410
Views
30
CrossRef citations to date
0
Altmetric
Drug Evaluation

Roflumilast: an oral, once-daily selective PDE-4 inhibitor for the management of COPD and asthma

, MD FRCPC
Pages 811-818 | Published online: 30 Apr 2008

Bibliography

  • Fitzgerald JM, Boulet LP, McIvor RA, et al. Asthma control in Canada remains suboptimal: the reality of asthma control (TRAC study). Can Respir J 2006;13:253-9
  • Boulet LP. Perception of the role and potential side effects of inhaled corticosteroids among asthmatic patients. Chest 1998;113:587-92
  • Jemal A, Ward E, Hao Y, et al. Trends in the leading causes of death in the United States, 1970 – 2002. JAMA 2005;294:1255-9
  • Turato G, Zuin R, Miniati M, et al. Airway inflammation in severe chronic obstructive pulmonary disease: relationship with lung function and radiologic emphysema. Am J Respir Crit Care Med 2002;166:105-10
  • Agusti A. Systemic effects of chronic obstructive pulmonary disease: what we know and what we don't know (but should). Proc Am Thorac Soc 2007;4:522-5
  • Hogg JC, Chu F, Utokaparch S, et al. The nature of small-airway obstruction in chronic obstructive pulmonary disease. New Engl J Med 2004;350:2645-53
  • O'Donnell DE, Aaron S, Bourbeau J, et al. Canadian Thoracic Society recommendations for management of chronic obstructive pulmonary disease-2007 update. Can Respir J 2007;14(Suppl B):B5-32
  • Tattersfield AE, Harrison TW, Hubbard RB, et al. Safety of inhaled corticosteroids. Proc Am Thorac Soc 2004;1:171-5
  • Torphy TJ. Phosphodiesterase isozymes. Molecular targets for novel antiasthma agents. Am J Respir Crit Care Med 1998;157:351-70
  • Reid P. Roflumilast Altana Pharma. Current Opin Invest Drugs 2002;3:1165-70
  • Boswell-Smith V, Cazola M, Page CP. Are phosphodiesterase 4 inhibitors just more theophylline? J Allergy Clin Immunol 2006;117:1237-43
  • Barnes PJ. Theophylline for COPD. Thorax 2006;61:742-4
  • Barnes PJ. Theophylline. New perspectives for an old drug. Am J Respir Crit Care Med 2003;167:813-8
  • Wenzel SE, Schwartz LB, Langmack EL, et al. Evidence that severe asthma can be divided into two inflammatory subtypes with distinct physiologic and clinical characteristics. Am J Respir Crit Care Med 1999;160:1001-8
  • Spina D. Phosphodiesterase-4 inhibitors in the treatment of inflammatory lung disease. Drugs 2003;63:2575-94
  • Card GL, England BP, Suzuki Y, et al. Structural basis for the activity of drugs that inhibit phosphodiesterases. Structure 2004;12:2233-47
  • Lipworth BJ. Phosphodiesterase-4 inhibitors for asthma and chronic obstructive pulmonary disease. Lancet 2005;365:167-75
  • Hauns B, Hermann R, Huennemeyer A, et al. Investigation of a potential food effect on the pharmacokinetics of roflumilast, an oral, once-daily phosphodiesterase 4 inhibitor, in healthy subjects. J Clin Pharmacol 2006;46:1146-53
  • Nassr N, Lahu G, von Richter O, et al. Magnesium hydroxide/aluminium hydroxide-containing antacid does not affect the pharmacokinetics of the targeted phosphodiesterase 4 inhibitor roflumilast. J Clin Pharmacol 2007;47:660-6
  • Hermann R, Nassr N, Lahu G, et al. Steady-state pharmacokinetics of roflumilast and roflumilast N-oxide in patients with mild and moderate liver cirrhosis. Clin Pharmacokinet 2007;46:403-16
  • Herrmann R, Siegmund W, Giessmann T, et al. The oral, once daily phosphodiesterase 4 inhibitor roflumilast lacks relevant pharmacokinetic interactions with inhaled budesonide. J Clin Pharmacol 2007;47:1005-13
  • Bethke TD, Giessmann T, Westphal K, et al. Roflumilast, once-daily oral phosphodiesterase 4 inhibitor, lacks relevant pharmacologic interactions with inhaled salbutamol when co-administered in healthy subjects. Int J Pharmacol Ther 2006;44:572-9
