Drug intelligence / Profile preview

budesonide + prednisone + zafirlukast

Development stage
Preclinical
Lead developer
AstraZeneca
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Inhalation, Oral
01

Overview

This is a combination therapy consisting of three active pharmaceutical ingredients: - **Budesonide** is a synthetic corticosteroid with potent anti-inflammatory properties, primarily used to treat respiratory and gastrointestinal inflammatory conditions. It acts by binding to glucocorticoid receptors, reducing inflammation in the airways and other tissues. - **Prednisone** is an oral corticosteroid that suppresses the immune system and decreases inflammation by modulating gene expression through glucocorticoid receptor activation. - **Zafirlukast** is a leukotriene receptor antagonist that blocks leukotriene D4 at the cysteinyl leukotriene receptor (CysLT1) in the lungs, leading to decreased bronchoconstriction and inflammation. The combination of these drugs has been studied for use in asthma management, particularly for patients with persistent symptoms despite standard therapies. The rationale behind this regimen is to provide broad anti-inflammatory effects (via two corticosteroids) while also targeting leukotriene-mediated pathways involved in asthma pathogenesis. Clinical studies have shown that this combination can reduce allergen-induced cytokine secretion (notably IFN-gamma), decrease lymphocyte proliferation, improve asthma symptoms, and reduce bronchial hyperresponsiveness[1][2][3][5].

02

Targets

CYSLTR1 (Cysteinyl-leukotriene type 1 receptor)GR (Glucocorticoid receptor)

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