indacaterol 🐶 Veterinary Use | 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
  • Status: OFM
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

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
BA (Bioavailability) 0.46 % Kawashima H, Watanabe R, Esaki T, Kuroda M, Nagao C, Natsume-Kitatani Y, Ohashi R, Komura H, Mizuguchi K
BA (Bioavailability) 0.43 % Kawashima H, Watanabe R, Esaki T, Kuroda M, Nagao C, Natsume-Kitatani Y, Ohashi R, Komura H, Mizuguchi K

Approvals:

DateAgencyCompanyOrphan
July 1, 2011 FDA NOVARTIS
June 29, 2020 PMDA Novartis Pharma K.K.
Nov. 29, 2009 EMA Novartis Europharm Limited

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
Bacterial disease carrier 216.62 28.26 42 4230 1289 63483461
Superinfection 188.47 28.26 42 4230 2565 63482185
Bronchial secretion retention 185.89 28.26 42 4230 2731 63482019
Bronchospasm 158.62 28.26 55 4217 17225 63467525
Hyper IgE syndrome 153.16 28.26 27 4245 483 63484267
Sleep disorder due to a general medical condition 152.51 28.26 49 4223 12139 63472611
Restrictive pulmonary disease 130.17 28.26 29 4243 1766 63482984
Scoliosis 120.73 28.26 37 4235 7851 63476899
Asthma 119.16 28.26 85 4187 127476 63357274
Eosinophilia 112.28 28.26 46 4226 22710 63462040
Sinus operation 104.43 28.26 26 4246 2560 63482190
Polycystic ovaries 103.88 28.26 29 4243 4442 63480308
Dyspnoea 102.87 28.26 169 4103 661144 62823606
Atelectasis 101.15 28.26 42 4230 21441 63463309
Wheezing 99.24 28.26 68 4204 95527 63389223
Nonspecific reaction 92.33 28.26 23 4249 2269 63482481
Dyslipidaemia 89.49 28.26 29 4243 7364 63477386
Aggression 84.56 28.26 38 4234 23460 63461290
Rib fracture 82.77 28.26 37 4235 22560 63462190
Obstructive airways disorder 76.15 28.26 34 4238 20665 63464085
Chronic obstructive pulmonary disease 70.74 28.26 47 4225 62639 63422111
Treatment noncompliance 70.63 28.26 39 4233 37286 63447464
Blood test abnormal 68.34 28.26 29 4243 15600 63469150
Abscess 66.54 28.26 29 4243 16639 63468111
Restless legs syndrome 63.59 28.26 29 4243 18502 63466248
Illness 63.25 28.26 40 4232 49019 63435731
Impaired quality of life 61.67 28.26 26 4246 13757 63470993
Brain injury 55.37 28.26 20 4252 7023 63477727
Heart rate increased 53.68 28.26 47 4225 94191 63390559
Coronary artery disease 53.59 28.26 31 4241 32346 63452404
Therapeutic product effect incomplete 53.19 28.26 53 4219 125003 63359747
Sleep apnoea syndrome 51.18 28.26 29 4243 29104 63455646
Loss of personal independence in daily activities 50.42 28.26 46 4226 97244 63387506
Skin lesion 49.75 28.26 29 4243 30692 63454058
Disability 48.51 28.26 24 4248 18323 63466427
Eczema 48.41 28.26 29 4243 32262 63452488
Lung neoplasm malignant 46.97 28.26 24 4248 19609 63465141
Atrial fibrillation 46.96 28.26 48 4224 116588 63368162
Palpitations 46.48 28.26 47 4225 112723 63372027
Paranoia 45.56 28.26 20 4252 11659 63473091
Respiratory failure 44.83 28.26 44 4228 101814 63382936
Pneumonia 40.05 28.26 92 4180 456675 63028075
Myalgia 39.61 28.26 49 4223 146480 63338270
Type 2 diabetes mellitus 38.66 28.26 33 4239 63835 63420915
Cough 34.98 28.26 67 4205 292676 63192074
Blood pressure increased 34.20 28.26 48 4224 162014 63322736
Gastrooesophageal reflux disease 32.52 28.26 36 4236 95603 63389147
Sinus disorder 31.57 28.26 20 4252 24533 63460217
Myocardial infarction 31.24 28.26 36 4236 99857 63384893
Second primary malignancy 29.03 28.26 13 4259 7940 63476810
Depression 28.56 28.26 49 4223 196443 63288307

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
Dyspnoea 66.17 21.78 116 2868 376666 34577281
Rheumatoid nodule 50.74 21.78 16 2968 2931 34951016
Mesenteric vein thrombosis 34.48 21.78 9 2975 840 34953107
Cardiac failure 31.78 21.78 39 2945 91209 34862738
Scleroderma renal crisis 27.60 21.78 6 2978 255 34953692
Concomitant disease aggravated 26.97 21.78 12 2972 5689 34948258
Rhinovirus infection 26.79 21.78 11 2973 4288 34949659
Intestinal ischaemia 26.33 21.78 13 2971 7781 34946166
Productive cough 25.46 21.78 23 2961 37790 34916157
Pneumonia 24.48 21.78 77 2907 362550 34591397

FDA Adverse Event Reporting System (Geriatric)

