Long-acting beta-agonists and their association with inhaled corticosteroids in COPD

Current Medicinal Chemistry

Volumn 20, Issue 12, 2013, Pages 1477-1495

  Fuso, L ^a   Mores, N ^b   Valente, S ^a   Malerba, M ^c   Montuschi, P ^b  

^a CATHOLIC UNIVERSITY   (Italy)

^b CATHOLIC UNIVERSITY   (Italy)

^c UNIVERSITY OF BRESCIA   (Italy)

Author keywords

Beta2 adrenergic receptors; Chronic obstructive pulmonary disease; Formoterol; Inhaled bronchodilators; Inhaled corticosteroids; Inhaled long acting beta agonist inhaled corticosteroid combinations; Inhaled long acting beta2 agonists; Salmeterol; Ultra long acting beta agonists

Indexed keywords

ABEDITEROL; ARFORMOTEROL; BECLOMETASONE DIPROPIONATE PLUS FORMOTEROL FUMARATE; BETA 2 ADRENERGIC RECEPTOR STIMULATING AGENT; BUDESONIDE; BUDESONIDE PLUS FORMOTEROL; CARMOTEROL; CORTICOSTEROID; FENOTEROL; FLUTICASONE FUROATE; FLUTICASONE PROPIONATE PLUS SALMETEROL; FORMOTEROL; INDACATEROL; MILVETEROL; MUSCARINIC RECEPTOR BLOCKING AGENT; OLODATEROL; PF 610355; PLACEBO; SALBUTAMOL; SALMETEROL; TIOTROPIUM BROMIDE; TIOTROPIUM PLUS FORMOTEROL; UNCLASSIFIED DRUG; VILANTEROL; VILANTEROL TRIFENATATE;

ARTICLE; BRONCHODILATATION; CHRONIC OBSTRUCTIVE LUNG DISEASE; CLINICAL EFFECTIVENESS; DISEASE COURSE; DRUG BIOAVAILABILITY; DRUG EFFICACY; DRUG STRUCTURE; EXERCISE TOLERANCE; FUNCTIONAL RESIDUAL CAPACITY; HEART ARRHYTHMIA; HUMAN; IN VITRO STUDY; IN VIVO STUDY; LUNG FUNCTION; MONOTHERAPY; MORTALITY; PRACTICE GUIDELINE; QUALITY OF LIFE; RISK ASSESSMENT; STRUCTURE ACTIVITY RELATION; SUPRAVENTRICULAR TACHYCARDIA; TACHYCARDIA; TREMOR;

ADMINISTRATION, INHALATION; ADRENAL CORTEX HORMONES; ADRENERGIC BETA-AGONISTS; ANIMALS; BRONCHODILATOR AGENTS; DRUG THERAPY, COMBINATION; HUMANS; LUNG; PULMONARY DISEASE, CHRONIC OBSTRUCTIVE; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 84877672552     PISSN: 09298673     EISSN: 1875533X     Source Type: Journal    
DOI: 10.2174/0929867311320120003     Document Type: Article

References (163)

1. Global Strategy for the Diagnosis, Management and Prevention of COPD, Global Initiative for Chronic Obstructive Lung Disease (GOLD) 2011. Available from: Www.goldcopd.org.
2. Palmqvist, M.; Persson, G.; Lazer, L.; Rosenborg, J.; Larsson, P.; Lotvall, J. Inhaled dry-powder formoterol and salmeterol in asthmatic patients: Onset of action, duration of effect and potency. Eur. Respir. J. 1997, 10, 2484-2489.
3. Johnson, M. The-2-adrenoceptor. Am. J. Respir. Crit. Care Med., 1998, 158, S146-S153.
4. Cave, A.C.; Hurst, M.M. The use of long acting-2-agonists, alone or in combination with inhaled corticosteroids, in Chronic Obstructive Pulmonary Disease (COPD). Pharmacol. Ther., 2011, 130, 114-143.
5. Procopiou, P.A.; Barrett, V.J.; Bevan, N.J.; Biggadike, K.; Butchers, P.R.; Coe, D.M.; Conroy, R.; Edney, D.D.; Field, R.N.; Ford, A.J.; Guntrip, S.B.; Looker, B.E.; McLay, I.M.; Monteith, M.J.; Morrison, V.S.; Mutch, P.J.; Richards, S.A.; Sasse, R.; Smith, C.E. Synthesis and structure-activity relationships of long-acting beta2 adrenergic receptor agonists incorporating arylsulfonamide groups. J. Med. Chem., 2009, 52, 2280-2288.
6. Molimard, M.; Naline, E.; Zhang, Y.; Le Gros; V.; Begaud, B.; Advenier, C. Long and short acting beta2 adrenoceptor agonists: Interactions in human contracted bronchi. Eur. Respir. J., 1998, 11, 583-588.
7. Cazzola, M.; Matera, M. G.; Santangelo, G.; Vinciguerra, A.; Rossi, F.; D'Amato, G. Salmeterol and formoterol in partially reversible severe chronic obstructive pulmonary disease: A dose-response study. Respir. Med., 1995, 89, 357-362.
8. Cazzola, M.; Santangelo, G.; Piccolo, A.; Salzillo, A.; Matera, M. G.; D'Amato, G.; Rossi F. Effect of salmeterol and formoterol in patients with chronic obstructive pulmonary disease. Pulm. Pharmacol., 1994, 7, 103-107.
9. Steiropoulos, P.; Papanas, N.; Nena, E.; Kouros, D. Indacaterol: A new long-acting-2-agonist in the management of chronic obstructive pulmonary disease. Expert Opin. Pharmacother., 2012, 13, 1015-1029.
10. Baur, F.; Beattie, D.; Beer, D.; Bentley, D.; Bradley, M.; Bruce, I.; Charlton, S.J.; Cuenoud, B.; Ernst, R.; Fairhurst, R.A.; Faller, B.; Farr, D.; Keller, T.; Fozard, J.R.; Fullerton, J.; Barman, S.; Hatto, J.; Hayden, C.; He, H.; Howes, C.; Janus, D.; Jiang, Z.; Lewis, C.; Loeuillet-Ritzler, F.; Moser, H.; Reilly, J.; Steward, A.; Sykes, D.; Tedaldi, L.; Trifilieff, A.; Tweed, M.; Watson, S.; Wissler, E.; Wyss, D. The identification of indacaterol as an ultra long-acting inhaled beta2-adrenoceptor agonist. J. Med. Chem., 2010, 53, 3675-3684.
11. Szczuka, A.; Wennerberg, M.; Packeu, A.; Vauquelin, G. Molecular mechanisms for the persistent bronchodilatory effect of the beta2-adrenoceptor agonist salmeterol. Br. J. Pharmacol., 2009, 158, 183-194.
