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

Stem definitionDrug idCAS RN
muscarinic receptors agonists/antagonists 4816 869113-09-7

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • incruse
  • umeclidinium
  • GSK573719A
  • umeclidinium bromide
a long-acting antimuscarinic agent with 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
  • Molecular weight: 428.60
  • Formula: C29H34NO2
  • CLOGP: 1.60
  • LIPINSKI: 0
  • HAC: 3
  • HDO: 1
  • TPSA: 29.46
  • ALOGS: -7.38
  • ROTB: 8

  • Status: ONP

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

Drug dosage:

DoseUnitRoute
55 mcg Inhal.powder

ADMET properties:

PropertyValueReference
Vd (Volume of distribution) 1.23 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 35.95 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.11 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 19 hours Lombardo F, Berellini G, Obach RS

Approvals:

DateAgencyCompanyOrphan
Dec. 18, 2013 FDA GLAXOSMITHKLINE

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 174.59 73.16 54 146 78679 2279206
Cough 154.98 73.16 41 159 33076 2324809
Asthma 152.13 73.16 33 167 11281 2346604
Obstructive airways disorder 138.17 73.16 22 178 1351 2356534
Wheezing 116.12 73.16 24 176 6360 2351525
Nasal polyps 115.92 73.16 15 185 201 2357684
Respiratory symptom 97.95 73.16 13 187 213 2357672
Chronic obstructive pulmonary disease 96.48 73.16 21 179 7056 2350829
Sputum increased 92.22 73.16 12 188 167 2357718
Osteoporosis 88.26 73.16 18 182 4396 2353489
Chest discomfort 86.31 73.16 22 178 14573 2343312
Salpingo-oophorectomy unilateral 84.97 73.16 9 191 14 2357871
Embolism venous 84.48 73.16 12 188 329 2357556
Sinusitis fungal 80.21 73.16 10 190 96 2357789
Female genital tract fistula 80.21 73.16 12 188 475 2357410
Productive cough 79.17 73.16 17 183 5304 2352581
Emphysema 77.56 73.16 13 187 1072 2356813
Diastolic dysfunction 76.93 73.16 12 188 628 2357257
Sputum discoloured 76.63 73.16 13 187 1153 2356732
Hiatus hernia 75.47 73.16 14 186 2070 2355815

FDA Adverse Event Reporting System (Male)

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
Chronic obstructive pulmonary disease 94.13 52.28 22 185 5931 1740643
Asthma 92.87 52.28 21 186 4883 1741691
Dyspnoea 84.69 52.28 33 174 52026 1694548
Urinary retention 59.67 52.28 15 192 5380 1741194

Pharmacologic Action:

SourceCodeDescription
ATC R03AL03 RESPIRATORY SYSTEM
DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES
ADRENERGICS, INHALANTS
Adrenergics in combination with anticholinergics incl. triple combinations with corticosteroids
ATC R03AL08 RESPIRATORY SYSTEM
DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES
ADRENERGICS, INHALANTS
Adrenergics in combination with anticholinergics incl. triple combinations with corticosteroids
ATC R03BB07 RESPIRATORY SYSTEM
DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES
OTHER DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES, INHALANTS
Anticholinergics
CHEBI has role CHEBI:48876 muscarinic antagonist
FDA EPC N0000175574 Anticholinergic
FDA MoA N0000175370 Cholinergic Antagonists

