Drug intelligence / Profile preview

ebastine (Almirall)

Development stage
Unknown
Lead developer
Almirall
Modality
Small Molecules
Administration
Oral
01

Overview

Obstine (ebastine) is a second-generation, long-acting, non-sedating histamine H1 receptor antagonist. It is a piperidine derivative that acts as a prodrug, undergoing rapid and extensive first-pass hepatic metabolism via cytochrome P450 3A4 (CYP3A4) to its active carboxylic acid metabolite, carebastine. Ebastine selectively binds to peripheral H1 receptors, preventing histamine from initiating allergic responses. It is widely approved and marketed for the symptomatic relief of allergic conditions, including allergic rhinitis (seasonal and perennial) and chronic idiopathic urticaria. Due to its low penetration of the blood-brain barrier, ebastine has a favorable safety profile with minimal sedative or anticholinergic side effects.

Brand names
Obstine
Other names
ebastinaebastineebastinum
02

Targets

ADRA1A (α1A)HRH1 (Histamine H1 Receptor)M1 (Muscarinic acetylcholine receptor M1)CHRM2 (M2)KCNH2 (Voltage-gated potassium channel subfamily H member 2)

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