Antihistamines in late-phase clinical development for allergic disease

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Abstract
Allergic rhinitis (AR) is a global health concern and shares a high comorbidity with asthma. Recent research suggests that different allergic diseases, such as AR, asthma, allergic conjunctivitis and chronic idiopathic urticaria (CIU), are evoked by common pathological mechanisms characterised by the release of histamine and other inflammatory mediators. Although H1 receptor antagonists are the mainstay of therapy for allergic disease, the unacceptably high incidence of anticholinergic and CNS-related side effects of first-generation H1 antagonists led to the search for improved second-generation H1 antagonists. While many of these agents were largely devoid of CNS side effects, their tendency for drug-drug interactions (e.g., terfenadine and astemizole) resulted in an increased incidence of cardiotoxicity. Furthermore, second-generation H1 antagonists exhibited weak anti-inflammatory properties and had no effect on nasal congestion. These observations emphasised the need for newer anti-allergic agents wi...