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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
Zontivity
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
ZONTIVITYXspire PharmaN-204886 RX2014-05-08
1 products, RLD, RS
Labels
FDA
EMA
Brand Name
Status
Last Update
zontivityNew Drug Application2022-09-22
Indications
FDA
EMA
Indication
Ontology
MeSH
ICD-10
coronary disease—D003327—
myocardial infarctionEFO_0000612D009203I21
peripheral arterial diseaseEFO_0004265D058729—
Agency Specific
FDA
EMA
No data
Patent Expiration
Patent
Expires
Flag
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
17 clinical trials
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Indications Phases 4
Indication
MeSH
Ontology
ICD-10
Ph 1
Ph 2
Ph 3
Ph 4
Other
Total
Von willebrand diseasesD014842D68.02—71212
Indications Phases 3
Indication
MeSH
Ontology
ICD-10
Ph 1
Ph 2
Ph 3
Ph 4
Other
Total
Postpartum hemorrhageD006473O72——1——1
Indications Phases 2
No data
Indications Phases 1
No data
Indications Without Phase
Indication
MeSH
Ontology
ICD-10
Ph 1
Ph 2
Ph 3
Ph 4
Other
Total
Type 3 von willebrand diseaseD056729Orphanet_166096D68.03————11
CarcinomaD002277C80.0————11
Coagulation protein disordersD020147————11
Febrile seizuresD003294HP_0002373R56.0————11
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
Image (chem structure or protein)
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
PDB3VW7
CAS-ID618385-01-6
RxCUI1537034
ChEMBL IDCHEMBL493982
ChEBI ID82702
PubChem CID10077130
DrugBankDB09030
UNII IDZCE93644N2 (ChemIDplus, GSRS)
Target
Agency Approved
F2R
F2R
Organism
Homo sapiens
Gene name
F2R
Gene synonyms
CF2R, PAR1, TR
NCBI Gene ID
2149
Protein name
proteinase-activated receptor 1
Protein synonyms
Coagulation factor II receptor, protease-activated receptor 1, Thrombin receptor
Uniprot ID
P25116
Mouse ortholog
F2r (14062)
proteinase-activated receptor 1 (Q3TVP3)
Alternate
No data
Variants
Clinical Variant
No data
Financial
No data
Trends
PubMed Central
Top Terms for Disease or Syndrome:
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Additional graphs summarizing 947 documents
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Safety
Black-box Warning
Black-box warning for: Zontivity
Adverse Events
Top Adverse Reactions
Mock data
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56 adverse events reported
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