The effect of MP29‐02* is mediated via bitter taste receptors (TAS2R)

Sandra Ekstedt,Susanna Kumlien Georén,Lars‐Olaf Cardell

doi:10.1186/2045-7022-5-s4-p17

Sandra Ekstedt, Susanna Kumlien Georén + Show 1 more

Open Access

https://doi.org/10.1186/2045-7022-5-s4-p17

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Abstract

Background Dymista (MP29-02*) is a novel intranasal formulation of azelastine hydrochloride (AZE) and fluticasone propionate (FP) in an advanced delivery system with a welldocumented effect on allergic rhinitis. Its somewhat bitter taste is probably derived from AZE, a potent histamineH1-receptor antagonist. The taste is sometimes looked upon as a disadvantage. However, it might be that AZE induces some of its beneficial effect through activation of bitter taste receptors. Recent evidence indicates that bitter taste receptors are present in human upper airway mucosa in regions associated with high airflow and particulate deposition. Consequently the MP29-02* effects might be due not only to its anti-histaminic, mast-cell stabilizing, anti-leukotriene, and anti-inflammatory properties but also as due to activation of bitter taste receptors.

Highlights

Dymista (MP29-02*) is a novel intranasal formulation of azelastine hydrochloride (AZE) and fluticasone propionate (FP) in an advanced delivery system with a welldocumented effect on allergic rhinitis
Aim To explore if MP29-02* has the ability to activate bitter taste receptors using an in-vitro model of isolated murine airways and to probe the potential bitter taste effects of MP29-02* on human nasal epithelial cells
MP29-02* is a potent dilator of pre-contracted airways, an effect probably mediated by its AZE component

Summary

Introduction

Dymista (MP29-02*) is a novel intranasal formulation of azelastine hydrochloride (AZE) and fluticasone propionate (FP) in an advanced delivery system with a welldocumented effect on allergic rhinitis. The effect of MP29-02* is mediated via bitter taste receptors (TAS2R) Its somewhat bitter taste is probably derived from AZE, a potent histamineH1-receptor antagonist. It might be that AZE induces some of its beneficial effect through activation of bitter taste receptors.

Results

Conclusion