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Indacaterol pp 67–76Cite as

The Early Clinical Development of Indacaterol

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Part of the book series: Milestones in Drug Therapy ((MDT))

Abstract

Indacaterol is a novel once-daily β2-adrenoceptor agonist developed for the treatment of obstructive airway diseases. While indacaterol is now approved for the maintenance treatment of chronic obstructive pulmonary disease (COPD) in several countries worldwide, the early clinical development of indacaterol was conducted in both asthma and COPD patients. During these early clinical studies, the bronchodilator profile of action on patients with established airflow obstruction was investigated, including duration and onset of action, optimal dosage and delivery, and safety. The early clinical development of indacaterol confirmed preclinical data characterizing indacaterol as a long-acting β2-agonist with a sustained 24 h duration of bronchodilation, thus suitable for once-daily dosing, a rapid onset of action and a favourable safety profile over a range of dosages and delivery modes, both in asthma and COPD patients of various severities.

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References

  1. Bateman ED, Hurd SS, Barnes PJ, Bousquet J, Drazen JM, Fitzgerald M et al (2008) Global strategy for asthma management and prevention: GINA executive summary. Eur Respir J 31:143–78

    Article  PubMed  CAS  Google Scholar 

  2. Rabe KF, Jörres R, Nowak D, Behr N, Magnussen H (1993) Comparison of the effects of salmeterol and formoterol on airway tone and responsiveness over 24 hours in bronchial asthma. Am Rev Respir Dis 147:1436–41

    Article  PubMed  CAS  Google Scholar 

  3. Vestbo J, Hurd SS, Agustí AG, Jones PW, Vogelmeier C, Anzueto A, Barnes PJ, Fabbri LM, Martinez FJ, Nishimura M, Stockley RA, Sin DD, Rodriguez-Roisin R (2013) Global strategy for the diagnosis, management, and prevention of chronic obstructive pulmonary disease: GOLD executive summary. Am J Respir Crit Care Med 187(4):347–65.

    Article  PubMed  CAS  Google Scholar 

  4. Maltais F, Hamilton A, Marciniuk D, Hernandez P, Sciurba FC, Richter K et al (2005) Improvements in symptom-limited exercise performance over 8 h with once-daily tiotropium in patients with COPD. Chest 128:1168–78

    Article  PubMed  CAS  Google Scholar 

  5. O’Donnell DE, Fluege T, Gerken F, Hamilton A, Webb K, Aguilaniu B et al (2004) Effects of tiotropium on lung hyperinflation, dyspnoea and exercise tolerance in COPD. Eur Respir J 23:832–40

    Article  PubMed  Google Scholar 

  6. Tashkin DP, Celli BR, Senn S, Burkhart D, Kesten S, Menjoge SS et al (2008) A 4-year trial of tiotropium in chronic obstructive pulmonary disease. N Engl J Med 359:1543–53

    Article  PubMed  CAS  Google Scholar 

  7. Vincken W, Van Noord JA, Greefhorst APM, Bantje TA, Kesten S, Korducki L et al (2002) Improved health outcomes in patients with COPD during 1 year treatment with tiotropium. Eur Respir J 19:209–16

    Article  PubMed  CAS  Google Scholar 

  8. Vogelmeier C, Hederer B, Glaab T, Schmidt H, Rutten-van Moelken MPMH, Beeh KM et al (2011) Tiotropium versus salmeterol for the prevention of exacerbations of COPD. N Engl J Med 364:1093–103

    Article  PubMed  CAS  Google Scholar 

  9. Breekveldt-Postma NS, Koerselman J, Erkens JA, Lammers JW, Herings RM (2009) Enhanced persistence with tiotropium compared with other respiratory drugs in COPD. Respir Med 101:1398–405

    Article  Google Scholar 

  10. Campbell LM (1999) Once-daily inhaled corticosteroids in mild to moderate asthma: improving acceptance of treatment. Drugs 58:25–33

    Article  PubMed  CAS  Google Scholar 

  11. van der Woude HJ, Postma DS, Politiek MJ, Winter TH, Aalbers R (2004) Relief of dyspnoe by beta2-agonists after methacholine-induced bronchoconstriction. Respir Med 98:816–20

    Article  PubMed  Google Scholar 

  12. Welte T, Miravitlles M, Hernandez P, Eriksson G, Peterson S, Polanowski T et al (2009) Efficacy and tolerability of budesonide/formoterol added to tiotropium in patients with chronic obstructive pulmonary disease. Am J Respir Crit Care Med 180:741–50

    Article  PubMed  CAS  Google Scholar 

  13. Nelson HS (2006) The salmeterol multicentre asthma research trial: a comparison of usual pharmacotherapy for asthma or usual pharmacotherapy plus salmeterol. Chest 129:15–26

    Article  PubMed  CAS  Google Scholar 

  14. Battram C, Charlton SJ, Cuenoud B, Dowling MR, Fairhurst RA, Farr D et al (2006) 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 Exp Ther 317:762–70

