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The molecular basis for the inhibition of phosphodiesterase-4D by three natural resveratrol analogs. Isolation, molecular docking, molecular dynamics simulations, binding free energy, and bioassay.
Biochimica et biophysica acta 20131001
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Simultaneous quantitation of IC87114, roflumilast and its active metabolite roflumilast N-oxide in plasma by LC-MS/MS: application for a pharmacokinetic study.
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Der Internist 20121101
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The glucose-lowering effects of the PDE4 inhibitors roflumilast and roflumilast-N-oxide in db/db mice.
Diabetologia 20121001
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Alternatives to indicating roflumilast and the chronic obstructive pulmonary disease classification.
Archivos de bronconeumologia 20120901
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Effect of the phosphodiesterase 4 inhibitor roflumilast on glucose metabolism in patients with treatment-naive, newly diagnosed type 2 diabetes mellitus.
The Journal of clinical endocrinology and metabolism 20120901
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Spanish COPD Guidelines (GesEPOC): pharmacological treatment of stable COPD. Spanish Society of Pulmonology and Thoracic Surgery.
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Superiority of PC-SOD to other anti-COPD drugs for elastase-induced emphysema and alteration in lung mechanics and respiratory function in mice.
American journal of physiology. Lung cellular and molecular physiology 20120615
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Phosphodiesterase-4 inhibition as a therapeutic approach to treat capillary leakage in systemic inflammation.
The Journal of physiology 20120601
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Physiological effects of roflumilast at rest and during exercise in COPD.
The European respiratory journal 20120501
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Roflumilast enhances the renal protective effects of retinoids in an HIV-1 transgenic mouse model of rapidly progressive renal failure.
Kidney international 20120501
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Can we cure HIV-1-associated nephropathy in transgenic mice?
Kidney international 20120501
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Sensitive quantification of roflumilast and roflumilast N-oxide in human plasma by LC-MS/MS employing parallel chromatography and electrospray ionisation.
Journal of chromatography. B, Analytical technologies in the biomedical and life sciences 20120415
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Additive anti-inflammatory effects of beta 2 adrenoceptor agonists or glucocorticosteroid with roflumilast in human peripheral blood mononuclear cells.
Pulmonary pharmacology & therapeutics 20120401
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Roflumilast: a novel treatment for chronic obstructive pulmonary disease.
The Annals of pharmacotherapy 20120401
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Roflumilast inhibits the release of chemokines and TNF-α from human lung macrophages stimulated with lipopolysaccharide.
British journal of pharmacology 20120301
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Lack of involvement of type 7 phosphodiesterase in an experimental model of asthma.
The European respiratory journal 20120301
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The Consultant pharmacist : the journal of the American Society of Consultant Pharmacists 20120301
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Bioorganic & medicinal chemistry letters 20120215
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Anti-asthmatic effect of ASP3258, a novel phosphodiesterase 4 inhibitor.
International immunopharmacology 20120101
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Anti-neutrophilic inflammatory activity of ASP3258, a novel phosphodiesterase type 4 inhibitor.
International immunopharmacology 20120101
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Clinical therapeutics 20120101
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Combination of roflumilast with a beta-2 adrenergic receptor agonist inhibits proinflammatory and profibrotic mediator release from human lung fibroblasts.
Respiratory research 20120101
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Cost-effectiveness of available treatment options for patients suffering from severe COPD in the UK: a fully incremental analysis.
International journal of chronic obstructive pulmonary disease 20120101
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Does roflumilast decrease exacerbations in severe COPD patients not controlled by inhaled combination therapy? The REACT study protocol.
International journal of chronic obstructive pulmonary disease 20120101
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Roflumilast--a phosphodiesterase-4 inhibitor licensed for add-on therapy in severe COPD.
Swiss medical weekly 20120101
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PloS one 20120101
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Terapevticheskii arkhiv 20120101
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Pharmacological validation of Trypanosoma brucei phosphodiesterases B1 and B2 as druggable targets for African sleeping sickness.
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Pharmacokinetic evaluation of roflumilast.
Expert opinion on drug metabolism & toxicology 20111201
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[New goals in COPD treatment. From symptom control to prevention of exacerbations].
