aclidinium bromide Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
4484 320345-99-1

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • aclidinium bromide
  • Tudorza Pressair
  • aclidinium
  • LAS 34273
  • LAS W-330
a long-acting, inhaled antimuscarinic; in phase I trial 8/2008
  • Molecular weight: 484.65
  • Formula: C26H30NO4S2
  • CLOGP: 2.34
  • LIPINSKI: 0
  • HAC: 5
  • HDO: 1
  • TPSA: 55.76
  • ALOGS: -5.53
  • ROTB: 10

  • Status: ONP

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

Drug dosage:

DoseUnitRoute
0.64 mg Inhal.powder

ADMET properties:

PropertyValueReference
Vd (Volume of distribution) 4.30 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 48.50 mL/min/kg Lombardo F, Berellini G, Obach RS

Approvals:

DateAgencyCompanyOrphan
July 20, 2012 EMA
July 23, 2012 FDA ASTRAZENECA PHARMS

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
Device malfunction 327.34 42.99 56 281 3251 2354497
Dyspnoea 197.68 42.99 68 269 78665 2279083
Product quality issue 161.34 42.99 38 299 10791 2346957
Product dose omission 159.94 42.99 49 288 38208 2319540
Asthma 103.83 42.99 27 310 11287 2346461
Chronic obstructive pulmonary disease 100.56 42.99 24 313 7053 2350695
Intentional device misuse 86.78 42.99 12 325 153 2357595
Intentional product misuse 83.80 42.99 22 315 9467 2348281
Device failure 82.52 42.99 16 321 1749 2355999
Device issue 68.01 42.99 17 320 5982 2351766
Circumstance or information capable of leading to medication error 64.28 42.99 12 325 1066 2356682
Wheezing 47.67 42.99 13 324 6371 2351377

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
Device malfunction 183.18 55.95 33 225 1991 1744532
Dyspnoea 146.55 55.95 52 206 52007 1694516
Intentional device misuse 99.27 55.95 13 245 82 1746441
Product quality issue 93.64 55.95 23 235 6070 1740453
Product dose omission 91.76 55.95 30 228 22410 1724113
Device issue 67.86 55.95 15 243 2467 1744056
Device failure 59.07 55.95 11 247 762 1745761
Intentional product misuse 56.17 55.95 16 242 7342 1739181

Pharmacologic Action:

SourceCodeDescription
ATC R03AL05 RESPIRATORY SYSTEM
DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES
ADRENERGICS, INHALANTS
Adrenergics in combination with anticholinergics incl. triple combinations with corticosteroids
ATC R03BB05 RESPIRATORY SYSTEM
DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES
OTHER DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES, INHALANTS
Anticholinergics
FDA EPC N0000175574 Anticholinergic
FDA MoA N0000175370 Cholinergic Antagonists
CHEBI has role CHEBI:48876 muscarinic antagonist
CHEBI has role CHEBI:35523 bronchodilator agent

