U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

Details

Stereochemistry ABSOLUTE
Molecular Formula C29H33FN2O4
Molecular Weight 492.5817
Optical Activity UNSPECIFIED
Defined Stereocenters 7 / 7
E/Z Centers 1
Charge 0

SHOW SMILES / InChI
Structure of VORAPAXAR

SMILES

[H][C@@]12C[C@]3([H])C[C@@]([H])(CC[C@@]3([H])[C@]([H])(\C=C\C4=CC=C(C=N4)C5=CC(F)=CC=C5)[C@]1([H])[C@@H](C)OC2=O)NC(=O)OCC

InChI

InChIKey=ZBGXUVOIWDMMJE-QHNZEKIYSA-N
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

HIDE SMILES / InChI
Molecular Formula C29H33FN2O4
Molecular Weight 492.5817
Charge 0
Count
Stereochemistry ABSOLUTE
Additional Stereochemistry No
Defined Stereocenters 7 / 7
E/Z Centers 1
Optical Activity UNSPECIFIED

Description
Curator's Comment: description was created based on several sources, including http://www.ncbi.nlm.nih.gov/pubmed/26022529

Vorapaxar is a tricyclic himbacine-derived oral thrombin receptor antagonist that acts by reversible inhibition of the protease-activated receptor-1 (PAR-1). PAR-1 is expressed on platelets and its inhibition prevents platelets from aggregation. Vorapaxar is approved by FDA and is indicated for the reduction of recurring thrombotic cardiovascular events in patients with a history of myocardial infarction or with peripheral arterial disease. Vorapaxar at the same time may cause bleeding complications including intracranial haemorrhage (ICH), when compared to standard therapy alone. That is why Vorapaxar is contraindicated in patients with prior stroke, transient ischemic attack and ICH.

Originator

Schering-Plough
34
Curator's Comment: The drug was discovered by Schering-Plough and developed by Merck.

Approval Year

2014
494
Targets

Targets

Primary TargetPharmacologyConditionPotency
Proteinase-activated receptor 1
5
Target ID: P25116
Gene ID: 2149.0
Gene Symbol: F2R
Target Organism: Homo sapiens (Human)
Antagonist
2778
 13.0 nM [IC50]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Preventing
Approved
8429
ZONTIVITY

Approved Use

Indicated for the reduction of thrombotic cardiovascular events in patients with a history of myocardial infarction (MI) or with peripheral arterial disease (PAD).

Launch Date

1.39950726E12
Preventing
Approved
8429
ZONTIVITY

Approved Use

Indicated for the reduction of thrombotic cardiovascular events in patients with a history of myocardial infarction (MI) or with peripheral arterial disease (PAD).

Launch Date

1.39950726E12
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
262 ng/mL
EXPERIMENT
https://www.ncbi.nlm.nih.gov/pubmed/27121783
40 mg single, oral
dose: 40 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
VORAPAXAR plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
18400 ng × h/mL
EXPERIMENT
https://www.ncbi.nlm.nih.gov/pubmed/27121783
40 mg single, oral
dose: 40 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
VORAPAXAR plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
240 h
EXPERIMENT
https://www.ncbi.nlm.nih.gov/pubmed/27121783
40 mg single, oral
dose: 40 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
VORAPAXAR plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
Doses

