This review summarizes the mechanism of action of some of the most promising novel oral direct factor IIa and Xa inhibitors with a focus on published preclinical trials that led to their clinical development.doi:10.2174/157488412800958695Deftereos,S....
Mechanism of action The concept of coagulation as a sequential series of steps (cascade), in which a proenzyme is converted to an active enzyme, and with two partially independent pathways (the so called intrinsic and extrinsic pathways) converging at the activation of factor X (FX) and finall...
PURPOSE: The mechanism of action, pharmacodynamics, pharmacokinetics, efficacy in clinical trials, interactions, adverse effects and toxicity, and place in therapy of rivaroxaban are reviewed. SUMMARY: Rivaroxaban, the first oral, direct factor Xa (FXa) inhibitor to reach Phase III trials, inhibits ...
Expert Commentary: Andexanet alfa shows promise to become a highly effective, novel antidote for factor Xa anticoagulation. Its biochemical profile and mechanism of action are immediately more attractive than other drugs on the market and under development due to its inert nature within the normal ...
The mechanism of ACH-11 inhibition of platelet aggregation and its pharmacokinetics and pharmacodynamics in vivo are under investigation. Methods Preparation of Agkistrodon acutus venom hydrolysates. Agkistrodon acutus venom (0.4 g) was dissolved in 10 mL of 0.1 M phosphate buffer solution...
In addition to aspirin, the drug clopidogrel interferes with prostaglandin synthesis in the platelet but via a different mechanism of action. By blocking the ADP receptor on the surface of the platelet, clopidogrel causes a reduction in the activity of platelet membrane lipases, leading t...
To study the mechanism(s) of the antiviral activity of FXa, we compared the binding between FXa and various subunits of the SARS-CoV-2 S protein. Compared to control Fc protein, FXa had the strongest binding affinity toward the full-length S protein and, to a lesser extent, to subunit ...
TFPI inhibits the TF/fVIIa complex in a two-step mechanism which includes the initial interaction of the second Kunitz domain of TFPI with the active site of factor Xa, thereby inhibiting the proteolytic activity of factor Xa. The second step involves the inhibition of the TF/fVIIa complex ...
of (1) vesicle enumeration using nanoparticle tracking assay, imaging flow cytometry, and TF immunofluorescence localization in a single-vesicle analysis using microarrays; (2) cellular origin; and (3) TF-dependent Xa generation capacity, as well as assessing the contribution of the TF inhibitor, ...
The absence of an adequate reversal strategy to prevent and stop potential life-threatening bleeding complications is a major drawback to the clinical use of the direct oral inhibitors of blood coagulation factor Xa. Here we show that specific modificati