Dabigatran etexilate

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Dabigatran is a direct thrombin inhibitor, for the prevention of venous thromboembolic events in patients who have undergone total hip- or knee-replacement surgery.
Venous thromboembolism (VTE) — occlusion of veins by blood clots — is the third most common cause of cardiovascular-associated death, after heart attacks and stroke. Without preventive treatment, patients undergoing hip- or knee-replacement surgery are at high risk of developing VTE2. Indeed, many clinical studies have demonstrated the importance of primary thromboprophylaxis in reducing morbidity and mortality for such patients.
The serine protease thrombin is the final mediator in the coagulation cascade that leads to the production of fibrin, the main protein component of blood clots. Thrombin is also a potent activator of platelets. Consequently, thrombin has been a popular target for the development of
novel anticoagulants.


Several peptidic direct thrombin inhibitors (DTIs) have been approved for clinical use in the prevention of thrombosis, such as desirudin1,3. However, these agents still require parenteral administration, limiting their chronic use. An orally available DTI, ximelagatran was approved in Europe in 2004, but was subsequently withdrawn from the market owing to issues with liver toxicity. The development of other DTIs has continued, and dabigatran is the first to receive regulatory approval in a major market.


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