Drug intelligence / Profile preview

long-acting beta2-agonist + long-acting muscarinic antagonist + inhaled corticosteroid

Development stage
Unknown
Lead developer
GSK
Modality
Small Molecules
Administration
Inhalation
01

Overview

Triple therapy inhalers are fixed-dose combination products containing a **long-acting beta2-adrenergic receptor agonist (LABA)**, a **long-acting muscarinic antagonist (LAMA)**, and an **inhaled corticosteroid (ICS)**. These inhalers are primarily indicated for the maintenance treatment of **chronic obstructive pulmonary disease (COPD)** and sometimes for **asthma** in patients not adequately controlled by dual therapy. **Mechanism of Action:** - LABAs act as bronchodilators by stimulating beta2-adrenergic receptors, leading to relaxation of airway smooth muscle and improved airflow. - LAMAs antagonize muscarinic acetylcholine receptors (specifically M3), preventing bronchoconstriction. - ICSs exert anti-inflammatory effects by activating glucocorticoid receptors, leading to reduced airway inflammation. **Examples:** - **Trelegy Ellipta:** fluticasone furoate (ICS) + umeclidinium (LAMA) + vilanterol (LABA) - **Trimbow:** beclometasone dipropionate (ICS) + formoterol fumarate (LABA) + glycopyrronium bromide (LAMA) - **Trixeo Aerosphere:** budesonide (ICS) + formoterol fumarate (LABA) + glycopyrronium bromide (LAMA) Triple therapy is recommended for patients with COPD who experience frequent exacerbations or worsening symptoms despite use of dual inhaled therapy. These combination inhalers improve adherence and convenience. Side effects vary per component and commonly include oral thrush (ICS), tremor/tachycardia (LABA), and dry mouth (LAMA)[2][4].

Brand names
Trelegy ElliptaTrimbowTrixeo Aerosphere
Other names
triple therapy inhalerLABA + LAMA + ICS inhaler
02

Targets

mAChR (Muscarinic acetylcholine receptors)GR (Glucocorticoid receptor)ADRB2 (β2)

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