Drug intelligence / Profile preview

roflumilast + inhaled corticosteroids

Development stage
Unknown
Lead developer
Takeda
Modality
Small Molecules
Administration
Oral (for Roflumilast), Inhalation (for Corticosteroids)
01

Overview

**Roflumilast + inhaled corticosteroids** refers to the co-administration of **roflumilast**, a selective phosphodiesterase-4 (PDE4) inhibitor, with **inhaled corticosteroids (ICS)**, a standard class of anti-inflammatory agents used in airways disease. This combination is not marketed under a unique fixed-dose combination product but represents a widely studied, guideline-endorsed adjunctive regimen in patients with severe **chronic obstructive pulmonary disease (COPD)**, especially those with chronic bronchitis and a history of frequent exacerbations. Roflumilast works by inhibiting PDE4, elevating intracellular cyclic AMP levels, downregulating inflammatory responses, and reducing inflammatory cell activity. ICS act through glucocorticoid receptor agonism, suppressing pro-inflammatory cytokine transcription, and decreasing airway inflammation. The combination provides **additive or synergistic anti-inflammatory effects** and greater reduction in COPD exacerbation rates compared to either agent alone, particularly in frequent exacerbators with severe disease and chronic bronchitis[1][3][5][7].

02

Targets

GR (Glucocorticoid receptor)PDE4B (3',5'-cyclic-AMP phosphodiesterase 4B)

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