revefenacin Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
5303 864750-70-9

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • revefenacin
  • yupelri
  • TD-4208
  • GSK 1160724
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.
  • Molecular weight: 597.76
  • Formula: C35H43N5O4
  • CLOGP: 3.21
  • LIPINSKI: 1
  • HAC: 9
  • HDO: 2
  • TPSA: 108.21
  • ALOGS: -4.92
  • ROTB: 11

  • Status: ONP

  • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

None

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
Nov. 9, 2018 FDA MYLAN IRELAND LTD

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

Pharmacologic Action:

SourceCodeDescription
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

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Chronic obstructive lung disease indication 13645005 DOID:3083

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (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)

None

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
175MCG/3ML YUPELRI MYLAN IRELAND LTD N210598 Nov. 9, 2018 RX SOLUTION INHALATION Nov. 9, 2023 NEW CHEMICAL ENTITY

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA 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:

IDSource
4038020 VANDF
C4519232 UMLSCUI
CHEMBL3833319 ChEMBL_ID
D10978 KEGG_DRUG
DB11855 DRUGBANK_ID
10129 IUPHAR_LIGAND_ID
C583570 MESH_SUPPLEMENTAL_RECORD_UI
10112 INN_ID
G2AE2VE07O UNII
11753673 PUBCHEM_CID
2102775 RXNORM
298858 MMSL
35639 MMSL
d09073 MMSL
017843 NDDF
782975006 SNOMEDCT_US
782999006 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
YUPELRI HUMAN PRESCRIPTION DRUG LABEL 1 49502-806 SOLUTION 175 ug RESPIRATORY (INHALATION) NDA 27 sections