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Drug Evaluation

Roflumilast: a phosphodiesterase-4 inhibitor for the treatment of respiratory disease

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Pages 1105-1113 | Published online: 17 Aug 2006

Bibliography

  • MASOLI M, FABIAN D, HOLT S, BEASLEY R: The global burden of asthma: executive summary of the GINA Dissemination Committee report. Allergy (2004) 59:469-478.
  • PAUWELS RA, BUIST AS, CALVERLEY PM, JENKINS CR, HURD SS: Global strategy for the diagnosis, management, and prevention of chronic obstructive pulmonary disease. NHLBI/WHO Global Initiative for Chronic Obstructive Lung Disease (GOLD) workshop summary. Am. J. Respir. Crit. Care Med. (2005) 163(5):1256-1276.
  • REDD SC: Asthma in the United States: burden and current theories. Environ. Health Perspect. (2002) 1109(4):557-560.
  • HOGG JC: Pathophysiology of airflow limitation in chronic obstructive pulmonary disease. Lancet (2004) 364(9435):709-721.
  • JOOS L, PARE P, SANDFORD A: Genetic risk factors of chronic obstructive pulmonary disease. Swiss Med. Wkly (2002) 132(3-4):27-37.
  • STRAND A, LUCKOW A: Initiation of maintenance treatment of persistent asthma: salmeterol/fluticasone propionate combination treatment is more effective than inhaled steroid alone. Respir. Med. (2004) 98(10):1008-1015.
  • KELLOWAY JS, WYATT RA, ADLIS SA: Comparison of patients’ compliance with prescribed oral and inhaled asthma medications. Arch. Intern. Med. (1994) 154(12):1349-1352.
  • BARNES PJ, STOCKLEY: New treatments for COPD. Eur. Respir. J. (2005) 25:1084-1106.
  • RAHMAN I: Oxidative stress and gene transcription in asthma and chronic obstructive pulmonary disease: antioxidant therapeutic targets. Curr. Drug Targets Inflamm. Allergy (2002) 1(3):291-315.
  • ESSAYAN DM: Cyclic nucleotide phosphodiesterases. J. Allergy Clin. Immunol. (2001) 108(5):671-680.
  • SALONIA A, RIGATTI P, MONTORSI F: Sildenafil in erectile dysfunction: a critical review. Curr. Med. Res. Opin. (2003) 19(4):241-262.
  • PACKER M, CARVER JR, RODEHEFFER RJ et al.: Effect of oral milrinone on mortality in severe chronic heart failure. The PROMISE Study Research Group. N. Engl. J. Med. (1991) 325(21):1468-1475.
  • LEWIS GD, SEMIGRAN MJ: Type 5 phosphodiesterase inhibition in heart failure and pulmonary hypertension. Curr. Heart Fail. Rep. (2004) 1(4):183-189.
  • O’DONNELL JM, ZHANG HT: Antidepressant effects of inhibitors of cAMP phosphodiesterase (PDE4). Trends Pharmacol. Sci. (2004) 25(3):158-163.
  • HOUSLAY MD: PDE4 cAMP-specific phosphodiesterases. Prog. Nucleic Acid Res. Mol. Biol. (2001) 69:249-315.
  • HOUSLAY MD, ADAMS: PDE4 cAMP phosphodiesterases: modular enzymes that orchestrate signalling cross-talk, desensitization and compartmentalization. Biochem. J. (2003) 370:1-18.
  • CATHERINE JIN S-L, LAN L, ZOUDILOVA M, Conti M: Specific role of phosphodiesterase 4B in lipopoly- saccharide-induced signaling in mouse macrophages J. Immunol. (2005) 175:1523-1531.
  • LYNCH MJ, BAILLIE GS, MOHAMED A et al.: RNA silencing identifies PDE4D5 as the functionally relevant cAMP phosphodiesterase interacting with β-arrestin to control the protein kinase A/AKAP79-mediated switching of the 2-adrenergic receptor to activation of ERK in HEK293B2 cells. J. Biol. Chem. (2005) 280:33178-33189.
  • WATCHELL H: Characteristic behavioural alterations in rats induced by rolipram and others selective adenosine cyclic 3,4 phosphodiesterase 4 inhibitors. Psychophamacology (1982) 77(4):309-316.
  • SCOTT AI, PERINI AF, SHERING PA, WHALLEY LJ: In-patient major depression: is rolipram as effective as amitriptyline? Eur. J. Clin. Pharmacol. (1991) 40(2):127-129.
