Efficacy and safety of long-acting beta-2-agonists
https://doi.org/10.18093/0869-0189-2015-25-1-113-118
Abstract
Beta-2-adrenoreceptor agonists (#b2-АA) are one of the key drugs used for treatment of chronic obstructive pulmonary disease (COPD) and asthma. Recently, novel #b2-АA with ultra-long half-life which allows once-day administration have been developed such as indacaterol, olodaterol, vilanterol, carmoterol, PF-610355 and AZD-3199. Pharmacodynamics, pharmacokinetics and clinical effects of these drugs in COPD and asthma are reviewed in the article. Published data suggest that the rational and individualized use of novel ultralong-acting #b2-АA could increase safety and efficacy of treatment in patients with COPD and asthma.
About the Authors
L. V. Shul'zhenko
State Budget High-Level Educational Institution “Kuban State Medical University”, Healthcare Ministry of Russia: 4, Sedina ul., Krasnodar, 350063, Russia
Russian Federation
Russian Federation
MD, Professor, Head of Chair of Pulmonology, Postgraduate Education Faculty, State Budget High-Level Educational Institution “Kuban State Medical University”, Healthcare Ministry of Russia; tel.: (988) 244-82-49;
E. V. Bolotova
State Budget High-Level Educational Institution “Kuban State Medical University”, Healthcare Ministry of Russia: 4, Sedina ul., Krasnodar, 350063, Russia
Russian Federation
Russian Federation
MD, Professor, Chair of Pulmonology, Postgraduate Education Faculty, State Budget High-Level Educational Institution “Kuban State Medical University”, Healthcare Ministry of Russia; tel.: (862)252-73-93;
References
1. Cazzola M., Page C.P., Rogliani P., Matera M.G. #b2-agonist therapy in lung disease. Am. J. Respir. Crit. Care Med. 2013; 187 (7): 690–696.
2. Spina D. Current and novel bronchodilators in respiratory disease. Curr. Opin. Pulm. Med. 2014; 20 (1): 73–86.
3. Battram C., Charlton S.J., Cuenoud B. 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’-quinolm-2-one (indacaterol), a novel inhaled #b2-adrenoceptor agonist with a 24-h duration of action. J. Pharmacol. Exp. Ther. 2006; 317: 762–770.
4. Sturton R.G., Trifilieff A., Nicholson A.G., Barnes P.J. Pharmacological characterization of indacaterol, a novel once daily inhaled #b2-adrenoceptor agonist, on small airways in human and rat precision-cut lung slices. J. Pharmacol. Exp. Ther. 2008; 324: 270–275.
5. Naline E., Trifilieff A., Fairhurst R.A. et al. Effect of indacaterol, a novel long acting #b2-agonist, on isolated human bronchi. Eur. Respir. J. 2007; 29: 575–581.
6. Rosethorne E.M., Turner R.J., Fairhurst R.A., Charlton S.J. Efficacy is a contributing factor to the clinical onset of bronchodilation of inhaled #b2-adrenoceptor agonists. Naunyn. Schmiedebergs Arch. Pharmacol. 2010; 382: 255–263.
7. Cazzola M., Calzetta L., Page C.P., Matera M.G. Use of indacaterol for the treatment of COPD: a pharmacokinetic evaluation. Exp. Opin. Drug Metab. Toxicol. 2014; 10 (1): 129–137.
8. Renard D., Looby M., Kramer B. et al. Characterization of the bronchodilatory dose response to indacaterol in patients with chronic obstructive pulmonary disease using model-based approaches. Respir. Res. 2011; 12: 54.
9. O’Donnell D.E., Casaburi R., Vincken W. et al. Effect of indacaterol on exercise endurance and lung hyperinflation in COPD. Respir. Med. 2011; 105: 1030–1036.
10. Rossi A., Polese G. Indacaterol: a comprehensive review. Int. J. Chron. Obstruct. Pulm. Dis. 2013; 8: 353–363.
11. Cope S., Capkun-Niggli G., Gale R. et al. Comparative efficacy of indacaterol 150 / xg and 300 / xg versus fixed-dose combinations of formoterol + budesonide or salmeterol + fluticasone for the treatment of chronic obstructive pulmonary disease – a network meta-analysis. Int. J. Chron. Obstruct. Pulm. Dis. 2011; 6: 329–344.
