Drug intelligence / Profile preview

salmeterol xinafoate + ciclesonide

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

Overview

Salmeterol xinafoate + ciclesonide is a fixed-dose combination drug composed of salmeterol xinafoate, a long-acting beta-2 adrenergic receptor agonist, and ciclesonide, an inhaled corticosteroid prodrug. Salmeterol acts by stimulating beta-2 adrenoceptors in bronchial smooth muscle, resulting in bronchodilation and improved airflow. Ciclesonide is converted in the lungs to its active metabolite desisobutyryl-ciclesonide, which acts as a high-affinity agonist of the glucocorticoid receptor, exerting anti-inflammatory effects through suppression of pro-inflammatory cytokines and inhibition of leukocyte infiltration. The combination is primarily indicated for the prophylaxis and treatment of respiratory conditions such as asthma, chronic obstructive pulmonary disease (COPD), and other diseases characterized by reversible airway obstruction. The combination may provide complementary bronchodilation (via salmeterol) and reduction of airway inflammation (via ciclesonide), administered via inhalation formulations[1][5][6].

02

Targets

GR (Glucocorticoid receptor)ADRB2 (β2)

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