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revefenacin 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| muscarinic receptors antagonists | 5303 | 864750-70-9 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
Revefenacin is a long-acting muscarinic antagonist, which is often referred to as an anticholinergic. It has similar affinity to the subtypes of muscarinic receptors M1 to M5. In the airways, it exhibits pharmacological effects through inhibition of M3 receptor at the smooth muscle leading to bronchodilation. The competitive and reversible nature of antagonism was shown with human and animal origin receptors and isolated organ preparations. In preclinical in vitro as well as in vivo models, prevention of methacholine- and acetylcholine-induced bronchoconstrictive effects was dose-dependent and lasted longer than 24 hours. The clinical relevance of these findings is unknown. The bronchodilation following inhalation of revefenacin is predominantly a site-specific effect.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
None
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| S (Water solubility) | 0.06 mg/mL | Bocci G, Oprea TI, Benet LZ |
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 1 | Bocci G, Oprea TI, Benet LZ |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| kinase-safety-class | ACVR2B,AXL,BRAF,CAMK2B,CAMK2D,CDK5,CDK9,DDR1,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,ITK,JAK2,MAP3K7,MAPK10,MAPK12,MAPK7,MAPKAPK2,MET,NTRK2,PDK2,PDK4,PIK3CB,PIM2,PRKDC,SIK2,SIK3,STK33,TEK,TTK | 32 | |||
| kinase-selectivity-class | AKT3,AXL,CDK9,SIK2 | 4 | |||
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Nov. 9, 2018 | FDA | MYLAN IRELAND LTD |
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 |
|---|---|---|---|---|---|---|
| Dyspnoea | 58.13 | 38.51 | 39 | 343 | 880916 | 89747149 |
FDA Adverse Event Reporting System (Male)
| 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 |
|---|---|---|---|---|---|---|
| Dyspnoea | 49.83 | 45.85 | 22 | 73 | 442599 | 42178641 |
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 |
|---|---|---|---|---|---|---|
| Dyspnoea | 56.99 | 36.52 | 39 | 344 | 1106833 | 109482083 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | R03BB08 | RESPIRATORY SYSTEM DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES OTHER DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES, INHALANTS Anticholinergics |
| FDA MoA | N0000175370 | Cholinergic Antagonists |
| FDA EPC | N0000175574 | Anticholinergic |
| CHEBI has role | CHEBI:231911 | renoprotective agent |
Related Drugs by ATC class:
R03BB Anticholinergics 6 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Chronic obstructive lung disease | indication | 13645005 | DOID:3083 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 10.95 | acidic |
| pKa2 | 13.41 | acidic |
| pKa3 | 8.02 | Basic |
| pKa4 | 6.97 | 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 |
|---|---|---|---|---|---|---|---|---|---|---|
| 175MCG/3ML | YUPELRI | MYLAN IRELAND LTD | N210598 | Nov. 9, 2018 | RX | SOLUTION | INHALATION | 11008289 | July 14, 2030 | FOR THE MAINTENANCE TREATMENT OF PATIENTS WITH CHRONIC OBSTRUCTIVE PULMONARY DISEASE (COPD) |
| 175MCG/3ML | YUPELRI | MYLAN IRELAND LTD | N210598 | Nov. 9, 2018 | RX | SOLUTION | INHALATION | 11858898 | July 14, 2030 | FOR THE MAINTENANCE TREATMENT OF PATIENTS WITH CHRONIC OBSTRUCTIVE PULMONARY DISEASE (COPD) |
| 175MCG/3ML | YUPELRI | MYLAN IRELAND LTD | N210598 | Nov. 9, 2018 | RX | SOLUTION | INHALATION | 12048692 | Aug. 29, 2039 | FOR THE MAINTENANCE TREATMENT OF PATIENTS WITH CHRONIC OBSTRUCTIVE PULMONARY DISEASE (COPD) |
| 175MCG/3ML | YUPELRI | MYLAN IRELAND LTD | N210598 | Nov. 9, 2018 | RX | SOLUTION | INHALATION | 12285417 | Aug. 29, 2039 | FOR THE MAINTENANCE TREATMENT OF PATIENTS WITH CHRONIC OBSTRUCTIVE PULMONARY DISEASE (COPD) |
| 175MCG/3ML | YUPELRI | MYLAN IRELAND LTD | N210598 | Nov. 9, 2018 | RX | SOLUTION | INHALATION | 11484531 | Oct. 23, 2039 | FOR THE MAINTENANCE TREATMENT OF PATIENTS WITH CHRONIC OBSTRUCTIVE PULMONARY DISEASE (COPD) |
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 |
|---|---|---|---|---|---|---|---|---|---|
| Muscarinic acetylcholine receptor M1 | GPCR | ANTAGONIST | Ki | 9.38 | SCIENTIFIC LITERATURE | DRUG LABEL | |||
| Muscarinic acetylcholine receptor M2 | GPCR | ANTAGONIST | Ki | 9.52 | SCIENTIFIC LITERATURE | DRUG LABEL | |||
| Muscarinic acetylcholine receptor M3 | GPCR | ANTAGONIST | Ki | 9.75 | SCIENTIFIC LITERATURE | DRUG LABEL | |||
| Muscarinic acetylcholine receptor M4 | GPCR | ANTAGONIST | Ki | 9.26 | SCIENTIFIC LITERATURE | DRUG LABEL | |||
| Muscarinic acetylcholine receptor M5 | GPCR | ANTAGONIST | Ki | 8.20 | SCIENTIFIC LITERATURE | DRUG LABEL |
External reference:
| ID | Source |
|---|---|
| G2AE2VE07O | UNII |
| 4038020 | VANDF |
| C4519232 | UMLSCUI |
| CHEBI:755916 | CHEBI |
| CHEMBL3833319 | ChEMBL_ID |
| 11753673 | PUBCHEM_CID |
| DB11855 | DRUGBANK_ID |
| D10978 | KEGG_DRUG |
| 10112 | INN_ID |
| C583570 | MESH_SUPPLEMENTAL_RECORD_UI |
| 10129 | IUPHAR_LIGAND_ID |
| 782975006 | SNOMEDCT_US |
| 782999006 | SNOMEDCT_US |
| 298858 | MMSL |
| 35639 | MMSL |
| d09073 | MMSL |
| 017843 | NDDF |
| 2102775 | RXNORM |
| G2AE2VE07O | INXIGHT DRUGS |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| YUPELRI | HUMAN PRESCRIPTION DRUG LABEL | 1 | 49502-806 | SOLUTION | 175 ug | RESPIRATORY (INHALATION) | NDA | 27 sections |