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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]
Ximelagatran showed good efficacy compared with warfarin in several trials in prevention and treatment of deep vein thrombosis and as thromboprophylaxis in atrial fibrillation. [1] Development was stopped by manufacturer AstraZeneca , however, because of reports of liver enzyme derangements and liver failure .
In the EU, apixaban is indicated for the prevention of venous thromboembolic events (VTE) in adults who have undergone elective hip or knee replacement surgery, the prevention of stroke and systemic embolism in adults with non-valvular atrial fibrillation (NVAF) with one or more risk factors, for the treatment of deep vein thrombosis (DVT) and ...
AMPLIFY-EXT (Apixaban after the initial Management of PuLmonary embolIsm and deep vein thrombosis with First-line therapY-EXTended Treatment), a randomized, double-blind, multicenter trial ...
The p-methoxy group of apixaban connects to S1 pocket of FXa but does not appear to have any interaction with any residues in this region of FXa. The pyrazole N-2 nitrogen atom of apixaban interacts with Gln-192 and the carbonyl oxygen interacts with Gly-216. The phenyl lactam group of apixaban is positioned between Tyr-99 and Phe-174 and due ...
ELIQUIS ® (apixaban) Demonstrates Consistent Reductions in Stroke and Systemic Embolism, Major Bleeding and Mortality Compared to Warfarin in Patients with Nonvalvular Atrial Fibrillation at ...
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