    Article  PubMed  CAS  Google Scholar 

  15. Naline E, Trifilieff A, Fairhurst RA, Advenier C, Molimard M (2007) Effect of indacaterol, a novel long-acting beta2-agonist, on isolated human bronchi. Eur Respir J 29:575–81

    Article  PubMed  CAS  Google Scholar 

  16. Sturton RG, Trifilieff A, Nicholson AG, Barnes PJ (2008) Pharmacological characterization of indacaterol, a novel once daily inhaled beta2 adrenoceptor agonist, on small airways in human and rat precision cut slices. J Pharmacol Exp Ther 324:270–5

    Article  PubMed  CAS  Google Scholar 

  17. Tarral A, Fauchoux N, Knight H, Perry S, Wood J, Brookman L (2005) Safety and tolerability of multiple-dose indacaterol, a novel 2-agonist, in patients with mild asthma. Eur Respir J 26(Suppl 49):253s

    Google Scholar 

  18. Duvauchelle T, Elharrar B, Knight H, Krebbs-Brown A, Perry S (2005) Single-dose indacaterol, a novel 24-hour ·2-agonist, is well tolerated in patients with mild asthma. Eur Respir J 26(Suppl 49):253s

    Google Scholar 

  19. Perry S, Woessner R, Kaiser G, Campestrini J, Picard F, Khindri S et al (2010) Pharmakokinetics of indacaterol after single and multiple inhaled doses. Am J Respir Crit Care Med 181:A4420

    Google Scholar 

  20. Beeh KM, Derom EY, Kanniess F, Cameron R, Higgins M, van As A (2007) Indacaterol, a novel once-daily ·2-agonist, provides sustained 24-hour bronchodilator efficacy in asthma. Eur Respir J 29:871–8

    Article  PubMed  CAS  Google Scholar 

  21. Pearlman DS, Greos L, LaForce C, Orevillo CJ, Owen R, Higgins M (2008) Bronchodilator efficacy of indacaterol, a novel once-daily beta2-agonist, in patients with persistent asthma. Ann Allergy Asthma Immunol 101:90–5

    Article  PubMed  CAS  Google Scholar 

  22. LaForce C, Korenblat P, Osborne P, Dong F, Higgins M (2009) 24-hour bronchodilator efficacy of single doses of indacaterol in patients with persistent asthma: comparison with placebo and formoterol. Curr Med Res Opin 25:2353–9

    Article  PubMed  CAS  Google Scholar 

  23. Sugihara N, Kanada S, Haida M, Ichinose M, Adachi M, Hosoe M et al (2010) 24-h bronchodilator efficacy of single doses of indacaterol in Japanese patients with asthma: a comparison with placebo and salmeterol. Respir Med 104:1629–37

    Article  PubMed  Google Scholar 

  24. LaForce C, Alexander M, Deckelmann R, Fabbri LM, Aisanov Z, Cameron R et al (2008) Indacaterol provides sustained 24 h bronchodilation on once-daily dosing in asthma: a 7-day dose-ranging study. Eur J Allergy Clin Immunol 63:103–11

    Article  CAS  Google Scholar 

  25. Kanniess F, Cameron R, Owen R, Higgins M (2008) Indacaterol, a novel 24-hour 2-agonist, demonstrates 24-hour efficacy and is well tolerated in patients with asthma. A multiple-dose, dose-ranging study. J Asthma 45:887–92

    Article  PubMed  CAS  Google Scholar 

  26. Chuchalin A, Tsoi AN, Richter K, Krug N, Dahl R, Luursema PB et al (2007) Safety and tolerability of indacaterol in asthma: a randomized, placebo-controlled 28-day study. Respir Med 101:2065–75

    Article  PubMed  Google Scholar 

  27. Brookman L, Knowles LJ, Barbier M, Elharrar B, Fuhr R, Pascoe S (2007) Efficacy and safety of single therapeutic and supratherapeutic doses of indacaterol versus salmeterol and salbutamol in patients with asthma. Curr Med Res Opin 23:3113–22

    Article  PubMed  CAS  Google Scholar 

  28. Castle W, Fuller R, Hall J, Palmer J (1993) Serevent nationwide surveillance study comparison of salmeterol with salbutamol in asthmatic patients who require regular bronchodilator treatment. Br Med J 306:1034–7

    Article  CAS  Google Scholar 

  29. Nelson HS (2006) Is there a problem with inhaled long-acting beta-adrenergic agonists? J Allergy Clin Immunol 117:3–16

    Article  PubMed  CAS  Google Scholar 

  30. Bousquet J (2009) Mometasone furoate: an effective anti-inflammatory with a well-defined safety and tolerability profile in the treatment of asthma. Int J Clin Pract 63:806–19

    Article  PubMed  CAS  Google Scholar 

  31. Bauwens O, Ninane V, van de Maele B, Firth R, Dong F, Owen R et al (2009) 24-hour bronchodilator efficacy of single doses of indacaterol in subjects with COPD: comparison with placebo and formoterol. Curr Med Res Opin 25:463–70

    Article  PubMed  CAS  Google Scholar 

  32. Rennard S, Bantje T, Centanni S, Chanez P, Chuchalin A, D’Urzo A et al (2008) A dose-ranging study of indacaterol in obstructive airways disease, with a tiotropium comparison. Respir Med 102:1033–44

