Pharmacological profile and clinical efficacy of transdermal patch containing emedastine difumarate (ALLESAGA_® TAPE)

Abstract

ALLESAGA_® TAPE is the first transdermal drug delivery system of emedastine difumarate, as a second-generation antihistamine, for allergic rhinitis. It has been suggested that the efficacy of emedastine difumarate in allergic rhinitis is mediated through a combination of chemical mediator release inhibitory effects and eosinophil chemotaxis inhibitory effects, in addition to a strong anti-histaminic effect. In the pharmacological evaluation on histamine-induced vascular hyperpermeability in rats, ALLESAGA_® TAPE showed an anti-histaminic effect in a dose-dependent manner and exhibited a long-lasting anti-histaminic effect until 24 hours after administration. In the patients having allergic nasal symptoms, the plasma concentration of emedastine reached at steady-state within 7 days after multiple administration of ALLESAGA_® TAPE. ALLESAGA_® TAPE was effective for treating seasonal allergic rhinitis with sustained action throughout the day. Long-term application of ALLESAGA_® TAPE raised no safety concerns in patients with perennial allergic rhinitis. Plasma drug concentrations showed little change over a long period and there was no decrease of efficacy. Based on the above results, ALLESAGA_® TAPE is possible to provide a new option for the treatment of allergic rhinitis.