Drug intelligence / Profile preview

roflumilast + formoterol

Development stage
Unknown
Lead developer
Takeda
Modality
Small Molecules
Administration
Oral, Inhalation
01

Overview

**roflumilast + formoterol** is a combination of two drugs used primarily in the management of chronic obstructive pulmonary disease (COPD). Roflumilast is an oral, selective phosphodiesterase 4 (PDE4) inhibitor with anti-inflammatory properties, while formoterol is an inhaled long-acting β2-adrenoceptor agonist (LABA) that functions as a bronchodilator. This combination is used to improve lung function and reduce inflammation in patients with moderate-to-severe COPD who do not respond adequately to long-acting bronchodilators alone. The mechanism involves roflumilast increasing intracellular cyclic AMP by inhibiting PDE4, thereby reducing inflammatory mediators, and formoterol stimulating β2-adrenoceptors to promote airway smooth muscle relaxation. No clinically relevant pharmacokinetic or pharmacodynamic interactions were found when both drugs are administered together, and the combination may enhance anti-inflammatory effects, particularly in conjunction with corticosteroids[1][2][3][4].

02

Targets

PDE4B (3',5'-cyclic-AMP phosphodiesterase 4B)ADRB2 (β2)

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