Doses

DosePopulationAdverse events​
40 mg single, oral (starting)
Highest studied dose
Dose: 40 mg
Route: oral
Route: single
Dose: 40 mg
Sources:
https://pubmed.ncbi.nlm.nih.gov/19286091
unhealthy, 63.5 years
n = 173
Health Status: unhealthy
Condition: coronary artery disease
Age Group: 63.5 years
Sex: M+F
Population Size: 173
Sources:
https://pubmed.ncbi.nlm.nih.gov/19286091
Sources:
https://pubmed.ncbi.nlm.nih.gov/19286091
2.5 mg 1 times / day multiple, oral
Recommended
Dose: 2.5 mg, 1 times / day
Route: oral
Route: multiple
Dose: 2.5 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204886Orig1s000MedR.pdf
Page: p. 142
unhealthy, adult
n = 13186
Health Status: unhealthy
Age Group: adult
Sex: M+F
Population Size: 13186
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204886Orig1s000MedR.pdf
Page: p. 142
Disc. AE: Melaena, Rectal haemorrhage...
Other AEs: Venous thrombosis...
AEs leading to
discontinuation/dose reduction:
Melaena (0.2%)
Rectal haemorrhage (0.2%)
Haemorrhage intracranial (0.3%)
Haematuria (0.2%)
Epistaxis (0.4%)
Increased tendency to bruise (0.2%)
Anaemia (0.3%)
Visual acuity reduced (0.1%)
Hypertransaminasaemia (0.1%)
Transaminases abnormal (0.1%)
Initial insomnia (0.1%)
Depressive symptom (0.1%)
Varicose vein (0.1%)
Vein pain (0.1%)
Other AEs:
Venous thrombosis (0.1%)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204886Orig1s000MedR.pdf
Page: p. 142
2.5 mg 1 times / day multiple, oral
Recommended
Dose: 2.5 mg, 1 times / day
Route: oral
Route: multiple
Dose: 2.5 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/204886s000lbl.pdf
unhealthy, adult
Health Status: unhealthy
Condition: intracranial hemorrhage | transient ischemic attack
Age Group: adult
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/204886s000lbl.pdf
Other AEs: Bleeding...
Other AEs:
Bleeding
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/204886s000lbl.pdf
AEs

