ximelagatran

Ximelagatran is an oral anticoagulant developed as a direct thrombin inhibitor and was the first member of this class available for oral administration. It is a synthetic small molecule prodrug that is rapidly absorbed in the gastrointestinal tract and converted in vivo to its active form, melagatran, primarily through hydrolysis and reduction in the liver and other tissues. Melagatran acts by directly, competitively, and reversibly inhibiting thrombin (factor IIa), thereby preventing fibrin formation and clot development. Ximelagatran was investigated as an alternative to warfarin for several indications including prevention of stroke in atrial fibrillation, prevention of venous thromboembolism (VTE) after orthopedic surgery, long-term secondary prevention of VTE following standard treatment, acute therapy for deep vein thrombosis (DVT), and secondary prevention after myocardial infarction. The drug offered advantages such as fixed dosing without routine coagulation monitoring or significant food/drug interactions; however, it was associated with hepatotoxicity leading to abnormal liver function tests or dysfunction during long-term use. Due to these safety concerns—specifically reports of liver damage—AstraZeneca discontinued its development globally in 2006[1][2][3][4][5][6][7].

Brand names

ExantaExarta

Other names

ximelagatran