A BIOEQUIVALENCE STUDY OF TRELAGLIPTIN 100 MG TABLETS IN HEALTHY VOLUNTEERS: AN OPEN-LABEL, RANDOMIZED, TWO-TREATMENT, TWO-PERIOD, SINGLE-DOSE, CROSSOVER STUDY

Dr. Bhupesh Dewan*, Mr. Siddheshwar Shinde

ABSTRACT

Background: Once-weekly therapies like Trelagliptin, a long-acting Dipeptidyl Peptidase-4 (DPP-4) inhibitor, can enhance medication adherence and simplify treatment. Pharmacokinetic data on Trelagliptin in Indians are limited, necessitating a bioequivalence study with the reference product for regulatory approval and therapeutic consistency. Objective: To evaluate the pharmacokinetics and bioequivalence of the test product, Trelagliptin 100 mg tablet of Zuventus Healthcare Limited, compared to the reference product, Zafatek® (Takeda Pharmaceutical Company Limited, Japan), in healthy Indian adults under fasting conditions. Methods: This was an open-label, randomized, two-treatment, two-period, crossover, single-dose, truncated, bioequivalence study with a 25-day washout period. Pharmacokinetic parameters (Cmax, AUC0-72, Tmax) were assessed up to 72 hours post-dose. Plasma concentrations were measured using a validated liquid chromatography-tandem mass spectrometry (LC–MS/MS) method. Bioequivalence was established if the 90% confidence intervals (CI) of the geometric mean ratios (GMRs) for log-transformed primary parameters, Cmax and AUC0-72 fell within the 80.00–125.00% acceptance range. Results: Thirty-two male volunteers were enrolled, and 31 completed the study. The test and reference products demonstrated comparable pharmacokinetic profiles. The GMRs were 104.55% and 102.31% for Cmax and AUC0-72, respectively. The intra-subject coefficient of variation (ISCV) was 23.04% for Cmax and 4.25% for AUC0-72. The 90% CI for Trelagliptin was 94.77–115.34% for Cmax and 100.45–104.20% for AUC0-72, falling within the accepted bioequivalence range. Both products were well-tolerated, with only mild adverse events reported. Conclusions: Trelagliptin 100 mg tablet of Zuventus Healthcare Limited is bioequivalent to the Originator Product, Zafatek® from Japan and well-tolerated in healthy Indian subjects.

Keywords: Bioequivalence, Dipeptidyl Peptidase-4 inhibitor, Once-weekly, Oral antidiabetic, Trelagliptin.