MMW Fortschritte der Medizin 20111201
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Roflumilast in Asian patients with COPD: A randomized placebo-controlled trial.
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Deutsche medizinische Wochenschrift (1946) 20111101
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Synthesis and biological activity of pyrido[3',2':4,5]furo[3,2-d]pyrimidine derivatives as novel and potent phosphodiesterase type 4 inhibitors.
European journal of medicinal chemistry 20111001
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Roflumilast with long-acting β2-agonists for COPD: influence of exacerbation history.
The European respiratory journal 20110901
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PDE4-inhibitors: a novel, targeted therapy for obstructive airways disease.
Pulmonary pharmacology & therapeutics 20110801
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The differential impact of PDE4 subtypes in human lung fibroblasts on cytokine-induced proliferation and myofibroblast conversion.
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Influence of renal impairment on the pharmacokinetics of oral roflumilast: an open-label, parallel-group, single-center study.
International journal of clinical pharmacology and therapeutics 20110801
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Roflumilast (Daliresp) for COPD.
The Medical letter on drugs and therapeutics 20110725
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Supra-therapeutic doses of roflumilast have no effect on cardiac repolarization in healthy subjects.
Expert opinion on drug safety 20110701
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Study investigating pharmacokinetic interaction between theophylline and roflumilast in healthy adults.
International journal of clinical pharmacology and therapeutics 20110701
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ASP3258, an orally active potent phosphodiesterase 4 inhibitor with low emetic activity.
International immunopharmacology 20110601
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Lack of pharmacokinetic and pharmacodynamic interactions of roflumilast with (R, S)-warfarin in healthy adult subjects.
International journal of clinical pharmacology and therapeutics 20110601
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Phosphodiesterase 4 inhibitors for chronic obstructive pulmonary disease.
The Cochrane database of systematic reviews 20110511
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Update on roflumilast, a phosphodiesterase 4 inhibitor for the treatment of chronic obstructive pulmonary disease.
British journal of pharmacology 20110501
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Effect of steady-state enoxacin on single-dose pharmacokinetics of roflumilast and roflumilast N-oxide.
Journal of clinical pharmacology 20110401
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No dose adjustment on coadministration of the PDE4 inhibitor roflumilast with a weak CYP3A, CYP1A2, and CYP2C19 inhibitor: an investigation using cimetidine.
Journal of clinical pharmacology 20110401
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Roflumilast for severe COPD?
Drug and therapeutics bulletin 20110401
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Revue medicale suisse 20110119
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Inhibition of cyclooxygenase-2 prevents adverse effects induced by phosphodiesterase type 4 inhibitors in rats.
British journal of pharmacology 20110101
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High absolute bioavailability of the new oral phosphodiesterase-4 inhibitor roflumilast.
International journal of clinical pharmacology and therapeutics 20110101
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Reduction of exacerbations by the PDE4 inhibitor roflumilast--the importance of defining different subsets of patients with COPD.
Respiratory research 20110101
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New therapeutic options in the management of COPD - focus on roflumilast.
International journal of chronic obstructive pulmonary disease 20110101
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Pneumonologia i alergologia polska 20110101
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No relevant cardiac, pharmacokinetic or safety interactions between roflumilast and inhaled formoterol in healthy subjects: an open-label, randomised, actively controlled study.
BMC clinical pharmacology 20110101
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Reduce disease burden and improve lung function-roflumilast: approved for moderate to severe COPD: update for the clinical nurse specialist.
Clinical nurse specialist CNS 20110101
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Roflumilast, indacaterol maleate, and abiraterone acetate.
Journal of the American Pharmacists Association : JAPhA 20110101
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Cost-effectiveness analysis of roflumilast/tiotropium therapy versus tiotropium monotherapy for treating severe-to-very severe COPD.
Journal of medical economics 20110101
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Roflumilast attenuates allergen-induced inflammation in mild asthmatic subjects.
Respiratory research 20110101
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Tuberkuloz ve toraks 20110101
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The use of roflumilast in COPD: a primary care perspective.