AEs

AESignificanceDosePopulation
Venous thrombosis 0.1%
2.5 mg 1 times / day multiple, oral
Recommended
Dose: 2.5 mg, 1 times / day
Route: oral
Route: multiple
Dose: 2.5 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204886Orig1s000MedR.pdf
Page: p. 142
unhealthy, adult
n = 13186
Health Status: unhealthy
Age Group: adult
Sex: M+F
Population Size: 13186
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204886Orig1s000MedR.pdf
Page: p. 142
Depressive symptom 0.1%
Disc. AE
2.5 mg 1 times / day multiple, oral
Recommended
Dose: 2.5 mg, 1 times / day
Route: oral
Route: multiple
Dose: 2.5 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204886Orig1s000MedR.pdf
Page: p. 142
unhealthy, adult
n = 13186
Health Status: unhealthy
Age Group: adult
Sex: M+F
Population Size: 13186
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204886Orig1s000MedR.pdf
Page: p. 142
Hypertransaminasaemia 0.1%
Disc. AE
2.5 mg 1 times / day multiple, oral
Recommended
Dose: 2.5 mg, 1 times / day
Route: oral
Route: multiple
Dose: 2.5 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204886Orig1s000MedR.pdf
Page: p. 142
unhealthy, adult
n = 13186
Health Status: unhealthy
Age Group: adult
Sex: M+F
Population Size: 13186
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204886Orig1s000MedR.pdf
Page: p. 142
Initial insomnia 0.1%
Disc. AE
2.5 mg 1 times / day multiple, oral
Recommended
Dose: 2.5 mg, 1 times / day
Route: oral
Route: multiple
Dose: 2.5 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204886Orig1s000MedR.pdf
Page: p. 142
unhealthy, adult
n = 13186
Health Status: unhealthy
Age Group: adult
Sex: M+F
Population Size: 13186
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204886Orig1s000MedR.pdf
Page: p. 142
Transaminases abnormal 0.1%
Disc. AE
2.5 mg 1 times / day multiple, oral
Recommended
Dose: 2.5 mg, 1 times / day
Route: oral
Route: multiple
Dose: 2.5 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204886Orig1s000MedR.pdf
Page: p. 142
unhealthy, adult
n = 13186
Health Status: unhealthy
Age Group: adult
Sex: M+F
Population Size: 13186
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204886Orig1s000MedR.pdf
Page: p. 142
Varicose vein 0.1%
Disc. AE
2.5 mg 1 times / day multiple, oral
Recommended
Dose: 2.5 mg, 1 times / day
Route: oral
Route: multiple
Dose: 2.5 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204886Orig1s000MedR.pdf
Page: p. 142
unhealthy, adult
n = 13186
Health Status: unhealthy
Age Group: adult
Sex: M+F
Population Size: 13186
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204886Orig1s000MedR.pdf
Page: p. 142
Vein pain 0.1%
Disc. AE
2.5 mg 1 times / day multiple, oral
Recommended
Dose: 2.5 mg, 1 times / day
Route: oral
Route: multiple
Dose: 2.5 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204886Orig1s000MedR.pdf
Page: p. 142
unhealthy, adult
n = 13186
Health Status: unhealthy
Age Group: adult
Sex: M+F
Population Size: 13186
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204886Orig1s000MedR.pdf
Page: p. 142
Visual acuity reduced 0.1%
Disc. AE
2.5 mg 1 times / day multiple, oral
Recommended
Dose: 2.5 mg, 1 times / day
Route: oral
Route: multiple
Dose: 2.5 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204886Orig1s000MedR.pdf
Page: p. 142
unhealthy, adult
n = 13186
Health Status: unhealthy
Age Group: adult
Sex: M+F
Population Size: 13186
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204886Orig1s000MedR.pdf
Page: p. 142
Haematuria 0.2%
Disc. AE
2.5 mg 1 times / day multiple, oral
Recommended
Dose: 2.5 mg, 1 times / day
Route: oral
Route: multiple
Dose: 2.5 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204886Orig1s000MedR.pdf
Page: p. 142
unhealthy, adult
n = 13186
Health Status: unhealthy
Age Group: adult
Sex: M+F
Population Size: 13186
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204886Orig1s000MedR.pdf
Page: p. 142
Increased tendency to bruise 0.2%
Disc. AE
2.5 mg 1 times / day multiple, oral
Recommended
Dose: 2.5 mg, 1 times / day
Route: oral
Route: multiple
Dose: 2.5 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204886Orig1s000MedR.pdf
Page: p. 142
unhealthy, adult
n = 13186
Health Status: unhealthy
Age Group: adult
Sex: M+F
Population Size: 13186
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204886Orig1s000MedR.pdf
Page: p. 142
Melaena 0.2%
Disc. AE
2.5 mg 1 times / day multiple, oral
Recommended
Dose: 2.5 mg, 1 times / day
Route: oral
Route: multiple
Dose: 2.5 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204886Orig1s000MedR.pdf
Page: p. 142
unhealthy, adult
n = 13186
Health Status: unhealthy
Age Group: adult
Sex: M+F
Population Size: 13186
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204886Orig1s000MedR.pdf
Page: p. 142
Rectal haemorrhage 0.2%
Disc. AE
2.5 mg 1 times / day multiple, oral
Recommended
Dose: 2.5 mg, 1 times / day
Route: oral
Route: multiple
Dose: 2.5 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204886Orig1s000MedR.pdf
Page: p. 142
unhealthy, adult
n = 13186
Health Status: unhealthy
Age Group: adult
Sex: M+F
Population Size: 13186
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204886Orig1s000MedR.pdf
Page: p. 142
Anaemia 0.3%
Disc. AE
2.5 mg 1 times / day multiple, oral
Recommended
Dose: 2.5 mg, 1 times / day
Route: oral
Route: multiple
Dose: 2.5 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204886Orig1s000MedR.pdf
Page: p. 142
unhealthy, adult
n = 13186
Health Status: unhealthy
Age Group: adult
Sex: M+F
Population Size: 13186
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204886Orig1s000MedR.pdf
Page: p. 142
Haemorrhage intracranial 0.3%
Disc. AE
2.5 mg 1 times / day multiple, oral
Recommended
Dose: 2.5 mg, 1 times / day
Route: oral
Route: multiple
Dose: 2.5 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204886Orig1s000MedR.pdf
Page: p. 142
unhealthy, adult
n = 13186
Health Status: unhealthy
Age Group: adult
Sex: M+F
Population Size: 13186
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204886Orig1s000MedR.pdf
Page: p. 142
Epistaxis 0.4%
Disc. AE
2.5 mg 1 times / day multiple, oral
Recommended
Dose: 2.5 mg, 1 times / day
Route: oral
Route: multiple
Dose: 2.5 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204886Orig1s000MedR.pdf
Page: p. 142
unhealthy, adult
n = 13186
Health Status: unhealthy
Age Group: adult
Sex: M+F
Population Size: 13186
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/204886Orig1s000MedR.pdf
Page: p. 142
Bleeding
2.5 mg 1 times / day multiple, oral
Recommended
Dose: 2.5 mg, 1 times / day
Route: oral
Route: multiple
Dose: 2.5 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/204886s000lbl.pdf
unhealthy, adult
Health Status: unhealthy
Condition: intracranial hemorrhage | transient ischemic attack
Age Group: adult
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/204886s000lbl.pdf
Overview