12. Anderson, G.P. Formoterol: Pharmacology, molecular basis of agonism, and mechanism of long duration of a highly potent and selective beta2-adrenoceptor agonist bronchodilator. Life Sci., 1993, 52, 2145-2160.
13. Anderson, G.P.; Lindén, A.; Rabe, K.F. Why are long-acting betaadrenoceptor agonists long-acting? Eur. Respir. J., 1994, 7, 569-578.
14. Rhodes, D.G.; Newton, R.; Butler, R.; Herbette, L. Equilibrium and kinetic studies of the interactions of salmeterol with membrane bilayers. Mol. Pharmacol., 1992, 42, 596-602.
15. Bergendal, A.; Lindén, A.; Skoogh, B.E.; Gerspacher, M.; Anderson, G.P.; Löfdahl, C.G. Extent of salmeterol-mediated reassertion of relaxation in guinea-pig trachea pretreated with aliphatic side chain structural analogues. Br. J. Pharmacol., 1996, 117, 1009-1115.
16. Johnson, M. Beta2-adrenoceptors: Mechanisms of action of beta2-agonists. Paediatr. Respir. Rev., 2001, 2, 57-62.
17. Johnson, M.; Butchers, P.R.; Coleman, R.A.; Nials, A.T.; Strong, P.; Sumner, M.J.; Vardey, C.J.; Whelan, C.J. The pharmacology of salmeterol. Life Sci., 1993, 52, 2131-2143.
18. Coleman, R.A.; Johnson, M.; Nials, A.T.; Vardey, C.J. Exosites: Their current status, and their relevance to the duration of action of long-acting beta2-adrenoceptor agonists. Trends Pharmacol. Sci., 1996, 17, 324-330.
19. Teschemacher, A.; Lemoine, H. Kinetic analysis of drug-receptor interactions of long-acting beta2 sympathomimetics in isolated receptor membranes: Evidence against prolonged effects of salmeterol and formoterol on receptor-coupled adenylyl cyclase. J. Pharmacol. Exp. Ther., 1999, 288, 1084-1092.
20. Austin, R.P.; Barton, P.; Bonnert, R.V.; Brown, R.C.; Cage, P.A.; Cheshire, D.R.; Davis, A.M.; Dougall, I.G.; Ince, F.; Pairaudeau, G.; Young, A. QSAR and the rational design of long-acting dual D2-receptor/beta2-adrenoceptor agonists. J. Med. Chem., 2003, 46, 3210-3220.
21. Rossi, A.; Khirani, S.; Cazzola, M. Long-acting-2-agonists (LABA) in chronic obstructive pulmonary disease: Efficacy and safety. Int. J. Chron. Obstruct. Pulmon. Dis., 2008, 3, 521-529.
22. Mason, R.P.; Rhodes, D.G.; Herbette, LG. Reevaluating equilibrium and kinetic binding parameters for lipophilic drugs based on a structural model for drug interaction with biological membranes. J. Med. Chem., 1991, 34, 869-877.
23. Herbette, L.G. Membrane pathways for drug/ion channel interactions: Molecular basis for pharmacokinetic properties. Drug Devel. Res., 1994, 33, 214-222.
24. Johnson M. Molecular mechanisms of beta2-adrenergic receptor function, response, and regulation. J. Allergy Clin. Immunol., 2006, 117, 18-24.
25. Brown, A.D.; Bunnage, M.E.; Glossop, P.A.; James, K.; Jones, R.; Lane, C.A.; Lewthwaite, R.A.; Mantell, S.; Perros-Huguet, C.; Price, D.A.; Trevethick, M.; Webster, R. The discovery of long acting beta2-adrenoreceptor agonists. Bioorg. Med. Chem. Lett., 2007, 17, 4012-4015.
26. Polczewski, K.; Kumasaka, T.; Hori, T.; Behnke, C. A.; Motoshima, H.; Fox, B. A.; Le Trong, I.; Teller, D. C.; Okada, T.; Stenkamp, R. E.; Yamamoto, M.; Miyano, M. Crystal structure of rhodopsin: A G protein-coupled receptor. Science 2000, 289, 739-745.
27. Blaney, F. E.; Tennant, M. Computational tools and results in the construction of G protein-coupled receptor models. In Membrane Protein Models; Findlay, J.B.C., Ed.; Bios Scientific Publishers, Ltd: Oxford, 1996; pp 161-176.
28. Isogaya, M.; Yamagiwa, Y.; Fujita, S.; Sugimoto, Y.; Nagao, T.; Kurose, H. Identification of a key amino acid of the-2-adrenergic receptor for high affinity binding of salmeterol. Mol. Pharmacol., 1998, 54, 616-622.
29. Isogaya, M.; Sugimoto, Y.; Tanimura, R.; Tanaka, R.; Kikkawa, H.; Nagao, T.; Kurose, H. Binding pockets of the-1 and-2 adrenergic receptors for sub-type selective agonists. Mol. Pharmacol. 1999, 56, 875-885.
30. Green, S.A.; Spasoff, A.P.; Coleman, R.R.; Johnson, M.; Liggett, S.B. Sustained activation of a G-protein-coupled receptor via "anchored" agonist binding. Molecular localization of the salmeterol exosite within the-2-adrenergic receptor. J. Biol. Chem. 1996, 271, 24029-24035.
31. Liu, K.K.; Sakya, S.M.; O'Donnell, C.J.; Flick, A.C.; Li, J. Synthetic approaches to the 2009 new drugs. Bioorg. Med. Chem., 2011, 19, 1136-1154.
32. Prashad, M.; Hu, B.; Har, D.; Repic, O.; Blacklock, T.J. An Efficient and economical synthesis of 5,6-Diethyl-2,3-dihydro-1Hinden-2-amine hydrochloride Org. Process Res. Dev., 2006, 10, 135-141.
33. Cherezov, V.; Rosenbaum, D.M.; Hanson, M.A.; Rasmussen, S.G.F.; Thian, F.S.; Kobilka, T.S.; Choi, H.-J.; Kuhn, P.; Weis, W.I.; Kobilka, B.K.; Stevens, R.C. High-resolution crystal structure of an engineered human-2-adrenergic G protein-coupled receptor. Science, 2007, 318, 1258-1265.
34. Rosenbaum, D.M.; Cherezov, V.; Hanson, M.A.; Rasmussen, S.G.F.; Thian, F.S.; Kobilka, T.S.; Choi, H.-J.; Yao, X.-J.; Weis, W.I.; Stevens, R.C.; Kobilka, B.K. GPCR engineering yields highresolution structural insights into-2-adrenergic receptor function. Science 2007, 318, 1266-1273.
35. Rasmussen, S.G.F.; Choi, H.-J.; Rosenbaum, D.M.; Kobilka, T.S.; Thian, F.S.; Edwards, P. C.; Burghammer, M.; Ratnala, V.R.P.; Sanishvili, R.; Fischetti, R.F.; Schertler, G.F.X.; Weis, W. I.; Kobilka, B. K. Crystal structure of the human-2 adrenergic G-proteincoupled receptor. Nature, 2007, 450, 383-388.
