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grazoprevir 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| Hepatitis Virus C (HVC) protease inhibitors | 5081 | 1350514-68-9 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
has antiviral activity
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 0.10 | g | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 4 | Bocci G, Oprea TI, Benet LZ |
| BA (Bioavailability) | 0.16 % | Kawashima H, Watanabe R, Esaki T, Kuroda M, Nagao C, Natsume-Kitatani Y, Ohashi R, Komura H, Mizuguchi K |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| kinase-safety-class | EIF2AK3,GRK2,PDK1,PDK2,PDK4 | 5 | |||
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Jan. 28, 2016 | FDA | MERCK SHARP DOHME |
FDA Adverse Event Reporting System (Female)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Pancreas transplant rejection | 81.90 | 55.13 | 7 | 8 | 164 | 90628268 |
FDA Adverse Event Reporting System (Male)
None
FDA Adverse Event Reporting System (Geriatric)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Pancreas transplant rejection | 75.64 | 70.56 | 7 | 12 | 369 | 110588911 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | J05AP11 | ANTIINFECTIVES FOR SYSTEMIC USE ANTIVIRALS FOR SYSTEMIC USE DIRECT ACTING ANTIVIRALS Antivirals for treatment of HCV infections |
| ATC | J05AP54 | ANTIINFECTIVES FOR SYSTEMIC USE ANTIVIRALS FOR SYSTEMIC USE DIRECT ACTING ANTIVIRALS Antivirals for treatment of HCV infections |
| MeSH PA | D000890 | Anti-Infective Agents |
| MeSH PA | D000998 | Antiviral Agents |
| CHEBI has role | CHEBI:36044 | antiviral drug |
| CHEBI has role | CHEBI:62868 | hepatoprotective agent |
| CHEBI has role | CHEBI:64924 | hepatitis C protease inhibitor |
Related Drugs by ATC class:
J05AP Antivirals for treatment of HCV infections 18 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Chronic hepatitis C | indication | 128302006 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 4.1 | acidic |
| pKa2 | 1.52 | 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 |
|---|---|---|---|---|---|---|---|---|---|---|
| 50MG;100MG | ZEPATIER | MSD SUB MERCK | N208261 | Jan. 28, 2016 | DISCN | TABLET | ORAL | 7973040 | July 24, 2029 | TREATMENT OF PATIENTS INFECTED WITH HEPATITIS C VIRUS |
| 50MG;100MG | ZEPATIER | MSD SUB MERCK | N208261 | Jan. 28, 2016 | DISCN | TABLET | ORAL | 8871759 | May 4, 2031 | TREATMENT OF PATIENTS INFECTED WITH HEPATITIS C VIRUS |
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 |
|---|---|---|---|---|---|---|---|---|---|
| Genome polyprotein | Polyprotein | INHIBITOR | EC50 | 12.30 | DRUG LABEL | DRUG LABEL | |||
| Genome polyprotein | Polyprotein | INHIBITOR | EC50 | 12.40 | DRUG LABEL | DRUG LABEL | |||
| Genome polyprotein | Polyprotein | INHIBITOR | EC50 | 12.52 | DRUG LABEL | DRUG LABEL | |||
| NS3 | Enzyme | Ki | 10.40 | CHEMBL | |||||
| Genome polyprotein | Polyprotein | Ki | 10.40 | CHEMBL | |||||
| Genome polyprotein | Polyprotein | Ki | 9.85 | CHEMBL | |||||
| NS3 protease | Enzyme | IC50 | 10.15 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| 4O2AB118LA | UNII |
| D10639 | KEGG_DRUG |
| 4035374 | VANDF |
| C4080053 | UMLSCUI |
| CHEBI:132975 | CHEBI |
| CHEMBL3039533 | ChEMBL_ID |
| 44603531 | PUBCHEM_CID |
| DB11575 | DRUGBANK_ID |
| CHEMBL2063090 | ChEMBL_ID |
| C578009 | MESH_SUPPLEMENTAL_RECORD_UI |
| 11573 | IUPHAR_LIGAND_ID |
| 1734630 | RXNORM |
| 31483 | MMSL |
| d08417 | MMSL |
| 016674 | NDDF |
| 716041004 | SNOMEDCT_US |
| 816104003 | SNOMEDCT_US |
| SUE | PDB_CHEM_ID |
| 1350462-55-3 | SECONDARY_CAS_RN |
Pharmaceutical products:
None