摘要

Apixaban is a potent reversible inhibitor of the activated human coagulation factor X. This new oral anticoagulant has favourable pharmacokinetic and pharmocodynamic properties which include a concentration-dependent anticoagulant effect, good oral bioavailability, balanced elimination and excretion, infrequent drug or food interactions, and the lack of liver toxicity. Apixaban has already completed a large part of its phase 3 clinical trial programme. In the ARISTOTLE study, which focused on stroke prevention in atrial fibrillation, apixaban showed a balanced efficacy and safety profile, being superior to warfarin both in the prevention of strokes and in the risk of causing major bleeding. A further trial related to this indication, AVERROES, demonstrated the clear superiority of apixaban compared to aspirin treatment. In the primary prophylaxis of venous thromboembolism after orthopaedic surgery, apixaban successfully completed the ADVANCE study programme and was approved in Europe for patients undergoing elective hip or knee replacement. The results of the AMPLIFY and AMPLIFY-EXT studies will soon show whether the inhibitor is also effective in the treatment and secondary prophylaxis after acute deep vein thrombosis and pulmonary embolism. On the other hand, the use of apixaban in the primary prophylaxis of venous thrombosis in hospitalised medical patients, and its administration on top of antiplatelet therapy to patients who have suffered an acute coronary syndrome, have not received support by the results of ADOPT and APPRAISE-II, respectively. In conclusion, on the basis of the available evidence, apixaban appears to be a valuable therapeutic option for the prevention of venous thrombosis and embolic stroke.

  • 出版日期2012-8