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Erschienen in: Drugs 13/2014

01.09.2014 | Adis Drug Evaluation

Fluticasone Furoate/Vilanterol: A Review of Its Use in Chronic Obstructive Pulmonary Disease

verfasst von: Kate McKeage

Erschienen in: Drugs | Ausgabe 13/2014

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Abstract

Fluticasone furoate/vilanterol (Relvar®, Breo®, Revinty®) is a fixed combination of a corticosteroid and a long-acting β2-adrenergic agonist (LABA) for once-daily use via a dry powder inhaler (Ellipta®). Fluticasone furoate/vilanterol 100/25 µg is approved for the treatment of chronic obstructive pulmonary disease (COPD) in several countries. This article reviews the clinical use of the combination in COPD and summarises pharmacological properties. Fluticasone furoate has enhanced affinity for the glucocorticoid receptor compared with other clinically used inhaled corticosteroids (ICS) and longer lung retention than fluticasone propionate. Vilanterol is highly selective for β2-adrenoreceptors and provides a rapid and prolonged duration of action. In phase 3 trials in patients with moderate to very severe COPD, overall, once-daily fluticasone furoate/vilanterol 100/25 µg improved pulmonary function more than placebo and fluticasone furoate alone and improved exacerbation rates more than vilanterol alone. With regard to pulmonary function, once-daily fluticasone furoate/vilanterol 100/25 μg was more effective than twice-daily fluticasone propionate/salmeterol 250/50 µg and similarly effective as twice-daily fluticasone propionate/salmeterol 500/50 μg. In 12-month trials, fluticasone furoate/vilanterol was generally well tolerated, and in 12- and 24-week trials, the incidence of adverse events was similar overall to that associated with the individual components or fluticasone propionate/salmeterol. However, as with the long-term use of all ICS agents, 12-month data indicate an increase in the risk of pneumonia with fluticasone furoate/vilanterol. In conclusion, fluticasone furoate/vilanterol is an effective and generally well tolerated additional LABA/ICS agent for the treatment of COPD with the added convenience of once-daily administration, which may improve treatment adherence in some patients.
Literatur
2.
Zurück zum Zitat Simoni-Wastila L, Wei YJ, Qian J, et al. Association of chronic obstructive pulmonary disease maintenance medication adherence with all-cause hospitalization and spending in a Medicare population. Am J Geriatr Pharmacother. 2012;10:201–10.PubMedCrossRef Simoni-Wastila L, Wei YJ, Qian J, et al. Association of chronic obstructive pulmonary disease maintenance medication adherence with all-cause hospitalization and spending in a Medicare population. Am J Geriatr Pharmacother. 2012;10:201–10.PubMedCrossRef
3.
Zurück zum Zitat Restrepo RD, Alvarez MT, Wittnebel LD, et al. Medication adherence issues in patients treated for COPD. Int J Chron Obstruct Pulmon Dis. 2008;3:371–84.PubMedCentralPubMed Restrepo RD, Alvarez MT, Wittnebel LD, et al. Medication adherence issues in patients treated for COPD. Int J Chron Obstruct Pulmon Dis. 2008;3:371–84.PubMedCentralPubMed
4.
Zurück zum Zitat Toy EL, Beaulieu NU, McHale JM, et al. Treatment of COPD: relationships between daily dosing frequency, adherence, resource use, and costs. Respir Med. 2011;105:435–41.PubMedCrossRef Toy EL, Beaulieu NU, McHale JM, et al. Treatment of COPD: relationships between daily dosing frequency, adherence, resource use, and costs. Respir Med. 2011;105:435–41.PubMedCrossRef
5.
Zurück zum Zitat Vestbo J, Anderson JA, Calverley PMA, et al. Adherence to inhaled therapy, mortality and hospital admission in COPD. Thorax. 2009;64:939–43.PubMedCrossRef Vestbo J, Anderson JA, Calverley PMA, et al. Adherence to inhaled therapy, mortality and hospital admission in COPD. Thorax. 2009;64:939–43.PubMedCrossRef
6.