  • CHUNG KF: Phosphodiesterase inhibitors in airways disease. Eur. J. Pharmacol. (2006) 533(1-3):110-117.
  • HAUNS B, HUNNEMEYER A, SEIBERLING A et al.: Investigation of pharmacokinetics of roflumilast and roflumilast N-oxide in healthy subjects after a single morning or evening oral administration of 500µg roflumilast in healthy subjects-an open, randomised, two-period crossover study. Am. J. Respir. Crit. Care Med. (2003) 167(7):A92.
  • DAVID ME, ZECH K, SEIBERLING A et al.: Roflumilast, a novel, oral, selective PDE4 inhibitor, shows high absolute bioavalability. J. Allergy Clin. Immunol. (2004) 113(2):P780.
  • HAUNS B, HUNNEMEYER A, DUURSEMA L et al.: Roflumilast and its active metabolite roflumilast N-oxide do not interact with R- and S-warfarin. Eur. Respir. J. (2003) 22(Suppl. 45):103s.
  • HUNNEMEYER A, BETHKE T, DAVID ME et al.: No interaction of roflumilast and its active metabolite, roflumilast N-oxide, with inhaled budesonide. Am. J. Respir. Crit. Care Med. (2002) 165(8):.
  • WEIMAR C, BETHKE T, WESTPHAL K et al.: Roflumilast and its active metabolite, roflumilast N-oxide, do not interact with inhaled salbutamol. Am. J. Respir. Crit. Care Med. (2002) 165(8):A594.
  • BETHKE T, HARTMANN M, ZECH K et al.: No dose adjustment of roflumilast in patients with severe renal impairment. Am. J. Respir. Crit. Care Med. (2002) 165(8):A594.
  • HATZELMANN A, SCHUDT C: Anti-inflammatory and immuomodulatory potential of the novel PDE4 inhibitor roflumilast in vitro. J. Pharmacol. Exp. Ther. (2001) 297(1):267-279.
  • JONES NA, BOSWELL-SMITH V, LEVER R, PAGE CP: The effect of selective phosphodiesterase isoenzyme inhibition on neutrophil function in vitro. Pulm. Pharmacol. Ther. (2005) 18(2):93-101.
  • CROCKER IC, TOWNLEY RG, KHAN MM: Phosphodiesterase inhibitors suppress proliferation of peripheral blood mononuclear cells and interleukin-4 and -5 secretion by human T-helper type cells, Immunopharmacology (1996) 31(2-3):223-235.
  • GROWCOTT E, REN X, BANNER KH et al.: Anti-proliferative effect of phosphodiesterase 4 inhibitors in human pulmonary artery smooth muscle cells. Am. J. Respir. Crit. Care Med. (2005) 169:A721.
  • MATA M, SARRIA B, BUENESTADO A, CORTIJO J, CERDA M, ORCILLO EJ: Phosphodiesterase 4 inhibition decreases MUC5AC expression induced by epidermal growth factor in human airway epithelial cells. Thorax (2005) 60(2):144-152.
  • BUNDSCHUH DS, ELTZE M, BARSIG J, WOLLIN L, HATZELMANN A, BEUME R: In vivo efficacy in airway disease models of roflumilast, a novel orally active PDE4 inhibitor. J. Pharmacol. Exp. Ther. (2001) 297(1):280-290.
  • BOSWELL-SMITH V, SPINA D, PAGE CP: Regulation by selective phosphodiesterase 4 isoenzyme inhibitors of non-adrenergic non-cholinergic contraction in guinea pig isolated main bronchus. Am. J. Respir. Crit. Care Med. (2004) 168:A180.
  • SHAH S, SPINA D, PAGE C: The release of substance P-like immunoreactivity from guinea-pig isolated bronchus. Am. J. Respir. Crit. Care Med. (1996) 153(4):A848.
  • WOLLIN L, MARX D, WOHLSEN A, BEUME R: Roflumilast inhibition of pulmonary leukotriene production and bronchoconstriction in ovalbumin- sensitized and -challenged guinea pigs. J. Asthma (2005) 42(10):873-878.
  • WOLLIN L, BUNDSCHUH DS, WOHLSEN A, MARX D, BEUME R: Inhibition of airway hyperresponsiveness and pulmonary inflammation by roflumilast and other PDE4 inhibitors. Pulm. Pharmacol. Ther. (2006) 19(5):343-352.
  • WOLLIN L, BARSIG J, MARX D, WOHLSEN A, BEUME R: Inhibition by roflumilast versus cilomilast of pulmonary leukocyte accumulation and TNF-α release in a rat model of LPS-induced pulmonary neutrophilia. Eur Respir. J (2003) 22(Suppl. 45):107s.
