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Drug ReportsVorapaxar
Zontivity(vorapaxar)
Zontivity (vorapaxar) is a small molecule pharmaceutical. Vorapaxar was first approved as Zontivity on 2014-05-08. It is used to treat coronary disease, myocardial infarction, and peripheral arterial disease in the USA. It has been approved in Europe to treat myocardial infarction. The pharmaceutical is active against proteinase-activated receptor 1.
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Commercial
Therapeutic Areas
Therapeutic Area
MeSH
cardiovascular diseasesD002318
signs and symptoms pathological conditionsD013568
Trade Name
FDA
EMA
No data
Drug Products
FDA
EMA
New Drug Application (NDA)
New Drug Application (NDA)
Abbreviated New Drug Application (ANDA)
Abbreviated New Drug Application (ANDA)
Vorapaxar sulfate
Tradename
Company
Number
Date
Products
ZONTIVITYKey TherapeuticsN-204886 DISCN2014-05-08
1 products, RLD
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FDA
EMA
Brand Name
Status
Last Update
zontivityNew Drug Application2022-10-18
Agency Specific
FDA
EMA
No data
Patent Expiration
Patent
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FDA Information
Vorapaxar Sulfate, Zontivity, Xspire Pharma
73040782027-12-23DS, DPU-1512
77139992024-05-30DS, DPU-2291
ATC Codes
B: Blood and blood forming organ drugs
— B01: Antithrombotic agents
— B01A: Antithrombotic agents
— B01AC: Platelet aggregation inhibitors excl. heparin
— B01AC26: Vorapaxar
HCPCS
Code
Description
G9531
Patient has documentation of ventricular shunt, brain tumor, multisystem trauma, or is currently taking an antiplatelet medication including: abciximab, anagrelide, cangrelor, cilostazol, clopidogrel, dipyridamole, eptifibatide, prasugrel, ticlopidine, ticagrelor, tirofiban, or vorapaxar
Clinical
Clinical Trials
15 clinical trials
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Indications Phases 4
Indication
MeSH
Ontology
ICD-10
Ph 1
Ph 2
Ph 3
Ph 4
Other
Total
InfarctionD007238EFO_0009463——233—8
Myocardial infarctionD009203EFO_0000612I21—133—7
Peripheral arterial diseaseD058729EFO_0004265———14—5
Peripheral vascular diseasesD016491EFO_0003875I73.9——13—4
Coronary artery diseaseD003324—I25.1———1—1
Vascular diseasesD014652EFO_0004264I77———1—1
Intermittent claudicationD007383EFO_0003876I73.9———1—1
Diabetes mellitusD003920EFO_0000400E08-E13———1—1
EndotoxemiaD019446—————1—1
Healthy volunteers/patients——————1—1
Indications Phases 3
Indication
MeSH
Ontology
ICD-10
Ph 1
Ph 2
Ph 3
Ph 4
Other
Total
IschemiaD007511EFO_0000556——13——4
AtherosclerosisD050197EFO_0003914I25.1—13——4
Acute coronary syndromeD054058EFO_0005672—111——3
Myocardial ischemiaD017202EFO_1001375I20-I25—11——2
StrokeD020521EFO_0000712I63.9——2——2
Indications Phases 2
Indication
MeSH
Ontology
ICD-10
Ph 1
Ph 2
Ph 3
Ph 4
Other
Total
Cerebral infarctionD002544—I63—1———1
Arteriovenous fistulaD001164—Q27.3—1———1
FistulaD005402———1———1
HivD006678—O98.711———1
Coronary diseaseD003327———1———1
Arterial occlusive diseasesD001157EFO_0009085——1———1
Indications Phases 1
No data
Indications Without Phase
No data
Epidemiology
Epidemiological information for investigational and approved indications
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Drug
General
Drug common nameVorapaxar
INNvorapaxar
Description
Vorapaxar is a carbamate ester that is the ethyl ester of [(1R,3aR,4aR,6R,8aR,9S,9aS)-9-{(E)-2-[5-(3-fluorophenyl)pyridin-2-yl]ethynyl}-1-methyl-3-oxododecahydronaphtho[2,3-c]furan-6-yl]carbamic acid. A protease-activated receptor-1 antagonist used (as its sulfate salt) for the reduction of thrombotic cardiovascular events in patients with a history of myocardial infarction (MI) or with peripheral arterial disease. It has been shown to reduce the rate of a combined endpoint of cardiovascular death, MI, stroke and urgent coronary revascularisation. It has a role as a protease-activated receptor-1 antagonist, a platelet aggregation inhibitor and a cardiovascular drug. It is a member of pyridines, a carbamate ester, an organofluorine compound, a naphthofuran and a lactone. It is a conjugate base of a vorapaxar(1+).
Classification
Small molecule
Drug classProtease-activated receptor 1 (PAR1) antagonists
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Structure (InChI/SMILES or Protein Sequence)
CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2cccc(F)c2)cn1
Identifiers
PDB—
CAS-ID618385-01-6
RxCUI—
ChEMBL IDCHEMBL493982
ChEBI ID82702
PubChem CID10077130
DrugBank—
UNII IDZCE93644N2 (ChemIDplus, GSRS)
Target
Agency Approved
F2R
F2R
Organism
Homo sapiens
Gene name
F2R
Gene synonyms
CF2R, PAR1, TR
NCBI Gene ID
Protein name
proteinase-activated receptor 1
Protein synonyms
Coagulation factor II receptor, protease-activated receptor 1, Thrombin receptor
Uniprot ID
Mouse ortholog
F2r (14062)
proteinase-activated receptor 1 (Q3TVP3)
Alternate
No data
Variants
No data
Financial
No data
Trends
PubMed Central
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Safety
Black-box Warning
Black-box warning for: Zontivity
Adverse Events
Top Adverse Reactions
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189 adverse events reported
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