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]
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Affected Organisms

Humans

ATC Code

R03BB08: Revefenacin

R03BB: Anticholinergics

R03B: OTHER DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES, INHALANTS

R03: DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES

R: RESPIRATORY SYSTEM

Structure

3D MOL

2D MOL

#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
UNII: G2AE2VE07O
DrugBank ID: DB11855
TTD ID: D0K1ST
INTEDE ID: DR1412
ACDINA ID: D01385

Combinatorial Drugs (CBD)

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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]

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Drug-Metabolizing Enzyme (DME)

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

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Molecular Interaction Atlas (MIA)

MIA Detail

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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]
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⏷ Show the Full List of 6 DDI Information of This Drug

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
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Pharmaceutical Formulation

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

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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]