  • MARTORANA, PA, BEUME, R, LUCATTELLI, M, WOLLIN, L, LUNGARELLA, G. Roflumilast fully prevents emphysema in mice chronically exposed to cigarette smoke. Am. J. Respir. Crit. Care Med. (2005) 172(7):848-853.
  • KUMAR RK, HERBERT C, THOMAS PS et al.: Inhibition of inflammation and remodeling by roflumilast and dexamethasone in murine chronic asthma. J. Pharmacol. Exp. Ther. (2003) 307(1):349-355.
  • LEICHTL S, SCHMID-WIRLITSCH C, BREDENBROKER D et al.: Dose-related efficacy of once-daily roflumilast, a new orally active, selective phosphodiesterase 4 inhibitor, in asthma. Am. J. Respir. Crit. Care Med. (2002) 165(8):A185.
  • 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(2):292-298.
  • ENGELSTATTER R, WINGERTZAHN M, SCHMID-WIRLITSCH C et al.: Roflumilast, an oral, once-daily phosphodiesterase 4 (PDE4) inhibitor, does not exhibit bronchodilatory activity. Ann. Allergy Asthma Immunol. (2005) 94(1):P159.
  • 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-α ex vivo. J. Clin. Pharmacol. (2002) 42(3):297-303.
  • BOUSQUET J, AUBIER M, SASTRE J et al.: Comparison of roflumilast, an oral anti-inflammatory, with beclamethasone diproprionate in the treatment of persistent asthma. Allergy (2006) 61(1):72.
  • RABE KF, BATEMAN ED, O’DONNELL D, WITTE S, BREDENBROKER D, BETHKE TD: Roflumilast – an oral anti-inflammatory treatment for chronic obstructive pulmonary disease: a randomised controlled trial. Lancet (2005) 366(9485):563-571.
  • BOSZORMENYI-NAGY G, PIETERS W, STEFFEN H et al.: The effect of roflumilast treatment and subsequent withdrawal in patients with COPD. Proc. Am. Thorac. Soc. (2005) 2:A544.
  • GROOTENDORST DC, GAUW SA, STERK PJ et al.: Treatment with PDE4 inhibitor roflumilast reduces sputum neutrophil and eosinophil numbers in patients with COPD. Proc. Am. Thorac. Soc. (2005) 2:A543.
  • SCHMIDT BM, USMA M, EURING M et al.: The phosphodiesterase 4 inhibitor roflumilast is effective in the treatment of allergic rhinitis. J. Allergy Clin. Immunol. (2001) 108(4):530-536.
  • IZQUIERDO JL, BATEMAN ED, VILLASANTE C, SCHMID-WIRLITSCH C, BREDENBROKER D, WURST W: Long term efficacy and safety over once year or once daily roflumilast. A new orally active, selective phosphodiesterase 4 inhibitor, in asthma. Am. J. Respir. Crit. Care Med. (2003) 167(7):A765.
  • LOSCO PE, EVANS EW, BARAT SA et al.: The toxicity of SCH 351591, a novel phosphodiesterase-4 inhibitor, in cynomolgus monkeys. Toxicol. Pathol. (2004) 32(3):295-308.
  • MECKLENBURG L, HEUSER A, JUENGLING T et al.: Mesenteritis precedes vasculitis in the rat mesentery after subacute administration of a phosphodiesterase type 4 inhibitor. Toxicol. Lett. (2006) 163(1):54-64.
  • SPINA D: The potential of PDE4 inhibitors in respiratory disease. Curr. Drug Targets Inflamm. Allergy. (2004) 3(3):231-236.

Websites

  • http://www.who.int/mediacentre/ factsheets/fs206/en/print.html WHO fact sheet 206 on bronchial asthma (2000).
  • http://www.brit-thoracic.org.uk/ BurdenofLungDisease2.html Burden of disease, British Thoracic Society, second edition (2006).
  • http://www.altana.com/root/index.php?page_id=202&cms_press_id=355 Altana website (2005).
  • www.datamonitor.com/∼ 90c3cffcaf0546f7ad089c97929631c8∼ /companies/company/?pid=E915DFB3- 6FBF-4C67 AE8F29EB1160FC4C&nid =816AB3F2-982C-44B3-887C-3451D89A6362&type=NewsWire&article1 Merck press release, DataMonitor: Merck discontinues development of PDE-4 inhibitor compound (2003).
  • http://www.fda.gov/ohrms/dockets/ac/03/ slides/3976S1_01_Glaxo-Ariflo_files/frame.htm#slide0648.htm FDA website: Ariflo (2003).

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