36. Procopiou, P.A.; Barrett, V.J.; Bevan, N.J.; Biggadike, K.; Box, P.C.; Butchers, P.R.; Coe, D.M.; Conroy, R.; Emmons, A.; Ford, A.J.; Holmes, D.S.; Horsley, H.; Kerr, F.; Li-Kwai-Cheung, A.M.; Looker, B.E.; Mann, I.S.; McLay, I.M.; Morrison, V.S.; Mutch, P.J.; Smith, C.E.; Tomlin, P. Synthesis and structure-activity relationships of long-acting beta2 adrenergic receptor agonists incorporating metabolic inactivation: An antedrug approach. J. Med. Chem., 2010, 53, 4522-4530.
37. Kempsford, R.D.; Norris, V.; Siederer, S.K. GW642444, a novel long-acting beta2 adrenoceptor agonist (LABA), at single doses of 25, 50 and 100 μg demonstrates prolonged bronchodilation and a favourable safety and tolerability profile in asthmatic patients. Am. J. Respir. Crit. Care Med., 2010, 181, A4447.
38. Brown, A.D.; Bunnage, M.E; Glossop, P.A; James, K.; Jones, R.; Lane, C.A.; Lewthwaite, R.A.; Mantell, S.; Perros-Huguet, C.; Price, D.A.; Trevethick, M.; Webster, R. The discovery of adamantyl-derived, inhaled, long acting beta2-adrenoreceptor agonists. Bioorg. Med. Chem. Lett., 2008, 18, 1280-1283.
39. Brown, A.D.; Bunnage, M.E.; Glossop, P.A.; Holbrook, M.; Jones, R.D.; Lane, C.A.; Lewthwaite, R.A.; Mantell, S.; Perros-Huguet, C.; Price, D.A.; Webster, R. The discovery of indole-derived long acting beta2-adrenoceptor agonists for the treatment of asthma and COPD. Bioorg. Med. Chem. Lett., 2007, 17, 6188-6191.
40. Glossop, P.A.; Lane, C.A.; Price, D.A.; Bunnage, M.E.; Lewthwaite, R.A.; James, K.; Brown, A.D.; Yeadon, M.; Perros-Huguet, C.; Trevethick, M.A.; Clarke, N.P.; Webster, R.; Jones, R.M.; Burrows, J.L.; Feeder, N.; Taylor, S.C.; Spence, F.J. Inhalation by design: Novel ultra-long-acting-2-adrenoreceptor agonists for inhaled once-daily treatment of asthma and chronic obstructive pulmonary disease that utilize a sulfonamide agonist headgroup. J. Med. Chem., 2010, 53, 6640-6652.
41. Bouyssou, T.; Rudolf, K.; Hoenke, C.; Lustenberger, P.; Schnapp, A.; Konetzki, I. Studies towards topical selective-2-adrenoceptor agonists with a long duration of action. Bioorg. Med. Chem. Lett., 2009, 19, 5237-5240.
42. Hoenke, C.; Bouyssou, T.; Tautermann, C. S.; Rudolf, K.; Schnapp, A.; Konetzki, I. Use of 5-hydroxy-4H-benzo[1,4]oxazin-3-ones as-2-adrenoceptor agonists. Bioorg. Med. Chem. Lett., 2009, 19, 6640-6644.
43. Bouyssou, T.; Hoenke, C.; Rudolf, K.; Lustenberger, P.; Pestel, S.; Sieger, P.; Lotz, R.; Heine, C.; Buttner, F. H.; Schnapp, A.; Konetzki, I. Discovery of olodaterol, a novel inhaled-2-adrenoceptor agonist with a 24 h bronchodilatory efficacy. Bioorg. Med. Chem. Lett., 2010, 20, 1410-1414.
44. Connolly, S.; Alcaraz, L.; Bailey, A.; Cadogan, E.; Christie, J.; Cook, A.R.; Fisher, A.J.; Hill, S.; Humphries, A.; Ingall, A.H.; Kane, Z.; Paine, S.; Pairaudeau, G.; Stocks, M.J.; Young, A. Design-driven LO: The discovery of new ultra long acting dibasic-2-adrenoceptor agonists. Bioorg. Med. Chem. Lett., 2011, 21, 4612-4616.
45. Alcaraz, L.; Bailey, A.; Cadogan, E.; Connolly, S.; Jewell, R.; Jordan, S.; Kindon, N.; Lister, A.; Lawson, M.; Mullen, A.; Dainty, I.; Nicholls, D.; Paine, S.; Pairaudeau, G.; Stocks, M.J.; Thorne, P.; Young, A. From libraries to candidate: The discovery of new ultra long-acting dibasic-adrenoceptor agonists. Bioorg. Med. Chem. Lett., 2012, 22, 689-695.
46. Sin, D.D.; McAlister, F.A.; Man, S.F.; Anthonisen, N.R. Contemporary management of chronic obstructive pulmonary disease: Scientific review. JAMA, 2003, 290, 2301-2312.
47. Ramirez-Venegas, A.; Ward, J.; Lentine, T.; Mahler, D.A. Salmeterol reduces dyspnea and improves lung function in patients with COPD. Chest, 1997, 112, 336-340.
48. Cazzola, M.; Donner, C.F. Long-acting beta2 agonists in the management of stable chronic obstructive pulmonary disease. Drugs, 2000, 60, 307-320.
49. van Noord, J.A.; Aumann, J.L.; Janssens, E.; Verhaert, J.; Smeets, J.J.; Mueller, A.; Cornelissen, P.J. Effects of tiotropium with and without formoterol on airflow obstruction and resting hyperinflation in patients with COPD. Chest, 2006, 129, 509-517.
50. Rennard, S.I.; Anderson, W.; ZuWallack, R.; Broughton, J.; Bailey, W.; Friedman, M.; Wisniewski, M.; Rickard, K. Use of a longacting inhaled beta2-adrenergic agonist, salmeterol xinafoate, in patients with chronic obstructive pulmonary disease. Am. J. Respir. Crit. Care Med., 2001, 163, 1087-1092.
51. Stockley, R.A.; Chopra, N.; Rice, L. Addition of salmeterol to existing treatment in patients with COPD: A 12 month study. Thorax, 2006, 61, 122-128.
52. Tashkin, D.P.; Fabbri, L.M. Long-acting beta-agonists in the management of chronic obstructive pulmonary disease: Current and future agents. Respir. Res., 2010, 11, 149.
53. Dahl, R.; Greefhorst, L.A.; Nowak, D.; Nonikov, V.; Byrne, A.M.; Thomson, M.H.; Till, D.; Della Cioppa, G.; the Formoterol in Chronic Obstructive Pulmonary Disease I Study Group. Inhaled formoterol dry powder versus ipratropium bromide in chronic obstructive pulmonary disease. Am. J. Respir. Crit. Care Med., 2001, 164, 778-784.