Primary care respiratory journal : journal of the General Practice Airways Group 20101201
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Topical effects of roflumilast on 1-chloro-2,4-dinitrobenzene-induced atopic dermatitis-like skin lesions in NC/Nga mice.
Die Pharmazie 20101201
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Archivos de bronconeumologia 20101201
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Expert review of respiratory medicine 20101001
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Nature reviews. Drug discovery 20101001
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The clinical respiratory journal 20101001
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Chronopharmacology of roflumilast: a comparative pharmacokinetic study of morning versus evening administration in healthy adults.
Chronobiology international 20101001
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Population pharmacokinetic modelling of roflumilast and roflumilast N-oxide by total phosphodiesterase-4 inhibitory activity and development of a population pharmacodynamic-adverse event model.
Clinical pharmacokinetics 20100901
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Drugs 20100820
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The preclinical pharmacology of roflumilast--a selective, oral phosphodiesterase 4 inhibitor in development for chronic obstructive pulmonary disease.
Pulmonary pharmacology & therapeutics 20100801
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Exposing rodents to a combination of tobacco smoke and lipopolysaccharide results in an exaggerated inflammatory response in the lung.
British journal of pharmacology 20100801
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The divergent opinions of regulatory authorities on roflumilast are puzzling but we need new drugs for treating chronic obstructive pulmonary disease.
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Effect of cyclic AMP-elevating agents on airway ciliary beat frequency in central and lateral airways in rat precision-cut lung slices.
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Bioorganic & medicinal chemistry letters 20100501
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Internal and emergency medicine 20100401
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Treatment of chronic obstructive pulmonary disease with roflumilast, a new phosphodiesterase 4 inhibitor.
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Expert opinion on pharmacotherapy 20100201
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The role of the phosphodiesterase-4 inhibitor, roflumilast, in chronic obstructive pulmonary disease.
Polskie Archiwum Medycyny Wewnetrznej 20100101
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PDE4 inhibitors: a review of current developments (2005 - 2009).
Expert opinion on therapeutic patents 20091101
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Effects of rifampicin on the pharmacokinetics of roflumilast and roflumilast N-oxide in healthy subjects.
British journal of clinical pharmacology 20091001
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The identification of a novel phosphodiesterase 4 inhibitor, 1-ethyl-5-{5-[(4-methyl-1-piperazinyl)methyl]-1,3,4-oxadiazol-2-yl}-N-(tetrahydro-2H-pyran-4-yl)-1H-pyrazolo[3,4-b]pyridin-4-amine (EPPA-1), with improved therapeutic index using pica feeding in rats as a measure of emetogenicity.
The Journal of pharmacology and experimental therapeutics 20090901
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Lancet (London, England) 20090829
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Lancet (London, England) 20090829
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Roflumilast in moderate-to-severe chronic obstructive pulmonary disease treated with longacting bronchodilators: two randomised clinical trials.
Lancet (London, England) 20090829
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Effects of roflumilast, a phosphodiesterase-4 inhibitor, on hypoxia- and monocrotaline-induced pulmonary hypertension in rats.
The Journal of pharmacology and experimental therapeutics 20090701
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PDE4 inhibitors roflumilast and rolipram augment PGE2 inhibition of TGF-{beta}1-stimulated fibroblasts.
American journal of physiology. Lung cellular and molecular physiology 20090601
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Roflumilast increases Clara cell secretory protein in cigarette smoke-exposed mice.
COPD 20090601
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The targeted oral, once-daily phosphodiesterase 4 inhibitor roflumilast and the leukotriene receptor antagonist montelukast do not exhibit significant pharmacokinetic interactions.
Journal of clinical pharmacology 20090401
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Effect of repeated dose of erythromycin on the pharmacokinetics of roflumilast and roflumilast N-oxide.
International journal of clinical pharmacology and therapeutics 20090401
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Discovery of (S)-N-[2-[1-(3-ethoxy-4-methoxyphenyl)-2-methanesulfonylethyl]-1,3-dioxo-2,3-dihydro-1H-isoindol-4-yl] acetamide (apremilast), a potent and orally active phosphodiesterase 4 and tumor necrosis factor-alpha inhibitor.
