Ximelagatran: An oral direct thrombin inhibitor for anticoagulant therapy

Ximelagatran is a prodrug that is rapidly converted to melagatran, a direct, competitive and reversible inhibitor of the active site of human α-thrombin. Its effect is independent from diet, plasma antithrombin levels, obesity or ethnicity. It has little effect on bleeding time at doses up to twice those required, and interference with other drugs is avoided by the absence of interaction with cytochrome P450. Ximelagatran has been documented in a large clinical programme with proven efficacy in prevention and treatment of venous thromboembolism, prevention of stroke in patients with atrial fibrillation and prevention of major cardiovascular events following a recent myocardial infarction. Bleeding has not been a problem, but increase in liver enzymes is a cause of concern for long term use until more information is available.