54. Calverley, P.M.; Boonsawat, W.; Cseke, Z.; Zhong, N.; Peterson, S.; Olsson, H. Maintenance therapy with budesonide and formoterol in chronic obstructive pulmonary disease. Eur. Respir. J., 2003, 22, 912-919.
55. Szafranski, W.; Cukier, A.; Ramirez, A.; Menga, G.; Sansores, R.; Nahabedian, S.; Peterson, S.; Olsson, H. Efficacy and safety of budesonide/formoterol in the management of chronic obstructive pulmonary disease. Eur. Respir. J., 2003, 21, 74-81.
56. Aalbers, R.; Ayres, J.; Backer, V.; Decramer, M.; Lier, P.A.; Magyar, P.; Malolepszy, J.; Ruffin, R.; Sybrecht, G.W. Formoterol in patients with chronic obstructive pulmonary disease: A randomized, controlled, 3-month trial. Eur. Respir. J., 2002, 19, 936-943.
57. Baumgartner, R.A.; Hanania, N.A.; Calhoun, W.J.; Sahn, S.A.; Sciarappa, K.; Hanrahan, J.P. Nebulized arformoterol in patients with COPD: A 12-week, multicenter, randomized, double-blind, double-dummy, placebo-and active-controlled trial. Clin. Ther., 2007, 29, 261-278.
58. Benhamou, D.; Cuvelier, A.; Muir, J.F.; Leclerc, V.; Le Gros, V.; Kottakis, J.; Bourdeix, I. Rapid onset of bronchodilation in COPD: A placebo-controlled study comparing formoterol (Foradil Aerolizer) with salbutamol (Ventodisk). Respir. Med., 2001, 95, 817-821
59. Calverley, P.; Pauwels, R.; Vestbo, J.; Jones, P.; Pride, N.; Gulsvik, A.; Anderson, J.; Maden, C.; the TRial of Inhaled STeroids ANd long-acting beta2 agonists study group. Combined salmeterol and fluticasone in the treatment of chronic obstructive pulmonary disease: A randomised controlled trial. Lancet, 2003, 361, 449-456.
60. Gross, N.J.; Nelson, H.S.; Lapidus, R.J.; Dunn, L.; Lynn, L.; Rinehart, M.; Denis-Mize, K.; the Formoterol Study Group. Efficacy and safety of formoterol fumarate delivered by nebulisation to COPD patients. Respir. Med., 2008, 102, 189-197.
61. Grove, A.; Lipworth, B.J.; Reid, P.; Smith, R.P.; Ramage, L.; Ingram, C.G.; Jenkins, R.J.; Winter, J.H.; Dhillon, D.P. Effects of regular salmeterol on lung function and exercise capacity in patients with chronic obstructive airways disease. Thorax, 1996, 51, 689-693.
62. Hanania, N.A.; Darken, P.; Horstman, D.; Reisner, C.; Lee, B.; Davis, S.; Shah, T. 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, 834-843.
63. Mahler, D.A.; Wire, P.; Horstman, D.; Chang, C.N.; Yates, J.; Fischer, T.; Shah, T. Effectiveness of fluticasone propionate and salmeterol combination delivered via the Diskus device in the treatment of chronic obstructive pulmonary disease. Am. J. Respir. Crit. Care Med., 2002, 166, 1084-1091.
64. Rossi, A.; Kristufek, P.; Levine, B.E.; Thomson, M.H.; Till, D.; Kottakis, J.; Della Cioppa, G.; the Formoterol in Chronic Obstructive Pulmonary Disease (FICOPD) II Study Group. Comparison of the efficacy, tolerability, and safety of formoterol dry powder and oral, slow-release theophylline in the treatment of COPD. Chest, 2002, 121, 1058-1069.
65. van Noord, J.A.; de Munck, D.R.; Bantje, T.A.; Hop, W.C.; Akveld, M.L.; Bommer, A.M. Long-term treatment of chronic obstructive pulmonary disease with salmeterol and the additive effect of ipratropium. Eur. Respir. J., 2000, 15, 878-885.
66. Wadbo, M.; Löfdahl, C.G.; Larsson, K.; Skoogh, B.E.; Tornling, G., Arweström, E.; Bengtsson, T.; Ström, K.; Swedish Society of Respiratory Medicine. Effects of formoterol and ipratropium bromide in COPD: A 3-month placebo-controlled study. Eur. Respir. J., 2002, 20, 1138-1146.
67. Tashkin, D.P.; Rennard, S.I.; Martin, P.; Ramachandran, S.; Martin, U.J.; Silkoff, P.E.; Goldman, M. Efficacy and safety of budesonide and formoterol in one pressurized metered-dose inhaler in patients with moderate to very severe chronic obstructive pulmonary disease: Results of a 6-month randomized clinical trial. Drugs, 2008, 68, 1975-2000.
68. Stockley, R.A.; Whitehead, P.; Williams, K.M. Improved outcomes in patients with chronic obstructive pulmonary disease treated with salmeterol compared with placebo/usual therapy: Results of a metaanalysis. Respir. Res., 2006, 7, 147.
69. Appleton, S.; Poole, P.; Veale, A.; Lasserson, T. J.; Chan, M.M.; Cates, C.J. Long-acting beta2-agonists for poorly reversible chronic obstructive pulmonary disease. Cochrane Libr., 2007, 2, 1-84.
70. Calverley, P.M.A.; Anderson, J.A.; Celli, B.; Ferguson, G.T.; Jenkins, C.; Jones, P.W.; Yates, J.C.; Vestbo, J.; for the TORCH investigators. Salmeterol and fluticasone propionate and survival in chronic obstructive pulmonary disease. N. Engl. J. Med., 2007, 356, 775-789.
71. Celli, B.; Thomas, N.E.; Anderson, J.A.; Ferguson, G.T.; Jenkins, C.; Jones, W.P.; Vestbo, J.; Knobil, K.; Yates, J.C.; Calverley, P.M. Effect of pharmacotherapy on rate of decline of lung function in chronic obstructive pulmonary disease. Am. J. Respir. Crit. Care Med., 2008, 178, 332-338.
72. Ferguson, G.T.; Anzueto, A.; Fei, R.; Emmett, A.; Knobil, K.; Kalberg, C. Effect of fluticasone propionate/salmeterol (250/50 μg) or salmeterol (50 μg) on COPD exacerbations. Respir. Med., 2008, 102, 1099-1108.
73. Campbell, M.; Eliraz, A.; Johansson, G.; Tornling, G.; Nihlen, U.; Bengtsson, T.; Rabe, K.F. Formoterol for maintenance and asneeded treatment of chronic obstructive pulmonary disease. Respir. Med., 2005, 99, 1511-1520.
