Details of the Drug

General Information of Drug (ID: DMMP5SI)

• Drug Name: Revefenacin
• Synonyms: UNII-G2AE2VE07O; G2AE2VE07O; Revefenacin [INN]; Revefenacin [WHO-DD]; Revefenacin [USAN:INN]; Revefenacin (USAN/INN); SCHEMBL356480; EX-A1722; DB11855; GSK1160724; CS-7743; GSK-1160724; HY-15851; D10978; 1211931-83-7

Indication

Disease Entry	ICD 11	Status	REF
Chronic obstructive pulmonary disease	CA22	Approved	[1]

• #Ro5 Violations (Lipinski): 2:
  Molecular Weight (mw); 597.7
  Logarithm of the Partition Coefficient (xlogp); 4.1
  Rotatable Bond Count (rotbonds); 11
  Hydrogen Bond Donor Count (hbonddonor); 2
  Hydrogen Bond Acceptor Count (hbondacc); 6
• ADMET Property:
  Absorption AUC: The area under the plot of plasma concentration (AUC) of drug is 0.03-0.36 mcgh/L [2]
  Absorption Cmax: The maximum plasma concentration (Cmax) of drug is 0.02-0.15 mcg/L [2]
  Absorption Tmax: The time to maximum plasma concentration (Tmax) is 0.48-0.51 h [2]
  Elimination: 27% of drug is excreted in urine, and 54% is excreted in feces [2]
  Half-life: The concentration or amount of drug in body reduced by one-half in 22.3 - 70 hours [2]
  Metabolism: The drug is metabolized via the lung [2]
  Vd: The volume of distribution (Vd) of drug is 218 L []
• Chemical Identifiers:
  Formula: C35H43N5O4
  IUPAC Name: [1-[2-[[4-[(4-carbamoylpiperidin-1-yl)methyl]benzoyl]-methylamino]ethyl]piperidin-4-yl] N-(2-phenylphenyl)carbamate
  Canonical SMILES: CN(CCN1CCC(CC1)OC(=O)NC2=CC=CC=C2C3=CC=CC=C3)C(=O)C4=CC=C(C=C4)CN5CCC(CC5)C(=O)N
  InChI: InChI=1S/C35H43N5O4/c1-38(34(42)29-13-11-26(12-14-29)25-40-19-15-28(16-20-40)33(36)41)23-24-39-21-17-30(18-22-39)44-35(43)37-32-10-6-5-9-31(32)27-7-3-2-4-8-27/h2-14,28,30H,15-25H2,1H3,(H2,36,41)(H,37,43)
  InChIKey: FYDWDCIFZSGNBU-UHFFFAOYSA-N
• Cross-matching ID:
  PubChem CID: 11753673
  CAS Number: 864750-70-9
  DrugBank ID: DB11855
  TTD ID: D0K1ST
  INTEDE ID: DR1412
  ACDINA ID: D01385

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Muscarinic acetylcholine receptor (CHRM)	TTOXS3C	NOUNIPROTAC	Antagonist	[1]

Drug-Metabolizing Enzyme (DME)

DME Name	DME ID	UniProt ID	MOA	REF
Cytochrome P450 2D6 (CYP2D6) Main DME	DECB0K3	CP2D6_HUMAN	Substrate	[3]

Drug-Drug Interaction (DDI) Information of This Drug

Coadministration of a Drug Treating the Disease Different from Revefenacin (Comorbidity)

DDI Drug Name	DDI Drug ID	Severity	Mechanism	Comorbidity	REF
Arn-509	DMT81LZ	Moderate	Accelerated clearance of Revefenacin due to the transporter induction by Arn-509.	Acute myeloid leukaemia [2A60]	[4]
Ag-221	DMS0ZBI	Moderate	Decreased clearance of Revefenacin due to the transporter inhibition by Ag-221.	BCR-ABL1-negative chronic myeloid leukaemia [2A41]	[5]
MK-8228	DMOB58Q	Moderate	Decreased clearance of Revefenacin due to the transporter inhibition by MK-8228.	Cytomegaloviral disease [1D82]	[6]
Bempedoic acid	DM1CI9R	Moderate	Decreased clearance of Revefenacin due to the transporter inhibition by Bempedoic acid.	Hyper-lipoproteinaemia [5C80]	[6]
Belladonna	DM2RBWK	Moderate	Additive anticholinergic effects by the combination of Revefenacin and Belladonna.	Infectious gastroenteritis/colitis [1A40]	[7]
Darolutamide	DMV7YFT	Moderate	Decreased clearance of Revefenacin due to the transporter inhibition by Darolutamide.	Prostate cancer [2C82]	[6]

Drug Inactive Ingredient(s) (DIG) and Formulation(s) of This Drug

DIG

DIG Name	DIG ID	PubChem CID	Functional Classification
Kyselina citronova	E00014	311	Acidulant; Antioxidant; Buffering agent; Complexing agent; Flavoring agent
Sodium citrate anhydrous	E00102	6224	Alkalizing agent; Buffering agent; Complexing agent; Emulsifying agent
Sodium chloride	E00077	5234	Diluent; Tonicity agent
Water	E00035	962	Solvent

Pharmaceutical Formulation

Formulation Name	Drug Dosage	Dosage Form	Route
Revefenacin 175 mcg/3 ml solution	175 mcg/3 ml	Solution	Oral

Jump to Detail Pharmaceutical Formulation Page of This Drug

References

• [1] 2018 FDA drug approvals.Nat Rev Drug Discov. 2019 Feb;18(2):85-89.
• [2] A 28-day, randomized, double-blind, placebo-controlled, parallel group study of nebulized revefenacin in patients with chronic obstructive pulmonary disease. Respir Res. 2017 Nov 2;18(1):182. doi: 10.1186/s12931-017-0647-1.
• [3] A 28-day, randomized, double-blind, placebo-controlled, parallel group study of nebulized revefenacin in patients with chronic obstructive pulmonary disease. Respir Res. 2017 Nov 2;18(1):182.
• [4] Cerner Multum, Inc. "UK Summary of Product Characteristics.".
• [5] Cerner Multum, Inc. "Australian Product Information.".
• [6] Product Information. Nexletol (bempedoic acid). Esperion Therapeutics, Ann Arbor, MI.
• [7] Cole JM, Sheehan AH, Jordan JK "Concomitant use of ipratropium and tiotropium in chronic obstructive plmonary disease." Ann Pharmacother 46 (2012): 1717-21. [PMID: 23170031]