12. Singh M.P. Indacaterol therapy in moderate-to-severe chronic obstructive pulmonary disease: findings from a single-center primary care cohort. Int. J. Chron. Obstruct. Pulm. Dis. 2013; 8: 613–619.
13. Ridolo E., Montagni M., Olivieri E. et al. Role of indacaterol and the newer very long-acting #b2-agonists in patients with stable COPD: A review. Int. J. Chron. Obstruct. Pulm. Dis. 2013; 8: 425–432.
14. Chowdhury B.A., Dal Pan G. The FDA and safe use of long-acting beta-agonists in the treatment of asthma. N. Engl. J. Med. 2010; 362: 1169–1171.
15. Kanniess F., Boulet L.P., Pierzchala W. et al. Efficacy and safety of indacaterol, a new 24-h #b2-agonist, in patients with asthma: a dose-ranging study. J. Asthma. 2008; 45: 887–892.
16. La Force C., Alexander M., Deckelmann R. et al. Indacaterol provides sustained 24 h bronchodilation on once-daily dosing in asthma: a 7-day dose-ranging study. Allergy. 2008; 63: 103–111.
17. Chowdhury B.A., Seymour S.M., and Levenson M.S. Assessing the safety of adding LABAs to inhaled corticosteroids for treating asthma. N. Engl. J. Med. 2011; 364: 2473–2475.
18. Cazzola M., Segreti A., Matera M.G. Novel bronchodilators in asthma. Curr. Opin. Pulm. Med. 2010; 16: 6–12.
19. Bouyssou T., Casarosa P., Naline E. et al. Pharmacological characterization of olodaterol, a novel inhaled #b2-adrenoceptor agonist exerting a 24-hour-long duration of action in preclinical models. J. Pharmacol. Exp. Ther. 2010; 334: 53–62.
20. McKeage K. Indacaterol: a review of its use as maintenance therapy in patients with chronic obstructive pulmonary disease. Drugs. 2012; 72 (4): 543–563.
21. Naline E., Ostermann A., Devillier P., Casarosa P. #b2-agonist intrinsic activity: comparison of BI 1744 and formoterol in different functional settings. Am. J. Respir. Crit. Care Med. 2010; 181: A4443.
22. Gibb A., Yang L.P. Olodaterol: first global approval. Drugs. 2013; 73 (16): 1841–1846.
23. Brown S.M., Barnes P.J., Donnelly L.E. Effect of olodaterol on the relaxation of small airways. Eur. Respir. J. 2011; 38: 308s.
24. Casarosa P., Kollak I., Kiechle T. et al. Functional and biochemical rationales for the 24-hour-long duration of action of olodaterol. J. Pharmacol. Exp. Ther. 2011; 337: 600–609.
25. van Noord J.A., Smeets J.J., Drenth B.M. et al. 24-Hour bronchodilation following a single dose of the novel #b2-agonist olodaterol in COPD. Pulm. Pharmacol. Ther. 2011; 24: 666–672.
26. Procopiou P.A., Barrett V.J., Bevan N.J. et al. Synthesis and structure-activity relationships of long-acting #b2-adrenergic receptor agonists incorporating metabolic inactivation: an antedrug approach. J. Med. Chem. 2010; 53: 4522–4530.
27. Ferguson G.T., Feldman G.J., Hofbauer P. et al. Efficacy and safety of olodaterol once daily delivered via Respimat#R in patients with GOLD 2–4 COPD: results from two replicate 48-week studies. Int. J. Chron. Obstruct. Pulm. Dis. 2014; 9: 629–645.
28. Costa L., Roth M., Miglino N. et al. Tiotropium sustains the anti-inflammatory action of olodaterol via the cyclic AMP pathway. Pulm. Pharmacol. Ther. 2014; 27 (1): 29–37.
