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

Stem definitionDrug idCAS RN
bronchodilators, phenethylamine derivatives 4183 312753-06-3

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • QAB149
  • QAB-149
  • QAB 149
  • indacaterol
  • Arcapta Neohaler
  • indacaterol maleate
Indacaterol is a long-acting beta2-adrenergic agonist. The pharmacological effects of beta2-adrenoceptor agonist drugs, including indacaterol, are at least in part attributable to stimulation of intracellular adenyl cyclase, the enzyme that catalyzes the conversion of adenosine triphosphate (ATP) to cyclic-3’, 5’-adenosine monophosphate (cyclic monophosphate). Increased cyclic AMP levels cause relaxation of bronchial smooth muscle.
  • Molecular weight: 392.50
  • Formula: C24H28N2O3
  • CLOGP: 2.97
  • LIPINSKI: 0
  • HAC: 5
  • HDO: 4
  • TPSA: 81.59
  • ALOGS: -4.69
  • ROTB: 6

Drug dosage:

DoseUnitRoute
0.15 mg Inhal.powder

ADMET properties:

PropertyValueReference
Vd (Volume of distribution) 19.40 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 4.48 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.05 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 92.50 hours Lombardo F, Berellini G, Obach RS

Approvals:

DateAgencyCompanyOrphan
July 1, 2011 FDA NOVARTIS

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

Pharmacologic Action:

SourceCodeDescription
ATC R03AC18 RESPIRATORY SYSTEM
DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES
ADRENERGICS, INHALANTS
Selective beta-2-adrenoreceptor agonists
ATC R03AK14 RESPIRATORY SYSTEM
DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES
ADRENERGICS, INHALANTS
Adrenergics in combination with corticosteroids or other drugs, excl. anticholinergics
ATC R03AL04 RESPIRATORY SYSTEM
DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES
ADRENERGICS, INHALANTS
Adrenergics in combination with anticholinergics incl. triple combinations with corticosteroids
ATC R03AL12 RESPIRATORY SYSTEM
DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES
ADRENERGICS, INHALANTS
Adrenergics in combination with anticholinergics incl. triple combinations with corticosteroids
FDA MoA N0000009922 Adrenergic beta2-Agonists
FDA EPC N0000175779 beta2-Adrenergic Agonist
CHEBI has role CHEBI:35522 beta-adrenergic agonist
CHEBI has role CHEBI:35523 bronchodilator agent

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Prevention of Bronchospasm with Chronic Bronchitis indication
Prevention of Bronchospasms with Emphysema indication
Bronchospasm Prevention with COPD indication
Hypertensive disorder contraindication 38341003 DOID:10763
Hypokalemia contraindication 43339004
Conduction disorder of the heart contraindication 44808001
Diabetes mellitus contraindication 73211009 DOID:9351
Hyperglycemia contraindication 80394007 DOID:4195
Thyrotoxicosis contraindication 90739004 DOID:7997
Prolonged QT interval contraindication 111975006
Seizure disorder contraindication 128613002
Exacerbation of asthma contraindication 281239006
Chronic myocardial ischemia contraindication 413844008 DOID:3393
Congenital long QT syndrome contraindication 442917000
Acutely Deteriorating Chronic Obstructive Pulmonary Disease contraindication

