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 Table of Contents  
Year : 2015  |  Volume : 6  |  Issue : 2  |  Page : 175-177

Indacaterol: A novel, Inhaled Beta-2 agonist for COPD

1 Department of Pulmonary Medicine, King George's Medical University, Lucknow, Uttar Pradesh, India
2 Department of Pharmacology, GSVM Medical College, Kanpur, Uttar Pradesh, India

Date of Web Publication13-Jul-2015

Correspondence Address:
Dr. Arpita Singh
Department of Pharmacology, GSVM Medical College, Kanpur, Uttar Pradesh
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Source of Support: None, Conflict of Interest: None

DOI: 10.4103/0975-9727.160709

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How to cite this article:
Prakash V, Singh A, Singh A, Kant S, Verma AK, Bhatia A. Indacaterol: A novel, Inhaled Beta-2 agonist for COPD. Muller J Med Sci Res 2015;6:175-7

How to cite this URL:
Prakash V, Singh A, Singh A, Kant S, Verma AK, Bhatia A. Indacaterol: A novel, Inhaled Beta-2 agonist for COPD. Muller J Med Sci Res [serial online] 2015 [cited 2023 Mar 25];6:175-7. Available from: https://www.mjmsr.net/text.asp?2015/6/2/175/160709

Chronic Obstructive Pulmonary Disease (COPD) is one of the most common chronic respiratory diseases affecting the world. According to the 12-site Burden of Obstructive Lung Diseases (BOLD) study, the worldwide overall prevalence of COPD is 10.1%, with wide variation. [1] The prevalence of COPD in India, according to the Indian Study on Epidemiology of Asthma, Respiratory Symptoms and Chronic Bronchitis in Adults (INSEARCH) I and II, was 3.67%. [2] COPD is the 6 th leading cause of death worldwide and is projected to become the 4 th leading cause by 2020. [3]

Despite this high prevalence of disease, the treatment options for COPD are limited. The mainstay of treatment are bronchodilators, which cause airway smooth muscle relaxation, leading to bronchodilation, improvement in Forced Expiratory Volume in 1 st second (FEV1) and decrease air trapping and dynamic hyperinflation. The bronchodilators which are currently being used are short and long acting beta-agonists (LABA), anticholinergics, methlxanthines and newer modalities like PDE-4 (phosphodiesterase-4) inhibitors such as rofumilast along with inhaled corticosteroids (ICS) as the major anti-inflammatory agent. The short acting drugs are used for rescue of symptoms while the long acting agents are used as maintenance therapy. The choice of agents in a particular patient is variable according to individual response, cost, side-effect profile and availability.

  Need for a New Drug Top

All the available bronchodilators have a short duration of action. The short acting beta-agonists like salbutamol work for 2-4 hours, while the long acting agents like salmeterol and formeterol work for 12 hours, thus requiring twice daily dosing. Similarly, the short acting anticholinergics (ipratropium) work for 6 hours and the long acting agent acts for -24 hours. This twice-daily dosing schedule is inconvenient for the patients and decreases compliance and adherence. [4]

A once daily dosing of inhaled therapy provides patients with sustained bronchodilation, greater convenience, improves adherence and has better clinical outcomes. It is also preferred by the chronically ill patients. [5]

The onset of action of the available long acting agents is slow. It has been shown that the onset of bronchodilation plays an important role in the relief of symptoms in patients of asthma and COPD. [6],[7] So, a new drug is the need of the hour which combines fast onset with once daily dosing.

  About Indacaterol Top

Indacaterol is a novel, inhaled beta-2 adrenoceptor agonist. It is a full agonist at beta-2 and beta-3 and a weak partial agonist at beta-1. [8],[9] It has a lower beta-1/beta-2 selectivity ratio, but for an equivalent degree of bronchoprotection, indacaterol has a better cardiac safety profile than formeterol, salmeterol and salbutamol. [10] In various studies, it has been found that indacaterol attains rapid bronchodilation within 5 minutes, its onset of action is comparable to salbutamol and formeterol, [10] and faster than salmeterol. [11]

It has a duration of action compatible with once-daily dosing regimen in both in vitro and in vivo studies. [10],[11],[12] This 24 hour duration of action is related to its affinity for lipid membranes, which act as a depot for lipophillic ligands, maintaining high concentration of the drug at the receptor site, even when the bulk of the compound has been washed out of the lung. [13]

There is no tachyphylaxis with indacaterol, so tolerance does not develop. It is generally well tolerated and demonstrates a good overall safety profile.

