09, 2015 15:24 / Updated on September 25, 2016 02:16