  • de May C, Hauns B, Reutter F, et al. Repeated-dose co-administration of roflumilast and formoterol does not alter the pharmacokinetics of either drug. Am J Respir Crit Care Med 2007;175:A113
  • Nassr N, Lahu G, von Richter O, et al. Lack of a pharmacokinetic interaction between steady-state roflumilast and single-dose midazolam in healthy subjects. Br J Clin Pharmacol 2007;63:365-70
  • von Richter O, Lahu G, Huennemeyer A, et al. Effect of fluvoxamine on the pharmacokinetics of roflumilast and roflumilast N-oxide. Clin Pharmacokinet 2007;46:613-22
  • Lahu G, Huennemeyer A, Herzog R, et al. Effect of erythromycin on the pharmacokinetics of roflumilast and roflumilast N-oxide. Am J Respir Crit Care Med 2006;173:A850
  • Lahu G, Huennemeyer A, Reutter F, et al. Pharmacokinetics of roflumilast and roflumilast N-oxide with concomitant ketoconazole. Am J Respir Crit Care Med 2006;173:A850
  • Bundschuh DS, Eltze M, Barsig J, et al. In vivo efficacy in airway disease models of roflumilast, novel orally active PDE4 inhibitor. J Pharmacol Exp Ther 2001;297:280-90
  • Wollin L, Bundschuh DS, Wohlsen A, et al. Inhibition of airway hyperresponsiveness and pulmonary inflammation by roflumilast and other PDE4 inhibitors. Pulm Pharm Ther 2006;19:343-52
  • Wollin L, Marx D, Wohlsen A, et al. Roflumilast inhibition of pulmonary leukotriene production and bronchoconstriction in ovalbumin-sensitized and -challenged Guinea pigs. J Asthma 2005;42:873-8
  • Sanz M-J, Cortijo J, Taha MA, et al. Roflumilast inhibits leukocyte-endothelial cell interactions, expression of adhesion molecules and microvascular permeability. Br J Pharmacol 2007;152:481-92
  • Jones NA, Boswell-Smith V, Lever R, Page CP. The effect of selective phosphodiesterase isozyme inhibition on neutrophil function in vitro. Pulm Pharmacol Ther 2005;18:93-101
  • Hatzelmann A, Schudt C. Anti-inflammatory and immunomodulatory potential of the novel PDE4 inhibitor roflumilast in vitro. J Pharmacol Exp Ther 2001;297:267-79
  • Timmer W, Leclerc V, Birraux G, et al. The new phosphodiesterase 4 inhibitor roflumilast is efficacious in exercise-induced asthma and leads to suppression of LPS-stimulated TNF-alpha ex vivo. J Clin Pharmacol 2002;42:297-303
  • Sumi Y, Hamid Q. Airway remodeling in asthma. Allergol Int 2007;56:341-8
  • Boero S, Silvestri M, Sabatini F, et al. Inhibition of lung fibroblast proinflammatory functions by roflumilast N-oxide. Am J Respir Crit Care Med 2006;173:A33
  • Klar J, Sabatini F, Schatton E, et al. Roflumilast N-oxide reduces human fibroblast function. Eur Respir J 2007;30(Suppl 51):544S
  • Burgess JK, Oliver BG, Poniris MH, et al. A phosphodiesterase 4 inhibitor inhibits matrix protein deposition in airways in vitro. J Allergy Clin Immunol 2006;118:649-57
  • Louw C, Williams Z, Venter L, et al. Roflumilast, a phosphodiesterase 4 inhibitor, reduces airway hyperresponsiveness after allergen challenge. Respiration 2007;74:411-7
  • Kanniess F, Beler J, Beeh K-M, et al. Effects of roflumilast on exhaled NO, airway hyperresponsiveness, and inflammatory markers in patients with asthma. Eur Respir J 2006;28(Suppl 50):670S
  • Gauvreau GM, Boulet LP, Cote J, et al. Effects of roflumilast on airway inflammation and function following allergen challenge in patients with allergic asthma. Am J Respir Crit Care Med 2007;175:A484
  • van Schalkwyk E, Strydom K, Williams Z, et al. Roflumilast, an oral, once-daily phosphodiesterase 4 inhibitor, attenuates allergen-induced asthmatic reactions. J Allergy Clin Immunol 2005;116:292-8
