Drug intelligence / Profile preview

mometasone furoate + levocetirizine + oxymetazoline

Development stage
Preclinical
Lead developer
UCB
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Intranasal
01

Overview

This is a fixed-dose combination drug containing three active ingredients: - **Mometasone furoate** is a synthetic corticosteroid with potent anti-inflammatory activity, primarily used to treat allergic rhinitis and nasal polyps by reducing inflammation in the nasal passages. - **Levocetirizine** is a third-generation non-sedating antihistamine that acts as an antagonist at the histamine H1 receptor, providing relief from allergy symptoms such as sneezing, itching, and rhinorrhea. - **Oxymetazoline** is an imidazoline derivative and direct-acting sympathomimetic agent that acts as an agonist at alpha-1A adrenergic receptors (and to some extent alpha-2B), causing vasoconstriction of nasal blood vessels and rapid relief of nasal congestion. The combination targets multiple mechanisms involved in allergic rhinitis and related conditions—reducing inflammation (mometasone), blocking histamine-mediated symptoms (levocetirizine), and relieving congestion through vasoconstriction (oxymetazoline). Clinical studies on similar combinations have shown improved symptom control for allergic rhinitis compared to monotherapy[1][2][9].

02

Targets

GR (Glucocorticoid receptor)ADRA1A (α1A)ADRA2B (α2B)HRH1 (Histamine H1 Receptor)

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