INDACATEROL MALEATE

US Previously Marketed

Details

Stereochemistry	ABSOLUTE
Molecular Formula	C24H28N2O3.C4H4O4
Molecular Weight	508.5629
Optical Activity	UNSPECIFIED
Defined Stereocenters	1 / 1
E/Z Centers	1
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

OC(=O)\C=C/C(O)=O.CCC1=C(CC)C=C2CC(CC2=C1)NC[C@H](O)C3=CC=C(O)C4=C3C=CC(=O)N4

InChI

InChIKey=IREJFXIHXRZFER-PCBAQXHCSA-N

InChI=1S/C24H28N2O3.C4H4O4/c1-3-14-9-16-11-18(12-17(16)10-15(14)4-2)25-13-22(28)19-5-7-21(27)24-20(19)6-8-23(29)26-24;5-3(6)1-2-4(7)8/h5-10,18,22,25,27-28H,3-4,11-13H2,1-2H3,(H,26,29);1-2H,(H,5,6)(H,7,8)/b;2-1-/t22-;/m0./s1

HIDE SMILES / InChI

Description
Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2012/022383s002lbl.pdf

Indacaterol is an ultra-long-acting beta-adrenoceptor agonist developed by Novartis. It was approved by the European Medicines Agency (EMA) under the trade name Onbrez Breezhaler on November 30, 2009, and by the United States Food and Drug Administration (FDA), under the trade name Arcapta Neohaler, on July 1, 2011. It needs to be taken only once a day, unlike the related drugs formoterol and salmeterol. It is licensed only for the treatment of chronic obstructive pulmonary disease (COPD) (long-term data in patients with asthma are thus far lacking). It is delivered as an aerosol formulation through a dry powder inhaler.

CNS Activity

Originator

Approval Year

Targets

Primary Target	Pharmacology	Potency
Beta-2 adrenergic receptor 209 Target ID: CHEMBL210 Sources: https://www.ncbi.nlm.nih.gov/pubmed/20402514	Agonist 2752	76.0 nM [Ki]
Beta-1 adrenergic receptor 163 Target ID: CHEMBL213 Sources: https://www.ncbi.nlm.nih.gov/pubmed/20655218	Agonist 2752	91.4 nM [Ki]
Beta-2 adrenergic receptor 209 Target ID: CHEMBL210 Sources: https://www.ncbi.nlm.nih.gov/pubmed/20402514	Agonist 2752	76.0 nM [Ki]
Beta-1 adrenergic receptor 163 Target ID: CHEMBL213 Sources: https://www.ncbi.nlm.nih.gov/pubmed/20655218	Agonist 2752	91.4 nM [Ki]

Conditions

Condition	Modality	Targets	Highest Phase	Product
Airflow obstruction in patients with chronic obstructive pulmonary disease (COPD), 4 Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2012/022383s002lbl.pdf	Primary		Approved 8583	ARCAPTA NEOHALER Approved Use UTIBRONTM NEOHALER® is a combination of indacaterol and glycopyrrolate indicated for the long-term, maintenance treatment of airflow obstruction in patients with chronic obstructive pulmonary disease (COPD), including chronic bronchitis and/or emphysema. Important Limitations of Use: UTIBRON NEOHALER is NOT indicated for the relief of acute bronchospasm or for the treatment of asthma [see Warnings and Precautions (5.1, 5.2) Launch Date 2011
Airflow obstruction in patients with chronic obstructive pulmonary disease (COPD) 4 Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2012/022383s002lbl.pdf	Primary		Approved 8583	ARCAPTA Approved Use INDICATIONS AND USAGE. ARCAPTA NEOHALER is a long-acting beta2-adrenergic agonist indicated for: 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. Important limitations: ARCAPTA NEOHALER is NOT indicated to treat acute deteriorations of chronic obstructive pulmonary disease. ARCAPTA NEOHALER is NOT indicated for asthma. Launch Date 2011

