title: An overview of bilastine metabolism during preclinical investigations.
abstract: Knowledge of the biotransformation of oral H₁ antihistamines is clinically important because it can define their pharmacokinetic profile through possible effects on absorption (i.e., first-pass metabolism) and elimination. Further, clinically significant interactions with inhibitors of cytochrome P450 (CYP) have previously been reported for drugs of this therapeutic group, such as terfenadine and astemizole, indicating the possibility of drug-drug interactions involving agents that share the same metabolic pathway. The aim of this article was to review the preclinical testing of a new antihistamine (i.e., bilastine) in terms of its biotransformation in various animal species, including humans, and to evaluate its potential for possible drug-drug interactions involving the CYP system. A wide array of preclinical experiments were reviewed, all of which demonstrated that bilastine undergoes minimal metabolism in all species tested to date, including humans. Further, bilastine did not interact significantly, either as an inhibitor or inducer, with the CYP enzyme system, suggesting a low propensity for involvement in drug-drug interactions. These characteristics demonstrate the potential for bilastine to be a good choice for allergic patients receiving treatment for other concomitant diseases, including those with renal or hepatic dysfunction.
authors.affiliation: Faes Farma, SA, R&D and Innovation Department, Bizkaia, Spain. mlucero@faes.es
authors.forename: María Luisa
authors.initials: ML
authors.lastname: Lucero
authors.forename: Ana
authors.initials: A
authors.lastname: Gonzalo
authors.forename: Rory
authors.initials: R
authors.lastname: Mumford
authors.forename: Mónica
authors.initials: M
authors.lastname: Betanzos
authors.forename: Ana
authors.initials: A
authors.lastname: Alejandro
mesh_terms: D000818:Animals; D001562:Benzimidazoles / Q000378:metabolism* / Q000493:pharmacokinetics / Q000494:pharmacology; D001711:Biotransformation; D004353:Drug Evaluation, Preclinical; D004347:Drug Interactions; D039563:Histamine H1 Antagonists, Non-Sedating / Q000378:metabolism* / Q000493:pharmacokinetics / Q000494:pharmacology; D006801:Humans; D010880:Piperidines / Q000378:metabolism* / Q000493:pharmacokinetics / Q000494:pharmacology; D013045:Species Specificity
chemical_list: D001562:Benzimidazoles; D039563:Histamine H1 Antagonists, Non-Sedating; D010880:Piperidines; C445659:bilastine