In the INLIGHT I study, [14] to confirm the efficacy and safety of Indacaterol 150 μg once daily for 12 weeks in patients with moderate to severe COPD, Indacaterol demonsrated significantly higher peak FEV1, than placebo.

The INHANCE study had 3 stages. The 1 st stage used pre-set criteria to select 2 Indacaterol doses (150 μg and 300 μg) after 14 days of treatment[15] to be used in the 6 month stage, which included an open label tiotropium arm. [16] In the 3 rd stage, comprising of another 6 months, efficacy and safety were studied. Trough FEV1 at week 12 increased versus placebo with both Indacaterol doses and the changes in FEV1 were maintained through the course of the study. The difference between Indacaterol and tiotropium was significant. These results were supported by other similar studies.

Regarding patient related outcomes, 3 randomised controlled trials were performed, comparing the effect of placebo, tiotropium, formeterol and salbutamol with Indacaterol. Indacaterol achieved consistent improvement in dysnea, significant reduction in as-needed use of salbutamol and improvement in health status of patients. Also, time to first exacerbation and exercise endurance was increased with Indacaterol. [17],[18],[19]

  Future Directions Top

COPD is a gradually progressive, irreversible disease and till date, no treatment modality has been found to reverse or prevent disease progression. With increasing knowledge of the pathophysiology and cellular mechanisms responsible for the disease development and progression, newer modalities of treatment are under way.

Other than Indacaterol, other once daily inhaled beta-2 agonists like vilanterol, olodaterol and carmoterol are now in clinical development. [20] Other long acting anticholinergics like aclidinium bromide and glycopyrrolate are also under development. [21],[22]

Since LABA monotherapy is discouraged in asthma, Indacaterol is not suitable for use in asthma patients. For such patients, combination inhalers of Indacaterol with ICS as a fixed dose once daily inhaler are under study. [23]

Combination inhalers with LABA and long acting anticholinergics (LAMA) are also under development as there is an additive effect between these 2 bronchodilators. [24]

Other drugs under development are anti-inflammatory agents like anti-proteases, anti-oxidants, PDE-4 inhibitors and drugs causing reversal of steroid resistance.

  Conclusion Top

In conclusion, with better understanding of COPD pathogenesis, more research needs to be done for the development of newer agents, both for the reversal of disease progression and for better clinical outcomes.

