Drug intelligence / Profile preview

mometasone furoate + formoterol fumarate + tiotropium bromide

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

Overview

**Mometasone furoate + formoterol fumarate + tiotropium bromide** is a triple combination inhaled pharmaceutical intended for treatment of chronic obstructive pulmonary disease (*COPD*) and asthma. - **Mometasone furoate** is a synthetic glucocorticoid corticosteroid that acts as a potent anti-inflammatory agent by binding to the glucocorticoid receptor, reducing airway inflammation. - **Formoterol fumarate** is a long-acting β2-adrenergic agonist (LABA) that stimulates β2-adrenoceptors on bronchial smooth muscle, causing prolonged bronchodilation. - **Tiotropium bromide** is a long-acting antimuscarinic bronchodilator (LAMA), acting as a competitive inhibitor of muscarinic M3 acetylcholine receptors, leading to sustained airway smooth muscle relaxation and improved airflow. While dual combinations (e.g., mometasone furoate + formoterol fumarate in the product *Dulera*) are approved and widely used, fixed triple combinations including tiotropium bromide are under investigation for enhanced maintenance therapy and exacerbation prevention in moderate to severe COPD and asthma.

02

Targets

GR (Glucocorticoid receptor)ADRB2 (β2)CHRM3 (M3)

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