C_max

Value	Dose	Co-administered	Analyte	Population
0.206 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/24705947/	150 μg single, respiratory dose: 150 μg route of administration: Respiratory experiment type: SINGLE co-administered:		INDACATEROL serum	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
0.518 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/24705947/	300 μg single, respiratory dose: 300 μg route of administration: Respiratory experiment type: SINGLE co-administered:		INDACATEROL serum	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
0.299 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/24705947/	150 μg 1 times / day steady-state, respiratory dose: 150 μg route of administration: Respiratory experiment type: STEADY-STATE co-administered:		INDACATEROL serum	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
0.697 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/24705947/	300 μg 1 times / day steady-state, respiratory dose: 300 μg route of administration: Respiratory experiment type: STEADY-STATE co-administered:		INDACATEROL serum	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
339 pg/mL OTHER GOV https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207930Orig1s000ClinPharmR.pdf	110 μg single, respiratory dose: 110 μg route of administration: Respiratory experiment type: SINGLE co-administered: GLYCOPYRROLATE	GLYCOPYRROLATE	INDACATEROL plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
528 pg/mL OTHER GOV https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207930Orig1s000ClinPharmR.pdf	110 μg 1 times / day steady-state, respiratory dose: 110 μg route of administration: Respiratory experiment type: STEADY-STATE co-administered: GLYCOPYRROLATE	GLYCOPYRROLATE	INDACATEROL plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN

AUC

Value	Dose	Co-administered	Analyte	Population
0.974 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/24705947/	150 μg single, respiratory dose: 150 μg route of administration: Respiratory experiment type: SINGLE co-administered:		INDACATEROL serum	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
2.43 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/24705947/	300 μg single, respiratory dose: 300 μg route of administration: Respiratory experiment type: SINGLE co-administered:		INDACATEROL serum	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
2.51 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/24705947/	150 μg 1 times / day steady-state, respiratory dose: 150 μg route of administration: Respiratory experiment type: STEADY-STATE co-administered:		INDACATEROL serum	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
6.52 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/24705947/	300 μg 1 times / day steady-state, respiratory dose: 300 μg route of administration: Respiratory experiment type: STEADY-STATE co-administered:		INDACATEROL serum	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
907 pg × h/mL OTHER GOV https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207930Orig1s000ClinPharmR.pdf	110 μg single, respiratory dose: 110 μg route of administration: Respiratory experiment type: SINGLE co-administered: GLYCOPYRROLATE	GLYCOPYRROLATE	INDACATEROL plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
2750 pg × h/mL OTHER GOV https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207930Orig1s000ClinPharmR.pdf	110 μg 1 times / day steady-state, respiratory dose: 110 μg route of administration: Respiratory experiment type: STEADY-STATE co-administered: GLYCOPYRROLATE	GLYCOPYRROLATE	INDACATEROL plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN

T_1/2

Value	Dose	Co-administered	Analyte	Population
116 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/24705947/	150 μg 1 times / day steady-state, respiratory dose: 150 μg route of administration: Respiratory experiment type: STEADY-STATE co-administered:		INDACATEROL serum	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
118 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/24705947/	300 μg 1 times / day steady-state, respiratory dose: 300 μg route of administration: Respiratory experiment type: STEADY-STATE co-administered:		INDACATEROL serum	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN

Doses

Dose	Population	Adverse events
800 ug 1 times / day multiple, respiratory Highest studied dose Dose: 800 ug, 1 times / day Route: respiratory Route: multiple Dose: 800 ug, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/18219838	unhealthy, 43.5 years (range: 12.0–64.0 years) Health Status: unhealthy Age Group: 43.5 years (range: 12.0–64.0 years) Sex: M+F Sources: https://pubmed.ncbi.nlm.nih.gov/18219838	Disc. AE: Dyspnea, Wheezing... AEs leading to discontinuation/dose reduction: Dyspnea (serious, 1 patient) Wheezing (serious, 1 patient) Asthma (moderate, 1 patient) Cough (moderate, 1 patient) Sources: https://pubmed.ncbi.nlm.nih.gov/18219838
75 ug 1 times / day multiple, respiratory Dose: 75 ug, 1 times / day Route: respiratory Route: multiple Dose: 75 ug, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/022383s000lbl.pdf	unhealthy Health Status: unhealthy Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/022383s000lbl.pdf	Other AEs: Adverse event... Other AEs: Adverse event (grade 5) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/022383s000lbl.pdf