74. Rennard, S.I.; Tashkin, D.P.; McElhattan, J.; Goldman, M.; Ram, S.; Martin, U.J.; Silkoff, P.E. Efficacy and tolerability of budesonide/formoterol in one hydrofluoroalkane pressurized metered-dose inhaler in patients with chronic obstructive pulmonary disease: Results from a 1-year randomized controlled clinical trial. Drugs, 2009, 69, 549-565.
75. Donohue, J.F.; Menjoge, S.; Kesten, S. Tolerance to bronchodilating effects of salmeterol in COPD. Respir. Med., 2003, 97, 1014-1120.
76. Tsagaraki, V.; Amfilochiou, A.; Markantonis, S.L. Evidence of tachyphylaxis associated with salmeterol treatment of chronic obstructive pulmonary disease patients. Int. J. Clin. Pract., 2006, 60, 415-421.
77. Dahl, R.; Chung, K.F.; Buhl, R.; Magnussen, H.; Nonikov, V.; Jack, D.; Bleasdale, P.; Owen, R.; Higgins, M.; Kramer, B.; the INVOLVE (indacaterol: Value in COPD pulmonary disease: Longer term validation of efficacy and safety) study investigators. Efficacy of a new once-daily LABA, indacaterol, versus the twice-daily LABA, formoterol, in COPD. Thorax, 2010, 65, 473-479.
78. Hanania, N.A.; Kalberg, C.; Yates, J.; Emmett, A.; Horstman, D.; Knobil, K. The bronchodilator response to salmeterol is maintained with regular, long-term use in patients with COPD. Pulm. Pharmacol. Ther., 2005, 18, 19-22.
79. Pauwels, R.A.; Lofdahl, C.G.; Postma, D.S.; Tattersfield, A.E.; O'Byrne, P.; Barnes, P.J.; Ullman, A. Effect of inhaled formoterol and budesonide on exacerbations of asthma. N. Engl. J. Med. 1997, 337, 1405-1411.
80. Vogelmeier, C.; Kardos, P.; Harari, S.; Gans, S.J.; Stenglein, S.; Thirlwell, J. Formoterol mono-and combination therapy with tiotropium in patients with COPD: A 6-month study. Respir. Med., 2008, 102, 1511-1520.
81. Donohue, J.F.; van Noord, J.A.; Bateman, E.D.; Langley, S.J.; Lee, A.; Witek, T.J., Jr.; Kesten, S.; Towse, L. A 6-month, placebocontrolled study comparing lung function and health status changes in COPD patients treated with tiotropium or salmeterol. Chest, 2002, 122, 47-55.
82. Man, W.D.; Mustfa, N.; Nikoletou, D.; Kaul, S.; Hart, N.; Rafferty, G.F.; Donaldson, N.; Polkey, M.I., Moxham, J. Effect of salmeterol on respiratory muscle activity during exercise in poorly reversible COPD. Thorax, 2004, 59, 471-476.
83. Neder, J.A., Fuld, J.P.; Overend, T.; Thirlwell, J.; Carter, R.; Stevenson, R.; Ward, S.A. Effects of formoterol on exercise tolerance in severely disabled patients with COPD. Respir. Med., 2007, 101, 2056-2064.
84. O'Donnell, D.E.; Voduc, N.; Fitzpatrick, M.; Webb, K.A. Effect of salmeterol on the ventilatory response to exercise in chronic obstructive pulmonary disease. Eur. Respir. J., 2004, 24, 86-94.
85. Calverley, P.M.A.; Koulouris, N.G. Flow limitation and dynamic hyperinflation: Key concepts in modern respiratory physiology. Eur. Respir. J., 2005, 25, 186-199.
86. Beeh, K.M.; Wagner, F.; Khindri, S.; Drollmann, A.F. Effect of indacaterol on dynamic lung hyperinflation and breathlessness in hyperinflated patients with COPD. COPD, 2011, 8, 340-345.
87. O'Donnell, D.E.; Casaburi, R.; Vincken, W.; Puente-Maestu, L.; Swales, J.; Lawrence, D.; Kramer, B; INABLE 1 study group. Effect of indacaterol on exercise endurance and lung hyperinflation in COPD. Respir. Med., 2011, 105, 1030-1036.
88. Gayan-Ramirez, G.; Koulouris, N.; Roca J, Decramer, M. Respiratory and skeletal muscles in chronic obstructive pulmonary disease. Eur. Respir. Mon., 2006, 38, 201-223.
89. Di Marco, F.; Milic-Emili, J.; Boveri, B.; Carlucci, P.; Santus, P.; Casanova, F.; Cazzola, M.; Centanni, S. Effect of inhaled bronchodilators on inspiratory capacity and dyspnoea at rest in COPD. Eur. Respir. J., 2003, 21, 86-94.
90. Cooper, C.B. The connection between chronic obstructive pulmonary disease symptoms and hyperinflation and its impact on exercise and function. Am. J. Med., 2006, 119, S21-S31.
91. Jones, P.W.; Bosh, T.K. Quality of life changes in COPD patients treated with salmeterol. Am. J. Respir. Crit. Care Med., 1997, 155, 1283-1289.
92. Wedzicha, J.A.; Calverley, P.M.A.; Seemungal, T.A.; Hagan, G.; Ansari, Z.; Stockley, R.A.; Stockley, R.A.; INSPIRE Investigators. The prevention of chronic obstructive pulmonary disease exacerbations by salmeterol/fluticasone propionate or tiotropium bromide. Am. J. Respir. Crit. Care Med., 2008, 177, 19-26.
93. Anzueto, A.; Ferguson, G.T.; Feldman, G.; Chinsky, K.; Seibert, A.; Emmett, A.; Knobil, K.; O'Dell, D.; Kalberg, C.; Crater, G. Effect of fluticasone propionate/salmeterol (250/50) on COPD exacerbations and impact on patient outcomes. J. COPD, 2009, 6, 320-329.
94. Anzueto, A.; Sethi, S.; Martinez, F.J. Exacerbations of chronic obstructive pulmonary disease. Proc. Am. Thorac. Soc., 2007, 4, 554-564.
95. Donaldson, G.C.; Seemungal, T.; Bhowmik, A.; Wedzicha, J.A. Relationship between exacerbation frequency and lung function decline in chronic obstructive pulmonary disease. Thorax, 2002, 57, 847-852.
96. Soler-Cataluna, J.J.; Martinez-Garcia, M.A.; Sanchez, P.R.; Salcedo, E.; Navarro, M.; Ochando, R. Severe acute exacerbations and mortality in patients with chronic obstructive pulmonary disease. Thorax, 2005, 60, 925-931.
97. Hurst, J.R.; Vestbo, J.; Anzueto, A.; Locantore, N.; Müllerova, H.; Tal-Singer, R.; Miller, B.; Lomas, D.A.; Agusti, A.; Macnee, W.; Calverley, P.; Rennard, S.; Wouters, E.F.; Wedzicha, J.A.; Evaluation of COPD Longitudinally to Identify Predictive Surrogate Endpoints (ECLIPSE) Investigators. Susceptibility to exacerbation in chronic obstructive pulmonary disease. N. Engl. J. Med., 2010, 363, 1128-1138.