29. Barrett V.J., Emmons A., Ford A.J., Knowles R. In vitro pharmacological characterisation of GW642444, a novel long acting #b-agonist (LABA) using human recombinant #b1/2/3-adrenoceptor cAMP assays. Am. J. Respir. Crit. Care Med. 2010; 181: A4451.
30. Ford A.J., Hughes S., Morrison V.et al. In vitro and in vivo pharmacological characterisation of GW642444, a novel long-acting #b2-agonist (LABA), with fast onset and long duration in the guinea-pig. Am. J. Respir. Crit. Care Med. 2010; 181: A5677.
31. Slack R.J., Barrett V.J., Morrison V.S. et al. In vitro pharmacological characterization of vilanterol, a novel long-acting #b2-adrenoceptor agonist with 24-hour duration of action. J. Pharmacol. Exp. Ther. 2013; 344 (1): 218–230.
32. Ford A.J., Hughes S., Smith C. et al. The therapeutic index of vilanterol trifenatate. Eur. Respir. J. 2010; 24: 208s.
33. Kempsford R., Norris V., Siederer S. GW642444, a novel inhaled long-acting #b2-adrenoceptor agonist (LABA), at single doses of 25, 50 and 100 mcg, is well tolerated and demonstrates prolonged bronchodilation in asthmatic patients. Am. J. Respir. Crit. Care Med. 2010; 181: A5413.
34. Kempsford R., Norris V., Siederer S. Vilanterol trifenatate, a novel inhaled long-acting beta2-adrenoceptor agonist, is well tolerated in healthy subjects and demonstrates prolonged bronchodilation in subjects with asthma and COPD. Pulm. Pharmacol. Ther. 2013; 26 (2): 256–264.
35. Kempsford R., Norris V., Siederer S. GW642444, a novel inhaled long-acting #b2-adrenoceptor agonist (LABA), at single doses of 25, 50 and 100 mcg, is well tolerated and demonstrates prolonged bronchodilation in COPD patients. Am. J. Respir. Crit. Care Med. 2010; 181: A4447.
36. Lotvall J., Bateman E.D., Bleecker E.R. et al. Dose-related efficacy of vilanterol trifena- tate, a long-acting beta2 agonist with inherent 24-hour activity, in patients with persistent asthma. Eur. Respir. J. 2010; 24: 1013s.
37. Lotvall J., Bateman E.D., Bleecker E.R. et al. 24-h duration of the novel LABA vilanterol trifenatate in asthma patients treated with inhaled corticosteroids. Eur. Respir. J. 2012; 40 (3): 570–579.
38. Sterling R., Lim J., Frith L. et al. Dose-related efficacy and optimal once-daily (OD) dosing interval of the long-acting beta2-agonist (LABA), vilanterol trifenatate (VI), in adults with persistent asthma. Am. J. Respir. Crit. Care Med. 2011; 183: A4488.
39. Hanania N.A., Feldman G., Zachgo W. et al. The efficacy and safety of the novel long-acting #b2-agonist vilanterol in COPD patients: a randomized placebo-controlled trial. Chest. 2012; 142 (1): 119–127.
40. Kikkawa H., Naito K., Ikezawa K. Tracheal relaxing effects and #b2-selectivity of TA-2005, a newly developed bronchodilating agent, in isolated guinea-pig tissues. Jpn. J. Pharmacol. 1991; 57: 175–185.
41. Voss H.P., Donnell D., Bast A. Atypical molecular pharmacology of a new long-acting #b2-adrenoceptor agonist, TA-2005. Eur. J. Pharmacol. 1992; 227: 403–409.
42. Standifer K.M., Pitha J., Baker S.P. Carbostyril-based #b2-adrenergic agonists: evidence for long lasting or apparent irreversible receptor binding and activation of adenylate cyclase activity in vitro. Naunyn. Schmiedebergs Arch. Pharmacol. 1989; 339: 129–137.
43. Kikkawa H., Kanno K., Ikezawa K. TA-2005, a novel, long-acting and selective p2-adrenocepter agonist: characterization of its in vivo bronchodilating action in guinea pigs and cats in comparison with other #b2-agonists. Biol. Pharm. Bull. 1994; 17: 1047–1052.
