Drug intelligence / Profile preview

loratadine + zafirlukast

Development stage
Preclinical
Lead developer
Merck
Modality
Small Molecules
Administration
Oral
01

Overview

Loratadine + zafirlukast is a combination of two small molecule drugs used for their additive effects in the management of asthma and allergic conditions. Loratadine is a second-generation antihistamine that acts as a selective antagonist of the histamine H1 receptor, thereby reducing symptoms caused by histamine release such as sneezing, runny nose, and itchy eyes or throat. Zafirlukast is a leukotriene receptor antagonist that blocks cysteinyl-leukotriene 1 (CysLT1) receptors, inhibiting leukotriene-mediated bronchoconstriction and inflammation in the airways. The combination has been studied for its potential to provide enhanced protection against exercise-induced bronchoconstriction (EIB) compared to either agent alone; however, clinical studies suggest that while zafirlukast provides significant benefit in EIB, adding loratadine does not confer additional protective effect beyond that achieved with zafirlukast alone[1]. This combination may be considered for patients with asthma who have both allergic symptoms and exercise-induced airway obstruction.

Other names
loratadine + zafirlukast
02

Targets

CYSLTR1 (Cysteinyl-leukotriene type 1 receptor)HRH1 (Histamine H1 Receptor)

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