582
Views
8
CrossRef citations to date
0
Altmetric
Drug Evaluation

Pharmacodynamic and pharmacokinetic assessment of fluticasone furoate + vilanterol for the treatment of asthma

, , &
Pages 813-822 | Received 10 Feb 2016, Accepted 17 May 2016, Published online: 09 Jun 2016

References

  • Global Initiative for Asthma (GINA). Global strategy for asthma management and prevention; 2015; [ cited 2016 Jan 26]. Available from: www.ginasthma.com/Guidelines/guidelines-resources.html
  • Papi A, Cazzola M. Combination treatment in asthma: reviewing old and new options. Pulm Pharmacol Ther. 2015;34:72–74.
  • Ricciardolo FL, Blasi F, Centanni S, et al. Therapeutic novelties of inhaled corticosteroids and bronchodilators in asthma. Pulm Pharmacol Ther. 2015;33:1–10.
  • Newman SP, Chan H-K. In vitro/in vivo comparisons in pulmonary drug delivery. J Aerosol Med Pulm Drug Deliv. 2008;21:77–84.
  • Danhof M, De Lange EC, Della Pasqua OE, et al. Mechanism-based pharmacokinetic-pharmacodynamic (PK-PD) modeling in translational drug research. Trends Pharmacol Sci. 2008;29:186–191.
  • Tayab ZR, Hochhaus G. Pharmacokinetic/pharmacodynamic evaluation of inhalation drugs: application to targeted pulmonary delivery systems. Expert Opin Drug Deliv. 2005;2:519–532.
  • Cazzola M, Rogliani P, Sanduzzi A, et al. Influence of ethnicity on response to asthma drugs. Expert Opin Drug Metab Toxicol. 2015;11:1089–1097.
  • Sheikh A, Halani L, Bhopal R, et al. Facilitating the recruitment of minority ethnic people into research: qualitative case study of South Asians and asthma. PLoS Med. 2009;6:e1000148.
  • Rogliani P, Matera MG, Cazzola M. Fluticasone furoate/vilanterol combination for the treatment of COPD and asthma. Drugs Today (Barc). 2015;51:469–478.
  • 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.
  • Villa E, Magnoni MS, Micheli D, et al. A review of the use of fluticasone furoate since its launch. Expert Opin Pharmacother. 2011;12:2107–2117.
  • Winkler J, Hochhaus G, Derendorf H. How the lung handles drugs: pharmacokinetics and pharmacodynamics of inhaled corticosteroids. Proc Am Thorac Soc. 2004;1:356–363.
  • Derendorf H, Nave R, Drollmann A, et al. Relevance of pharmacokinetics and pharmacodynamics of inhaled corticosteroids to asthma. Eur Respir J. 2006;28:1042–1050.
  • Lipworth BJ. Clinical pharmacology of corticosteroids in bronchial asthma. Pharmacol Ther. 1993;58:173–209.
  • Derendorf H, Meltzer EO. Molecular and clinical pharmacology of intranasal corticosteroids: clinical and therapeutic implications. Allergy. 2008;63:1292–1300.
  • Daley-Yates PT. Inhaled corticosteroids: potency, dose equivalence and therapeutic index. Br J Clin Pharmacol. 2015;80:372–380.
  • Valotis A, Högger P. Human receptor kinetics and lung tissue retention of the enhanced-affinity glucocorticoid fluticasone furoate. Respir Res. 2007;8:54.
  • 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;670:244–251.
  • McCormack PL, Scott LJ. Fluticasone furoate. Drugs. 2007;67:1905–1915.
  • Hochhaus G. Relative receptor affinity comparisons among inhaled/intranasal corticosteroids: perspectives on clinical relevance. Respir Res. 2008;9:75.
  • Hochhaus G, Möllmann H, Derendorf H, et al. Pharmacokinetic/pharmacodynamic aspects of aerosol therapy using glucocorticoids as a model. J Clin Pharmacol. 1997;37:881–892.
  • Hughes SC, Shardlow PC, Hollis FJ, et al. Metabolism and disposition of fluticasone furoate, an enhanced-affinity glucocorticoid, in humans. Drug Metab Dispos. 2008;36:2337–2344.