AEs

AE	Significance	Dose	Population
Asthma	moderate, 1 patient Disc. AE	800 ug 1 times / day multiple, respiratory Highest studied dose Dose: 800 ug, 1 times / day Route: respiratory Route: multiple Dose: 800 ug, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/18219838	unhealthy, 43.5 years (range: 12.0–64.0 years) Health Status: unhealthy Age Group: 43.5 years (range: 12.0–64.0 years) Sex: M+F Sources: https://pubmed.ncbi.nlm.nih.gov/18219838
Cough	moderate, 1 patient Disc. AE	800 ug 1 times / day multiple, respiratory Highest studied dose Dose: 800 ug, 1 times / day Route: respiratory Route: multiple Dose: 800 ug, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/18219838	unhealthy, 43.5 years (range: 12.0–64.0 years) Health Status: unhealthy Age Group: 43.5 years (range: 12.0–64.0 years) Sex: M+F Sources: https://pubmed.ncbi.nlm.nih.gov/18219838
Dyspnea	serious, 1 patient Disc. AE	800 ug 1 times / day multiple, respiratory Highest studied dose Dose: 800 ug, 1 times / day Route: respiratory Route: multiple Dose: 800 ug, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/18219838	unhealthy, 43.5 years (range: 12.0–64.0 years) Health Status: unhealthy Age Group: 43.5 years (range: 12.0–64.0 years) Sex: M+F Sources: https://pubmed.ncbi.nlm.nih.gov/18219838
Wheezing	serious, 1 patient Disc. AE	800 ug 1 times / day multiple, respiratory Highest studied dose Dose: 800 ug, 1 times / day Route: respiratory Route: multiple Dose: 800 ug, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/18219838	unhealthy, 43.5 years (range: 12.0–64.0 years) Health Status: unhealthy Age Group: 43.5 years (range: 12.0–64.0 years) Sex: M+F Sources: https://pubmed.ncbi.nlm.nih.gov/18219838
Adverse event	grade 5	75 ug 1 times / day multiple, respiratory Dose: 75 ug, 1 times / day Route: respiratory Route: multiple Dose: 75 ug, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/022383s000lbl.pdf	unhealthy Health Status: unhealthy Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/022383s000lbl.pdf

Overview

CYP3A4	CYP2C9	CYP2D6	hERG
substrate 1946	substrate 1193 inhibitor 2438	substrate 1388 inhibitor 2507	inhibitor 2217

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
CYP2E1 1060 CYP3A4/5 296 CYP1A2 2153 CYP2C8 1057 CYP2C19 2057 P-gp 1741 MRP2 499 BCRP 910 hOCT1 10	UGT1A1 479 UGT1A3 470 UGT1A4 399 UGT1A6 343 UGT1A8 323 UGT1A9 423 UGT1A10 331 UGT2B7 456 UGT2B15 236 CYP1A1 389 CYP1A2 1197 CYP1B1 104 CYP2A6 626 CYP2B6 776 CYP2C8 810 CYP2C18 149 CYP2C19 1119 CYP2E1 729 CYP3A5 446 CYP4A11 137 P-gp 2052	P-gp 301 MRP2 146

Drug as perpetrator

Target	Modality	Activity
MRP2 625	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022383Orig1s000ClinPharmR.pdf#page=23 Page: 23.0	negligible
P-gp 1932	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022383Orig1s000ClinPharmR.pdf#page=23 Page: 23.0	negligible
CYP2C9 2497	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022383Orig1s000ClinPharmR.pdf#page=96 Page: 96.0	no
CYP2E1 1146	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022383Orig1s000ClinPharmR.pdf#page=96 Page: 96.0	no
CYP3A4/5 357	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022383Orig1s000ClinPharmR.pdf#page=96 Page: 96.0	no
BCRP 985	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022383Orig1s000ClinPharmR.pdf#page=23 Page: 23.0	unlikely
MRP2 625	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022383Orig1s000ClinPharmR.pdf#page=23 Page: 23.0	unlikely
P-gp 1932	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022383Orig1s000ClinPharmR.pdf#page=23 Page: 23.0	unlikely
hOCT1 10	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022383Orig1s000ClinPharmR.pdf#page=23 Page: 23.0	unlikely
CYP1A2 2333	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022383Orig1s000ClinPharmR.pdf#page=96 Page: 96.0	weak [IC50 10 uM]
CYP2C19 2141	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022383Orig1s000ClinPharmR.pdf#page=96 Page: 96.0	weak [IC50 25 uM]
CYP2C8 1117	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022383Orig1s000ClinPharmR.pdf#page=96 Page: 96.0	weak [IC50 25 uM]
CYP2D6 2546	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022383Orig1s000ClinPharmR.pdf#page=96 Page: 96.0	weak [IC50 5 uM]