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

None

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
EQ 0.0625MG BASE/INH TRELEGY ELLIPTA GLAXOSMITHKLINE N209482 Sept. 18, 2017 RX POWDER INHALATION 6537983 Aug. 3, 2021 THE TREATMENT OF AN INFLAMMATORY DISORDER OF THE RESPIRATORY TRACT BY ONCE-PER-DAY ADMINISTRATION OF A PHARMACEUTICAL FORMULATION COMPRISING FLUTICASONE FUROATE AND A LONG-ACTING BETA2 ADRENORECEPTOR AGONIST
EQ 0.0625MG BASE/INH TRELEGY ELLIPTA GLAXOSMITHKLINE N209482 Sept. 18, 2017 RX POWDER INHALATION 6759398 Aug. 3, 2021 THE TREATMENT OF AN INFLAMMATORY DISORDER OF THE RESPIRATORY TRACT BY ONCE-PER-DAY ADMINISTRATION OF A PHARMACEUTICAL FORMULATION COMPRISING FLUTICASONE FUROATE AND A LONG-ACTING BETA2 ADRENORECEPTOR AGONIST
EQ 0.0625MG BASE/INH TRELEGY ELLIPTA GLAXOSMITHKLINE N209482 Sept. 18, 2017 RX POWDER INHALATION 6878698 Aug. 3, 2021 THE TREATMENT OF CHRONIC OBSTRUCTIVE PULMONARY DISEASE BY ONCE-PER-DAY ADMINISTRATION OF A PHARMACEUTICAL FORMULATION COMPRISING FLUTICASONE FUROATE AND A LONG-ACTING BETA2 ADRENORECEPTOR
EQ 0.0625MG BASE/INH TRELEGY ELLIPTA GLAXOSMITHKLINE N209482 Sept. 18, 2017 RX POWDER INHALATION 7101866 Aug. 3, 2021 USE OF FLUTICASONE FUROATE FOR THE TREATMENT OF AN INFLAMMATORY OR ALLERGIC CONDITIONS, INCLUDING CHRONIC OBSTRUCTIVE PULMONARY DISEASE
EQ 0.0625MG BASE/INH ANORO ELLIPTA GLAXOSMITHKLINE N203975 Dec. 18, 2013 RX POWDER INHALATION RE44874 March 23, 2023 INDICATED FOR THE LONG-TERM, ONCE-DAILY, MAINTENANCE TREATMENT OF AIRFLOW OBSTRUCTION IN PATIENTS WITH CHRONIC OBSTRUCTIVE PULMONARY DISEASE (COPD), INCLUDING CHRONIC BRONCHITIS AND/OR EMPHYSEMA.
EQ 0.0625MG BASE/INH TRELEGY ELLIPTA GLAXOSMITHKLINE N209482 Sept. 18, 2017 RX POWDER INHALATION RE44874 March 23, 2023 INDICATED FOR THE LONG-TERM, ONCE-DAILY, MAINTENANCE TREATMENT OF PATIENTS WITH CHRONIC OBSTRUCTIVE PULMONARY DISEASE (COPD), INCLUDING CHRONIC BRONCHITIS AND/OR EMPHYSEMA
EQ 0.0625MG BASE/INH ANORO ELLIPTA GLAXOSMITHKLINE N203975 Dec. 18, 2013 RX POWDER INHALATION 8309572 April 27, 2025 INDICATED FOR THE LONG-TERM, ONCE-DAILY, MAINTENANCE TREATMENT OF AIRFLOW OBSTRUCTION IN PATIENTS WITH CHRONIC OBSTRUCTIVE PULMONARY DISEASE (COPD), INCLUDING CHRONIC BRONCHITIS AND/OR EMPHYSEMA.
EQ 62.5MCG BASE/INH INCRUSE ELLIPTA GLAXO GRP ENGLAND N205382 April 30, 2014 RX POWDER INHALATION 8309572 April 27, 2025 INDICATED FOR THE LONG-TERM, ONCE-DAILY, MAINTENANCE TREATMENT OF AIRFLOW OBSTRUCTION IN PATIENTS WITH CHRONIC OBSTRUCTIVE PULMONARY DISEASE (COPD), INCLUDING CHRONIC BRONCHITIS AND/OR EMPHYSEMA.
EQ 0.0625MG BASE/INH TRELEGY ELLIPTA GLAXOSMITHKLINE N209482 Sept. 18, 2017 RX POWDER INHALATION 8309572 April 27, 2025 METHOD OF INHIBITING THE BINDING OF ACETYLCHOLINE TO AN ACETYLCHOLINE RECEPTOR IN THE RESPIRATORY TRACT OF A HUMAN, COMPRISING CONTACTING THE RECEPTOR WITH AN EFFECTIVE AMOUNT OF UMECLIDINIUM, VIA TOPICAL APPLICATION
EQ 0.0625MG BASE/INH ANORO ELLIPTA GLAXOSMITHKLINE N203975 Dec. 18, 2013 RX POWDER INHALATION 7439393 May 21, 2025 INDICATED FOR THE LONG-TERM, ONCE-DAILY, MAINTENANCE TREATMENT OF AIRFLOW OBSTRUCTION IN PATIENTS WITH CHRONIC OBSTRUCTIVE PULMONARY DISEASE (COPD), INCLUDING CHRONIC BRONCHITIS AND/OR EMPHYSEMA.
EQ 0.0625MG BASE/INH TRELEGY ELLIPTA GLAXOSMITHKLINE N209482 Sept. 18, 2017 RX POWDER INHALATION 7439393 May 21, 2025 INDICATED FOR THE LONG-TERM, ONCE-DAILY, MAINTENANCE TREATMENT OF PATIENTS WITH CHRONIC OBSTRUCTIVE PULMONARY DISEASE (COPD), INCLUDING CHRONIC BRONCHITIS AND/OR EMPHYSEMA
EQ 0.0625MG BASE/INH ANORO ELLIPTA GLAXOSMITHKLINE N203975 Dec. 18, 2013 RX POWDER INHALATION 8183257 July 27, 2025 INDICATED FOR THE LONG-TERM, ONCE-DAILY, MAINTENANCE TREATMENT OF AIRFLOW OBSTRUCTION IN PATIENTS WITH CHRONIC OBSTRUCTIVE PULMONARY DISEASE (COPD), INCLUDING CHRONIC BRONCHITIS AND/OR EMPHYSEMA.
EQ 62.5MCG BASE/INH INCRUSE ELLIPTA GLAXO GRP ENGLAND N205382 April 30, 2014 RX POWDER INHALATION 8183257 July 27, 2025 INDICATED FOR THE LONG-TERM, ONCE-DAILY, MAINTENANCE TREATMENT OF AIRFLOW OBSTRUCTION IN PATIENTS WITH CHRONIC OBSTRUCTIVE PULMONARY DISEASE (COPD), INCLUDING CHRONIC BRONCHITIS AND/OR EMPHYSEMA.
EQ 0.0625MG BASE/INH TRELEGY ELLIPTA GLAXOSMITHKLINE N209482 Sept. 18, 2017 RX POWDER INHALATION 8183257 July 27, 2025 METHOD OF INHIBITING THE BINDING OF ACETYLCHOLINE TO AN ACETYLCHOLINE RECEPTOR IN THE RESPIRATORY TRACT OF A HUMAN, COMPRISING CONTACTING THE RECEPTOR WITH AN EFFECTIVE AMOUNT OF UMECLIDINIUM, VIA INHALATION
EQ 0.0625MG BASE/INH ANORO ELLIPTA GLAXOSMITHKLINE N203975 Dec. 18, 2013 RX POWDER INHALATION 8511304 June 14, 2027 INDICATED FOR THE LONG-TERM, ONCE-DAILY, MAINTENANCE TREATMENT OF AIRFLOW OBSTRUCTION IN PATIENTS WITH CHRONIC OBSTRUCTIVE PULMONARY DISEASE (COPD), INCLUDING CHRONIC BRONCHITIS AND/OR EMPHYSEMA.

