Indacaterol

Summary

Indacaterol (CHEMBL1095777) is an approved small-molecule β-adrenergic agonist (ATC R03AC18) targeting ADRB1 and ADRB2; indicated across 5 conditions including obstructive lung disease and chronic obstructive pulmonary disease.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: R03AC18
• Targets: 2 (ADRB1, ADRB2)
• Indications: 5 conditions
• Clinical trials: 103
• Chemistry: 392.5 Da · C24H28N2O3

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL1095777
Name	Indacaterol
Type	Small molecule
Max phase	4
FDA approved	no
PubChem CID	6918554
ChEBI	CHEBI:68575
ATC	R03AC18
Molecular formula	C24H28N2O3
Molecular weight	392.5
InChIKey	QZZUEBNBZAPZLX-QFIPXVFZSA-N

SMILES: CCC1=C(C=C2CC(CC2=C1)NC[C@@H](C3=C4C=CC(=O)NC4=C(C=C3)O)O)CC

IUPAC name: 5-[(1R)-2-[(5,6-diethyl-2,3-dihydro-1H-inden-2-yl)amino]-1-hydroxyethyl]-8-hydroxy-1H-quinolin-2-one

ChEBI definition: A monohydroxyquinoline that consists of 5-[(1R)-2-amino-1-hydroxyethyl]-8-hydroxyquinolin-2-one having a 5,6-diethylindan-2-yl group attached to the amino function. Used as the maleate salt for treatment of chronic obstructive pulmonary disease.

Pharmacological roles (ChEBI): β-adrenergic agonist, bronchodilator agent.

Also known as: Indacaterol, Indacterol, Onbrez, QAB-149, QAB149, QABI49, indacaterol, INDACATEROL, Indacaterol Maleate

Parent form; salt/anhydrous children: CHEMBL1789842, CHEMBL3527369, CHEMBL4297657

Patent coverage: 1,057 distinct patent families (2,735 SureChEMBL compound mentions), from 3 matched compound structure(s). One matched structure accounts for 1,964 (72%) of the total. Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.

Targets

Targets

Primary targets (GtoPdb curated mechanism): the Cancer dependency column is the DepMap CRISPR fitness signal (% of screened cell lines dependent on the target).

Gene	Target	Action	pAffinity	Cancer dependency	UniProt
ADRB1	β1-adrenoceptor	Agonist	6.7	0%	P08588
ADRB2	β2-adrenoceptor	Agonist	8.1	0.4%	P07550

Broader ChEMBL bioactivity targets: 15 (assay-derived). Sample: Beta-2 adrenergic receptor, Beta-1 adrenergic receptor, Sodium-dependent noradrenaline transporter, Alpha-1D adrenergic receptor, 5-hydroxytryptamine receptor 2A, 5-hydroxytryptamine receptor 2C, Sodium-dependent serotonin transporter, Alpha-1A adrenergic receptor, Alpha-1B adrenergic receptor, D(3) dopamine receptor.

Bioactivity

ChEMBL activities: 25 potent at pChembl ≥ 5 of 27 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
ADRB2	9.1	EC50	0.79	nM	CHEMBL_ACT_23194860
ADRB2	8.82	EC50	1.5	nM	CHEMBL_ACT_15052035
Q8K4Z4	8.1	IC50	7.9	nM	CHEMBL_ACT_15051897
Q8K4Z4	8.1	IC50	7.9	nM	CHEMBL_ACT_3294102
ADRB2	7.96	EC50	11	nM	CHEMBL_ACT_3294104
ADRB2	7.8	EC50	15.85	nM	CHEMBL_ACT_8022177
ADRB2	7.69	Ki	20.6	nM	CHEMBL_ACT_15051974
ADRB2	7.69	Ki	20.6	nM	CHEMBL_ACT_3423533
SLC6A3	7.12	Ki	75.02	nM	CHEMBL_ACT_25741397
ADRB2	7.12	Ki	76	nM	CHEMBL_ACT_3294105
ADRB2	7.08	EC50	83.28	nM	CHEMBL_ACT_25751333
ADRB1	7.04	Ki	91	nM	CHEMBL_ACT_15051949
ADRB1	7.04	Ki	91.4	nM	CHEMBL_ACT_3423534
ADRB2	6.97	Ki	106	nM	CHEMBL_ACT_25741391
TMEM97	6.97	Ki	106.9	nM	CHEMBL_ACT_25741399
ADRB1	6.5	IC50	316.2	nM	CHEMBL_ACT_8023145
ADRA1A	6.45	Ki	355.6	nM	CHEMBL_ACT_25741388
SLC6A2	6.25	Ki	568.7	nM	CHEMBL_ACT_25741396
ADRA1D	6.14	Ki	731.3	nM	CHEMBL_ACT_25741390
SLC6A4	6.11	Ki	770	nM	CHEMBL_ACT_25741398
DRD3	5.98	Ki	1048	nM	CHEMBL_ACT_15051924
DRD3	5.87	Ki	1339	nM	CHEMBL_ACT_25741392
HTR2C	5.75	Ki	1800	nM	CHEMBL_ACT_25741394
HTR2A	5.7	Ki	2020	nM	CHEMBL_ACT_25741393
ADRA1B	5.36	Ki	4323	nM	CHEMBL_ACT_25741389