Journal of medicinal chemistry 20090326
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Quinolines as a novel structural class of potent and selective PDE4 inhibitors: optimisation for oral administration.
Bioorganic & medicinal chemistry letters 20090301
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Roflumilast, a phosphodiesterase 4 inhibitor, alleviates bleomycin-induced lung injury.
British journal of pharmacology 20090201
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Effects of the phosphodiesterase type 4 inhibitor roflumilast on early and late allergic response and airway hyperresponsiveness in Aspergillus-fumigatus-sensitized mice.
Pharmacology 20090101
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Effect of single and repeated doses of ketoconazole on the pharmacokinetics of roflumilast and roflumilast N-oxide.
Journal of clinical pharmacology 20081101
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Curative effects of phosphodiesterase 4 inhibitors cilomilast, roflumilast, and rolipram in dermatitis mouse model.
Journal of dermatological science 20080901
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Roflumilast attenuates pulmonary inflammation upon segmental endotoxin challenge in healthy subjects: a randomized placebo-controlled trial.
Pulmonary pharmacology & therapeutics 20080801
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Anti-inflammatory modulation of chronic airway inflammation in the murine house dust mite model.
Pulmonary pharmacology & therapeutics 20080801
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Development and characterisation of a novel and rapid lung eosinophil influx model in the rat.
Pulmonary pharmacology & therapeutics 20080801
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Single-dose pharmacokinetics of roflumilast in children and adolescents.
Journal of clinical pharmacology 20080801
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Pyrazolopyridines as a novel structural class of potent and selective PDE4 inhibitors.
Bioorganic & medicinal chemistry letters 20080715
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The selective MMP-12 inhibitor, AS111793 reduces airway inflammation in mice exposed to cigarette smoke.
British journal of pharmacology 20080701
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PDE4 inhibitor, roflumilast protects cardiomyocytes against NO-induced apoptosis via activation of PKA and Epac dual pathways.
Cellular signalling 20080501
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Suppression of cytokine expression by roflumilast and dexamethasone in a model of chronic asthma.
Clinical and experimental allergy : journal of the British Society for Allergy and Clinical Immunology 20080501
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Roflumilast: an oral, once-daily selective PDE-4 inhibitor for the management of COPD and asthma.
Expert opinion on investigational drugs 20080501
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Inhibition of phosphodiesterase type 4 decreases stress-induced defecation in rats and mice.
Pharmacology 20080101
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Effect of roflumilast on inflammatory cells in the lungs of cigarette smoke-exposed mice.
BMC pulmonary medicine 20080101
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Tuberkuloz ve toraks 20080101
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Reduction in sputum neutrophil and eosinophil numbers by the PDE4 inhibitor roflumilast in patients with COPD.
Thorax 20071201
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Treating COPD with PDE 4 inhibitors.
International journal of chronic obstructive pulmonary disease 20071201
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Effect of inhaled roflumilast on the prevention and resolution of allergen-induced late phase airflow obstruction in Brown Norway rats.
European journal of pharmacology 20071001
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Roflumilast inhibits leukocyte-endothelial cell interactions, expression of adhesion molecules and microvascular permeability.
British journal of pharmacology 20071001
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Phosphodiesterase 4 inhibitors augment levels of glucocorticoid receptor in B cell chronic lymphocytic leukemia but not in normal circulating hematopoietic cells.
Clinical cancer research : an official journal of the American Association for Cancer Research 20070815
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The oral, once-daily phosphodiesterase 4 inhibitor roflumilast lacks relevant pharmacokinetic interactions with inhaled budesonide.
Journal of clinical pharmacology 20070801
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Effect of 1-year treatment with roflumilast in severe chronic obstructive pulmonary disease.
American journal of respiratory and critical care medicine 20070715
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L-454,560, a potent and selective PDE4 inhibitor with in vivo efficacy in animal models of asthma and cognition.
Biochemical pharmacology 20070615
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PDE4 inhibitors as potential therapeutic agents in the treatment of COPD-focus on roflumilast.
International journal of chronic obstructive pulmonary disease 20070601
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Magnesium hydroxide/aluminium hydroxide-containing antacid does not affect the pharmacokinetics of the targeted phosphodiesterase 4 inhibitor roflumilast.