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
EQ 0.0625MG BASE/INH TRELEGY ELLIPTA GLAXOSMITHKLINE N209482 Sept. 18, 2017 RX POWDER INHALATION April 24, 2021 REVISED INDICATION FOR FIXED-DOSE COMBINATION OF FLUTICASONE FUROATE, UMECLIDINIUM, AND VILANTEROL TO TREAT AIRFLOW OBSTRUCTION IN CHRONIC OBSTRUCTIVE PULMONARY DISEASE (COPD) AND TO REDUCE COPD EXACERBATIONS IN PTS WITH HISTORY OF EXACERBATIONS
EQ 0.0625MG BASE/INH ANORO ELLIPTA GLAXOSMITHKLINE N203975 Dec. 18, 2013 RX POWDER INHALATION June 9, 2022 ADDITIONAL INFORMATION ADDED TO THE LABELING BASED ON SAFETY AND EFFICACY DATA FROM THE IMPACT TRIAL

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Muscarinic acetylcholine receptor M3 GPCR ANTAGONIST Ki 10.22 SCIENTIFIC LITERATURE SCIENTIFIC LITERATURE
Muscarinic acetylcholine receptor M2 GPCR Ki 9.82 SCIENTIFIC LITERATURE
Muscarinic acetylcholine receptor M1 GPCR Ki 9.80 SCIENTIFIC LITERATURE
Muscarinic acetylcholine receptor M4 GPCR ANTAGONIST Ki 10.30 IUPHAR
Muscarinic acetylcholine receptor M5 GPCR ANTAGONIST Ki 9.90 IUPHAR

External reference:

IDSource
D10180 KEGG_DRUG
C3832899 UMLSCUI
7AN603V4JV UNII
9551 INN_ID
715611006 SNOMEDCT_US
1487514 RXNORM
d08187 MMSL
015344 NDDF
4033108 VANDF
706898002 SNOMEDCT_US
11519070 PUBCHEM_CID
CHEBI:79040 CHEBI
CHEMBL523299 ChEMBL_ID
CHEMBL1187833 ChEMBL_ID
DB09076 DRUGBANK_ID
C573971 MESH_SUPPLEMENTAL_RECORD_UI
7354 IUPHAR_LIGAND_ID

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Anoro Ellipta HUMAN PRESCRIPTION DRUG LABEL 2 0173-0869 POWDER 62.50 ug RESPIRATORY (INHALATION) NDA 18 sections
Incruse Ellipta HUMAN PRESCRIPTION DRUG LABEL 1 0173-0873 AEROSOL, POWDER 62.50 ug ORAL NDA 19 sections
Trelegy Ellipta HUMAN PRESCRIPTION DRUG LABEL 3 0173-0887 POWDER 62.50 ug RESPIRATORY (INHALATION) NDA 18 sections