Overview

CYP3A4CYP2C9CYP2D6hERG
substrate
1737
inhibitor
1767
inhibitor
1852
inhibitor
1612

OverviewOther

Other InhibitorOther SubstrateOther Inducer
CYP2C8
911

P-gp
1461

CYP2A6
707

CYP2C19
1478

CYP1A2
1524

CYP2B6
810

CYP2E1
882

CYP3A4/5
278

OATP1B1
788

OATP1B3
706

OAT1
599

OCT2
647

OAT3
642

BCRP
699

Ca2+ channels
57
CYP2J2
56

P-gp
1537
Drug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
CYP1A2
1692
 no
CYP2A6
739
 no
CYP2B6
1001
 no
CYP2C19
1553
 no
CYP2D6
1891
 no
CYP2E1
970
 no
CYP3A4/5
335
 no
Ca2+ channels
60
 no
OAT1
603
 no
OATP1B1
803
 no
OATP1B3
715
 no
OCT2
648
 no
P-gp
1650
 yes [IC50 1.2 uM]
no (co-administration study)
Comment: Based on in vitro results, the DDI potential of vorapaxar (as a P-gp inhibitor) with digoxin (as a P-gp substrate), is not expected to be of clinical consequences 2.5 mg dose.
Page: 63.0
CYP2C8
965
 yes [IC50 1.5 uM]
no (co-administration study)
Comment: In vivo drug interaction studies with warfarin and rosiglitazone were performed as vorapaxar showed a very modest potential to inhibit CYP2C8 [IC50=1.5 µM]
Page: 73.0
OAT3
644
 yes [IC50 2.2 uM]
BCRP
773
 yes [IC50 2.5 uM]
CYP2C9
1819
 yes [IC50 30 uM]
no (co-administration study)
Comment: Vorapaxar did not affect the pharmacokinetics or pharmacodynamics of warfarin.
Page: 70.0
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
P-gp
1537
 no
CYP2J2
56
 yes
CYP3A4
1737
 yes
yes (co-administration study)
Comment: Upon repeat co-administration, ketoconazole, a strong CYP3A inhibitor, increases the systemic exposures to vorapaxar by 2-fold, while rifampin, a strong CYP3A inducer, decreases the systemic exposure to vorapaxar by 55%.
Page: 100.0
Tox targets

Tox targets

TargetModalityActivityMetaboliteClinical evidence
hERG
1647
Sourcing

Sourcing

Vendor/AggregatorIDURL
ChEBI
CHEBI:82702
https://www.ebi.ac.uk/chebi/searchId.do?chebiId=CHEBI:82702
ChemicalBook
CB32628522
https://www.chemicalbook.com/ChemicalProductProperty_EN_CB32628522
MolPort
MolPort-039-062-225
https://www.molport.com/shop/molecule-link/MolPort-039-062-225
Selleck Chemicals
vorapaxar
http://www.selleckchem.com/products/vorapaxar.html
ZINC
ZINC000003925861
http://zinc15.docking.org/substances/ZINC000003925861
PubMed

