Drug intelligence / Profile preview

fluticasone + salmeterol + zileuton

Development stage
Preclinical
Lead developer
GSK
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 used in the management of asthma and potentially other obstructive airway diseases. - **Fluticasone** is a synthetic glucocorticoid corticosteroid that acts as an anti-inflammatory agent by binding to the glucocorticoid receptor, reducing airway inflammation and swelling. - **Salmeterol** is a long-acting beta2-adrenergic agonist (LABA) that relaxes bronchial smooth muscle via stimulation of beta2-adrenoceptors, leading to bronchodilation and improved airflow. - **Zileuton** is an oral inhibitor of 5-lipoxygenase, blocking leukotriene synthesis from arachidonic acid, thereby reducing leukotriene-mediated bronchoconstriction, inflammation, edema, and mucus secretion[6][8]. The combination aims to provide comprehensive control over asthma symptoms by targeting multiple inflammatory pathways (glucocorticoids for broad anti-inflammation; LABA for bronchodilation; leukotriene pathway inhibition for further reduction in inflammation and bronchospasm). This triple therapy may be considered in moderate-to-severe persistent asthma not adequately controlled with inhaled corticosteroids/LABA alone[2].

02

Targets

GR (Glucocorticoid receptor)ALOX5 (Arachidonate 5-lipoxygenase)ADRB2 (β2)

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