Comparable pharmacokinetics and pharmacodynamics of melagatran in Japanese and caucasian volunteers after oral administration of the direct thrombin inhibitor ximelagatran.

Objectives: Two studies were conducted to elucidate the pharmacokinetics and pharmacodynamics of melagatran after administration of the oral direct thrombin inhibitor ximelagatran to Caucasian and Japanese volunteers.

Methods: In study 1, with a single-blind, parallel-group design, young Japanese and Caucasian male volunteers were randomised to receive four single escalating oral doses of ximelagatran (12, 24, 36 and 60mg on separate days; n = 27 per ethnic group) or placebo (n = 6 per ethnic group). In study 2, with an open-label design, elderly Japanese male volunteers (n = 12) received three single escalating oral doses of ximelagatran (12, 24 and 36mg on separate days).

Pharmacokinetics and pharmacodynamics of the oral direct thrombin inhibitor ximelagatran in young healthy Japanese men.

Background And Objective: The direct thrombin inhibitor ximelagatran, which is rapidly bioconverted to its active form melagatran after oral administration, is being developed for the prevention and treatment of thromboembolism. This study assessed the effects of food and repeated dosing on the pharmacokinetics and pharmacodynamics of melagatran after oral administration of ximelagatran to young healthy Japanese males.

Methods: In part one of the two-part study, volunteers (n = 24) were randomised to receive in a crossover fashion a single oral dose of ximelagatran 48mg with or without breakfast on 2 days separated by a 2- to 7-day washout period.