  • Giavina-Bianchi P, Agondi R, Stelmach R, et al. Fluticasone furoate nasal spray in the treatment of allergic rhinitis. Ther Clin Risk Manag. 2008;4:465–472.
  • 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;52:37–42.
  • Kempsford R, Allen A, Kelly K, et al. A repeat-dose thorough QT study of inhaled fluticasone furoate/vilanterol combination in healthy subjects. Br J Clin Pharmacol. 2014;77:466–479.
  • Bateman ED, Bleecker ER, Lötvall J, et al. Dose effect of once-daily fluticasone furoate in persistent asthma: a randomized trial. Respir Med. 2012;106:642–650.
  • Busse WW, Bleecker ER, Bateman ED, et al. Fluticasone furoate demonstrates efficacy in patients with asthma symptomatic on medium doses of inhaled corticosteroid therapy: an 8-week, randomised, placebo-controlled trial. Thorax. 2012;67:35–41.
  • Oliver A, Allen A, VanBuren S, et al. Safety, tolerability, pharmacokinetics, and pharmacodynamics of fluticasone furoate, a novel inhaled corticosteroid, in children aged 5–11 years with persistent asthma: a randomized trial. Clin Pharmacol Drug Dev. 2013;3:144–150.
  • 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;77:808–820.
  • 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;34:2316–2332.
  • Raissy HH, Kelly HW, Harkins M, et al. Inhaled corticosteroids in lung diseases. Am J Respir Crit Care Med. 2013;187:798–803.
  • Van Den Berge M, Luijk B, Bareille P, et al. Prolonged protection of the new inhaled corticosteroid fluticasone furoate against AMP hyperresponsiveness in patients with asthma. Allergy. 2010;65:1531–1535.
  • Keith PK, Scadding GK. Are intranasal corticosteroids all equally consistent in managing ocular symptoms of seasonal allergic rhinitis? Curr Med Res Opin. 2009;25:2021–2041.
  • Gueron B, Demoly P, Kay S, et al. Do patients on intranasal fluticasone furoate, mometasone furoate and fluticasone propionate experience similar numbers of symptom-free days and quality of life? A cross-sectional study in three European countries. Poster 380, XXIX Congress of the European Academy of Allergy and Clinical Immunology, London, Jun 5–9, 2010.
  • Okubo K, Nakashima M, Miyake N, et al. Comparison of fluticasone furoate and fluticasone propionate for the treatment of Japanese cedar pollinosis. Allergy Asthma Proc. 2009;30:84–94.
  • Allen A. The relationship between fluticasone furoate systemic exposure and cortisol suppression. Clin Pharmacokinet. 2013;52:885–896.
  • Cazzola M, Page CP, Rogliani P, et al. β2-agonist therapy in lung disease. Am J Respir Crit Care Med. 2013;187:690–696.
  • Hanania NA, Sharafkhaneh A, Barber R, et al. Beta-agonist intrinsic efficacy: measurement and clinical significance. Am J Respir Crit Care Med. 2002;165:1353–1358.
  • Charlton SJ. Agonist efficacy and receptor desensitization: from partial truths to a fuller picture. Br J Pharmacol. 2009;158:165–168.
  • Slack RJ, Barrett VJ, Morrison VS, et al. In vitro pharmacological characterization of vilanterol, a novel long-acting β2-adrenoceptor agonist with 24-hour duration of action. J Pharmacol Exp Ther. 2013;344:218–230.
  • Morrison V, Sturton G, Barrett V, et al. Pharmacological characterisation of GW642444, a long-acting β2-agonist (LABA) with rapid onset and long duration, on isolated large and small human airways [abstract]. Am J Respir Crit Care Med. 2010;181:A4453.
  • Cazzola M, Testi R, Matera MG. Clinical pharmacokinetics of salmeterol. Clin Pharmacokinet. 2002;41:19–30.
  • Taburet AM, Schmit B. Pharmacokinetic optimisation of asthma treatment. Clin Pharmacokinet. 1994;26:396–418.
