An emerging antihistamine drug with multiple therapeutic benefits: Bilastine

Abstract

Second-generation antihistamines (AHs) like cetirizine and third-generation drugs like fexofenadine are currently in practice for allergic rhinoconjunctivitis and urticaria due to their reduced impact on the central nervous system and fewer side effects. Clinically, bilastine has similar AH activity. Numerous studies showed that bilastine is a nonsedating AH, safe and effective in treating the allergies of all age groups. It is primarily indicated for allergic conditions; its potential use in other medical areas is being explored. Clinical trials, scientific experiments, real-world experience, and expert opinions will guide decisions on broader applications. This review aims to provide updated information on bilastine’s potential off-target effects, interactions with food and drugs, and comparison with other newer H1 AHs. PubMed literature search using the drug name “bilastine” was conducted. Additionally, the authors have included literature from the reference list of cited publications in the public domain. Clinical trials have established bilastine safety and efficacy, making it a frontline treatment for allergic conditions due to selective second-generation H1 AH. It has gained approval for treating allergic rhinoconjunctivitis and urticaria in adolescents and adults in various countries, with recent approvals extending its use to children up to 12 years old. Many nations agreed to recommend bilastine as a first-line treatment for chronic urticaria due to minimal food and drug interaction, no CNS effect, long-acting, and environmentally safe. In addition, bilastine could be used as add-on therapy with other drugs for the treatment of inflammation and diabetic neuropathy and to reverse efflux-mediated drug resistance. More clinical trials are anticipated to support the use of this drug for other indications. However, several health benefits associated with bilastine, inadequate data on its safety during pregnancy, and pending US FDA approval rendered bilastine a lesser-known frontline H1-AH in many countries.