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Apixaban is a highly selective, orally bioavailable, and reversible direct inhibitor of free and clot-bound factor Xa. Factor Xa catalyzes the conversion of prothrombin to thrombin, the final enzyme in the coagulation cascade that is responsible for fibrin clot formation. [ 28 ]
The monitoring of warfarin and keeping the international normalized ratio (INR) between 2.0 and 3.0, along with avoiding over and under treatment, has driven a search for an alternative. [3] [14] A naturally occurring inhibitor of factor Xa was reported in 1971 by Spellman et al. from the dog hookworm. [15]
Thrombin demonstrates a high level of allosteric regulation. [2] Allosterism in thrombin is regulated by the exosites 1 and 2 and the sodium binding site. A recent patent review has shown that the general consensus among researchers is that allosteric inhibitors may provide a more regulatable anticoagulant. [3]
ELIQUIS ® (apixaban) Demonstrated Superiority In Reducing A Composite Of Recurrent Venous Thromboembolism And All-Cause Death Without Increasing The Rate Of Major Bleeding Versus Placebo During ...
U.S. FDA Approves ELIQUIS ® (apixaban) to Reduce the Risk of Stroke and Systemic Embolism in Patients with Nonvalvular Atrial Fibrillation ELIQUIS Demonstrated Superior Risk Reductions Versus ...
Patients were randomized to treatment with ELIQUIS 5 mg orally twice daily (or 2.5 mg twice daily in selected patients, representing 4.7 percent of all patients) or warfarin (target INR range 2.0 ...
Rivaroxaban, sold under the brand name Xarelto among others, is an anticoagulant medication (blood thinner) used to treat and prevent blood clots. [8] Specifically it is used to treat deep vein thrombosis and pulmonary emboli and prevent blood clots in atrial fibrillation and following hip or knee surgery. [8]
The European Society of Cardiology (ESC), [25] and National Institute for Health and Care Excellence (NICE) [27] guidelines recommend that if the patient has a CHA 2 DS 2-VASc score of 2 and above, oral anticoagulation therapy (OAC) with a vitamin K antagonist (VKA, e.g. warfarin with target INR of 2-3) or one of the direct oral anticoagulant ...