Drug intelligence / Profile preview

(R)-mequitazine

Development stage
Phase 2
Lead developer
Pierre Fabre
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Inhalation
01

Overview

(R)-mequitazine (V0162) is a phenothiazine derivative and the enantiomer of mequitazine developed as a novel long-acting anticholinergic bronchodilator. It acts as an antagonist at muscarinic acetylcholine receptors M1, M2, and M3. The drug was investigated for inhaled use in asthma and chronic obstructive pulmonary disease (COPD), with additional studies in overactive bladder and urinary incontinence. Preclinical studies demonstrated its ability to prevent bronchoconstriction induced by acetylcholine or histamine and to reverse airway inflammation in animal models of asthma. Clinical trials showed that inhaled V0162 improved lung function and reduced hyperinflation in COPD patients without significant safety concerns; however, development has been discontinued for all indications[1][4][5][6].

Other names
(R)-Mequitazine10-[(3R)-1-azabicyclo[2.2.2]oct-3-ylmethyl]-10H-phenothiazine
02

Targets

CHRM3 (M3)CHRM2 (M2)M1 (Muscarinic acetylcholine receptor M1)HRH1 (Histamine H1 Receptor)

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