Drug as victim

Target	Modality	Activity	Clinical evidence
CYP3A5 446	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022383Orig1s000ClinPharmR.pdf#page=98 Page: 98.0	likely
CYP1A1 389	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022383Orig1s000ClinPharmR.pdf#page=91 Page: 91.0	low
CYP2D6 1388	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022383Orig1s000ClinPharmR.pdf#page=91 Page: 91.0	low
CYP1A2 1197	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022383Orig1s000ClinPharmR.pdf#page=91 Page: 91.0	no
CYP1B1 104	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022383Orig1s000ClinPharmR.pdf#page=91 Page: 91.0	no
CYP2A6 626	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022383Orig1s000ClinPharmR.pdf#page=91 Page: 91.0	no
CYP2B6 776	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022383Orig1s000ClinPharmR.pdf#page=91 Page: 91.0	no
CYP2C18 149	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022383Orig1s000ClinPharmR.pdf#page=91 Page: 91.0	no
CYP2C19 1119	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022383Orig1s000ClinPharmR.pdf#page=91 Page: 91.0	no
CYP2C8 810	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022383Orig1s000ClinPharmR.pdf#page=91 Page: 91.0	no
CYP2C9 1193	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022383Orig1s000ClinPharmR.pdf#page=91 Page: 91.0	no
CYP2E1 729	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022383Orig1s000ClinPharmR.pdf#page=91 Page: 91.0	no
CYP4A11 137	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022383Orig1s000ClinPharmR.pdf#page=91 Page: 91.0	no
UGT1A10 331	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022383Orig1s000ClinPharmR.pdf#page=91 Page: 91.0	no
UGT1A3 470	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022383Orig1s000ClinPharmR.pdf#page=91 Page: 91.0	no
UGT1A4 399	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022383Orig1s000ClinPharmR.pdf#page=91 Page: 91.0	no
UGT1A6 343	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022383Orig1s000ClinPharmR.pdf#page=91 Page: 91.0	no
UGT1A8 323	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022383Orig1s000ClinPharmR.pdf#page=91 Page: 91.0	no
UGT1A9 423	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022383Orig1s000ClinPharmR.pdf#page=91 Page: 91.0	no
UGT2B15 236	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022383Orig1s000ClinPharmR.pdf#page=91 Page: 91.0	no
UGT2B7 456	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022383Orig1s000ClinPharmR.pdf#page=91 Page: 91.0	no
P-gp 2052	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022383Orig1s000ClinPharmR.pdf#page=96 Page: 96.0	weak	yes (co-administration study) Comment: Co-administration of indacaterol with verapamil (P-gp inhibitor) showed 2 fold increase in indacaterol AUC0-24, and 1.5-fold increase in indacaterol Cmax; Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022383Orig1s000ClinPharmR.pdf#page=96 Page: 96.0
UGT1A1 479	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022383Orig1s000ClinPharmR.pdf#page=91 Page: 91.0	yes	weak (pharmacogenomic study) Comment: Nonsignificant trends toward higher Cmax and AUC0-24 (19% and 20%, respectively) were noted in patients with the (TA)7 genotype Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022383Orig1s000ClinPharmR.pdf#page=91 Page: 91.0
CYP3A4 1946	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022383Orig1s000ClinPharmR.pdf#page=91 Page: 91.0	yes	yes (co-administration study) Comment: Co-administration of indacaterol with erythromycin (CYP3A4 inhibitor) showed a 1.4-fold increase in indacaterol AUC0-24, and 1.2-fold increase in indacaterol Cmax; Co-administration of indacaterol with ketoconazole caused a 1.9-fold increase in indacaterol AUC0-24, and 1.3-fold increase in indacaterol Cmax; Co-administration of indacaterol with ritonavir resulted in a 1.7-fold increase in indacaterol AUC0-24 whereas indacaterol Cmax was unaffected. Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022383Orig1s000ClinPharmR.pdf#page=91 Page: 91.0

