Drug intelligence / Profile preview

montelukast + salmeterol + theophylline + steroid

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

Overview

This is a combination therapy consisting of four active pharmaceutical ingredients commonly used in the management of asthma and chronic obstructive pulmonary disease (COPD): montelukast, salmeterol, theophylline, and a corticosteroid (steroid). - **Montelukast** is a leukotriene receptor antagonist that blocks cysteinyl leukotriene receptor type-1, reducing bronchoconstriction and inflammation[2][5][7]. - **Salmeterol** is a long-acting beta2-adrenergic agonist (LABA) that relaxes bronchial smooth muscle by stimulating beta2 receptors, leading to bronchodilation[4][6]. - **Theophylline** is a methylxanthine derivative that acts as a non-selective phosphodiesterase inhibitor, increasing intracellular cAMP and causing bronchodilation; it also has mild anti-inflammatory effects[4]. - **Steroid** refers to an inhaled or systemic corticosteroid (such as fluticasone or budesonide), which reduces airway inflammation by modulating gene expression via glucocorticoid receptors[3][4]. This combination targets multiple inflammatory pathways in asthma/COPD. It may be considered for patients with severe or poorly controlled symptoms despite standard therapies. The use of all four agents together is not standard but may be seen in complex cases under specialist supervision.

02

Targets

CYSLTR1 (Cysteinyl-leukotriene type 1 receptor)ADRB2 (β2)HDAC (HDAC family)GR (Glucocorticoid receptor)ADOR (Adenosine receptors)PDE (Phosphodiesterase family)

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