  • Harrell AW, Siederer SK, Bal J, et al. Metabolism and disposition of vilanterol, a long-acting β2-adrenoceptor agonist for inhalation use in humans. Drug Metab Dispos. 2013;41:89–100.
  • 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;5:165–173.
  • 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;26:256–264.
  • Anonymous. BREO ELLIPTA (fluticasone furoate and vilanterol inhalation powder); [ cited 2016 Jan 26]. Available from: https://www.gsksource.com/pharma/content/dam/GlaxoSmithKline/US/en/Prescribing_Information/Breo_Ellipta/pdf/BREO-ELLIPTA-PI-MG.PDF
  • Oliver A, VanBuren S, Allen A, et al. Safety, tolerability, pharmacokinetics, and pharmacodynamics of vilanterol, a novel inhaled long-acting β-agonist, in children aged 5-11 years with persistent asthma: a randomized trial. Clin Pharmacol Drug Dev. 2014;3:215–221.
  • Nakahara N, Takahashi N, Kelleher D, et al. Safety, tolerability and pharmacokinetics (PK) of single and repeat doses of GSK573719 in healthy Japanese subjects [abstract]. Am J Respir Crit Care Med. 2012;185:A2915.
  • Hu C, Jia J, Dong K, et al. Pharmacokinetics and tolerability of inhaled umeclidinium and vilanterol alone and in combination in healthy Chinese subjects: a randomized, open-label, crossover trial. PLoS One. 2015;10:e0121264.
  • Kempsford R, Allen A, Bal J, et al. The effect of ketoconazole on the pharmacokinetics and pharmacodynamics of inhaled fluticasone furoate and vilanterol trifenatate in healthy subjects. Br J Clin Pharmacol. 2013;75:1478–1487.
  • Lötvall J, Bateman ED, Bleecker ER, et al. 24-h duration of the novel LABA vilanterol trifenatate in asthma patients treated with inhaled corticosteroids. Eur Respir J. 2012;40:570–579.
  • Kempsford RD, Allen A, Bareille P, et al. The safety, tolerability, pharmacodynamics and pharmacokinetics of inhaled fluticasone furoate (FF) and vilanterol (VI) are unaffected by administration in combination [abstract]. Eur Respir J. 2011;38(Suppl 55):P824.
  • Allen A, Schenkenberger I, Trivedi R, et al. Inhaled fluticasone furoate/vilanterol does not affect hypothalamic-pituitary-adrenal axis function in adolescent and adult asthma: randomised, double-blind, placebo-controlled study. Clin Respir J. 2013;7:397–406.
  • Nakahara N, Wakamatsu A, Kempsford R, et al. The safety, pharmacokinetics and pharmacodynamics of a combination of fluticasone furoate and vilanterol in healthy Japanese subjects. Int J Clin Pharmacol Ther. 2013;51:660–671.
  • Chen X, Zheng X, Jiang J, et al. Pharmacodynamics and pharmacokinetics of fluticasone furoate/vilanterol in healthy Chinese subjects. Pharmacotherapy. 2015;35:586–599.
  • Gross AS, Goldfrad C, Hozawa S, et al. Ethnic sensitivity assessment of fluticasone furoate/vilanterol in East Asian asthma patients from randomized double-blind multicentre phase IIb/III trials. BMC Pulm Med. 2015;15:165.
  • European Medicines Agency. Summary of product characteristics: Relvar Ellipta inhalation powder; 2013; [ cited 2016 Jan 27]. Available from: http://www.ema.europa.eu/docs/en_GB/document_library/EPAR_-_Product_Information/human/002673/WC500157633.pdf
  • O’Byrne PM, Bleecker ER, Bateman ED, et al. Once-daily fluticasone furoate alone or combined with vilanterol in persistent asthma. Eur Respir J. 2014;43:773–782.
  • Bleecker ER, Lötvall J, O’Byrne PM, et al. Fluticasone furoate-vilanterol 100-25 mcg compared with fluticasone furoate 100 mcg in asthma: a randomized trial. J Allergy Clin Immunol Pract. 2014;2:553–561.
  • Woodcock A, Bleecker ER, Lötvall J, et al. Efficacy and safety of fluticasone furoate/vilanterol compared with fluticasone propionate/salmeterol combination in adult and adolescent patients with persistent asthma: a randomized trial. Chest. 2013;144:1222–1229.
