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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 ]
Side effects may include bleeding, most commonly from the nose, gastrointestinal tract (GI) or genitourinary system. [2] Compared to the risk of bleeding with warfarin use, direct factor Xa inhibitors have a higher risk of GI bleeding, but lower risk of bleeding in the brain . [ 2 ]
Beneficial side effects are less common; some examples, in many cases of side-effects that ultimately gained regulatory approval as intended effects, are: Bevacizumab ( Avastin ), used to slow the growth of blood vessels, has been used against dry age-related macular degeneration , as well as macular edema from diseases such as diabetic ...
Subanalysis of Phase III ARISTOTLE Trial of Eliquis® (apixaban) Demonstrated Consistent Results Versus Warfarin in Patients with Nonvalvular Atrial Fibrillation with or without Valvular Heart ...
The U.S. government on Tuesday released a list of 10 prescription medicines that will be subject to the first-ever price negotiations by the Medicare health program that covers Americans aged 65 ...
The Biden administration said Medicare negotiated discounts with pharmaceutical companies on 10 drugs prescribed to treat cancer and heart disease.
Another natural occurring direct Xa-inhibitor, the tick anticoagulant peptide (TAP), was discovered in 1990. It is a single-chain, 60 amino acid peptide and like antistasin it is a slow, tight-binding inhibitor with a similar Ki value (~0.6 nM). These two proteins were mostly used to validate factor Xa as a drug target.
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