Introduction

Several studies have established the efficacy and tolerability of bilastine 20 mg for the treatment of allergic rhinoconjunctivitis (ARC) and urticaria in adults and adolescents aged >12 years. Bilastine 10 mg daily dose was approved and evaluated in pediatric population. Once daily bilastine 10 mg for 12 weeks was found to be safe in children aged 2-11 years in a phase 3 clinical trial. However, the pharmacokinetics of bilastine 10 mg/day has not been thoroughly analyzed in children aged 2-5 years with ARC and/or urticaria as the number of children aged <6 years was very low in previous pharmacokinetic studies.

Aim

To assess the pharmacokinetics and safety of bilastine 10 mg/day in children aged 2-5 years for the treatment of ARC and/or urticaria

Patient Profile

• Children aged 2-5 years with >10 kg body weight with mild-to-moderate seasonal ARC (SARC) and/or perennial ARC (PARC) before or during the 1^stvisit
• Symptomatic ARC and/or urticaria at screening
• Atleast 1 positive skin prick test result and/or positive validated IgE test result with atleast 1 seasonal or perennial allergen in their lifetime

Method

Study Design

• Multicenter, open-label, noncontrolled, phase 3 clinical study

Treatment

• The trial consisted of 5 visits
  • Visit 1 – screening period for upto 7 days
  • Visit 2 – 1-day baseline period
  • Visit 3 – treatment period of 7 days
  • Visit 4 – treatment period of 14 days
  • Visit 5 – follow-up period of 7 days
• The children were treated once daily with bilastine 10 mg dispersible tablets
• They were assigned to 3 blood sampling groups stratified by age with 2 age subgroups: children aged between >2 to <4 years and 4 to <5 years
• Group 1 underwent blood sampling at 0.5, 2 and 4 hours after intake of bilastine at visit 3
• Group 2 underwent sampling at 24 hours after intake of bilastine on the day before visit 3 and at 0.25 hours and 1 hr after intake at visit 3
• Group 3 were sampled at 6 hours and 12 hours after intake of bilastine at visit 3
• Adverse events, vital signs, and physical examination was recorded
• Pharmacokinetic data were combined with information from an earlier pediatric study, and pharmacokinetic modelling was conducted to evaluate consistency

  Endpoints

• Treatment-emergent adverse events (TEAEs)

Results

• The final analysis included 36 children; mean age was 3.7 years and 70.3% were boys
• PARC was prevalent in 45.9%, SARC in 2.7% and a combination of both in 32.4%
• About 81.1% had ARC, with 8.1% presenting with urticaria and 10.8% with combined ARC and urticaria
• The highest plasma concentrations of bilastine of 634.91 ng/mL were attained 1 hour after the intake of 10 mg dose of bilastine
• One TEAE each was experienced by 21.6%; and only 1 of those (fatigue) was probably treatment-related
• No serious TEAEs or death was reported
• No safety concerns were observed after physical examinations and measurement of vital signs
• Analysis revealed that age and body weight did not significantly affect clearance or volume of distribution

Conclusion

• The pharmacokinetics of bilastine were found to be linear and aligned with findings from a prior trial, indicating that a 10-mg dose is appropriate for children aged 2 to under 12 years without the need for dose adjustments
• Additionally, once-daily dose of 10 mg bilastine demonstrated a favorable safety profile in children aged 2-5 years

J Investig Allergol Clin Immunol. 2024 May 10:0. Doi: 10.18176/jiaci.1003.