Target pathways

Aggregated over 2 target gene(s): ADRB1, ADRB2.

Top Reactome pathways

16 total, by targets touching each:

Pathway	Targets	Genes
Signal Transduction	2	ADRB1, ADRB2
Signaling by GPCR	2	ADRB1, ADRB2
Class A/1 (Rhodopsin-like receptors)	2	ADRB1, ADRB2
Amine ligand-binding receptors	2	ADRB1, ADRB2
GPCR downstream signalling	2	ADRB1, ADRB2
Adrenoceptors	2	ADRB1, ADRB2
G alpha (s) signalling events	2	ADRB1, ADRB2
GPCR ligand binding	2	ADRB1, ADRB2
Membrane Trafficking	1	ADRB2
Metabolism of proteins	1	ADRB2
Vesicle-mediated transport	1	ADRB2
Deubiquitination	1	ADRB2
Ub-specific processing proteases	1	ADRB2
Post-translational protein modification	1	ADRB2
Cargo recognition for clathrin-mediated endocytosis	1	ADRB2
Clathrin-mediated endocytosis	1	ADRB2

Dominant GO biological processes

GO term	Targets
diet induced thermogenesis	2
norepinephrine-epinephrine-mediated vasodilation involved in regulation of systemic arterial blood pressure	2
adenylate cyclase-activating G protein-coupled receptor signaling pathway	2
response to cold	2
positive regulation of cardiac muscle cell apoptotic process	2
heat generation	2
negative regulation of multicellular organism growth	2
positive regulation of MAPK cascade	2
brown fat cell differentiation	2
adenylate cyclase-activating adrenergic receptor signaling pathway	2
positive regulation of cold-induced thermogenesis	2
signal transduction	2
G protein-coupled receptor signaling pathway	2
positive regulation of heart rate by epinephrine-norepinephrine	1
positive regulation of the force of heart contraction by epinephrine-norepinephrine	1

Indications & clinical

Indications

5 indications (1 at ChEMBL trial phase 4). Phase below is the highest clinical-trial phase recorded for this drug against each disease — not the molecule’s overall approval status (that is in the Summary).

Indication	Trial phase	MONDO	EFO
obstructive lung disease	4	MONDO:0002267	HP:0006536
chronic obstructive pulmonary disease	3	MONDO:0005002	EFO:0000341
heart failure	3	MONDO:0005252	EFO:0003144
asthma	3	MONDO:0004979	MONDO:0004979
lung disorder	2	MONDO:0005275	EFO:0003818

Clinical trials

Total trials: 103.