  References Top

Buist AS, McBurnie MA, Vollmer WM, Gillespie S, Burney P, Mannino DM, et al.; BOLD Collaborative Research Group. International variation in the prevalence of COPD (The BOLD Study): A population-based prevalence study. Lancet 2007;370:741-50.  Back to cited text no. 1
Gupta D, Agarwal R, Agarwal AN, Mathur VN, Dhooria S, Prasad KT, et al.; S. K. Jindal for the COPD Guidelines Working Group. Guidelines for diagnosis and management of chronic obstructive pulmonary disease: Joint ICS/NCCP(I) recommendations. Lung India 2013;30:228-67.  Back to cited text no. 2
Global Initiative for Chronic Obstructive Lung Disease (GOLD). Global Strategy for the Diagnosis, Management and Prevention of COPD, 2014. Available from: http://www.goldcopd.org/. [Last accessed on 2014 Aug 14].   Back to cited text no. 3
Breeekveldt-Postma NS, Koerselman J, Erkens JA, Lammers JW, Herings RM. Enhanced persistence with tiotropium compared with other respiratory drugs in COPD. Respir Med 2009;101:1398-405.  Back to cited text no. 4
Campbell LM. Once-daily inhaled corticosteroids in mild to moderate asthma: Improving acceptance of treatment. Drugs 1999;58(Suppl 4):25-33; discussion 52.  Back to cited text no. 5
Van der Woude HJ, Postma DS, Politiek MJ, Winter TH, Aalbers R. Releif of dyspnoea by beta2-agonists after methacholine-induced bronchoconstriction. Respir Med 2004;98:816-20.  Back to cited text no. 6
Welte T, Miravitlles M, Hernandez P, Eriksson G, Peterson S, Polanowski T, et al. Efficacy and tolerability of budesonide/formeterol added to tiotropium in patients with chronic obstructive pulmonary disease. Am J Respir Crit Care Med 2009;180:741-50.  Back to cited text no. 7
Sayers I, Hawley J, Stewart CE, Billington CK, Henry A, Leighton-Davies JR, et al. Pharmacogenetic characterization of indacaterol, a novel beta 2-adrenoceptor agonist. Br J Pharmacol 2009;158:277-86.  Back to cited text no. 8
Rosenthorne EM, Turner RJ, Fairhurst RA, Charlton SJ. Efficacy is a contributing factor to the clinical onset of bronchodilation of inhaled beta(2)-adrenoceptor agonists. Naunyn Schmiedebergs Arch Pharmacol 2010;382:255-63.  Back to cited text no. 9
Battram C, Charlton SJ, Cuenoud B, Dowling MR, Fairhurst RA, Farr D, et al. In vitro and in vivo pharmacological characterization of 5-[(R)-2-(5,6-diethyl-indan-2-ylamino)-1-hydroxy-ethyl]-8-hydroxy-1H-quinolin-2-one (indacaterol), a novel inhaled beta(2) adrenoceptor agonist with a 24-h duration of action. J Pharmacol ExpTher 2006;317:762-70.  Back to cited text no. 10
Naline E, Trifilieff A, Fairhurst RA, Advenier C, Molimard M. Effect of indacaterol, a novel long-acting beta2-agonist, on isolated human bronchi. Eur Respir J 2007;29:575-81.  Back to cited text no. 11
Sturton RG, Trifilieff A, Nicholson AG, Barnes PJ. Pharmacological characterization of indacaterol, a novel once daily inhaled 2 adrenoceptor agonist, onsmall airways in human and rat precision-cut lung slices. J Pharmacol ExpTher 2008;324:270-5.  Back to cited text no. 12
Anderson GP, Linden A, Rabe KF. Why are long-acting beta-adrenoceptor agonists long-acting? Eur Respir J 1994;7:569-78.  Back to cited text no. 13
Feldman G, Siler T, Prasad N, Jack D, Piggott S, Owen R, et al. INLLIGHT 1 Study Group. Efficacy and safety of indacaterol 150 microg once daily in COPD: A double blind, randomised, 12-week study. BMC Pulm Med 2010;10:11.  Back to cited text no. 14
Barnes PJ, Poock SJ, Magnussen H, Iqbal A, Kramer B, Higgins M, et al. Integrating indacaterol dose selection in a clinical study in COPD using an adaptive seamless design. Pulm Pharmacol Ther 2010;23:165-71.  Back to cited text no. 15
Donohue JF, Fogarty C, Lötvall J, Mahler DA, Worth H, Yorgancioglu A, et al. INHANCE Study Investigators. Once daily bronchodilators for chronic obstructive pulmonary disease: Indacaterol versus tiotropium. Am J Respir Crit Care Med 2010;182:155-62.  Back to cited text no. 16
Hanania NA, Darken P, Horstman D, Reisner C, Lee B, Davis S, et al. The efficacy and safety of fluticasone propionate (250 microg)/salmeterol (50 microg) combined in the diskus inhaler for the treatment of COPD. Chest 2003;124:834-43.  Back to cited text no. 17
Casaburi R, Mahler DA, Jones PW, Wanner A, San PG, ZuWallack RL, et al. A long-term evaluation of once-daily inhaled tiotropium in chronic obstructive pulmonary disease. Eur Respir J 2002;19:217-24.  Back to cited text no. 18
Fabri LM, Calverley PM, Izquierdo-Alonso JL, Bundschuh DS, Brose M, Martinez FJ, et al.; M2-127 and M2-128 study groups. Roflumilast in moderate-to-severe chronic obstructive pulmonary disease treated with longacting bronchodilators: Two randomised clinical trials. Lancet 2009;374:695-703.  Back to cited text no. 19
Cazzola M, Matera MG. Emaeging inhaled bronchodilators: An update. Eur Respir J 2009;34;757-69.  Back to cited text no. 20
Hansel TT, Neighbour H, Erin EM, Tan AJ, Tennant RC, Maus JG, et al. Glycopyrrolate causes prolonged bronchoprotection and bronchodilation in patients with asthma. Chest 2005;128:1974-9.  Back to cited text no. 21
Cazzola M. Aclidinium bromide, a novel long acting muscarinic M3 antagonist for the treatment of COPD. Curr Opin Investig Drugs 2009;10:482-90.  Back to cited text no. 22
Partridge MR, Schuermann W, Beckman O, Persson T, Polanowski T. Effect on lung function and morning activities of budesonide/formoterol versus salmeterol/fluticasone in patients with COPD. Ther Adv Respir Dis 2009;3:1-11.  Back to cited text no. 23
van Noord JA, Buhl R, Laforce C, Martin C, Jones F, Dolker M, et al. QVA149 demonstrates superior bronchodilation compared with indacaterol or placebo in patients with chronic obstructive pulmonary disease. Thorax 2010;65:1086-91.  Back to cited text no. 24


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