98. Nannini, L.; Cates, C.J.; Lasserson, T.J.; Poole, P. Combined corticosteroid and long-acting beta-agonist in one inhaler versus placebo for chronic obstructive pulmonary disease. Cochrane Database Syst. Rev., 2007, 4, CD003794.
99. Nannini, L.; Cates, C.J.; Lasserson, T.J.; Poole, P. Combined corticosteroid and long-acting beta-agonist in one inhaler versus longacting beta-agonists for chronic obstructive pulmonary disease. Cochrane Database Syst. Rev., 2007, 4, CD006829.
100. Rodrigo, G.J.; Nannini, L.J.; Rodríguez-Roisin, R. Safety of longacting-agonists in stable COPD. Chest, 2008, 133, 1079-1087.
101. Baker, W.L.; Baker, E.L.; Coleman, C.I. Pharmacologic treatments for chronic obstructive pulmonary disease: A mixed treatment comparison meta-analysis. Pharmacotherapy, 2009, 29, 891-905.
102. Soriano, J.B.; Sin, D.D.; Zhang, X.; Camp, P.; Anderson, A.J.; Anthonisen, N.; Buist, A.S.; Burge, P.S.; Calverley, P.M.; Connett, J.E.; Petersson, S.; Postma, D.S.; Szafranski, W.; Vestbo, J. A pooled analysis of FEV1 decline in COPD patients randomized to inhaled corticosteroids or placebo. Chest, 2007, 131, 682-689.
103. Kliber, A.; Lynd, L.D.; Sin, D.D. The effects of long-acting bronchodilators on total mortality in patients with stable chronic obstructive pulmonary disease. Respir. Res., 2010, 11, 56.
104. Nannini, L.J.; Lasserson, T.J.; Poole, P. Combined corticosteroid and long-acting beta2-agonist in one inhaler versus long-acting beta2-agonists for chronic obstructive pulmonary disease. Cochrane Database Syst. Rev., 2012, 9, CD006829.
105. Cazzola, M.; Imperatore, F.; Salzillo, A.; Di Perna, F.; Calderaro, F.; Imperatore, A.; Matera, M.G. Cardiac effects of formoterol and salmeterol in patients suffering from COPD with preexisting cardiac arrhythmias and hypoxemia. Chest, 1998, 114, 411-415.
106. Rutten, F.H.; Cramer, M.J.; Lammers, J.W.; Grobbee, D.E.; Hoes, A.W. Heart failure and chronic obstructive pulmonary disease: An ignored combination? Eur. J. Heart Fail., 2006, 8, 706-711.
107. Hawkins, N.M.; Wang, D.; Petrie, M.; Pfeffer, M.A.; Swedberg, K.; Granger, C.B.; Yusuf, S.; Solomon, S.D.; Stergren, J.O.; Michelson, E.L.; Pocock, S.J.; Maggioni, A.P.; McMurray, J.J.V.; for the CHARM investigators and committees: Baseline characteristics and outcomes of patients with heart failure receiving bronchodilators in the CHARM programme. Eur J Heart Fail., 2010, 12, 557-565.
108. Campbell, S.C.; Criner, G.J.; Levine, B.E.; Simon, S.J.; Smith, J.S.; Orevillo, C.J.; Ziehmer, B.A. Cardiac safety of formoterol 12 microg twice daily in patients with chronic obstructive pulmonary disease. Pulm. Pharmacol. Ther., 2007, 20, 571-579.
109. Ferguson, G.T; Gary, M.D.; Funck-Brentano, C.; Fischer, T.; Darken, P.; Reisner, C. Cardiovascular safety of salmeterol in COPD. Chest, 2003, 123, 1817-1824.
110. Randell, J.; Saarinen, A.; Walamies, M.; Vahteristo, M.; Silvasti, M.; Lähelmä, S. Safety of formoterol after cumulative dosing via Easyhaler and Aerolizer. Respir. Med., 2005, 99, 1485-1493.
111. Hanrahan, J.P.; Grogan, D.R.; Baumgartner, R.A.; Wilson, A.; Cheng, H.; Ziometbaum, P.J.; Morganroth, J. Arrhythmias in patients with chronic obstructive pulmonary disease (COPD) occurrence: Frequency and the effect of treatment with the inhaled longacting beta2-agonists arformoterol and salmeterol. Medicine (Baltimore), 2008, 87, 319-328.
112. Pinto-Plata VM; Müllerova, H.; Toso, J.F.; Feudjo-Tepie, M.; Soriano, J.B.; Vessey, R.S.; Celli, B.R. C-reactive protein in patients with COPD, control smokers and non-smokers. Thorax, 2006, 61, 23-28.
113. Ozol, D.; Aysan, T.; Solak, Z.A.; Mogulkoc, N.; Veral, A.; Sebik, F. The effect of inhaled corticosteroids on bronchoalveolar lavage cells and IL-8 levels in stable COPD patients. Respir. Med., 2005, 99, 1494-1500.
114. Sin, D.D.; Lacy, P.; York, E.; Man, S.F. Effects of fluticasone on systemic markers of inflammation in chronic obstructive pulmonary disease. Am. J. Respir. Crit. Care Med., 2004, 170, 760-765.
115. Lapperre, T.S.; Snoeck-Stroband, J.B.; Gosman, M.M.; Jansen, D.F.; van Schadewijk, A.; Thiadens, H.A.; Vonk, J.M.; Boezen, H.M.; Ten Hacken, N.H.; Sont, J.K.; Rabe, K.F.; Kerstjens, H.A.; Hiemstra, P.S.; Timens, W.; Postma, D.S.; Sterk, P.J.; Groningen Leiden Universities Corticosteroids in Obstructive Lung Disease Study Group. Effect of fluticasone with and without salmeterol on pulmonary outcomes in chronic obstructive pulmonary disease: A randomized trial. Ann. Intern. Med., 2009, 151, 517-527.
116. Mak, J.C.W.; Nishikawa, M.; Shirasaki, H.; Miyayasu, K.; Barnes, P.J. Protective effects of a glucocorticoid on downregulation of pulmonary-2- adrenergic receptors in vivo. J. Clin, Invest., 1995, 96, 99-106.
117. Schramm, C.M. Adrenergic relaxation of rabbit tracheal smooth muscle: A receptor deficit that improves with corticosteroid administration. J. Pharmacol. Exp. Ther., 2000, 292, 280-287.
118. Chong, L.K.; Drury, D.E.J.; Dummer, J.F.; Ghahramani, P.; Schleimer, R.P.; Peachell, P.T. Protection by dexamethasone of the functional desensitization to-2-adrenoceptor-mediated responses in human lung mast cells. Br. J. Pharmacol., 1997, 121, 717-722.