Zurück zum Zitat Horne R. Is once enough? Understanding the preferences of COPD and asthma patients for once- versus twice-daily treatment. Prim Care Respir J. 2013;22(2):140–2.PubMedCrossRef Horne R. Is once enough? Understanding the preferences of COPD and asthma patients for once- versus twice-daily treatment. Prim Care Respir J. 2013;22(2):140–2.PubMedCrossRef
7.
Zurück zum Zitat Price D, Robertson A, Bullen K, et al. Improved adherence with once-daily versus twice-daily dosing of mometasone furoate administered via a dry powder inhaler: a randomized open-label study. BMC Pulm Med. 2010 (1471-2466/10/1). Price D, Robertson A, Bullen K, et al. Improved adherence with once-daily versus twice-daily dosing of mometasone furoate administered via a dry powder inhaler: a randomized open-label study. BMC Pulm Med. 2010 (1471-2466/10/1).
10.
Zurück zum Zitat Haque R, KHakim A, Moodley T, et al. Inhaled long-acting b2 agonists enhance glucocorticoid receptor nuclear translocation and efficacy in sputum macrophages in COPD. J Allergy Clin Immunol. 2013;132:1166–73.PubMedCrossRef Haque R, KHakim A, Moodley T, et al. Inhaled long-acting b2 agonists enhance glucocorticoid receptor nuclear translocation and efficacy in sputum macrophages in COPD. J Allergy Clin Immunol. 2013;132:1166–73.PubMedCrossRef
11.
Zurück zum Zitat Hamilton M, Prime D, Leggett R, et al. Ex-vivo product performance of fluticasone furoate/vilanterol delivered from a novel dry powder inhaler, using the electronic lung to replicate asthma and COPD patient inhaler profiles [abstract no. A2940]. Am J Respir Crit Care Med. 2012;185. Hamilton M, Prime D, Leggett R, et al. Ex-vivo product performance of fluticasone furoate/vilanterol delivered from a novel dry powder inhaler, using the electronic lung to replicate asthma and COPD patient inhaler profiles [abstract no. A2940]. Am J Respir Crit Care Med. 2012;185.
12.
Zurück zum Zitat Salter M, Biggadike K, Matthews JL, et al. Pharmacological properties of the enhanced-affinity glucocorticoid fluticasone furoate in vitro and in an in vivo model of respiratory inflammatory disease. Am J Physiol Lung Cell Mol Physiol. 2007;293:L660–7.PubMedCrossRef Salter M, Biggadike K, Matthews JL, et al. Pharmacological properties of the enhanced-affinity glucocorticoid fluticasone furoate in vitro and in an in vivo model of respiratory inflammatory disease. Am J Physiol Lung Cell Mol Physiol. 2007;293:L660–7.PubMedCrossRef
13.
Zurück zum Zitat Caramori G, Adcock I. Pharmacology of airway inflammation in asthma and COPD. Pulm Pharmacol Ther. 2003;16:247–77.PubMedCrossRef Caramori G, Adcock I. Pharmacology of airway inflammation in asthma and COPD. Pulm Pharmacol Ther. 2003;16:247–77.PubMedCrossRef
14.
Zurück zum Zitat Biggadike K, Bledsoe RK, Hassell AM, et al. X-ray crystal structure of the novel enhanced-affinity glucocorticoid agonist fluticasone furoate in the glucocorticoid receptor-ligand binding domain. J Med Chem. 2008;51(12):3349–52.PubMedCrossRef Biggadike K, Bledsoe RK, Hassell AM, et al. X-ray crystal structure of the novel enhanced-affinity glucocorticoid agonist fluticasone furoate in the glucocorticoid receptor-ligand binding domain. J Med Chem. 2008;51(12):3349–52.PubMedCrossRef
15.
Zurück zum Zitat Valotis A, Hogger P. Human receptor kinetics and lung tissue retention of the enhanced-affinity glucocorticoid fluticasone furoate. Respir Res. 2007;8:54.PubMedCentralPubMedCrossRef Valotis A, Hogger P. Human receptor kinetics and lung tissue retention of the enhanced-affinity glucocorticoid fluticasone furoate. Respir Res. 2007;8:54.PubMedCentralPubMedCrossRef
16.
