A Bioequivalence Trial of Lenvatinib Mesylate Capsules in Healthy Subjects Under Fasting and Postprandial Conditions.

Abstract

The aim of this study was to evaluate the comparative effectiveness and safety profiles of generic lenvatinib mesylate capsules and the reference product in a cohort of healthy Chinese individuals. The research design consisted of a randomized, open-label trial with a single-dose regimen, 2 crossover periods, and 2 distinct phases involving participants from the Chinese population. A total of 24 individuals were enrolled in the fasting study, with an additional 27 participants included in the postmeal study. Each participant received a single dose of either 4mg of the reference product or the study product per cycle. The washout period was 14days between each period. Bioequivalence was assessed through the analysis of geometric mean and ratio of pharmacokinetic parameters, while the safety of both drugs was evaluated by monitoring adverse events (AEs). Following a single oral administration of lenvatinib (4mg), linear pharmacokinetics were observed. The rate of absorption was found to be significantly faster under fasting conditions (median time to maximum concentration, 2.3-2.5hours), while the presence of a high-fat diet resulted in delayed absorption (median tmax, 5.3-6.1hours). Furthermore, the 90% confidence intervals for the reference and test pharmacokinetic parameters under both fasting and postprandial conditions fell within the bioequivalence standard range of 80%-125%. AEs were reported in 34.78% of cases during fasting and in 48.15% of cases after eating. There was no significant difference in AE rates between the reference and study products. The study determined that both the study product and the reference product were bioequivalent and well tolerated by healthy Chinese participants in both fasting and postprandial conditions.