Tox targets

Target	Modality	Activity	Metabolite	Clinical evidence
hERG 2263	inhibitor 2237 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022383Orig1s000PharmR.pdf#page=46 Page: 46.0

Sourcing

Vendor/Aggregator	ID	URL
ChEBI	CHEBI:68575	https://www.ebi.ac.uk/chebi/searchId.do?chebiId=CHEBI:68575
ChemicalBook	CB72566367	https://www.chemicalbook.com/ChemicalProductProperty_EN_CB72566367
ChemicalBook	CB82512068	https://www.chemicalbook.com/ChemicalProductProperty_EN_CB82512068
MolPort	MolPort-023-219-171	https://www.molport.com/shop/molecule-link/MolPort-023-219-171
ZINC	ZINC000035801098	http://zinc15.docking.org/substances/ZINC000035801098

PubMed

Title	Date	PubMed
Ultra long-acting beta 2-agonists in development for asthma and chronic obstructive pulmonary disease.	2005 Jul	16022567
Gateways to clinical trials.	2006 Dec	17235418
Gateways to clinical trials.	2006 Jan-Feb	16541195
Gateways to clinical trials.	2006 May	16801985
Indacaterol Novartis/skyePharma.	2006 May	16729723
ultra-long-acting beta2-adrenoceptor agonists: an emerging therapeutic option for asthma and COPD?	2007	17352511
Safety, tolerability and efficacy of indacaterol, a novel once-daily beta(2)-agonist, in patients with COPD: a 28-day randomised, placebo controlled clinical trial.	2007	17088091
Gateways to clinical trials.	2007 Jan-Feb	17344945
Effect of indacaterol, a novel long-acting beta2-agonist, on isolated human bronchi.	2007 Mar	17135231
Indacaterol, a novel inhaled beta2-agonist, provides sustained 24-h bronchodilation in asthma.	2007 May	17251236
New approaches to managing asthma: a US perspective.	2008 Apr	18728834
Efficacy and safety of indacaterol, a new 24-hour beta2-agonist, in patients with asthma: a dose-ranging study.	2008 Dec	19085578
Pharmacological characterization of indacaterol, a novel once daily inhaled 2 adrenoceptor agonist, on small airways in human and rat precision-cut lung slices.	2008 Jan	17916760
Bronchodilator efficacy of indacaterol, a novel once-daily beta2-agonist, in patients with persistent asthma.	2008 Jul	18681090
Gateways to clinical trials.	2008 May	18773127
Gateways to clinical trials.	2008 Oct	19088949
Gateways to clinical trials.	2009 Apr	19536362
Bronchodilator effects of indacaterol and formoterol in patients with COPD.	2009 Dec	19465142
Effect of pre-contraction on β-adrenoceptor-mediated relaxation of rat urinary bladder.	2009 Dec	19449014
Lipid membrane interactions of indacaterol and salmeterol: do they influence their pharmacological properties?	2009 Dec 8	19819331
24-hour bronchodilator efficacy of single doses of indacaterol in subjects with COPD: comparison with placebo and formoterol.	2009 Feb	19192991
Gateways to clinical trials.	2009 Jan-Feb	19357798
Indacaterol, a novel inhaled, once-daily, long-acting beta2-agonist for the treatment of obstructive airways diseases.	2009 Jul	19609496
Indacaterol, A Novel Once Daily Inhaled beta2-Adrenoreceptor Agonist.	2009 Mar 12	19452036
Mometasone furoate: an effective anti-inflammatory with a well-defined safety and tolerability profile in the treatment of asthma.	2009 May	19392928
24-hour bronchodilator efficacy of single doses of indacaterol in patients with persistent asthma: comparison with placebo and formoterol.	2009 Oct	19650753
Gateways to clinical trials.	2009 Sep	19907722
Pharmacogenetic characterization of indacaterol, a novel beta 2-adrenoceptor agonist.	2009 Sep	19422388
The long-acting beta-adrenoceptor agonist, indacaterol, inhibits IgE-dependent responses of human lung mast cells.	2009 Sep	19371332
Cardiovascular safety of QVA149, a combination of Indacaterol and NVA237, in COPD patients.	2010 Dec	21166630
QVA149 demonstrates superior bronchodilation compared with indacaterol or placebo in patients with chronic obstructive pulmonary disease.	2010 Dec	20978028
Indacaterol: in chronic obstructive pulmonary disease.	2010 Dec 3	21080743
Novel bronchodilators in asthma.	2010 Jan	19816179
Integrating indacaterol dose selection in a clinical study in COPD using an adaptive seamless design.	2010 Jun	20080201
The short, the long and the "ultra-long": why duration of bronchodilator action matters in chronic obstructive pulmonary disease.	2010 Mar	20411368
[Indacaterol is a new once-daily beta2-agonist for treatment of COPD].	2010 Nov 22	21092722
Long-acting beta-agonists in the management of chronic obstructive pulmonary disease: current and future agents.	2010 Oct 29	21034447
Indacaterol provides 24-hour bronchodilation in COPD: a placebo-controlled blinded comparison with tiotropium.	2010 Oct 5	20920365
Onset of action of indacaterol in patients with COPD: comparison with salbutamol and salmeterol-fluticasone.	2010 Sep 7	20856830
An investigation into the structure-activity relationships associated with the systematic modification of the β(2)-adrenoceptor agonist indacaterol.	2012 Oct 1	22932315
Metabolism and pharmacokinetics of indacaterol in humans.	2012 Sep	22648561
Emerging Therapeutic Options for the Management of COPD.	2013	23641160
An update on LAMA/LABA combinations for COPD.	2017 Jan	28057707