Zurück zum Zitat Rossios C, To Y, To M, et al. Long-acting fluticasone furoate has a superior pharmacological profile to fluticasone propionate in human respiratory cells. Eur J Pharmacol. 2011;670:244–51.PubMedCrossRef Rossios C, To Y, To M, et al. Long-acting fluticasone furoate has a superior pharmacological profile to fluticasone propionate in human respiratory cells. Eur J Pharmacol. 2011;670:244–51.PubMedCrossRef
17.
Zurück zum Zitat Slack RJ, Barrett VJ, Morrison VS, et al. In vitro pharmacological characterization of vilanterol, a novel long-acting beta2-adrenoceptor agonist with 24-hour duration of action. J Pharmacol Exp Ther. 2013;344(1):218–30.PubMedCrossRef Slack RJ, Barrett VJ, Morrison VS, et al. In vitro pharmacological characterization of vilanterol, a novel long-acting beta2-adrenoceptor agonist with 24-hour duration of action. J Pharmacol Exp Ther. 2013;344(1):218–30.PubMedCrossRef
18.
Zurück zum Zitat Cazzola M, Page CP, Calzetta L, et al. Pharmacology and therapeutics of bronchodilators. Pharmacol Rev. 2012;64:450–504.PubMedCrossRef Cazzola M, Page CP, Calzetta L, et al. Pharmacology and therapeutics of bronchodilators. Pharmacol Rev. 2012;64:450–504.PubMedCrossRef
19.
Zurück zum Zitat Hanania NA, Feldman G, Zachgo W, et al. The efficacy and safety of the novel long-acting beta2 agonist vilanterol in patients with COPD: a randomized placebo-controlled trial. Chest. 2012;142(1):119–27.PubMedCrossRef Hanania NA, Feldman G, Zachgo W, et al. The efficacy and safety of the novel long-acting beta2 agonist vilanterol in patients with COPD: a randomized placebo-controlled trial. Chest. 2012;142(1):119–27.PubMedCrossRef
20.
Zurück zum Zitat 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):256–64.PubMedCrossRef 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):256–64.PubMedCrossRef
21.
Zurück zum Zitat Allen A, Apoux L, Bal J, et al. The pharmacokinetics of fluticasone furoate and vilanterol following single inhaled administration in combination and intravenous administration of individual components in healthy subjects. J Bioequiv Availab. 2013;5:165–73. Allen A, Apoux L, Bal J, et al. The pharmacokinetics of fluticasone furoate and vilanterol following single inhaled administration in combination and intravenous administration of individual components in healthy subjects. J Bioequiv Availab. 2013;5:165–73.
22.
Zurück zum Zitat Allen A, Bareille PJ, Rousell VM. Fluticasone furoate, a novel inhaled corticosteroid, demonstrates prolonged lung absorption kinetics in man compared with inhaled fluticasone propionate. Clin Pharmacokinet. 2013;52(1):37–42.PubMedCentralPubMedCrossRef Allen A, Bareille PJ, Rousell VM. Fluticasone furoate, a novel inhaled corticosteroid, demonstrates prolonged lung absorption kinetics in man compared with inhaled fluticasone propionate. Clin Pharmacokinet. 2013;52(1):37–42.PubMedCentralPubMedCrossRef
23.
24.
Zurück zum Zitat Boscia JA, Pudi KK, Zvarich MT, et al. Effect of once-daily fluticasone furoate/vilanterol on 24-hour pulmonary function in patients with chronic obstructive pulmonary disease: a randomized, three-way, incomplete block, crossover study. Clin Ther. 2012;34(8):1655–66.PubMedCrossRef Boscia JA, Pudi KK, Zvarich MT, et al. Effect of once-daily fluticasone furoate/vilanterol on 24-hour pulmonary function in patients with chronic obstructive pulmonary disease: a randomized, three-way, incomplete block, crossover study. Clin Ther. 2012;34(8):1655–66.PubMedCrossRef
25.