Journal of clinical pharmacology 20070501
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A reporter gene assay for screening of PDE4 subtype selective inhibitors.
Biochemical and biophysical research communications 20070427
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Lack of a pharmacokinetic interaction between steady-state roflumilast and single-dose midazolam in healthy subjects.
British journal of clinical pharmacology 20070301
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Roflumilast, a phosphodiesterase 4 inhibitor, reduces airway hyperresponsiveness after allergen challenge.
Respiration; international review of thoracic diseases 20070101
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Dose-proportional intraindividual single- and repeated-dose pharmacokinetics of roflumilast, an oral, once-daily phosphodiesterase 4 inhibitor.
Journal of clinical pharmacology 20070101
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Steady-state pharmacokinetics of roflumilast and roflumilast N-oxide in patients with mild and moderate liver cirrhosis.
Clinical pharmacokinetics 20070101
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Effect of fluvoxamine on the pharmacokinetics of roflumilast and roflumilast N-oxide.
Clinical pharmacokinetics 20070101
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A 1-year prospective cost-effectiveness analysis of roflumilast for the treatment of patients with severe chronic obstructive pulmonary disease.
PharmacoEconomics 20070101
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Evaluation of PDE4 inhibition for COPD.
International journal of chronic obstructive pulmonary disease 20061201
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Roflumilast, a once-daily oral phosphodiesterase 4 inhibitor, lacks relevant pharmacokinetic interactions with inhaled salbutamol when co-administered in healthy subjects.
International journal of clinical pharmacology and therapeutics 20061101
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Phosphodiesterase type 4 inhibitors cause proinflammatory effects in vivo.
The Journal of pharmacology and experimental therapeutics 20061001
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Investigation of a potential food effect on the pharmacokinetics of roflumilast, an oral, once-daily phosphodiesterase 4 inhibitor, in healthy subjects.
Journal of clinical pharmacology 20061001
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Roflumilast: a phosphodiesterase-4 inhibitor for the treatment of respiratory disease.
Expert opinion on investigational drugs 20060901
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A phosphodiesterase 4 inhibitor inhibits matrix protein deposition in airways in vitro.
The Journal of allergy and clinical immunology 20060901
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The potential role of roflumilast: the new phosphodiesterase-4 inhibitor.
The Annals of pharmacotherapy 20060601
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Roflumilast for the treatment of chronic obstructive pulmonary disease.
Current opinion in investigational drugs (London, England : 2000) 20060501
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Phosphodiesterase type 4 inhibitors for asthma: a real breakthrough or just expensive theophylline?
Annals of allergy, asthma & immunology : official publication of the American College of Allergy, Asthma, & Immunology 20060501
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Efficacy and safety of roflumilast in the treatment of asthma.
Annals of allergy, asthma & immunology : official publication of the American College of Allergy, Asthma, & Immunology 20060501
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Phosphodiesterase inhibitors in airways disease.
European journal of pharmacology 20060308
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Phosphodiesterase 4 inhibition with roflumilast: a new approach to pulmonary disease.
Expert opinion on pharmacotherapy 20060301
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Pulmonary pharmacology & therapeutics 20060101
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Comparison of roflumilast, an oral anti-inflammatory, with beclomethasone dipropionate in the treatment of persistent asthma.
Allergy 20060101
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Phosphodiesterase type 4 expression and anti-proliferative effects in human pulmonary artery smooth muscle cells.
Respiratory research 20060101
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Phosphodiesterase 4 inhibitors for the treatment of asthma and COPD.
Current medicinal chemistry 20060101
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Roflumilast inhibits lipopolysaccharide-induced inflammatory mediators via suppression of nuclear factor-kappaB, p38 mitogen-activated protein kinase, and c-Jun NH2-terminal kinase activation.
The Journal of pharmacology and experimental therapeutics 20051201
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The inhibitory effects of roflumilast on lipopolysaccharide-induced nitric oxide production in RAW264.7 cells are mediated by heme oxygenase-1 and its product carbon monoxide.