Phase distribution

Phase	Trials
PHASE3	38
PHASE4	24
PHASE2	22
PHASE1	8
Not specified	6
PHASE2/PHASE3	4
PHASE1/PHASE2	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT01272362	PHASE4	COMPLETED	To Determine the Relationship Between Baseline Reversibility and the Efficacy of Indacaterol
NCT01377051	PHASE4	COMPLETED	Effect of Indacaterol Maleate in Chronic Obstructive Pulmonary Disease (COPD) on Lung Volume and Related Dyspnea
NCT01377428	PHASE4	WITHDRAWN	Efficacy of Indacaterol 150 µg Versus Formoterol
NCT01437748	PHASE4	COMPLETED	Closing Volume Interpretation and Bronchodilators Effect
NCT01543828	PHASE4	COMPLETED	Indacaterol 75 μg Compared to Placebo, Assessing Time to Patient’s Perception of Onset of Effect in Patients With Moderate to Severe Chronic Obstructive Pulmonary Disease
NCT01555138	PHASE4	COMPLETED	Comparison of Indacaterol 150 mcg Once Daily (o.d.) With Salmeterol/Fluticasone Propionate 50 mcg/500 mcg Twice Daily (b.i.d.)
NCT01693003	PHASE4	COMPLETED	Indacaterol Versus Tiotropium on Dynamic Hyperinflation in COPD
NCT01715311	PHASE4	WITHDRAWN	Comparison of Indacaterol With That of Placebo in ‘Maintenance naïve’ Patients With COPD Using Blinded Tiotropium as Active Control
NCT01727024	PHASE4	COMPLETED	Study Evaluating Preference, Satisfaction And Correct Use Of Inhalers In COPD Patients
NCT01985334	PHASE4	COMPLETED	Study to Evaluate the Efficacy and Safety of Glycopyrronium or Indacaterol Maleate and Glycopyrronium Bromide Fixed-dose Combination Regarding Symptoms and Health Status in Patients With Moderate COPD Switching From Treatment With Any Standard COPD Regimen
NCT01996124	PHASE4	COMPLETED	Acute Effect of Pulmonary Desufflation on Cardiac Performance in COPD Patients
NCT02039011	PHASE4	COMPLETED	Ultra-long Acting Bronchodilator Therapy in Asthmatics
NCT02055352	PHASE4	COMPLETED	Study to Evaluate Efficacy/Safety of Combination Budesonide/Indacaterol vs Fluticasone/Salmeterol in Patients With COPD
NCT02202616	PHASE4	COMPLETED	Prospective Cohort Study for the Real - Life Effectiveness Evaluation of GlycOpyrronium With IndacatERol Combination in the Management of COPD in Canada (POWER Study)
NCT02418468	PHASE4	COMPLETED	Effects of Indacaterol in Symptomatic COPD Patients With Low Risk of Exacerbations
NCT02473237	PHASE4	COMPLETED	Efficacy in Walked Distance of Indacaterol vs Tiotropium in Women With COPD Secondary to Biomass (EMERALD)
NCT02547558	PHASE4	UNKNOWN	Pulmonary Gas Exchange Response to Indacaterol in COPD
NCT02566031	PHASE4	COMPLETED	A Randomized, Multicenter, Open-label, Parallel-group, 12-week Study to Assess the Efficacy and Safety of Switching From Tiotropium to QVA149 (Indacaterol Maleate/Glycopyrronium Bromide) in Symptomatic Mild to Moderate COPD Patients
NCT02576626	PHASE4	COMPLETED	Single Dose Ultibro Breezhaler by Sd-DPI Versus Ipratropium/Salbutamol by Nebulizer in COPD
NCT02872090	PHASE4	COMPLETED	Effects of Long Acting Bronchodilators on CARDiac Autonomic Control in Chronic Obstructive Pulmonary Disease (COPD)
NCT02953041	PHASE4	COMPLETED	Effect of a LAMA and a uLABA on the Methacholine Dose-response Curve
NCT03364829	PHASE4	UNKNOWN	Utilizing Wearable Device to Observe the Clinical Response of COPD Patients Treated With Combined Bronchodilator and Home-based Pulmonary Rehabilitation Program
NCT05506865	PHASE4	COMPLETED	Efficacy and Safety of Indacaterol vs Tiotropium in Women With COPD Secondary to Biomass Exposure
NCT06282861	PHASE4	TERMINATED	ANTES B+ Clinical Trial
NCT00393458	PHASE3	COMPLETED	Efficacy, Safety, and Tolerability of Once Daily Indacaterol in Chronic Obstructive Pulmonary Disease (COPD) Using Formoterol Twice Daily as Active Control
NCT00396604	PHASE2/PHASE3	COMPLETED	Indacaterol Delivered Via a Single Dose Dry Powder Inhaler (SDDPI) in Chronic Obstructive Pulmonary Disease (COPD)
NCT00403637	PHASE2/PHASE3	COMPLETED	Efficacy and Safety of Single Doses of Indacaterol Delivered Via a Single Dose Dry Powder Inhaler (SDDPI) Compared to Placebo in Patients With Persistent Asthma
NCT00463567	PHASE2/PHASE3	COMPLETED	26 Week Efficacy, Safety and Tolerability Study of Indacaterol in Patients With Chronic Obstructive Pulmonary Disease (COPD)
NCT00529529	PHASE3	COMPLETED	Safety of Indacaterol in Patients (≥ 12 Years) With Moderate to Severe Persistent Asthma
NCT00567996	PHASE3	COMPLETED	Efficacy and Safety of Indacaterol in Patients With Chronic Obstructive Pulmonary Disease (COPD) Using Salmeterol as Active Control
NCT00615030	PHASE3	COMPLETED	Study of Indacaterol Dosed in the Evening in Patients With Chronic Obstructive Pulmonary Disease (COPD)
NCT00615459	PHASE3	COMPLETED	A Crossover Study to Determine the Effect on Lung Function of Indacaterol in Patients With Moderate to Severe Chronic Obstructive Pulmonary Disease (COPD), Using Tiotropium as an Active Control
NCT00620022	PHASE3	COMPLETED	The Effect of Indacaterol on Exercise Endurance in Patients With Moderate to Severe Chronic Obstructive Pulmonary Disease
NCT00622635	PHASE3	COMPLETED	A Crossover Study to Determine the 24 Hour Lung Function Profile of Indacaterol in Patients With Moderate-to-severe Chronic Obstructive Pulmonary Disease (COPD)
NCT00624286	PHASE3	COMPLETED	Efficacy and Safety of Indacaterol in Patients With Chronic Obstructive Pulmonary Disease (COPD)
NCT00669617	PHASE3	COMPLETED	Study to Determine the Onset of Action of Indacaterol in Patients With Moderate to Severe Chronic Obstructive Pulmonary Disease (COPD)
NCT00677807	PHASE3	COMPLETED	Safety, Tolerability and Efficacy of Indacaterol in Patients With Moderate-to-severe Chronic Obstructive Pulmonary Disease (COPD)
NCT00792805	PHASE3	COMPLETED	Efficacy and Safety of Indacaterol in Adults (40 Years and Above) With Chronic Obstructive Pulmonary Disease (COPD)
NCT00794157	PHASE3	COMPLETED	Confirmatory Study of Indacaterol in Patients With Chronic Obstructive Pulmonary Disease (COPD)
NCT00821093	PHASE3	COMPLETED	Safety and Efficacy of Indacaterol Once Daily Versus Salmeterol Twice Daily in Chronic Obstructive Pulmonary Disease (COPD)