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 10.25 acidic
pKa2 11.06 acidic
pKa3 13.25 acidic
pKa4 9.04 Basic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
EQ 75MCG BASE ARCAPTA NEOHALER NOVARTIS N022383 July 1, 2011 DISCN POWDER INHALATION 8067437 June 2, 2020 THE LONG TERM, ONCE-DAILY MAINTENANCE BRONCHODILATOR TREATMENT OF AIRFLOW OBSTRUCTION IN PATIENTS WITH CHRONIC OBSTRUCTIVE PULMONARY DISEASE (COPD), INCLUDING CHRONIC BRONCHITIS AND/OR EMPHYSEMA
EQ 75MCG BASE ARCAPTA NEOHALER NOVARTIS N022383 July 1, 2011 DISCN POWDER INHALATION 8658673 June 2, 2020 THE LONG TERM, ONCE-DAILY MAINTENANCE BRONCHODILATOR TREATMENT OF AIRFLOW OBSTRUCTION IN PATIENTS WITH CHRONIC OBSTRUCTIVE PULMONARY DISEASE (COPD), INCLUDING CHRONIC BRONCHITIS AND/OR EMPHYSEMA
27.5MCG/INH UTIBRON NOVARTIS N207930 Oct. 29, 2015 DISCN POWDER INHALATION 7820694 June 2, 2020 LONG - TERM MAINTENANCE TREATMENT OF AIRFLOW OBSTRUCTION IN PATIENTS WITH CHRONIC OBSTRUCTIVE PULMONARY DISEASE (COPD)
27.5MCG/INH UTIBRON NOVARTIS N207930 Oct. 29, 2015 DISCN POWDER INHALATION 8067437 June 2, 2020 LONG - TERM MAINTENANCE TREATMENT OF AIRFLOW OBSTRUCTION IN PATIENTS WITH CHRONIC OBSTRUCTIVE PULMONARY DISEASE (COPD)
27.5MCG/INH UTIBRON NOVARTIS N207930 Oct. 29, 2015 DISCN POWDER INHALATION 8283362 June 2, 2020 LONG - TERM MAINTENANCE TREATMENT OF AIRFLOW OBSTRUCTION IN PATIENTS WITH CHRONIC OBSTRUCTIVE PULMONARY DISEASE (COPD)
27.5MCG/INH UTIBRON NOVARTIS N207930 Oct. 29, 2015 DISCN POWDER INHALATION 8658673 June 2, 2020 LONG - TERM MAINTENANCE TREATMENT OF AIRFLOW OBSTRUCTION IN PATIENTS WITH CHRONIC OBSTRUCTIVE PULMONARY DISEASE (COPD)
27.5MCG/INH UTIBRON NOVARTIS N207930 Oct. 29, 2015 DISCN POWDER INHALATION 7229607 April 9, 2021 LONG - TERM MAINTENANCE TREATMENT OF AIRFLOW OBSTRUCTION IN PATIENTS WITH CHRONIC OBSTRUCTIVE PULMONARY DISEASE (COPD)
27.5MCG/INH UTIBRON NOVARTIS N207930 Oct. 29, 2015 DISCN POWDER INHALATION 8029768 April 9, 2021 LONG - TERM MAINTENANCE TREATMENT OF AIRFLOW OBSTRUCTION IN PATIENTS WITH CHRONIC OBSTRUCTIVE PULMONARY DISEASE (COPD)
EQ 75MCG BASE ARCAPTA NEOHALER NOVARTIS N022383 July 1, 2011 DISCN POWDER INHALATION 6878721 Feb. 25, 2025 THE LONG TERM, ONCE-DAILY MAINTENANCE BRONCHODILATOR TREATMENT OF AIRFLOW OBSTRUCTION IN PATIENTS WITH CHRONIC OBSTRUCTIVE PULMONARY DISEASE (COPD), INCLUDING CHRONIC BRONCHITIS AND/OR EMPHYSEMA
27.5MCG/INH UTIBRON NOVARTIS N207930 Oct. 29, 2015 DISCN POWDER INHALATION 6878721 Feb. 25, 2025 LONG - TERM MAINTENANCE TREATMENT OF AIRFLOW OBSTRUCTION IN PATIENTS WITH CHRONIC OBSTRUCTIVE PULMONARY DISEASE (COPD)

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Beta-2 adrenergic receptor GPCR AGONIST Ki 7.80 CHEMBL CHEMBL
Beta-1 adrenergic receptor GPCR Ki 7.04 CHEMBL
D(2) dopamine receptor GPCR IC50 4.60 CHEMBL
D(3) dopamine receptor GPCR Ki 5.98 CHEMBL
Beta-2 adrenergic receptor GPCR IC50 8.10 CHEMBL

External reference:

IDSource
4030903 VUID
N0000182968 NUI
C1722260 UMLSCUI
D09318 KEGG_DRUG
2JEC1ITX7R UNII
753498-25-8 SECONDARY_CAS_RN
703740005 SNOMEDCT_US
013439 NDDF
1114326 RXNORM
27231 MMSL
d07651 MMSL
4030903 VANDF
702801003 SNOMEDCT_US
8457 INN_ID
CHEMBL1095777 ChEMBL_ID
DB05039 DRUGBANK_ID
CHEBI:68575 CHEBI
CHEMBL1789842 ChEMBL_ID
6918554 PUBCHEM_CID
7455 IUPHAR_LIGAND_ID
C510790 MESH_SUPPLEMENTAL_RECORD_UI

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
ARCAPTA NEOHALER HUMAN PRESCRIPTION DRUG LABEL 1 63402-675 CAPSULE 75 ug ORAL NDA 19 sections
UTIBRON NEOHALER HUMAN PRESCRIPTION DRUG LABEL 2 63402-681 CAPSULE 27.50 ug RESPIRATORY (INHALATION) NDA 19 sections