melagatran

Melagatran, a direct and orally active thrombin inhibitor, specifically inhibits thrombin without affecting other enzymes in the coagulation cascade or fibrinolytic enzymes. It does not rely on endogenous co-factors to exert its antithrombin effect, and may alleviate the harmful effects of endotoxemia. As a result, Melagatran offers a promising strategy for the prevention of arterial occlusion.

Melagatran monohydrate is a thrombin inhibitor. Melagatran prevents tissue factor expression in human platelet-monocyte heterotypic complexes. Melagatran reduces advanced atherosclerotic lesion size and may promote plaque stability in apolipoprotein E-deficient mice.

Ximelagatran (H 376-95), a direct thrombin inhibitor, can be taken orally and acts solely by inhibiting the actions of thrombin. Ximelagatran is converted to the active agent melagatran in vivo.