vorapaxar 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| protease activated receptor type 1 (PAR1) antagonists | 4870 | 618385-01-6 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
Vorapaxar is a reversible antagonist of the protease-activated receptor-1 (PAR-1) expressed on platelets, but its long half-life makes it effectively irreversible. Vorapaxar inhibits thrombin-induced and thrombin receptor agonist peptide (TRAP)-induced platelet aggregation in vitro studies. Vorapaxar does not inhibit platelet aggregation induced by adenosine diphosphate (ADP), collagen or a thromboxane mimetic and does not affect coagulation parameters ex vivo. PAR-1 receptors are also expressed in a wide variety of cell types, including endothelial cells, neurons, and smooth muscle cells, but the pharmacodynamic effects of vorapaxar in these cell types have not been assessed.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 2.08 | mg | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| Vd (Volume of distribution) | 3.74 L/kg | Lombardo F, Berellini G, Obach RS |
| CL (Clearance) | 0.34 mL/min/kg | Lombardo F, Berellini G, Obach RS |
| fu (Fraction unbound in plasma) | 0.01 % | Lombardo F, Berellini G, Obach RS |
| t_half (Half-life) | 149 hours | Lombardo F, Berellini G, Obach RS |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Nov. 20, 2014 | EMA | Merck Sharp & Dohme Limited | |
| May 8, 2014 | FDA | MERCK SHARP DOHME |
FDA Adverse Event Reporting System (Female)
None
FDA Adverse Event Reporting System (Male)
None
FDA Adverse Event Reporting System (Geriatric)
None
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | B01AC26 | BLOOD AND BLOOD FORMING ORGANS ANTITHROMBOTIC AGENTS ANTITHROMBOTIC AGENTS Platelet aggregation inhibitors excl. heparin |
| MeSH PA | D006401 | Hematologic Agents |
| MeSH PA | D010975 | Platelet Aggregation Inhibitors |
| FDA MoA | N0000190995 | Protease-activated Receptor-1 Antagonists |
| FDA EPC | N0000190996 | Protease-activated Receptor-1 Antagonist |
| CHEBI has role | CHEBI:35554 | cardiovascular agent |
| CHEBI has role | CHEBI:50427 | platelet aggregation inhibitors |
| CHEBI has role | CHEBI:83313 | PAR-1 antagonist |
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Cerebrovascular accident | indication | 230690007 | |
| Myocardial Infarction Prevention | indication | ||
| Transient ischemic attack | contraindication | 266257000 | DOID:224 |
| Cerebral hemorrhage | contraindication | 274100004 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 3.9 | Basic |
Orange Book patent data (new drug applications)
| Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Patent number | Patent expiration date | Patent use |
|---|---|---|---|---|---|---|---|---|---|---|
| EQ 2.08MG BASE | ZONTIVITY | XSPIRE PHARMA | N204886 | May 8, 2014 | RX | TABLET | ORAL | 7713999 | May 30, 2024 | REDUCTION OF THROMBOTIC CARDIOVASCULAR EVENTS IN PATIENTS WITH A HISTORY OF MYOCARDIAL INFARCTION (MI) OR WITH PERIPHERAL ARTERIAL DISEASE (PAD) |
| EQ 2.08MG BASE | ZONTIVITY | XSPIRE PHARMA | N204886 | May 8, 2014 | RX | TABLET | ORAL | 7304078 | Dec. 23, 2027 | REDUCTION OF THROMBOTIC CARDIOVASCULAR EVENTS |
Orange Book exclusivity data (new drug applications)
None
Bioactivity Summary:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| Proteinase-activated receptor 1 | GPCR | ANTAGONIST | Ki | 8.09 | SCIENTIFIC LITERATURE | SCIENTIFIC LITERATURE |
External reference:
| ID | Source |
|---|---|
| ZCE93644N2 | UNII |
| D09765 | KEGG_DRUG |
| 4033329 | VUID |
| N0000190755 | NUI |
| 705260-08-8 | SECONDARY_CAS_RN |
| 4033329 | VANDF |
| 4033330 | VANDF |
| C2974521 | UMLSCUI |
| CHEBI:82702 | CHEBI |
| VPX | PDB_CHEM_ID |
| CHEMBL493982 | ChEMBL_ID |
| 10077130 | PUBCHEM_CID |
| DB09030 | DRUGBANK_ID |
| CHEMBL2107386 | ChEMBL_ID |
| 8852 | INN_ID |
| C530299 | MESH_SUPPLEMENTAL_RECORD_UI |
| 4047 | IUPHAR_LIGAND_ID |
| 1537034 | RXNORM |
| 220431 | MMSL |
| 30304 | MMSL |
| d08260 | MMSL |
| 015526 | NDDF |
| 015527 | NDDF |
| 708718003 | SNOMEDCT_US |
| 715596008 | SNOMEDCT_US |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| ZONTIVITY | HUMAN PRESCRIPTION DRUG LABEL | 1 | 66992-208 | TABLET, FILM COATED | 2.08 mg | ORAL | NDA | 30 sections |
| ZONTIVITY | HUMAN PRESCRIPTION DRUG LABEL | 1 | 70347-208 | TABLET, FILM COATED | 2.08 mg | ORAL | NDA | 30 sections |