PubMed

TitleDatePubMed
Discovery of a novel, orally active himbacine-based thrombin receptor antagonist (SCH 530348) with potent antiplatelet activity.
2008 Jun 12
Patents

Patents

20030216437
4
20040176418
2

Sample Use Guides

In Vivo Use Guide
One tablet of ZONTIVITY orally once daily (Tablets: 2.08 mg vorapaxar)
Route of Administration: Oral
In Vitro Use Guide
In human platelet-rich plasma,vorapaxar inhibited thrombin and TRAP-induced platelet aggregation with an IC50 of 47 and 25nM, respectively, without affecting aggregation induced by other reagents, such as ADP, TXA2 mimetic U46619 or collagen.
Substance Class Chemical
Created
by admin
on Fri Dec 15 19:47:54 UTC 2023
Edited
by admin
on Fri Dec 15 19:47:54 UTC 2023
Record UNII
ZCE93644N2
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
VORAPAXAR
DASH   INN   MART.   MI   USAN   VANDF   WHO-DD  
USAN   INN  
Official Name English
VORAPAXAR [USAN]
Common Name English
VORAPAXAR [VANDF]
Common Name English
VORAPAXAR [MART.]
Common Name English
vorapaxar [INN]
Common Name English
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
Common Name English
VORAPAXAR [MI]
Common Name English
Vorapaxar [WHO-DD]
Common Name English
ETHYL ((1R,3AR,4AR,6R,8AR,9S,9AS)-9-((1E)-2-(5-(3-FLUOROPHENYL)PYRIDINE-2-YL)ETHEN-1-YL)-1-METHYL-3-OXODODECAHYDRONAPHTHO(2,3-C)FURAN-6-YL)CARBAMATE
Common Name English
Classification Tree Code System Code
NCI_THESAURUS C78274
Created by admin on Fri Dec 15 19:47:54 UTC 2023 , Edited by admin on Fri Dec 15 19:47:54 UTC 2023
NCI_THESAURUS C1327
Created by admin on Fri Dec 15 19:47:54 UTC 2023 , Edited by admin on Fri Dec 15 19:47:54 UTC 2023
WHO-ATC B01AC26
Created by admin on Fri Dec 15 19:47:54 UTC 2023 , Edited by admin on Fri Dec 15 19:47:54 UTC 2023
NDF-RT N0000190996
Created by admin on Fri Dec 15 19:47:54 UTC 2023 , Edited by admin on Fri Dec 15 19:47:54 UTC 2023
Code System Code Type Description
DRUG CENTRAL
4870
Created by admin on Fri Dec 15 19:47:54 UTC 2023 , Edited by admin on Fri Dec 15 19:47:54 UTC 2023
PRIMARY
NDF-RT
N0000190995
Created by admin on Fri Dec 15 19:47:54 UTC 2023 , Edited by admin on Fri Dec 15 19:47:54 UTC 2023
PRIMARY Protease-activated Receptor-1 Antagonists [MoA]
DAILYMED
ZCE93644N2
Created by admin on Fri Dec 15 19:47:54 UTC 2023 , Edited by admin on Fri Dec 15 19:47:54 UTC 2023
PRIMARY
CHEBI
82702
Created by admin on Fri Dec 15 19:47:54 UTC 2023 , Edited by admin on Fri Dec 15 19:47:54 UTC 2023
PRIMARY
ChEMBL
CHEMBL493982
Created by admin on Fri Dec 15 19:47:54 UTC 2023 , Edited by admin on Fri Dec 15 19:47:54 UTC 2023
PRIMARY
CAS
618385-01-6
Created by admin on Fri Dec 15 19:47:54 UTC 2023 , Edited by admin on Fri Dec 15 19:47:54 UTC 2023
PRIMARY
RXCUI
1537034
