Drug intelligence / Profile preview

Inhaled Corticosteroid and Leukotriene Receptor Antagonist Combination Therapy

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

Overview

The combination of inhaled corticosteroids (ICS) and leukotriene receptor antagonists (LTRA) represents a therapeutic approach for asthma management. This combination leverages complementary mechanisms of action to control asthma symptoms and inflammation. Inhaled corticosteroids are considered the most effective long-term medication for control and management of asthma, providing broad anti-inflammatory effects in the airways[4]. However, they do not suppress the inflammatory effects of cysteinyl leukotrienes[6]. Leukotriene receptor antagonists work by blocking the cysteinyl leukotriene 1 receptor, preventing leukotrienes (LTC4, LTD4, and LTE4) from binding to these receptors[5][6]. This inhibits physiological actions of leukotrienes that contribute to asthma symptoms, including bronchoconstriction, increased vascular permeability, and mucus production[7]. The combination therapy is typically used as an add-on treatment when asthma symptoms remain uncontrolled despite medium-dose inhaled corticosteroids[7]. It may be particularly beneficial for patients with night-time symptoms, nasal symptoms (rhinitis), hay fever, or exercise-induced asthma[7].

02

Targets

CYSLTR1 (Cysteinyl-leukotriene type 1 receptor)

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