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vorapaxar 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | 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 |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | 4.051 | Moderate | 0.78 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 1.205 | Moderate | 0.78 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 35.400 | 10^-6 cm/s | Moderate | 0.78 |
| dh-clint | Dog hepatocyte intrinsic clearance | 35.075 | uL/min/10^6 cells | Moderate | 0.78 |
| dppb | Dog plasma protein binding (% unbound) | 0.650 | % | Moderate | 0.78 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 2.890 | % | Moderate | 0.78 |
| herg | hERG pIC50 | 5.175 | pIC50 | Moderate | 0.78 |
| hh-clint | Human hepatocyte intrinsic clearance | 6.486 | uL/min/10^6 cells | Moderate | 0.78 |
| hlm-clint | Human liver microsomal intrinsic clearance | 25.468 | uL/min/mg protein | Moderate | 0.78 |
| hppb | Human plasma protein binding (% unbound) | 0.820 | % | Moderate | 0.78 |
| kinase-safety-class | ACVR2B,EIF2AK3,GRK2,ITK,MAPK10,PDK1,PDK2,PDK4,PIK3CG,PRKDC | 10 | |||
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 1.138 | Moderate | 0.78 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 39.446 | Moderate | 0.78 | |
| mppb | Mouse plasma protein binding (% unbound) | 0.780 | Moderate | 0.78 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 3.926 | Moderate | 0.78 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 1.330 | % | Moderate | 0.78 |
| rh-clint | Rat hepatocyte intrinsic clearance | 27.227 | uL/min/10^6 cells | Moderate | 0.78 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 9.680 | % | Moderate | 0.78 |
| rppb | Rat plasma protein binding (% unbound) | 1.290 | % | Moderate | 0.78 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 2.193 | uM | Moderate | 0.78 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| May 8, 2014 | FDA | MERCK SHARP DOHME | |
| Nov. 20, 2014 | EMA | Merck Sharp & Dohme Limited |
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 drug |
| CHEBI has role | CHEBI:50249 | anticoagulant |
| CHEBI has role | CHEBI:50427 | platelet aggregation inhibitor |
| CHEBI has role | CHEBI:64946 | anti-HIV agent |
| CHEBI has role | CHEBI:83313 | protease-activated receptor-1 antagonist |
Related Drugs by ATC class:
B01AC Platelet aggregation inhibitors excl. heparin 24 drugs
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 | KEY THERAP | N204886 | May 8, 2014 | DISCN | 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 |
| ZCE93644N2 | INXIGHT DRUGS |
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 |