Pharmacokinetic and bioequivalence evaluation of teneligliptin hydrobromide tablets following single-dose administration in healthy Chinese volunteers under fasting and fed conditions.

Abstract

By inhibiting dipeptidyl peptidase-4 (DPP-4), teneligliptin provides a therapeutic option for type 2 diabetes mellitus (T2DM) that is widely used in Asia. A generic product could lessen treatment costs, provided that its systemic availability is equivalent to that of the branded formulation. Such comparative information remains scarce for Chinese recipients of teneligliptin hydrobromide. We therefore investigated a new generic tablet as the test product and Tenelia^® as the reference product in fasted and fed settings. A total of 52 healthy Chinese adults participated in a randomized, open-label crossover investigation involving one dose, two sequences, and two periods; 26 participants were assigned to each sequence. The test and reference products were each administered at 40 mg in the fasting and fed studies, and administrations were 7 days apart. A validated LC-MS/MS assay yielded plasma teneligliptin concentrations. After logarithmic transformation, AUC_0-t, AUC_0-∞, and C_max were subjected to analysis of variance (ANOVA). Equivalence required the 90% confidence interval (CI) of each test/reference geometric mean ratio (GMR) to fall completely between 80% and 125%. CTCAE v5.0 was used to grade adverse events (AEs). In each dietary setting, the two products produced similar teneligliptin exposure. For AUC_0-t, AUC_0-∞, and C_max, every test/reference GMR had a 90% CI between the predefined boundaries of 80% and 125%. Serious adverse events (SAEs) did not occur. Whether administered in the fasting or fed state, the generic tablet met the regulatory requirements for bioequivalence with Tenelia^®. The pharmacokinetic comparison consequently supports the generic product as an equivalent alternative. The study was registered retrospectively in the Chinese Clinical Trial Registry (ChiCTR2500112749; November 19, 2025). Ethical approval was obtained from the Ethics Committee of The Affiliated Panyu Central Hospital, Guangzhou Medical University (PYZXYYEC [2025-013 (YW)]-01).