Inflammation research : official journal of the European Histamine Research Society ... [et al.] 20051201
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Roflumilast inhibition of pulmonary leukotriene production and bronchoconstriction in ovalbumin-sensitized and -challenged Guinea pigs.
The Journal of asthma : official journal of the Association for the Care of Asthma 20051201
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Lancet (London, England) 20051126
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Lancet (London, England) 20051126
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Roflumilast for chronic obstructive pulmonary disease.
Lancet (London, England) 20051126
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Roflumilast for chronic obstructive pulmonary disease.
Lancet (London, England) 20051126
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Roflumilast for chronic obstructive pulmonary disease.
Lancet (London, England) 20051126
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Current opinion in investigational drugs (London, England : 2000) 20051101
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Roflumilast fully prevents emphysema in mice chronically exposed to cigarette smoke.
American journal of respiratory and critical care medicine 20051001
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Roflumilast for asthma and chronic obstructive pulmonary disease.
Issues in emerging health technologies 20051001
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Roflumilast: a selective phosphodiesterase 4 inhibitor.
Drugs of today (Barcelona, Spain : 1998) 20051001
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Dynamic activation of cystic fibrosis transmembrane conductance regulator by type 3 and type 4D phosphodiesterase inhibitors.
The Journal of pharmacology and experimental therapeutics 20050801
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Roflumilast, an oral, once-daily phosphodiesterase 4 inhibitor, attenuates allergen-induced asthmatic reactions.
The Journal of allergy and clinical immunology 20050801
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Roflumilast--an oral anti-inflammatory treatment for chronic obstructive pulmonary disease: a randomised controlled trial.
Lancet (London, England) 20050801
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PDE4 inhibitors as new anti-inflammatory drugs: effects on cell trafficking and cell adhesion molecules expression.
Pharmacology & therapeutics 20050601
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Current opinion in pulmonary medicine 20050301
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Lancet (London, England) 20050101
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The effect of selective phosphodiesterase isoenzyme inhibition on neutrophil function in vitro.
Pulmonary pharmacology & therapeutics 20050101
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Structural basis for the activity of drugs that inhibit phosphodiesterases.
Structure (London, England : 1993) 20041201
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Synthesis and potential anti-inflammatory activity of some tetrahydrophthalazinones.
Journal of enzyme inhibition and medicinal chemistry 20041201
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PDE4 inhibition: a novel approach for the treatment of inflammatory bowel disease.
Trends in pharmacological sciences 20040801
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Nihon yakurigaku zasshi. Folia pharmacologica Japonica 20040501
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Roflumilast: APTA 2217, B9302-107, BY 217, BYK 20869.
Drugs in R&D 20040101
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Inhibition of inflammation and remodeling by roflumilast and dexamethasone in murine chronic asthma.
The Journal of pharmacology and experimental therapeutics 20031001
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Pneumologia (Bucharest, Romania) 20030101
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Inhibition of phosphodiesterase 4 in allergic rhinitis.
Current allergy and asthma reports 20020501
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Chest 20020501
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The new phosphodiesterase 4 inhibitor roflumilast is efficacious in exercise-induced asthma and leads to suppression of LPS-stimulated TNF-alpha ex vivo.
Journal of clinical pharmacology 20020301
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Lack of DNA binding in the rat nasal mucosa and other tissues of the nasal toxicants roflumilast, a phosphodiesterase 4 inhibitor, and a metabolite, 4-amino-3,5-dichloropyridine, in contrast to the nasal carcinogen 2,6-dimethylaniline.
Drug and chemical toxicology 20020201
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Monaldi archives for chest disease = Archivio Monaldi per le malattie del torace 20020201
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The phosphodiesterase 4 inhibitor roflumilast is effective in the treatment of allergic rhinitis.
The Journal of allergy and clinical immunology 20011001
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Anti-inflammatory and immunomodulatory potential of the novel PDE4 inhibitor roflumilast in vitro.
The Journal of pharmacology and experimental therapeutics 20010401
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In vivo efficacy in airway disease models of roflumilast, a novel orally active PDE4 inhibitor.
The Journal of pharmacology and experimental therapeutics 20010401