119. Kardos, P.; Wencker, M.; Glaab, T.; Vogelmeier, C. Impact of salmeterol/fluticasone propionate versus salmeterol on exacerbations in severe chronic obstructive pulmonary disease. Am. J. Respir. Crit. Care Med., 2007, 175, 144-149.
120. Nannini, L.J.; Cates, C.J.; Lasserson, T.J.; Poole, P. Combined corticosteroid and long-acting beta-agonist in one inhaler versus inhaled steroids for chronic obstructive pulmonary disease. Cochrane Database Syst Rev., 2007, 4, CD006826.
121. Briggs, A.H.; Glick, H.A.; Lozano-Ortega, G.; Spencer, M.; Calverley, P.M.; Jones, P.W.; Vestbo, J.; TOwards a Revolution in COPD Health (TORCH) investigators. Is treatment with ICS and LABA cost-effective for COPD? Multinational economic analysis of the TORCH study. Eur. Respir. J., 2010, 35, 532-539.
122. Welsh, E.J.; Cates, C.J.; Poole, P. Combination inhaled steroid and long-acting beta2-agonist versus tiotropium for chronic obstructive pulmonary disease. Cochrane Database Syst. Rev., 2010, 5, CD007891.
123. Rabe, K.F.; Timmer, W.; Sagkriotis, A.; Viel, K. Comparison of a combination of tiotropium plus formoterol to salmeterol plus fluticasone in moderate COPD. Chest, 2008, 134, 255-262.
124. Rodrigo, G.J.; Castro-Rodriguez, J.A.; Plaza, V. Safety and efficacy of combined long-acting ?-agonists and inhaled corticosteroids vs long-acting ?-agonists monotherapy for stable COPD. Chest, 2009, 136, 1029-1038.
125. Suissa, S. Number needed to treat in COPD: Exacerbations versus pneumonias. Thorax, 2012, Nov 2. [Epub ahead of print]
126. Sobieraj D.M.; White, C.M.; Coleman, C.I. Benefits and risks of adjunctive inhaled corticosteroids in chronic obstructive pulmonary disease: A meta-analysis. Clin. Ther., 2008, 8, 1416-1425.
127. Crim, C.; Calverley, P.M.; Anderson, J.A.; Celli, B.; Ferguson, G.T.; Jenkins, C.; Jones, P.W.; Willit, L.R.; Yates, J.C.; Vestbo, J. Pneumonia risk in COPD patients receiving inhaled corticosteroids alone or in combination: TORCH study results. Eur. Respir. J., 2009, 34, 641-647.
128. Drummond, M.B.; Dasenbrook, E.C.; Pitz, M.W.; Murphy, D.J.; Fan, E. Inhaled corticosteroids in patients with stable chronic obstructive pulmonary disease: A systematic review and metaanalysis. JAMA, 2008, 300, 2407-2416.
129. Sin, D.D.; Tashkin, D.; Zhang, X.; Radner, F.; Sjöbring, U.; Thorén, A.; Calverley, P.M.; Rennard, S.I. Budesonide and the risk of pneumonia: A meta-analysis of individual patient data. Lancet, 2009, 374, 712-719.
130. Thorsson, L.; Edsbacker, S.; Kallen, A.; Lofdahl, C.G. Pharmacokinetics and systemic activity of fluticasone via Diskus and pMDI and of budesonide via Turbohaler. Br. J. Clin. Pharmacol., 2001, 52, 529-538.
131. Kallen, A.; Thorsson, L. Drug deposition analysis: A comparison between budesonide and fluticasone. J. Pharmacokinet. Phar., 2003, 30, 239-256.
132. Singh, S.; Loke, Y.K. Risk of pneumonia associated with long-term use of inhaled corticosteroids in chronic obstructive pulmonary disease: A critical review and update. Curr. Opin. Pulm. Med., 2010, 16, 118-122.
133. Chen, D.; Restrepo, M.I.; Fine, M.J.; Pugh, M.J.; Anzueto, A.; Metersky, M.L.; Nakashima, B.; Good, C.; Mortensen, E.M. Observational study of inhaled corticosteroids on outcomes for COPD patients with pneumonia. Am. J. Respir. Crit. Care Med., 2011, 184, 312-316.
134. Malo de Molina, R.; Mortensen, E.M.; Restrepo, M.I.; Copeland, L.A.; Pugh, M.J.; Anzueto, A. Inhaled corticosteroid use is associated with lower mortality for subjects with COPD and hospitalised with pneumonia. Eur. Respir. J., 2010, 36, 751-757.
135. Calverley, P.M.; Stockley, R.A.; Seemungal, T.A.; Hagan, G.; Willits, L.R.; Riley, J.H.; Wedzicha, J.A. Reported pneumonia in patients with COPD: Findings from the INSPIRE study. Chest, 2011, 139, 505-512.
136. Aaron, S.D.; Vandemheen, K.L.; Fergusson, D.; Maltais, F.; Bourbeau, J.; Goldstein, R.; Balter, M.; O'Donnell, D.; McIvor, A.; Sharma, S.; Bishop, G.; Anthony, J.; Cowie, R.; Field, S.; Hirsch, A.; Hernandez, P.; Rivington, R.; Road, J.; Hoffstein, V.; Hodder, R.; Marciniuk, D.; McCormack, D.; Fox, G.; Cox, G.; Prins, H.B.; Ford, G.; Bleskie, D.; Doucette, S.; Mayers, I.; Chapman, K.; Zamel, N.; FitzGerald, M.; Canadian Thoracic Society/Canadian Respiratory Clinical Research Consortium. Tiotropium in combination with placebo, salmeterol, or fluticasone-salmeterol for treatment of chronic obstructive pulmonary disease: A randomized trial. Ann. Intern. Med., 2007, 146, 545-555.
137. van Noord, J.A.; Aumann, J.L.; Janssens, E.; Smeets, J.J.; Verhaert, J.; Disse, B.; Mueller, A.; Cornelissen, P.J. Comparison of tiotropium once daily, formoterol twice daily and both combined once daily in patients with COPD. Eur. Respir. J., 2005, 26, 214-222.
138. Tashkin, D.P.; Varghese, S.T. Combined treatment with formoterol and tiotropium is more efficacious than treatment with tiotropium alone in patients with chronic obstructive pulmonary disease, regardless of smoking status, inhaled corticosteroid use, baseline severity, or gender. Pulm. Pharmacol. Ther., 2011, 24, 147-152.
139. Tashkin, D.P.; Celli, B.; Senn, S.; Burkhart, D.; Kesten, S.; Menjoge, S.; Decramer, M.; UPLIFT Study Investigators. A 4-year trial of tiotropium in chronic obstructive pulmonary disease. N. Engl. J. Med., 2008, 359, 1543-1554.
