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

Stem definitionDrug idCAS RN
muscarinic receptors antagonists 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:

PropertyValueReference
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

Approvals:

DateAgencyCompanyOrphan
Nov. 9, 2018 FDA MYLAN IRELAND LTD

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Dyspnoea 46.50 36.21 25 133 661288 62827576

FDA Adverse Event Reporting System (Male)

None

FDA Adverse Event Reporting System (Geriatric)

None

FDA Adverse Event Reporting System (Pediatric)

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 | Suggest Off label Use Form| |View source of the data|

DiseaseRelationSNOMED_IDDOID
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 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)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
175MCG/3ML YUPELRI MYLAN IRELAND LTD N210598 Nov. 9, 2018 RX SOLUTION INHALATION 10106503 March 10, 2025 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 10343995 March 10, 2025 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 7491736 March 10, 2025 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 7521041 March 10, 2025 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 7585879 March 10, 2025 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 8053448 March 10, 2025 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 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 11484531 Oct. 23, 2039 FOR THE MAINTENANCE TREATMENT OF PATIENTS WITH CHRONIC OBSTRUCTIVE PULMONARY DISEASE (COPD)

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

Pharmaceutical products:

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