Bilastine

Bilastine is a second-generation H1-selective antihistamine for the treatment of allergic conditions in adults and children. It has a rapid onset and a long duration of action. Its pharmacokinetic and pharmacodynamic properties are favorable for all ages, although there’s a lack of studies in older adults, who are heterogenous in different aspects, namely age, comorbidities and comedication.

The aim of this study was to assess the recommendation of the dose of bilastine in older adults.

This was done by integration of bilastine in vitro and in vivo physicochemical data from young adults and studying the effect of aging with two different approaches: a physiologically based pharmacokinetic (PBPK) model and a semi-mechanistic population pharmacokinetic model (Senescence). The PBPK model used intestinal apical efflux and basolateral influx transporters to capture the results from young adults after single IV (10 mg) and 20 mg oral doses, which supports the hypothesis of gut transporters involvement on secretion. The Senescence model was developed from a published PopPK model adding up declining functions on different physiological systems and body composition changes with age.

Both models were then qualified using data from 16 older adults, mean age 68,7 years. The PBPK model was also used to assess the dose in older people (80 years old).

Both models showed that a daily dose of 20 mg is safe and effective in older people, supporting the existing information in this age group.

Several tumors are treated with PD-1/PD-L1 inhibitors, such as nivolumab, pembrolizumab, atezolizumab. However, these are known to induce rash in some cases. Rash treatment included antihistamines and corticosteroids. Bilastine is a non-sedating second generation H1-antihistamine, but its effectiveness in rash caused by PD-1/PD-L1 inhibitors is unknown. The aim of this study was to assess the efficacy of bilastine in these cases.

This study included 84 patients with PD-1/PD-L1 rash of a group of 224 patients from a Japanese medical center between September 2014 and October 2018. They were classified into 4 groups according to the systemic antihistamine and topical corticosteroid therapy: (1) bilastine and corticosteroid group (n = 18), (2) another antihistamine and corticosteroid group (n = 22), (3) bilastine only group (n = 20) and (4) another antihistamine group (n = 24).

The group in bilastine and corticosteroid showed a significantly shorter median duration of treatment than group 2. Bilastine group had a significantly shorter period of systemic medications than the another antihistamine group. Adverse events reported included somnolence (3 %), headache (3 %) and dizziness (3 %) and no serious adverse events were reported.

In conclusion, bilastine treatment reduced the need and duration of topical corticosteroid use in PD-1/PD-L1 inhibitors induced rash with a good safety profile.