Drug intelligence / Profile preview

rupatadine

Development stage
Phase 4
Lead developer
Uriach
Modality
Small Molecules
Administration
Oral
01

Overview

Rupatadine is a second-generation tricyclic antihistamine with dual antagonistic activity against both the histamine H1 receptor and the platelet activating factor (PAF) receptor. It is used primarily for symptomatic relief of seasonal and perennial allergic rhinitis and chronic idiopathic urticaria. Its mechanism involves selective inhibition of peripheral H1 receptors as well as PAF receptors, providing anti-allergic effects by blocking two key mediators in allergic inflammation. Rupatadine also inhibits mast cell degranulation, neutrophil and eosinophil migration, and cytokine release. Developed originally by Uriach Pharmaceuticals in Spain, it was first launched in 2003. In China, it is marketed under the brand name Lusu by Yangtze River Pharmaceutical Group[3][5][6][7].

Brand names
RupafinRupallUrtimedRupanexLusu (卢苏)
Other names
卢帕他定富马酸卢帕他定 (rupatadine fumarate)8-chloro-11-[1-[(5-methylpyridin-3-yl)methyl]piperidin-4-ylidene]-5,6-dihydrobenzo[1,2]cyclohepta[2,4-b]pyridine
02

Targets

PTAFR (Platelet-activating factor receptor)HRH1 (Histamine H1 Receptor)

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