Zurück zum Zitat Hughes SC, Shardlow PC, Hollis FJ, et al. Metabolism and disposition of fluticasone furoate, an enhanced-affinity glucocorticoid, in humans. Drug Metab Dispos. 2008;36:2337–44.PubMedCrossRef Hughes SC, Shardlow PC, Hollis FJ, et al. Metabolism and disposition of fluticasone furoate, an enhanced-affinity glucocorticoid, in humans. Drug Metab Dispos. 2008;36:2337–44.PubMedCrossRef
26.
Zurück zum Zitat Harrell AW, Siederer SK, Bal J, et al. Metabolism and disposition of vilanterol, a long-acting β 2-adrenoceptor agonist for inhalation use in humans. Drug Metab Dispos. 2013;41:89–100.PubMedCrossRef Harrell AW, Siederer SK, Bal J, et al. Metabolism and disposition of vilanterol, a long-acting β 2-adrenoceptor agonist for inhalation use in humans. Drug Metab Dispos. 2013;41:89–100.PubMedCrossRef
27.
Zurück zum Zitat Kempsford R, Allen A, Bal J. The effect of ketoconazole on the pharmacokinetics and pharmacodynamics of inhaled fluticasone furoate and vilanterol trifenatate in healthy subjects. Br J Clin Pharmacol. 2012;75(6):1478–87.PubMedCentralCrossRef Kempsford R, Allen A, Bal J. The effect of ketoconazole on the pharmacokinetics and pharmacodynamics of inhaled fluticasone furoate and vilanterol trifenatate in healthy subjects. Br J Clin Pharmacol. 2012;75(6):1478–87.PubMedCentralCrossRef
28.
Zurück zum Zitat Allen A, Davis A, Hardes K, et al. Influence of renal and hepatic impairment on the pharmacokinetic and pharmacodynamic properties and tolerability of fluticasone furoate and vilanterol in combination. Clin Ther. 2012;34(12):2316–32.PubMedCrossRef Allen A, Davis A, Hardes K, et al. Influence of renal and hepatic impairment on the pharmacokinetic and pharmacodynamic properties and tolerability of fluticasone furoate and vilanterol in combination. Clin Ther. 2012;34(12):2316–32.PubMedCrossRef
29.
Zurück zum Zitat Allen A, Bal J, Cheesbrough A, et al. Pharmacokinetics and pharmacodynamics of intravenous and inhaled fluticasone furoate in healthy Caucasian and East Asian subjects. Br J Clin Pharmacol. 2014;77:808–20.PubMedCrossRef Allen A, Bal J, Cheesbrough A, et al. Pharmacokinetics and pharmacodynamics of intravenous and inhaled fluticasone furoate in healthy Caucasian and East Asian subjects. Br J Clin Pharmacol. 2014;77:808–20.PubMedCrossRef
30.
Zurück zum Zitat Kerwin EM, Scott-Wilson C, Sanford L, et al. A randomised trial of fluticasone furoate/vilanterol (50/25 µg; 100/25 µg) on lung function in COPD. Respir Med. 2013;107(4):560–9.PubMedCrossRef Kerwin EM, Scott-Wilson C, Sanford L, et al. A randomised trial of fluticasone furoate/vilanterol (50/25 µg; 100/25 µg) on lung function in COPD. Respir Med. 2013;107(4):560–9.PubMedCrossRef
31.
Zurück zum Zitat Martinez FJ, Boscia J, Feldman G, et al. Fluticasone furoate/vilanterol (100/25; 200/25 µg) improves lung function in COPD: a randomised trial. Respir Med. 2013;107(4):550–9.PubMedCrossRef Martinez FJ, Boscia J, Feldman G, et al. Fluticasone furoate/vilanterol (100/25; 200/25 µg) improves lung function in COPD: a randomised trial. Respir Med. 2013;107(4):550–9.PubMedCrossRef
32.
