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Enablex, Emselex(darifenacin)
Emselex, Enablex (darifenacin) is a small molecule pharmaceutical. Darifenacin was first approved as Emselex on 2004-10-22. It is used to treat overactive urinary bladder and urge urinary incontinence in the USA. It has been approved in Europe to treat overactive urinary bladder and urge urinary incontinence. The pharmaceutical is active against muscarinic acetylcholine receptor M3. In addition, it is known to target muscarinic acetylcholine receptor M1, muscarinic acetylcholine receptor M2, muscarinic acetylcholine receptor M5, and muscarinic acetylcholine receptor M4.
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Commercial
Therapeutic Areas
Therapeutic Area
MeSH
urogenital diseasesD000091642
signs and symptoms pathological conditionsD013568
Trade Name
FDA
EMA
No data
Drug Products
FDA
EMA
New Drug Application (NDA)
New Drug Application (NDA)
Abbreviated New Drug Application (ANDA)
Abbreviated New Drug Application (ANDA)
Darifenacin hydrobromide
Tradename
Company
Number
Date
Products
ENABLEXAbbVieN-021513 DISCN2004-12-22
2 products, RLD
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Labels
FDA
EMA
Brand Name
Status
Last Update
darifenacinANDA2023-01-25
enablexNew Drug Application2010-01-01
Indications
FDA
EMA
Indication
Ontology
MeSH
ICD-10
overactive urinary bladderEFO_1000781D053201N32.81
urge urinary incontinenceEFO_0006865D053202N39.41
Agency Specific
FDA
EMA
No data
Patent Expiration
No data
ATC Codes
G: Genito urinary system and sex hormones
— G04: Urologicals
— G04B: Urologicals
— G04BD: Drugs for urinary frequency and incontinence
— G04BD10: Darifenacin
HCPCS
No data
Clinical
Indications Phases 4
No data
Indications Phases 3
No data
Indications Phases 2
No data
Indications Phases 1
No data
Indications Without Phase
No data
Epidemiology
Epidemiological information for investigational and approved indications
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Drug
General
Drug common nameDARIFENACIN
INNdarifenacin
Description
Darifenacin is 2-[(3S)-1-Ethylpyrrolidin-3-yl]-2,2-diphenylacetamide in which one of the hydrogens at the 2-position of the ethyl group is substituted by a 2,3-dihydro-1-benzofuran-5-yl group. It is a selective antagonist for the M3 muscarinic acetylcholine receptor, which is primarily responsible for bladder muscle contractions, and is used as the hydrobromide salt in the management of urinary incontinence. It has a role as a muscarinic antagonist and an antispasmodic drug. It is a member of 1-benzofurans, a member of pyrrolidines and a monocarboxylic acid amide.
Classification
Small molecule
Drug classmuscarinic receptor antagonists
Image (chem structure or protein)
Structure (InChI/SMILES or Protein Sequence)
NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(CCc2ccc3c(c2)CCO3)C1
Identifiers
PDB—
CAS-ID133099-04-4
RxCUI136198
ChEMBL IDCHEMBL1346
ChEBI ID391960
PubChem CID444031
DrugBankDB00496
UNII IDAPG9819VLM (ChemIDplus, GSRS)
Target
Agency Approved
CHRM3
CHRM3
Organism
Homo sapiens
Gene name
CHRM3
Gene synonyms
NCBI Gene ID
1131
Protein name
muscarinic acetylcholine receptor M3
Protein synonyms
acetylcholine receptor, muscarinic 3, m3 muscarinic receptor
Uniprot ID
Q9HB60
Mouse ortholog
Chrm3 (12671)
muscarinic acetylcholine receptor M3 (Q9ERZ3)
Alternate
CHRM1
CHRM1
CHRM2
CHRM2
CHRM5
CHRM5
CHRM4
CHRM4
Organism
Homo sapiens
Gene name
CHRM1
Gene synonyms
NCBI Gene ID
1128
Protein name
muscarinic acetylcholine receptor M1
Protein synonyms
acetylcholine receptor, muscarinic 1
Uniprot ID
Q96RH1
Mouse ortholog
Chrm1 (12669)
muscarinic acetylcholine receptor M1 (Q8BJN3)
Variants
Clinical Variant
No data
Financial
No data
Trends
PubMed Central
Top Terms for Disease or Syndrome:
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Additional graphs summarizing 799 documents
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Safety
Black-box Warning
No Black-box warning
Adverse Events
Top Adverse Reactions
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1 adverse events reported
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