  • Schmidt BMW, Kusma M, Feuring M, et al. The phosphodiesterase 4 inhibitor roflumilast is effective in the treatment of allergic rhinitis. J Allergy Clin Immunol 2001;108:530-6
  • Bateman ED, Izqueirdo JL, Harnest U, et al. Efficacy and safety of roflumilast in the treatment of persistent asthma. Ann Allergy Asthma Immunol 2006;96:679-86
  • Bousquet J, Aubier M, Sastre J, et al. Comparison of roflumilast, an oral, anti-inflammatory, with beclomethasone diproprionate in the treatment of persistent asthma. Allergy 2006;61:72-8
  • Hogg JC. Pathophysiology of airflow limitation in chronic obstructive pulmonary disease. Lancet 2004;364:709-21
  • Martorana PA, Beume R, Lucattelli M, et al. Roflumilast fully prevents emphysema in mice chronically exposed to cigarette smoke. Am J Respir Crit Care Med 2005;172:848-53
  • Fitzgerald MF, Spicer D, McAulay AE, et al. Roflumilast but not methylprednisolone inhibited cigarette smoke-induced pulmonary inflammation in guinea pigs. Eur Respir J 2006;28(Suppl 50):663S
  • Grootendorst DC, Gauw SA, Verhoosel RM, et al. Reduction in sputum neutrophil and eosinophil numbers by the PDE4 inhibitor roflumilast in patients with COPD. Thorax 2007;62:1081-7
  • Rabe K, Bateman ED, O'Donnell D, et al. Roflumilast–an oral anti-inflammatory treatment for chronic obstructive pulmonary disease: a randomised controlled trial. Lancet 2005;366:563-71
  • Calverley PMA, McIvor A, et al. Effect of 1-year treatment with roflumilast in severe chronic obstructive pulmonary disease. Am J Respir Crit Care Med 2007;176:154-61
  • Rutten-van Molken MP, van Nooten FE, Lindemann M, et al. A 1-year prospective cost-effectiveness analysis of roflumilast for the treatment of patients with severe chronic obstructive pulmonary disease. Pharmacoeconomics 2007;25:695-711
  • Lipworth B. Phosphodiesterase type 4 inhibitors for asthma: a real breakthrough or just expensive theophylline? Ann Allergy Asthma Immunol 2006;96:640-1
  • Green RH, Brightling CE, Woltmann G, et al. Analysis of induced sputum in adults with asthma: identification of subgroup with isolated sputum neutrophilia and poor response to inhaled corticosteroids. Thorax 2002;57:875-9
  • Shannon J, Ernst P, Yamauchi Y, et al. Differences in airway cytokine profile in severe asthma compared to moderate asthma. Chest 2008;133:420-6
  • Suissa S, McGhan R, Niewohner D, Make B. Inhaled corticosteroids in chronic obstructive pulmonary disease. Proc Am Thorac Soc 2007;4:535-42
  • Calverley PMA, Anderson JA, Celli B, et al. Salmeterol and fluticasone propionate and survival in chronic obstructive pulmonary disease. New Engl J Med 2007;356:775-89
  • Aaron SD, Vandemheen KL, Fergusson D, et al. Tiotropium in combination with placebo, salmeterol, or fluticasone-salmeterol for treatment of chronic obstructive pulmonary disease. Ann Intern Med 2007;146:545-55
  • Wedzicha JA, Calverley PMA, Seemungal TA, et al. The prevention of COPD exacerbations by salmeterol/fluticasone propionate or tiotropium bromide. Am J Respir Crit Care Med 2008;177:19-26
  • Ernst P, Gonzalez AV, Brassard P, Suissa S. Inhaled corticosteroid use in obstructive pulmonary disease and the risk of hospitalization for pneumonia. Am J Respir Crit Care Med 2007;176:162-6
  • The Helios study BY217/M2-128. 24 weeks treatment with roflumilast or placebo in COPD patients treated with tiotropium 18 μg daily. Available from: http://clinicaltrials.gov/ct2/show/NCT00424268?term%20=%20roflumilast+and+tiotropium&rank=1

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.