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

Dissociation levelDissociation constantType (acidic/basic)
pKa1 13.97 acidic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
0.4MG/INH TUDORZA PRESSAIR CIRCASSIA N202450 July 23, 2012 RX POWDER, METERED INHALATION 10034867 July 7, 2020 MAINTENANCE TREATMENT OF BRONCHOSPASM ASSOCIATED WITH CHRONIC OBSTRUCTIVE PULMONARY DISEASE (COPD)
0.4MG/INH TUDORZA PRESSAIR CIRCASSIA N202450 July 23, 2012 RX POWDER, METERED INHALATION 10034867 July 7, 2020 MAINTENANCE TREATMENT OF CHRONIC OBSTRUCTIVE PULMONARY DISEASE (COPD)
0.4MG/INH TUDORZA PRESSAIR CIRCASSIA N202450 July 23, 2012 RX POWDER, METERED INHALATION 10588895 July 7, 2020 MAINTENANCE TREATMENT OF CHRONIC PULMONARY DISEASE (COPD)
0.4MG/INH TUDORZA PRESSAIR CIRCASSIA N202450 July 23, 2012 RX POWDER, METERED INHALATION 7078412 July 7, 2020 MAINTENANCE TREATMENT OF CHRONIC OBSTRUCTIVE PULMONARY DISEASE (COPD)
0.4MG/INH TUDORZA PRESSAIR CIRCASSIA N202450 July 23, 2012 RX POWDER, METERED INHALATION 9056100 July 7, 2020 MAINTENANCE TREATMENT OF CHRONIC OBSTRUCTIVE PULMONARY DISEASE (COPD)
0.4MG/INH TUDORZA PRESSAIR CIRCASSIA N202450 July 23, 2012 RX POWDER, METERED INHALATION 9333195 July 7, 2020 MAINTENANCE TREATMENT OF CHRONIC OBSTRUCTIVE PULMONARY DISEASE (COPD)
0.4MG/INH DUAKLIR PRESSAIR CIRCASSIA N210595 March 29, 2019 RX POWDER, METERED INHALATION 10034867 July 7, 2020 MAINTENANCE TREATMENT OF BRONCHOSPASM ASSOCIATED WITH CHRONIC OBSTRUCTIVE PULMONARY DISEASE (COPD)
0.4MG/INH DUAKLIR PRESSAIR CIRCASSIA N210595 March 29, 2019 RX POWDER, METERED INHALATION 10034867 July 7, 2020 MAINTENANCE TREATMENT OF CHRONIC OBSTRUCTIVE PULMONARY DISEASE (COPD)
0.4MG/INH DUAKLIR PRESSAIR CIRCASSIA N210595 March 29, 2019 RX POWDER, METERED INHALATION 7078412 July 7, 2020 MAINTENANCE TREATMENT OF CHRONIC OBSTRUCTIVE PULMONARY DISEASE (COPD)
0.4MG/INH DUAKLIR PRESSAIR CIRCASSIA N210595 March 29, 2019 RX POWDER, METERED INHALATION 7750023 July 7, 2020 MAINTENANCE TREATMENT OF CHRONIC OBSTRUCTIVE PULMONARY DISEASE (COPD)
0.4MG/INH DUAKLIR PRESSAIR CIRCASSIA N210595 March 29, 2019 RX POWDER, METERED INHALATION 8129405 July 7, 2020 MAINTENANCE TREATMENT OF CHRONIC OBSTRUCTIVE PULMONARY DISEASE (COPD)
0.4MG/INH DUAKLIR PRESSAIR CIRCASSIA N210595 March 29, 2019 RX POWDER, METERED INHALATION 9056100 July 7, 2020 MAINTENANCE TREATMENT OF CHRONIC OBSTRUCTIVE PULMONARY DISEASE (COPD)
0.4MG/INH DUAKLIR PRESSAIR CIRCASSIA N210595 March 29, 2019 RX POWDER, METERED INHALATION 9333195 July 7, 2020 MAINTENANCE TREATMENT OF CHRONIC OBSTRUCTIVE PULMONARY DISEASE (COPD)
0.4MG/INH DUAKLIR PRESSAIR CIRCASSIA N210595 March 29, 2019 RX POWDER, METERED INHALATION 10588895 Jan. 14, 2022 MAINTENANCE TREATMENT OF CHRONIC PULMONARY DISEASE (COPD)
0.4MG/INH TUDORZA PRESSAIR CIRCASSIA N202450 July 23, 2012 RX POWDER, METERED INHALATION RE46417 Feb. 10, 2025 MAINTENANCE TREATMENT OF CHRONIC OBSTRUCTIVE PULMONARY DISEASE (COPD)
0.4MG/INH DUAKLIR PRESSAIR CIRCASSIA N210595 March 29, 2019 RX POWDER, METERED INHALATION RE46417 Feb. 10, 2025 MAINTENANCE TREATMENT OF CHRONIC OBSTRUCTIVE PULMONARY DISEASE (COPD)
0.4MG/INH TUDORZA PRESSAIR CIRCASSIA N202450 July 23, 2012 RX POWDER, METERED INHALATION 10085974 March 13, 2029 MAINTENANCE TREATMENT OF CHRONIC OBSTRUCTIVE PULMONARY DISEASE (COPD)
0.4MG/INH DUAKLIR PRESSAIR CIRCASSIA N210595 March 29, 2019 RX POWDER, METERED INHALATION 10085974 March 13, 2029 MAINTENANCE TREATMENT OF CHRONIC OBSTRUCTIVE PULMONARY DISEASE (COPD)

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
0.4MG/INH TUDORZA PRESSAIR CIRCASSIA N202450 July 23, 2012 RX POWDER, METERED INHALATION March 29, 2022 INFORMATION ADDED TO THE CLINICAL STUDIES SECTION TO FULFILL A POST-MARKETING REQUIREMENT
0.4MG/INH DUAKLIR PRESSAIR CIRCASSIA N210595 March 29, 2019 RX POWDER, METERED INHALATION March 29, 2022 NEW COMBINATION

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Muscarinic acetylcholine receptor M3 GPCR ANTAGONIST Ki 10.15 CHEMBL CHEMBL
Muscarinic acetylcholine receptor M2 GPCR Ki 10.10 CHEMBL
Muscarinic acetylcholine receptor M1 GPCR Ki 10.10 CHEMBL
Muscarinic acetylcholine receptor M4 GPCR IC50 9.70 CHEMBL
Muscarinic acetylcholine receptor M5 GPCR IC50 9.80 CHEMBL

External reference:

IDSource
D08837 KEGG_DRUG
4031720 VUID
N0000185730 NUI
C2699758 UMLSCUI
CHEMBL551466 ChEMBL_ID
CHEMBL1194325 ChEMBL_ID
UQW7UF9N91 UNII
8544 INN_ID
DB08897 DRUGBANK_ID
CHEBI:65344 CHEBI
7449 IUPHAR_LIGAND_ID
C542859 MESH_SUPPLEMENTAL_RECORD_UI
11519741 PUBCHEM_CID
1303097 RXNORM
014614 NDDF
28687 MMSL
4031720 VANDF
703922001 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Tudorza Pressair HUMAN PRESCRIPTION DRUG LABEL 1 0310-0800 POWDER, METERED 400 ug RESPIRATORY (INHALATION) NDA 18 sections
DUAKLIR PRESSAIR HUMAN PRESCRIPTION DRUG LABEL 2 72124-001 POWDER, METERED 400 ug RESPIRATORY (INHALATION) NDA 17 sections
Tudorza Pressair HUMAN PRESCRIPTION DRUG LABEL 1 72124-002 POWDER, METERED 400 ug RESPIRATORY (INHALATION) NDA 18 sections