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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 ]
Bristol-Myers Squibb and Pfizer Announce Publication of ARISTOTLE Subanalysis in Circulation Subgroup analysis demonstrates that the treatment effects of Eliquis ® (apixaban) vs. warfarin, across ...
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 ...
The SAMe-TT 2 R 2 score [1] [2] is a clinical prediction rule to predict the quality of vitamin K antagonist anticoagulation therapy as measured by time in therapeutic INR range (TTR) (VKA e.g. warfarin). [3]
However, protamine appears only partially to neutralize the anti-factor Xa activity of LMWH. Because the molecular weight of heparin impacts its interaction with protamine, the lack of complete neutralization of anti-factor Xa is likely due to reduced protamine binding to the LMWH moieties in the preparation. Protamine is a medicine that ...
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]
Andexanet alfa, sold under the brand name Andexxa among others, is an antidote for the medications rivaroxaban and apixaban, when reversal of anticoagulation is needed due to uncontrolled bleeding. [8] It has not been found to be useful for other factor Xa inhibitors. [9] It is given by injection into a vein. [9]