Relative bioavailability study of ticagrelor in healthy subjects under fasting conditions

Abstract

Objectives: This is a randomized, single-dose, two-period, two-sequence, and crossover study to evaluate the bioequivalence (BE) profiles of two formulations of ticagrelor 90 mg, under fasting conditions. Materials and Methods: The plasma concentrations of ticagrelor were measured using a validated liquid chromatography mass spectrometry method. Enrolled for the study were 30 healthy adult volunteers (21 males and 9 females). All completed the study. The two formulations of ticagrelor were considered bioequivalent if a 90% confidence interval (CI) fell within 80.00–125.00% for Cmax and AUC0-t. Tolerability and safety were assessed throughout the study. Results: The pharmacokinetic (PK) parameters were similar between the test product (T) Clenosan® and reference product (R) Brilinta® under fasting conditions (90% CI for all PK parameters fell within 80.00–125.00%). The 90% CI of the test/reference ratios of log-transformed PK parameter point estimates were Cmax: 95.49% (87.99– 103.62%) and AUC0-t: 103.20% (97.52–109.21%), respectively. Conclusion: Our results demonstrated BE between the test and reference drug products of oral ticagrelor in healthy subjects under fasting conditions.