Patents

Sample Use Guides

In Vivo Use Guide

The recommended dosage of Indacaterol is the once-daily inhalation of the contents of one 75 mcg Indacaterol capsule using the NEOHALER inhaler.

Route of Administration: Respiratory

In Vitro Use Guide

In the isolated tracheal strip preparation, indacaterol, demonstrated concentration-dependent inhibition of electrically induced contraction (EC50= 45 ± 13 nM)

Name

Type

Language

ARCAPTA NEOHALER

Preferred Name

English

INDACATEROL MALEATE

Official Name

English

INDACTEROL MALEATE

Common Name

English

QVA-149 COMPONENT INDACATEROL MALEATE

Common Name

English

INDACATEROL (AS MALEATE)

Common Name

English

2(1H)-QUINOLINONE, 5-((1R)-2-((5,6-DIETHYL-2,3-DIHYDRO-1H-INDEN-2-YL)AMINO)-1-HYDROXYETHYL )-8-HYDROXY-, (2Z)-2-BUTENEDIOATE (1:1)

Common Name

English

QABI49

Code

English

INDACATEROL MALEATE [MI]

Common Name

English

INDACATEROL MALEATE [EMA EPAR]

Common Name

English

INDACATEROL MALEATE [ORANGE BOOK]

Common Name

English

ULTIBRO COMPONENT INDACATEROL MALEATE

Brand Name

English

INDACATEROL MALEATE [MART.]

Common Name

English

QAB149-AFA

Code

English

INDACATEROL MALEATE [JAN]

Common Name

English

QAB-149-AFA

Code

English

INDACATEROL MALEATE [USAN]

Common Name

English

5-((1R)-2-((5,6-DIETHYL-2,3-DIHYDRO-1H-INDEN-2-YL)AMINO)-1-HYDROXYETHYL)-8- HYDROXYQUINOLIN-2(1H)-ONE HYDROGEN (2Z)-2-BUTENEDIOATE (SALT)

Common Name

English

Indacaterol maleate [WHO-DD]

Common Name

English

QVA149 COMPONENT INDACATEROL MALEATE

Common Name

English

Classification Tree Code System Code

EMA ASSESSMENT REPORTS

OSLIF BREEZHALER (AUTHORIZED: PULMONARY DISEASE, CHRONIC OBSTRUCTIVE)