Drug intelligence / Profile preview

PF-03654764 + fexofenadine

Development stage
Discontinued
Lead developer
Pfizer
Modality
Small Molecules
Administration
Oral
01

Overview

PF-03654764 + fexofenadine is an investigational combination of two small molecule drugs developed for the treatment of allergic rhinitis. PF-03654764 is a potent and selective antagonist of the human histamine H3 receptor, while fexofenadine is a second-generation antihistamine that acts as an antagonist at peripheral histamine H1 receptors. The rationale for this combination was to provide enhanced relief from allergy symptoms by targeting both central and peripheral histaminergic pathways. Clinical trials showed that the combination did not provide superior symptom relief compared to existing therapies such as pseudoephedrine plus fexofenadine, and side effects were more significant in groups treated with PF-03654764. Development for allergic rhinitis was discontinued after phase II trials[3][4][5].

Brand names
Allegra (for fexofenadine)Allegra Allergy (for fexofenadine)Allegra OTC (for fexofenadine)Aller-Ease (for fexofenadine)
02

Targets

HRH3 (Histamine Receptor H3)HRH1 (Histamine H1 Receptor)

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