  • Bateman ED, O’Byrne PM, Busse WW, et al. Once-daily fluticasone furoate (FF)/vilanterol reduces risk of severe exacerbations in asthma versus FF alone. Thorax. 2014;69:312–319.
  • Busse WW, O’Byrne PM, Bleecker ER, et al. Safety and tolerability of the novel inhaled corticosteroid fluticasone furoate in combination with the β2 agonist vilanterol administered once daily for 52 weeks in patients ≥12 years old with asthma: a randomised trial. Thorax. 2013;68:513–520.
  • Committee for Medicinal Products for Human Use. Assessment report. Relvar Ellipta. International non-proprietary name: fluticasone furoate/vilanterol. Procedure No. EMEA/H/C/002673/0000; [ cited 2016 Feb 11]. Available from: http://www.ema.europa.eu/docs/en_GB/document_library/EPAR_-_Public_assessment_report/human/002673/WC500157635.pdf
  • Anonymous. RELVAR™ ELLIPTA™ gains approval in Japan for the treatment of asthma; [ cited 2016 Feb 11]. Available from: http://www.gsk.com/en-gb/media/press-releases/2013/relvar-ellipta-gains-approval-in-japan-for-the-treatment-of-asthma/
  • Anonymous. FDA approves BREO® ELLIPTA® for the treatment of adults with asthma in the US; [ cited 2016 Feb 11]. Available from: http://www.gsk.com/en-gb/media/press-releases/2015/fda-approves-breo-ellipta-for-the-treatment-of-adults-with-asthma-in-the-us/
  • Anonymous. GSK receives approval for BREO® ELLIPTA® for the treatment of adults with asthma; [ cited 2016 Feb 11]. Available from: http://ca.gsk.com/en-ca/media/press-releases/2015/gsk-receives-approval-for-breo-ellipta-for-the-treatment-of-adults-with-asthma/
  • Forbes B, Asgharian B, Dailey LA, et al. Challenges in inhaled product development and opportunities for open innovation. Adv Drug Deliv Rev. 2011;63:69–87.
  • Cooper AE, Ferguson D, Grime K. Optimisation of DMPK by the inhaled route: challenges and approaches. Curr Drug Metab. 2012;13:457–473.
  • Selg E, Ewing P, Acevedo F, et al. Dry powder inhalation exposures of the endotracheally intubated rat lung, ex vivo and in vivo: the pulmonary pharmacokinetics of fluticasone furoate. J Aerosol Med Pulm Drug Deliv. 2013;26:181–189.
  • Newman SP. Can lung deposition data act as a surrogate for the clinical response to inhaled asthma drugs? Br J Clin Pharmacol. 2000;49:529–537.
  • Wang Y-B, Watts AB, Peters JI, et al. The impact of pulmonary diseases on the fate of inhaled medicines – a review. Int J Pharm. 2014;461:112–128.
  • Blake K, Lima J. Pharmacogenomics of long-acting β2-agonists. Expert Opin Drug Metab Toxicol. 2015;11:1733–1751.
  • Ortega VE, Hawkins GA, Moore WC, et al. Effect of rare variants in ADRB2 on risk of severe exacerbations and symptom control during longacting β agonist treatment in a multiethnic asthma population: a genetic study. Lancet Respir Med. 2014;2:204–213.
  • Ortega VE, Meyers DA, Bleecker ER. Asthma pharmacogenetics and the development of genetic profiles for personalized medicine. Pharmgenomics Pers Med. 2015;8:9–22.

Reprints and Corporate Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

To request a reprint or corporate permissions for this article, please click on the relevant link below:

Academic Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

Obtain permissions instantly via Rightslink by clicking on the button below:

If you are unable to obtain permissions via Rightslink, please complete and submit this Permissions form. For more information, please visit our Permissions help page.