Drug intelligence / Profile preview

salmeterol + fluticasone + theophylline

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

Overview

This drug is a combination of three active pharmaceutical ingredients used in the management of asthma and chronic obstructive pulmonary disease (COPD): salmeterol, fluticasone, and theophylline. - **Salmeterol** is a long-acting beta-2 adrenergic receptor agonist (LABA) that acts as a bronchodilator by relaxing airway smooth muscle, leading to improved airflow. - **Fluticasone** is an inhaled corticosteroid that reduces inflammation in the airways by inhibiting multiple types of inflammatory cells and decreasing production of cytokines and other mediators involved in airway inflammation. - **Theophylline** is a methylxanthine bronchodilator with anti-inflammatory properties; it works primarily by inhibiting phosphodiesterase enzymes, increasing intracellular cAMP, resulting in bronchodilation and mild anti-inflammatory effects. Theophylline may also enhance histone deacetylase activity, potentially restoring steroid responsiveness in some patients[1][2][7]. This triple combination has been studied for its potential to provide greater protection against asthma exacerbations compared to dual therapy with just salmeterol/fluticasone[1]. In COPD, however, adding low-dose theophylline to inhaled corticosteroids plus LABA did not show additional benefit on exacerbation rates or anti-inflammatory effects[2]. The combination may be considered for patients whose symptoms are not adequately controlled on standard dual therapy.

02

Targets

PDE (Phosphodiesterase family)GR (Glucocorticoid receptor)ADRB2 (β2)

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