Drug intelligence / Profile preview

montelukast + roflumilast

Development stage
Unknown
Lead developer
AstraZeneca
Modality
Small Molecules
Administration
Oral
01

Overview

Montelukast + roflumilast is an oral combination therapy consisting of two small molecule drugs with distinct anti-inflammatory mechanisms, investigated primarily for the treatment of moderate-to-severe asthma not adequately controlled by inhaled corticosteroids and long-acting beta-agonists. Montelukast is a leukotriene receptor antagonist that blocks cysteinyl leukotriene type 1 (CysLT1) receptors, thereby reducing airway inflammation and bronchoconstriction. Roflumilast is a selective phosphodiesterase 4 (PDE4) inhibitor that increases intracellular cyclic AMP in lung cells, leading to reduced inflammatory cell activity. Clinical studies have shown that this combination improves lung function, asthma control scores, and reduces urinary leukotriene E4 levels compared to montelukast alone in patients with moderate-to-severe asthma[1][2][5][6]. The safety profile was consistent with known effects of the individual agents.

02

Targets

CYSLTR1 (Cysteinyl-leukotriene type 1 receptor)PDE4 (Phosphodiesterase 4A1)

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