DABIGATRAN ETEXILATE IN VENOUS THROMBOEMBOLISM

Dabigatran etexilate (Pradaxa (R)) is the orally available prodrug of dabigatran, a potent compound belonging to the new class of nonpeptide direct thrombin inhibitors (DTIs). Following oral administration, dabigatran etexilate reached peak plasma concentrations within 2 hours, showed linear pharmacokinetics across a wide dose range, a linear relationship between ecarin clotting time (ECT) and international normalized ratio (INR), and no significant food or drug interactions. Dabigatran etexilate at once-doily doses of 750 mg and 220 mg has demonstrated non-inferiority to once-doily enoxaparin 40 mg for the prevention of venous thromboembolism (VTE) in patients undergoing total hip or knee replacement surgery in two large, randomized, double-blind clinical trials. The safety profile of dabigatran etexilate was similar to that of enoxaparin with comparable rates of major bleeding, liver enzyme elevation and acute coronary events. Oral availability of dabigatran etexilate, together with a rapid onset and offset of action and predictable anticoagulation response, makes this compound on attractive alternative to traditional anticoagulant therapies for the prevention of VTE.