General
Preferred name
indacaterol
Synonyms
QAB149 ()
INDACATEROL MALEATE ()
Indacaterol (maleate) ()
Indacaterol acetate ()
Indacaterol maleate component of ultibro ()
Hirobriz breezhaler ()
Indacaterol maleate component of utibron ()
QAB149-AFA ()
QAB-149-AFA ()
Onbrez Breezhaler ()
Arcapta Neohaler ()
Indacterol maleate ()
Oslif breezhaler ()
Indacaterol (as maleate) ()
Indacaterol maleate component of qva149 ()
Indacaterol maleate component of qva-149 ()
QAB-149 ()
ONBREZ ()
INDACTEROL ()
QABI49 ()
Indacaterol-d3 ()
P&D ID
PD009338
CAS
312753-06-3
1000160-87-1
753498-25-8
2699828-16-3
Tags
available
drug
drug candidate
Approved by
EMA
PMDA
FDA
First approval
2009
Drug indication
Chronic obstructive pulmonary disease
Airway obstruction
Asthma
Drug Status
approved
investigational
Max Phase
3.0
4.0
Structure
Probe scores
P&D probe-likeness score
[[ v.score ]]%
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
DESCRIPTION Indacaterol maleate (QAB149) is an orally active ultra-long-acting ¦Â2 adrenergic receptor (ADRB2) agonist. Indacaterol maleate inhibits NF-¦ÊB activity in a ¦Â-arrestin2-dependent manner, preventing further lung damage and improving lung function in COPD (chronic obstructive pulmonary disorder). Indacaterol maleate can also be used in cardiovascular disease research[1][2].
PRICE 30
DESCRIPTION Indacaterol maleate (QAB149) is an ultra-long-acting ??-adrenoceptor agonist.
INDICATION For the long term, once-daily-dosing maintenance of airflow obstruction in patients with chronic obstructive pulmonary disease (COPD), including chronic bronchitis and/or emphysema.;
TOXICITY The expected signs and symptoms associated with overdosage of indacaterol are those of excessive beta-adrenergic stimulation and occurrence or exaggeration of any of the signs and symptoms, e.g., angina, hypertension or hypotension, tachycardia, with rates up to 200 bpm, arrhythmias, nervousness, headache, tremor, dry mouth, palpitation, muscle cramps, nausea, dizziness, fatigue, malaise, hypokalemia, hyperglycemia, metabolic acidosis and insomnia. As with all inhaled sympathomimetic medications, cardiac arrest and even death may be associated with an overdose of indacaterol.;
METABOLISM After oral administration of radiolabeled indacaterol, unchanged indacaterol was the main component in serum, accounting for about one third of total drug-related AUC over 24 hours. The monohydroxylated derivative, glucuronide conjugate, and the 8-O-glucuronide were the most prominent metabolites in serum. Other metabolites identified include a diastereomer of the hydroxylated derivative, a N-glucuronide of indacaterol, and C- and N-dealkylated products. ; ; In vitro investigations indicated that UGT1A1 was the only UGT isoform that metabolized indacaterol to the phenolic O-glucuronide. CYP3A4 is the predominant isoenzyme responsible for hydroxylation of indacaterol.
DESCRIPTION Only the R-enantiomer, as the maleate salt (PubChem CID 9827599) is contained in the medicinal product. (GtoPdb)
MOA Indacaterol works by stimulating adrenergic beta-2 receptors in the smooth muscle of the airways. This causes relaxation of the muscle, thereby increasing the diameter of the airways, which become constricted in asthma and COPD. It is also long acting due to its high affinity to the lipid raft domains in the airway membrane so it slowly dissociates from the receptors. Indacaterol also has a high intrinsic efficacy so it is also very rapid acting - onset of action occurs within 5 minutes. ; ; 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. In vitro studies have shown that indacaterol has more than 24-fold greater agonist activity at beta2-receptors compared to beta1-receptors and 20-fold greater agonist activity compared to beta3-receptors. This selectivity profile is similar to formoterol. The clinical significance of these findings is unknown.
PRICE 29
DESCRIPTION Indacaterol is an orally active ultra-long-acting ¦Â2 adrenergic receptor (ADRB2) agonist. Indacaterol inhibits NF-¦ÊB activity in a ¦Â-arrestin2-dependent manner, preventing further lung damage and improving lung function in COPD (chronic obstructive pulmonary disorder). Indacaterol can also be used in cardiovascular disease research[1][2].
DESCRIPTION Indacaterol (Onbrez; Arcapta) is a ??2-Adrenergic Agonist. The mechanism of action of indacaterol is as an Adrenergic beta2-Agonist.
DESCRIPTION Indacaterol maleate (QAB149) is an ultra-long-acting β-adrenoceptor agonist. (TargetMol Bioactive Compound Library)
DESCRIPTION Indacaterol (Onbrez; Arcapta) is a β2-Adrenergic Agonist. The mechanism of action of indacaterol is as an Adrenergic beta2-Agonist. (TargetMol Bioactive Compound Library)
Compound Sets
25
AdooQ Bioactive Compound Library
A10918
Cayman Chemical Bioactives
20070
28886
ChEMBL Approved Drugs
CHEMBL1789842
CHEMBL1095777
ChEMBL Drugs
CHEMBL1789842
CHEMBL1095777
CHEMBL4297657
Concise Guide to Pharmacology 2017/18
7455
Concise Guide to Pharmacology 2019/20
7455
Concise Guide to Pharmacology 2021/22
7455
Concise Guide to Pharmacology 2023/24
7455
Drug Repurposing Hub
DrugBank
DB05039
DrugBank Approved Drugs
DB05039
DrugCentral
4183
DrugCentral Approved Drugs
4183
DrugMAP
DMQJHR7
DrugMAP Approved Drugs
DMQJHR7
EU-OPENSCREEN Bioactive Compound Library
EOS100013
EUbOPEN Chemogenomics Library
EUB0000499
Guide to Pharmacology
7455
LSP-MoA library (Laboratory of Systems Pharmacology)
CHEMBL1095777
Mcule NIBR MoA Box Subset
MCULE-6133891152
MedChem Express Bioactive Compound Library
HY-14299A
HY-14299
Novartis Chemogenetic Library (NIBR MoA Box)
ReFrame library
Selleckchem Bioactive Compound Library
indacaterol-maleate
indacaterol
TargetMol Bioactive Compound Library
T1239
T2320
External IDs
66
Properties
(calculated by RDKit )
Molecular Weight
392.21
Hydrogen Bond Acceptors
4
Hydrogen Bond Donors
4
Rotatable Bonds
6
Ring Count
4
Aromatic Ring Count
3
cLogP
3.15
TPSA
85.35
Fraction CSP3
0.38
Chiral centers
1.0
Largest ring
6.0
QED
0.52
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Target
Adrenergic Receptor
β-adrenoceptor
β1-adrenoceptor
β2-adrenoceptor
ADRB1, ADRB2
Member status
member
MOA
beta2-Adrenoceptor Agonists
Adrenergic Receptor agonist
Indication
chronic obstructive pulmonary disease (COPD)
Pathway
GPCR/G protein
Neuroscience
Neuronal Signaling
Recommended Cell Concentration
100 nM
Source data