Indacaterol

Indacaterol

Systematic (IUPAC) name
5-[2-[(5,6-Diethyl-2,3-dihydro-1H-inden-2-yl)amino]-1-hydroxyethyl]-8-hydroxyquinolin-2(1H)-one
Clinical data
Trade names	Onbrez, Arcapta
AHFS/Drugs.com	International Drug Names
Licence data	EMA:Link, US FDA:link
Pregnancy category	US: C (Risk not ruled out)
Legal status	UK: POM (Prescription only) US: ℞-only
Routes of administration	Inhalation
Identifiers
CAS Number	312753-06-3 Y
ATC code	R03AC18 (WHO)
PubChem	CID: 6433117
IUPHAR/BPS	7455
ChemSpider	5293751 Y
UNII	8OR09251MQ Y
KEGG	D09318 Y
ChEBI	CHEBI:68575 N
ChEMBL	CHEMBL1095777 Y
Chemical data
Formula	C24H28N2O3
Molecular mass	392.490 g/mol
SMILES O=C4/C=C\c1c(c(O)ccc1[C@@H](O)CNC3Cc2cc(c(cc2C3)CC)CC)N4
InChI InChI=1S/C24H28N2O3/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/h5-10,18,22,25,27-28H,3-4,11-13H2,1-2H3,(H,26,29)/t22-/m0/s1 Y Key:QZZUEBNBZAPZLX-QFIPXVFZSA-N Y
NY (what is this?)  (verify)

Indacaterol (INN) 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.

Clinical trials

A Phase III trial published in March 2010 examined the efficacy and safety of indacaterol in COPD patients. This study, conducted in the U.S., New Zealand, and Belgium, compared indacaterol dry-powder inhaler to placebo in 416 COPD patients, mostly moderate to severe (mean FEV₁ of 1.5 L). Indacaterol produced statistically improved FEV₁ (both trough and AUC) and decreased use of rescue medication compared to placebo, but with safety and tolerability similar to those of placebo.

A year-long, placebo-controlled trial published in July 2010 suggests indacaterol may be significantly more effective than twice-daily formoterol in improving FEV₁. There were some reductions in the need for rescue medication, but these were not significantly different; nor was there any difference in the rate of exacerbation between the 2 active treatments.

A study published in October, 2011 in the European Respiratory Journal compared indacaterol with tiotropium over the study period of 12 weeks. The study found no statistical difference between the effects of the two drugs on FEV₁. Indacaterol yielded greater improvements in transition dyspnoea index (TDI) total score and St. George’s Respiratory Questionnaire (SGRQ) total score.

A recent Cochrane Library meta-analysis indicates that the clinical benefit in lung function from indacaterol is at least as good as that seen with twice-daily long-acting beta2-agonists.