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
Bacterial disease carrier 199.73 21.50 42 6858 1504 79735984
Bronchial secretion retention 158.95 21.50 42 6858 4062 79733426
Superinfection 151.55 21.50 42 6858 4860 79732628
Hyper IgE syndrome 143.30 21.50 27 6873 544 79736944
Bronchospasm 135.46 21.50 58 6842 24801 79712687
Sleep disorder due to a general medical condition 132.74 21.50 49 6851 14228 79723260
Dyspnoea 124.11 21.50 245 6655 856780 78880708
Asthma 122.61 21.50 98 6802 134997 79602491
Scoliosis 113.52 21.50 37 6863 7427 79730061
Restrictive pulmonary disease 112.25 21.50 29 6871 2566 79734922
Wheezing 102.35 21.50 83 6817 116581 79620907
Polycystic ovaries 101.46 21.50 29 6871 3750 79733738
Sinus operation 98.53 21.50 26 6874 2499 79734989
Nonspecific reaction 84.29 21.50 23 6877 2509 79734979
Obstructive airways disorder 84.09 21.50 45 6855 31414 79706074
Rib fracture 83.30 21.50 43 6857 27904 79709584
Eosinophilia 76.27 21.50 48 6852 45297 79692191
Atelectasis 74.78 21.50 42 6858 32215 79705273
Chronic obstructive pulmonary disease 73.24 21.50 60 6840 85359 79652129
Dyslipidaemia 69.53 21.50 29 6871 11604 79725884
Eczema 58.29 21.50 39 6861 40779 79696709
Blood test abnormal 57.86 21.50 29 6871 17681 79719807
Pneumonia 56.53 21.50 154 6746 660092 79077396
Illness 55.98 21.50 40 6860 46471 79691017
Atrial fibrillation 54.64 21.50 76 6824 197810 79539678
Restless legs syndrome 54.41 21.50 29 6871 20063 79717425
Impaired quality of life 54.31 21.50 26 6874 14360 79723128
Abscess 50.80 21.50 29 6871 22922 79714566
Lung neoplasm malignant 50.72 21.50 31 6869 27761 79709727
Aggression 50.51 21.50 39 6861 50919 79686569
Treatment noncompliance 49.63 21.50 39 6861 52229 79685259
Palpitations 46.47 21.50 56 6844 126554 79610934
Disability 44.36 21.50 24 6876 17096 79720392
Type 2 diabetes mellitus 42.50 21.50 37 6863 57085 79680403
Loss of personal independence in daily activities 42.01 21.50 48 6852 102532 79634956
Heart rate increased 40.43 21.50 51 6849 120673 79616815
Cough 39.00 21.50 93 6807 366696 79370792
Sleep apnoea syndrome 38.52 21.50 29 6871 36449 79701039
Therapeutic product effect incomplete 38.46 21.50 54 6846 141591 79595897
Brain injury 38.03 21.50 19 6881 11498 79725990
Blood pressure increased 37.16 21.50 66 6834 211294 79526194
Skin lesion 37.11 21.50 30 6870 41814 79695674
Gastrooesophageal reflux disease 33.26 21.50 43 6857 104203 79633285
Paranoia 31.23 21.50 20 6880 19412 79718076
Coronary artery disease 30.87 21.50 33 6867 65441 79672047
General physical health deterioration 30.53 21.50 71 6829 275167 79462321
Sinus disorder 28.59 21.50 20 6880 22444 79715044
Myalgia 27.64 21.50 54 6846 185587 79551901
Respiratory failure 27.39 21.50 53 6847 180858 79556630
Toxicity to various agents 23.71 21.50 4 6896 421536 79315952
Rheumatoid nodule 23.30 21.50 16 6884 17422 79720066
Scleroderma renal crisis 22.54 21.50 6 6894 595 79736893

FDA Adverse Event Reporting System (Pediatric)

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 agonists
CHEBI has role CHEBI:35523 bronchodilator

Drug Use | Suggest Off label Use Form| |View source of the data|

DiseaseRelationSNOMED_IDDOID
Asthma indication 195967001 DOID:2841
Prevention of Bronchospasms with Emphysema indication
Prevention of Bronchospasm with Chronic Bronchitis 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




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

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 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
15.6MCG/INH;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
Cytochrome P450 1B1 Enzyme IC50 4.23 CHEMBL
Beta-2 adrenergic receptor GPCR IC50 8.10 CHEMBL

External reference:

IDSource
4030903 VUID
N0000182968 NUI
D09318 KEGG_DRUG
753498-25-8 SECONDARY_CAS_RN
4030903 VANDF
C1722260 UMLSCUI
CHEBI:68575 CHEBI
CHEMBL1095777 ChEMBL_ID
CHEMBL1789842 ChEMBL_ID
DB05039 DRUGBANK_ID
C510790 MESH_SUPPLEMENTAL_RECORD_UI
7455 IUPHAR_LIGAND_ID
8457 INN_ID
8OR09251MQ UNII
6918554 PUBCHEM_CID
1114325 RXNORM
184350 MMSL
27231 MMSL
30721 MMSL
d07651 MMSL
013439 NDDF
013440 NDDF
702801003 SNOMEDCT_US
702802005 SNOMEDCT_US
703740005 SNOMEDCT_US

Pharmaceutical products:

None