44. Voss H.P. Long-acting #b2-adrenoceptor agonists in asthma: molecular pharmacological aspects. Vrije Universiteit: Amsterdam; 1994.
45. Kikkawa H., Isogaya M., Nagao T., Kurose H. The role of the seventh transmembrane region in high affinity binding of a #b2-selective agonist TA-2005. Mol. Pharmacol. 1998; 53: 128–134.
46. Cazzola M., Segreti A., Matera M.G. Novel bronchodilators in asthma. Curr. Opin. Pulm. Med. 2010; 16: 6–12.
47. Haeussermann S., Acerbi A., Brand P. et al. Lung deposition of carmoterol in healthy subjects, patients with asthma and patients with COPD. Eur. Respir. J. 2006; 28: 211s.
48. Kottakis I., Nandeuil A., Raptis H. et al. Efficacy of the novel very long-acting #b-agonist carmoterol following 7 days once daily dosing: comparison with twice daily formoterol in patient with persistent asthma. Eur. Respir. J. 2006; 28: 665s.
49. Nandeuil A., Kottakis I., Raptis H. et al. Safety and tolerability of the novel very long acting #b2-agonist carmoterol given as a 2 / xg qd dose; 8 days comparison with formoterol and placebo in patients with persistent asthma. Eur. Respir. J. 2006; 28: 665s.
50. Kanniess F., Make B.J., Petruzzelli S. Acute effect of carmoterol, a long-acting p2-agonist, in patients with COPD. Proc. Am. Thorac. Soc. 2008; 5: A655.
51. Make B.J., Kanniess F., Bateman E.D., Linberg S.E. Efficacy of 3 different doses of carmoterol, a long-acting #b2-agonist in patients with COPD. Proc. Am. Thorac. Soc. 2008; 5: A961.
52. Bateman E.D., Make B.J., Nandeuil M.A. Carmoterol – safety and tolerability of a long-acting #b2-agonist in patients with COPD. Proc. Am. Thorac. Soc. 2008; 5: A653.
53. Rossing T.H., Make B.J., Heyman E.R. Carmoterol does not induce tolerance in COPD. Proc. Am. Thorac. Soc. 2008; 5: A962.
54. Glossop P.A., Lane C.A., Price D.A. et al. Inhalation by design: novel ultra-long-acting #b2-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.
55. Li G.L., Mac Intyre F., Surujbally B. et al. Pharmacokinetics of PF-00610355, a novel inhaled long-acting #b2-adrenoreceptor agonist. Eur. Respir. J. 2009; 34: 777s.
56. Macintyre F., Jones I., Surujbally B. A randomised, double-blind study to determine the duration of action of lung pharmacodynamics by plethysmography (sGaw) of a #b2-adrenoreceptor agonist, PF-00610355. Eur. Respir. J. 2009; 34: 344s.
57. Ward J., Macintyre F., Jones I. et al. A randomised double-blind, study to determine the efficacy & safety of a once-daily inhaled #b2-adrenoreceptor agonist, PF-00610355 in asthmatic patients. Eur. Respir. J. 2009; 34: 778s.
58. Diderichsen P.M., Cox E., Martin S.W. et al. Predicted heart rate effect of inhaled PF-00610355, a long acting #b-adrenoceptor agonist, in volunteers and patients with chronic obstructive pulmonary disease. Br. J. Clin. Pharmacol. 2013; 76 (5): 752–762.
59. Young A., Nicholls D., Connolly S. et al. The in vivo profile ofAZD3199: a novel, fast acting #b2-agonist with a long duration of action (Abstract). Am. J. Respir. Crit. Care Med. 2011; 183: A1586.
60. Kuna P., Ivanov Y., Trofimov V. et al. Efficacy and safety of AZD3199, an inhaled ultra long-acting #b-agonist, in patients with COPD. Eur. Respir. J. 2011; 38: 148s.
Review
For citations:
Shul'zhenko L.V., Bolotova E.V. Efficacy and safety of long-acting beta-2-agonists. PULMONOLOGIYA. 2015;25(1):113-118. (In Russ.) https://doi.org/10.18093/0869-0189-2015-25-1-113-118
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