Clinical Evaluation of the Tolerability, Pharmacokinetics, and Inhibition of Platelet Aggregation of Eptifibatide in Healthy Chinese Subjects

摘要

Abstract The present study aimed to evaluate the pharmacokinetic properties and antiplatelet aggregation activity of eptifibatide in healthy Chinese subjects. Eptifibatide (180 μg/kg) was administrated by 2 bolus injections 10 minutes apart, followed by a 2.0 μg/kg/min infusion for 24 hours. The eptifibatide pharmacokinetic and antiplatelet aggregation activities were evaluated using nonlinear mixed‐effects modeling and noncompartmental analysis. Safety assessments included adverse events, hematology, and biochemistry tests. Twelve Chinese healthy subjects were enrolled and completed the study. Steady‐state concentrations were achieved at 0.5 to 24 hours after dosing. The median time to maximum concentration was 13 minutes, and the mean terminal elimination half‐life was 148.19 minutes. The effective inhibition of platelet aggregation (20% platelet aggregation) occurred by 3 minutes after starting dosing to 4 hours after termination of the infusion. Eptifibatide concentrations were fitted with a 3‐compartment model, and the typical value of clearance was 0.11 L/min, with no significant covariates found. Three mild adverse events were detected in the study. Eptifibatide displays high sensitivity and excellent tolerability in healthy Chinese subjects. The dosage of eptifibatide recommended on the label for whites can effectively inhibit platelet aggregation.