140. Lee, T.A.; Wilke, C.; Joo, M.; Stroupe, K.T.; Krishnan, J.A.; Schumock, G.T.; Pickard, A.S. Outcomes associated with tiotropium use in patients with chronic obstructive pulmonary disease. Arch. Intern. Med., 2009, 169, 1403-1410.
141. Welte, T.; Miravitlles, M.; Hernandez, P.; Eriksson, G.; Peterson, S.; Polanowski, T.; Kessler, R. Efficacy and tolerability of budesonide/formoterol added to tiotropium in patients with chronic obstructive pulmonary disease. Am. J. Respir. Crit. Care Med., 2009, 180, 741-750.
142. Cazzola, M.; Matera, M.G. Novel long-acting bronchodilators for COPD and asthma. Br. J. Pharmacol., 2008, 155, 291-299.
143. Battram, C.; Charlton, S.J.; Cuenoud, B.; Bowling, M.R.; Fairhurst, R.A.; Farr, D.; Fozard, J.R.; Leighton-Davies, J.R.; Lewis, C.A.; McEvoy, L.; Turner, R.J.; Trifilieff, A. 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 beta2 adrenoceptor agonist with a 24-h duration of action. J. Pharmacol. Exp. Ther., 2006, 317, 762-770.
144. Moen, M.D. Indacaterol: In chronic obstructive pulmonary disease. Drugs, 2010, 70, 2269-2280.
145. Lombardi, D.; Cuenoud, B., Kramer, S.D. Lipid membrane interactions of indacaterol and salmeterol: Do they influence their pharmacological properties? Eur. J. Pharm. Sci., 2009, 38, 533-547.
146. Rosethorne, E.M., Turner, R.J., Fairhurst, R.A.; Charlton SJ. Efficacy is a contributing factor to the clinical onset of bronchodilation of inhaled beta2-adrenoceptor agonists. Naunyn. Schmiedebergs Arch. Pharmacol., 2010, 382, 255-263.
147. Feldman, G.; Siler, T.; Prasad, N.; Jack, D.; Piggott, S.; Owen, R.; Higgins, M.; Kramer, B.; INLIGHT 1 study group. Efficacy and safety of indacaterol 150 ?g once-daily in COPD: A double-blind, randomised, 12-week study. BMC Pulm. Med., 2010, 10, 11
148. Donohue, J.F.; Fogarty, C.; Lotval, J.; Mahler, D.A.; Worth, H.; Yorgancioglu, A.; Iqbal, A.; Swales, J.; Owen, R.; Higgins, M.; Kramer, B.; INHANCE Study Investigators. Once-daily bronchodilators for chronic obstructive pulmonary disease: Indacaterol versus tiotropium. Am. J. Respir. Crit. Care Med., 2010, 182, 155-162.
149. Kornmann, O.; Dahl, R.; Centanni, S.; Dogra, A.; Owen, R.; Lassen, C.; Kramer, B.; INLIGHT-2 (Indacaterol Efficacy Evaluation Using 150-g Doses with COPD Patients) study investigators. Once-daily indacaterol vs twice-daily salmeterol for COPD: A placebo-controlled comparison. Eur. Respir. J., 2011, 37, 273-279.
150. Beeh, K.M.; Beier, J. Indacaterol: A new once daily long-acting beta2 adrenoceptor agonist. Core Evid., 2009, 4, 37-41.
151. Cazzola, M.; Calzetta, L.; Matera, M.G. ?2-adrenoceptor agonists: Current and future direction. Br. J. Pharmacol., 2011, 163, 4-17.
152. Cazzola, M.; Page, C.P.; Calzetta, L.; Matera, M.G. Pharmacology and therapeutics of bronchodilators. Pharmacol. Rev., 2012, 64, 450-504.
153. Kanniess, F.; Make, B.J.; Petruzzelli, S. Acute effect of carmoterol, a long-acting beta2-agonist, in patients with COPD. Am. J. Respir. Crit. Care Med., 2008, 177, A655.
154. Make, B.J.; Kanniess, F.; Bateman, E.D.; Linberg, S.E. Efficacy of 3 different doses of carmoterol, a long-acting beta2-agonist in patients with COPD. Am. J. Respir. Crit. Care Med., 2008, 177, A961.
155. Rossing, T.H.; Make, B.J., Heyman, E.R. Carmoterol does not induce tolerance in COPD. Am. J. Respir. Crit. Care Med., 2008, 177, A962.
156. Tashkin, D.P.; Kleerup, E.C.; Heyman, E.R.; Norris, D.; Tetruzzelli, S. Effect of carmoterol pMDI on 24-hour FEV1 in COPD patients. Eur. Respir. J., 2009, 34 (Suppl 53), E4346.
157. Bateman, E.D.; Make, B.J., Nandeuil, M.A. Safety and tolerability of a long-acting beta2-agonist in patients with COPD. Am. J. Respir. Crit. Care Med., 2008, 177, A653.
158. Bouyssou, T.; Casarosa. P.; Naline, E.; Pestel, S.; Konetzki, I.; Devillier, P.; Schnapp, A. Pharmacological characterization of olodaterol, a novel inhaled beta2-adrenoceptor agonist exerting a 24-hour-long duration of action in preclinical models. J. Pharmacol. Exp. Ther., 2010, 334, 53-62.
159. Aprici, M.; Gómez-Angelats, M.; Vitella, D.; Otal, R.; Carcasona, C.; Viñals, M.; Ramos, I.; Gavaldà, A.; De Alba, J.; Gras, J.; Cortijo, J.; Morbillo, E.; Puig, C.; Ryder, H.; Belata, J.; Miralpeix, M. Pharmacological characterization of abediterol, a novel inhaled ?2-adrenoceptor agonist with long duration of action and a favorable safety profile in preclinical models. J. Pharmacol. Exp. Ther., 2012, 342, 497-509.
160. van Noord, J.A.; Buhl, R.; Laforce, C.; Martin, C.; Jones, F.; Dolker, M.; Overend, T. QVA149 demonstrates superior bronchodilation compared with indacaterol or placebo in patients with chronic obstructive pulmonary disease. Thorax, 2010, 65, 1086-1091.
161. Van de Maele, B.; Fabbri, L.M.; Martin, C.; Horton, R.; Dolker, M.; Overend, T. Cardiovascular safety of QVA149, a combination of indacaterol and NVA237, in COPD patients. COPD, 2010, 7, 418-427.
162. Hughes, A.D; Jones, L.H. Dual-pharmacology muscarinic antagonist and-2 agonist molecules for the treatment of chronic obstructive pulmonary disease. Future Med. Chem., 2011, 3, 1585-1605.
163. Hughes, A.D.; McNamara, A.; Steinfeld, T. Multivalent dual pharmacology muscarinic antagonist and-2 agonist (MABA) molecules for the treatment of COPD. Prog. Med. Chem., 2012, 51, 71-95.