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

Stem definition	Drug id	CAS RN
bronchodilators, phenethylamine derivatives	4183	312753-06-3

Description:

Molecule	Description
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

Molecule

Description

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:

Dose	Unit	Route
0.15	mg	Inhal.powder

ADMET properties:

Property	Value	Reference
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:

Date	Agency	Company	Orphan
July 1, 2011	FDA	NOVARTIS
June 29, 2020	PMDA	Novartis Pharma K.K.

FDA Adverse Event Reporting System (Female)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Hyper IgE syndrome	134.64	26.70	23	2822	411	50601868
Restrictive pulmonary disease	107.36	26.70	23	2822	1401	50600878
Polycystic ovaries	94.63	26.70	23	2822	2461	50599818
Dyspnoea	78.27	26.70	122	2723	547486	50054793
Dyslipidaemia	74.58	26.70	23	2822	5965	50596314
Obstructive airways disorder	69.89	26.70	28	2817	15624	50586655
Blood test abnormal	60.24	26.70	23	2822	11296	50590983
Asthma	58.98	26.70	45	2800	89292	50512987
Bronchospasm	57.53	26.70	24	2821	14830	50587449
Abscess	55.07	26.70	23	2822	14249	50588030
Bacterial disease carrier	54.95	26.70	12	2833	799	50601480
Chronic obstructive pulmonary disease	54.12	26.70	35	2810	53400	50548879
Brain injury	53.94	26.70	18	2827	5996	50596283
Restless legs syndrome	52.68	26.70	23	2822	15874	50586405
Pneumonia	51.95	26.70	83	2762	378318	50223961
Respiratory failure	51.71	26.70	42	2803	91139	50511140
Lung neoplasm malignant	46.79	26.70	21	2824	15463	50586816
Nonspecific reaction	45.57	26.70	12	2833	1767	50600512
Eczema	44.87	26.70	23	2822	22679	50579600
Paranoia	44.41	26.70	18	2827	10330	50591949
Disability	44.01	26.70	19	2826	12756	50589523
Superinfection	43.85	26.70	12	2833	2044	50600235
Sleep apnoea syndrome	43.78	26.70	23	2822	23845	50578434
Type 2 diabetes mellitus	43.62	26.70	26	2819	34349	50567930
Bronchial secretion retention	42.59	26.70	11	2834	1502	50600777
Coronary artery disease	41.71	26.70	24	2821	29702	50572577
Cough	41.67	26.70	59	2786	241205	50361074
Skin lesion	41.34	26.70	23	2822	26704	50575575
Wheezing	40.34	26.70	31	2814	62016	50540263
Sleep disorder due to a general medical condition	39.29	26.70	15	2830	7356	50594923
Sinus operation	36.64	26.70	10	2835	1686	50600593
Depression	29.30	26.70	41	2804	165382	50436897
Gastrooesophageal reflux disease	28.88	26.70	28	2817	76400	50525879
Coma	27.65	26.70	24	2821	56855	50545424
Myocardial infarction	27.06	26.70	29	2816	88998	50513281

FDA Adverse Event Reporting System (Male)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Dyspnoea	63.72	22.93	109	2576	326623	29245219
Rheumatoid nodule	54.95	22.93	16	2669	2106	29569736
Mesenteric vein thrombosis	38.70	22.93	9	2676	489	29571353
Cardiac failure	30.94	22.93	37	2648	79250	29492592
Pneumonia	27.52	22.93	77	2608	320095	29251747
Concomitant disease aggravated	24.59	22.93	11	2674	4967	29566875
Intestinal ischaemia	24.43	22.93	12	2673	6680	29565162
Productive cough	23.93	22.93	21	2664	31238	29540604

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Hyper IgE syndrome	123.39	21.86	23	5156	472	64493081
Dyspnoea	98.29	21.86	192	4987	718482	63775071
Polycystic ovaries	89.69	21.86	23	5156	2132	64491421
Restrictive pulmonary disease	89.51	21.86	23	5156	2149	64491404
Obstructive airways disorder	75.59	21.86	37	5142	23148	64470405
Pneumonia	70.79	21.86	145	5034	559431	63934122
Asthma	63.38	21.86	56	5123	95169	64398384
Chronic obstructive pulmonary disease	60.11	21.86	48	5131	71000	64422553
Dyslipidaemia	56.77	21.86	23	5156	9219	64484334
Eczema	56.16	21.86	33	5146	29687	64463866
Lung neoplasm malignant	51.87	21.86	28	5151	21420	64472133
Blood test abnormal	49.32	21.86	23	5156	12920	64480633
Bronchospasm	48.82	21.86	27	5152	21655	64471898
Bacterial disease carrier	48.19	21.86	12	5167	987	64492566
Wheezing	46.95	21.86	44	5135	80535	64413018
Type 2 diabetes mellitus	44.69	21.86	30	5149	33990	64459563
Cough	43.68	21.86	83	5096	302065	64191488
Restless legs syndrome	43.22	21.86	23	5156	17093	64476460
Abscess	40.63	21.86	23	5156	19281	64474272
Nonspecific reaction	39.92	21.86	12	5167	1991	64491562
Disability	38.39	21.86	19	5160	12153	64481400
Brain injury	35.78	21.86	17	5162	9948	64483605
Bronchial secretion retention	33.14	21.86	11	5168	2516	64491037
Sinus operation	33.12	21.86	10	5169	1685	64491868
Sleep disorder due to a general medical condition	32.51	21.86	15	5164	8219	64485334
Superinfection	32.12	21.86	12	5167	3874	64489679
Respiratory failure	32.02	21.86	51	5128	161132	64332421
Sleep apnoea syndrome	31.46	21.86	23	5156	29809	64463744
Paranoia	30.47	21.86	18	5161	16334	64477219
Skin lesion	29.45	21.86	24	5155	36458	64457095
Rheumatoid nodule	29.15	21.86	16	5163	12635	64480918
Gastrooesophageal reflux disease	26.48	21.86	33	5146	83110	64410443
Coronary artery disease	22.54	21.86	26	5153	60407	64433146

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
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|

Disease	Relation	SNOMED_ID	DOID
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 level	Dissociation constant	Type (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 strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent 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:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Beta-2 adrenergic receptor	GPCR	P07550	ADRB2_HUMAN	AGONIST	Ki	7.80	CHEMBL	CHEMBL
D(3) dopamine receptor	GPCR	P35462	DRD3_HUMAN		Ki	5.98	CHEMBL
Beta-1 adrenergic receptor	GPCR	P08588	ADRB1_HUMAN		Ki	7.04	CHEMBL
D(2) dopamine receptor	GPCR	P14416	DRD2_HUMAN		IC50	4.60	CHEMBL
Beta-2 adrenergic receptor	GPCR		ADRB2_CAVPO		IC50	8.10	CHEMBL

External reference:

ID	Source
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