    Article  PubMed  Google Scholar 

  33. Beier J, Chanez P, Martinot JB, Schreurs AJM, Tkacova R, Bao W et al (2007) Safety, tolerability and efficacy of indacaterol, a novel once-daily·2-agonist, in patients with COPD: a 28-day randomised, placebo-controlled clinical trial. Pulm Pharmacol Ther 20:740–9

    Article  PubMed  CAS  Google Scholar 

  34. Yang WH, Martinot JB, Pohunek P, Beier J, Magula D, Cameron R et al (2007) Tolerability of indacaterol, a novel once-daily ·2-agonist, in patients with asthma: a randomized, placebo-controlled, 28-day safety study. Ann Allergy Asthma Immunol 99:555–61

    Article  PubMed  CAS  Google Scholar 

  35. Cazzola M, MacNee W, Martinez FJ, Rabe KF, Franciosi LG, Barnes PJ et al (2008) Outcomes for COPD pharmacological trials: from lung function to biomarkers. Eur Respir J 31:416–68

    Article  PubMed  CAS  Google Scholar 

  36. Beier J, Beeh KM, Pascoe S, Brookman L, Peachey G, Hmissi A (2009) Bronchodilator effects of indacaterol and formoterol in patients with COPD. Pulm Pharmacol Ther 22:492–6

    Article  PubMed  CAS  Google Scholar 

  37. Beeh KM, Wagner F, Khindri S, Drollmann AF (2011) Effect of indacaterol on dynamic lung hyperinflation and breathlessness in hyperinflated patients with COPD. COPD 8:340–5

    Article  PubMed  Google Scholar 

  38. O’Donnell DE, Casaburi R, Vincken W, Puente-Maestu L, Swales J, Lawrence D et al (2011) Effect of indacaterol on exercise endurance and lung hyperinflation in COPD. Respir Med 105:1030–6

    Article  PubMed  Google Scholar 

  39. Khindri S, Sabo R, Harris S, Woessner R, Jennings S, Drollmann AF (2011) Cardiac safety of indacaterol in healthy subjects: a randomized, multidose, placebo- and positive-controlled, parallel-group thorough QT study. BMC Pulm Med 11:31

    Article  PubMed  CAS  Google Scholar 

  40. Pascoe S, Reynolds C, Pleskow W, Perry S, Hmissi A, Kaiser G et al (2011) Safety, tolerability and pharmacokinetics of single escalating doses of indacaterol, a once-daily beta2-agonist bronchodilator, in subjects with COPD. Int J Clin Pharmacol 49:153–61

    Article  CAS  Google Scholar 

  41. Barnes PJ, Pocock SJ, Magnussen H, Iqbal A, Kramer B, Higgins M, Lawrence D (2010) Integrating indacaterol dose selection in a clinical study in COPD using an adaptive seamless design. Pulm Pharmacol Ther 23:165–71

    Article  PubMed  CAS  Google Scholar 

  42. Donohue JF, Fogarty C, Lotvall J, Mahler DA, Worth H, Yorgancioglu A et al (2010) Once-daily bronchodilators for chronic obstructive pulmonary disease: indacaterol versus tiotropium. Am J Respir Crit Care Med 182:155–62

    Article  PubMed  CAS  Google Scholar 

  43. Chapman KR, Rennard SI, Dogra A, Owen R, Lassen C, Kramer B (2011) Long-term Safety and Efficacy of indacaterol, a novel long-acting beta 2-agonist, in subjects with COPD: a randomized, placebo-controlled study. Chest 140:68–75

    Article  PubMed  CAS  Google Scholar 

  44. Kerwin EM, Gotfried MH, Lawrence D, Lassen C, Kramer B (2011) Efficacy and tolerability of indacaterol 75 μg once daily in patients aged ≥40 years with chronic obstructive pulmonary disease: results from 2 double-blind, placebo-controlled 12-week studies. Clin Ther 33:1974–84

    Article  PubMed  CAS  Google Scholar 

  45. Dahl R, Chung KF, Buhl R, Magnussen H, Nonikov V, Jack D et al (2010) Efficacy of a new once-daily long-acting inhaled beta2-agonist indacaterol versus twice-daily formoterol in COPD. Thorax 65:473–9

    Article  PubMed  Google Scholar 

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Author information

Authors and Affiliations

  1. Insaf Respiratory Research Institute GmbH, Biebricher Allee 34, 65187, Wiesbaden, Germany

    Jutta Beier & Kai M. Beeh

Authors
  1. Jutta Beier
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  2. Kai M. Beeh
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Correspondence to Kai M. Beeh .

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Editors and Affiliations

  1. Respiratory Diseases Area, Novartis Institutes for BioMedical Reseach, Basel, Switzerland

    Alexandre Trifilieff

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Beier, J., Beeh, K.M. (2014). The Early Clinical Development of Indacaterol. In: Trifilieff, A. (eds) Indacaterol. Milestones in Drug Therapy. Springer, Basel. https://doi.org/10.1007/978-3-0348-0709-8_4

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