Zurück zum Zitat Dransfield MT, Bourbeau J, Jones PW, et al. Once-daily inhaled fluticasone furoate and vilanterol versus vilanterol only for prevention of exacerbations of COPD: two replicate double-blind, parallel-group, randomised controlled trials [Erratum appears in Lancet Respir Med. 2013;1(3):186]. Lancet Respir Med. 2013;1(3):210–23.PubMedCrossRef Dransfield MT, Bourbeau J, Jones PW, et al. Once-daily inhaled fluticasone furoate and vilanterol versus vilanterol only for prevention of exacerbations of COPD: two replicate double-blind, parallel-group, randomised controlled trials [Erratum appears in Lancet Respir Med. 2013;1(3):186]. Lancet Respir Med. 2013;1(3):210–23.PubMedCrossRef
33.
Zurück zum Zitat Agusti A, de Teresa L, De Backer W, et al. A comparison of the efficacy and safety of once-daily fluticasone furoate/vilanterol with twice-daily fluticasone propionate/salmeterol in moderate to very severe COPD. Eur Respir J. 2014;43:763–72.PubMedCrossRef Agusti A, de Teresa L, De Backer W, et al. A comparison of the efficacy and safety of once-daily fluticasone furoate/vilanterol with twice-daily fluticasone propionate/salmeterol in moderate to very severe COPD. Eur Respir J. 2014;43:763–72.PubMedCrossRef
34.
Zurück zum Zitat Dransfield MT, Crim CC, Feldman G, et al. Once-daily (OD) fluticasone furoate/vilanterol (FF/VI: 100/25µg) compared with twice-daily (BD) fluticasone propionate/salmeterol (FSC: 250/50µg) in patients with COPD [abstract no. A2432]. Am J Respir Crit Care Med. 2013;187. Dransfield MT, Crim CC, Feldman G, et al. Once-daily (OD) fluticasone furoate/vilanterol (FF/VI: 100/25µg) compared with twice-daily (BD) fluticasone propionate/salmeterol (FSC: 250/50µg) in patients with COPD [abstract no. A2432]. Am J Respir Crit Care Med. 2013;187.
35.
Zurück zum Zitat Martinez FJ, Midwinter DA, Lettis S, et al. Effect of fluticasone furoate (FF)/vilanterol (VI) on lung function in COPD exacerbations: a pre-specified subgroup analysis [abstract no. A4269]. Am J Respir Crit Care Med. 2013;187. Martinez FJ, Midwinter DA, Lettis S, et al. Effect of fluticasone furoate (FF)/vilanterol (VI) on lung function in COPD exacerbations: a pre-specified subgroup analysis [abstract no. A4269]. Am J Respir Crit Care Med. 2013;187.
36.
Zurück zum Zitat Dransfield MT, Calverley PM, Bourbeau J, et al. Effect of fluticasone furoate (FF)/vilanterol (VI) compared with VI on COPD exacerbations: a pre-specified subgroup analysis [abstract no. A4269]. Am J Respir Crit Care Med. 2013;187. Dransfield MT, Calverley PM, Bourbeau J, et al. Effect of fluticasone furoate (FF)/vilanterol (VI) compared with VI on COPD exacerbations: a pre-specified subgroup analysis [abstract no. A4269]. Am J Respir Crit Care Med. 2013;187.
37.
38.
Zurück zum Zitat Vestbo J, Anderson J, Brook RD, et al. The study to understand mortality and morbidity in COPD (SUMMIT) study protocol. Eur Respir J. 2013;41:1017–22.PubMedCrossRef Vestbo J, Anderson J, Brook RD, et al. The study to understand mortality and morbidity in COPD (SUMMIT) study protocol. Eur Respir J. 2013;41:1017–22.PubMedCrossRef
39.
Metadaten
Titel
Fluticasone Furoate/Vilanterol: A Review of Its Use in Chronic Obstructive Pulmonary Disease
verfasst von
Kate McKeage
Publikationsdatum
01.09.2014
Verlag
Springer International Publishing
Erschienen in
Drugs / Ausgabe 13/2014
Print ISSN: 0012-6667
Elektronische ISSN: 1179-1950
DOI
https://doi.org/10.1007/s40265-014-0269-6

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