Created by admin on Fri Dec 15 19:47:54 UTC 2023 , Edited by admin on Fri Dec 15 19:47:54 UTC 2023
PRIMARY RxNorm
NCI_THESAURUS
C152912
Created by admin on Fri Dec 15 19:47:54 UTC 2023 , Edited by admin on Fri Dec 15 19:47:54 UTC 2023
PRIMARY
MERCK INDEX
m11500
Created by admin on Fri Dec 15 19:47:54 UTC 2023 , Edited by admin on Fri Dec 15 19:47:54 UTC 2023
PRIMARY Merck Index
SMS_ID
100000139516
Created by admin on Fri Dec 15 19:47:54 UTC 2023 , Edited by admin on Fri Dec 15 19:47:54 UTC 2023
PRIMARY
INN
8852
Created by admin on Fri Dec 15 19:47:54 UTC 2023 , Edited by admin on Fri Dec 15 19:47:54 UTC 2023
PRIMARY
IUPHAR
4047
Created by admin on Fri Dec 15 19:47:54 UTC 2023 , Edited by admin on Fri Dec 15 19:47:54 UTC 2023
PRIMARY
PUBCHEM
10077130
Created by admin on Fri Dec 15 19:47:54 UTC 2023 , Edited by admin on Fri Dec 15 19:47:54 UTC 2023
PRIMARY
DRUG BANK
DB09030
Created by admin on Fri Dec 15 19:47:54 UTC 2023 , Edited by admin on Fri Dec 15 19:47:54 UTC 2023
PRIMARY
MESH
C530299
Created by admin on Fri Dec 15 19:47:54 UTC 2023 , Edited by admin on Fri Dec 15 19:47:54 UTC 2023
PRIMARY
USAN
YY-21
Created by admin on Fri Dec 15 19:47:54 UTC 2023 , Edited by admin on Fri Dec 15 19:47:54 UTC 2023
PRIMARY
EPA CompTox
DTXSID201009336
Created by admin on Fri Dec 15 19:47:54 UTC 2023 , Edited by admin on Fri Dec 15 19:47:54 UTC 2023
PRIMARY
WIKIPEDIA
VORAPAXAR
Created by admin on Fri Dec 15 19:47:54 UTC 2023 , Edited by admin on Fri Dec 15 19:47:54 UTC 2023
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EVMPD
SUB88191
Created by admin on Fri Dec 15 19:47:54 UTC 2023 , Edited by admin on Fri Dec 15 19:47:54 UTC 2023
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FDA UNII
ZCE93644N2
Created by admin on Fri Dec 15 19:47:54 UTC 2023 , Edited by admin on Fri Dec 15 19:47:54 UTC 2023
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Related Record Type Details
CYTOCHROME P450 2J2
METABOLIC ENZYME -> SUBSTRATE
Structure of VORAPAXAR
EXCRETED UNCHANGED
Based on a mass balance study, <2% of vorapaxar is excreted unchanged in feces and none in urine.
FECAL
PLASMA PROTEIN FRACTION (HUMAN)
BINDER->LIGAND
BINDING
CYTOCHROME P450 3A4
METABOLIC ENZYME -> SUBSTRATE
Structure of VORAPAXAR SULFATE
SALT/SOLVATE -> PARENT
PROTEINASE-ACTIVATED RECEPTOR 1
TARGET -> INHIBITOR
Blocks thrombin activation of receptor on platelets
Ki
Related Record Type Details
Structure of SCH-2046273
METABOLITE ACTIVE -> PARENT
20% OF THE CIRCULATING DRUG
MAJOR
PLASMA
Related Record Type Details
Structure of VORAPAXAR
ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
Tmax PHARMACOKINETIC
Volume of Distribution PHARMACOKINETIC
Biological Half-life PHARMACOKINETIC
NIH
NCATS
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