Clinical evidence (CIViC)

No CIViC predictive evidence (expected for non-precision-medicine drugs).

Pharmacology

Pharmacogenomics

No CPIC/DPWG dosing guideline, but PharmGKB curates 0 clinical and 2 variant annotation(s) for this drug (gene-keyed; see PharmGKB).

Related molecules

Related molecules

Molecules sharing ≥1 of this drug’s curated primary targets, merged from two biobtree sources and ranked by shared-target count, then clinical phase: ChEMBL clinical-stage candidates (development phase ≥2) and PubChem drug-class bioactivity (approved / known drugs acting on the target). Deduplicated by drug name; the drug’s own salt forms are excluded. Note: for a drug with few primary targets a shared-target match can reflect off-target / promiscuous binding rather than the same therapeutic mechanism — the phase ordering surfaces bona-fide therapeutics first.

238 molecules share ≥1 primary target. Top 60 by shared-target count:

Molecule	Source	Status	Shared targets
Desloratadine	ChEMBL + PubChem	Phase 4 (approved)	ADRB1, ADRB2
Dihydroergotamine	ChEMBL + PubChem	Phase 4 (approved)	ADRB1, ADRB2
OLODATEROL	ChEMBL + PubChem	Phase 4 (approved)	ADRB1, ADRB2
Pramipexole	ChEMBL + PubChem	Phase 4 (approved)	ADRB1, ADRB2
TAMSULOSIN	ChEMBL + PubChem	Phase 4 (approved)	ADRB1, ADRB2
ACEBUTOLOL	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
ALBUTEROL	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
AMITRIPTYLINE	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
ARFORMOTEROL	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
ARIPIPRAZOLE	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
ATENOLOL	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
BENPERIDOL	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
BETAXOLOL	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
BISOPROLOL	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
BREXPIPRAZOLE	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
BROMOCRIPTINE	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
CANDESARTAN CILEXETIL	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
CARTEOLOL	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
CARVEDILOL	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
CELIPROLOL	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
CHLORHEXIDINE	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
CLEMASTINE	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
CLOMIPRAMINE	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
CLOTRIMAZOLE	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
DARIFENACIN	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
DOBUTAMINE	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
DOMPERIDONE	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
EPINEPHRINE	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
ERGOTAMINE	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
ESMOLOL	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
FENOTEROL	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
FLUSPIRILENE	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
FORMOTEROL	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
ISOPROTERENOL	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
LABETALOL	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
LEVOBUNOLOL	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
METOPROLOL	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
MONTELUKAST	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
NADOLOL	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
NEBIVOLOL	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
NITAZOXANIDE	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
NOREPINEPHRINE	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
NORTRIPTYLINE	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
OXPRENOLOL	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
PHENYLEPHRINE	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
PIMOZIDE	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
PINDOLOL	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
PRACTOLOL	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
PRENYLAMINE	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
PRIMAQUINE	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
PROPAFENONE	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
PROPRANOLOL	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
RANOLAZINE	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
RIFAMPIN	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
RIFAXIMIN	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
RITODRINE	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
SALMETEROL	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
SOTALOL	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
SUNITINIB	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
TAMOXIFEN	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2