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Pharmacokinetics and Safety of Bilastine 10 mg/d in Children Aged 2 to 5 Years With Allergic Rhinoconjunctivitis or Urticaria: A Phase 3 Clinical Trial

Majorek-Olechowska B1, Slomskis T2, Zollerová L3, Martín I4, Sánchez C4, Gilaberte I4, Arranz P4 on behalf of the BILA-4021/PED Research Group

1Alergo-Med Specjalistyczna Przychodnia Lekarska Sp. z o.o., Tarnów, Poland
2Center of Allergy Diagnosis and Treatment, Vilnius, Lithuania
3Ambulancia Klinickej imunológie a alergiológie - Allergy ambulance, Rimavská Sobota, Slovakia
4Department of Research, Development, and Innovation, FAES FARMA, Leioa, Spain

J Investig Allergol Clin Immunol 2025; Vol. 35(4)
doi: 10.18176/jiaci.1003

Background: Bilastine is a second-generation antihistamine for the symptomatic treatment of allergic rhinoconjunctivitis (ARC) and urticaria in adults, adolescents, and children. The pharmacokinetics and safety of oral bilastine 10 mg/d in children aged 2 to 5 years were evaluated.
Methods: This was a multicenter, open-label clinical trial in children aged 2 to 5 years with seasonal or perennial ARC or urticaria treated once daily with bilastine 10 mg orodispersible tablets. The safety evaluation included treatment-emergent adverse events (TEAEs), vital signs, and physical examination. Pharmacokinetic data were pooled with data from a prior pediatric study, and pharmacokinetic modeling was performed to assess consistency. 
Results: A total of 37 children with ARC (81.1%), urticaria (8.1%), or both (10.8%) were included in the study, with a mean (SD) age of 3.7 (1.2) years. The highest plasma concentrations of bilastine were observed 1 hour after administration (634.91 ng/mL). Eight patients (21.6%) experienced 1 TEAE each, none of which was severe. Body weight and age were not covariates of variation in either systemic clearance or the volume of distribution in children aged 2 to 5 years and did not affect the pharmacokinetic parameters of bilastine. 
Conclusions: The pharmacokinetics of bilastine was linear and consistent with data from a previous trial, suggesting that a 10-mg dose may be used in children (2 to <12 years). No dose adjustments are deemed necessary. Oral once-daily bilastine 10 mg presented a good safety profile in children aged 2 to 5. 

Key words: Children, Young children, Allergic rhinoconjunctivitis, Urticaria, Antihistamine, Bilastine, Pediatric, Nonsedating