Oral Thrombin Inhibitor Ximelagatran

Preclinical and initial clinical experiences with the direct oral thrombin inhibitor ximelagatran demonstrated both a short and long-term potential utility for this agent in the prevention and treatment of various thromboembolic disorders associated with both arterial and venous thrombosis. Oral administration of ximelagatran after surgery and continued for at least 6–12 d appears to be safe and effective as prophylaxis against venous thromboembolism after total knee replacement surgery. This was accomplished without laboratory monitoring of the intensity of ximelagatran anticoagulation or adjustment of the ximelagatran dose. Of the four postoperative oral ximelagatran dose regimens tested, the most effective is the 24 mg twice-daily; this regimen appears to provide at least comparable efficacy and safety as compared to postoperative low molecular weight heparin (LMWH) prophylaxis. Further testing of ximelagatran in phase III clinical trials in patients with various thromboembolic disorders is in progress.