Roflumilast
Roflumilast structure
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Common Name | Roflumilast | ||
|---|---|---|---|---|
| CAS Number | 162401-32-3 | Molecular Weight | 403.207 | |
| Density | 1.5±0.1 g/cm3 | Boiling Point | 430.6±45.0 °C at 760 mmHg | |
| Molecular Formula | C17H14Cl2F2N2O3 | Melting Point | 158°C | |
| MSDS | Chinese USA | Flash Point | 214.2±28.7 °C | |
| Symbol |
GHS07 |
Signal Word | Warning | |
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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 Clin. Pharmacol. 11 , 7, (2011) Roflumilast is an oral, selective phosphodiesterase 4 inhibitor with anti-inflammatory effects in chronic obstructive pulmonary disease (COPD). The addition of roflumilast to long-acting bronchodilators improves lung function in patients with moderate-to-seve... |
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β2-Agonist induced cAMP is decreased in asthmatic airway smooth muscle due to increased PDE4D.
PLoS ONE 6 , e20000, (2011) Asthma is associated with airway narrowing in response to bronchoconstricting stimuli and increased airway smooth muscle (ASM) mass. In addition, some studies have suggested impaired β-agonist induced ASM relaxation in asthmatics, but the mechanism is not kno... |
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Effect of roflumilast on exacerbations in patients with severe chronic obstructive pulmonary disease uncontrolled by combination therapy (REACT): a multicentre randomised controlled trial.
Lancet 385(9971) , 857-66, (2015) Roflumilast reduces exacerbations in patients with severe chronic obstructive pulmonary disease. Its effect in patients using fixed combinations of inhaled corticosteroids and longacting β2 agonists is unknown. We postulated that roflumilast would reduce exac... |
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Roflumilast inhibits lipopolysaccharide-induced tumor necrosis factor-α and chemokine production by human lung parenchyma.
PLoS ONE 8 , e74640, (2013) Roflumilast is the first phosphodiesterase-4 (PDE4) inhibitor to have been approved for the treatment of COPD. The anti-inflammatory profile of PDE4 inhibitors has not yet been explored in human lung tissues. We investigated the effects of roflumilast and its... |
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Roflumilast N-oxide inhibits bronchial epithelial to mesenchymal transition induced by cigarette smoke in smokers with COPD.
Pulm. Pharmacol. Ther. 28(2) , 138-48, (2014) Epithelial to mesenchymal transition (EMT) is under discussion as a potential mechanism of small airway remodelling in COPD. In bronchial epithelium of COPD and smokers markers of EMT were described. In vitro, EMT may be reproduced by exposing well-differenti... |
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Roflumilast improves corticosteroid resistance COPD bronchial epithelial cells stimulated with toll like receptor 3 agonist.
Respir. Res. 16 , 12, (2015) Chronic obstructive pulmonary disease (COPD) is characterised by chronic pulmonary inflammation punctuated by periods of viral exacerbations. Recent evidence suggests that the combination of roflumilast with corticosteroids may improve the compromised anti-in... |
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Practical guidance on the recognition of uncontrolled asthma and its management.
J Am Assoc Nurse Pract 27 , 466-75, (2015) To highlight the significance of asthma in primary care and offer a practitioner-friendly interpretation of the asthma guidelines for the busy provider, while introducing new treatment options currently in clinical trials, such as the once-daily long-acting a... |