Loading...
*  Factor X
And they may be more effective against Factor Xa in that they inhibit both free Factor Xa and Factor Xa in the prothrombinase ... Factor X is activated, by hydrolysis, into factor Xa by both factor IX (with its cofactor, factor VIII in a complex known as ... Factor Xa is the activated form of the coagulation factor thrombokinase, known eponymously as Stuart-Prower factor. Factor X is ... The result is a Factor VIIa/TF complex which catalyzes the activation of Factor X and Factor IX. Factor Xa formed on the ...
*  Factor V Leiden
In the normal person, factor V functions as a cofactor to allow factor Xa to activate prothrombin, resulting in the enzyme ... Factor V Leiden (rs6025) is a variant (mutated form) of human factor V (one of several substances that helps blood clot), which ... is a natural anticoagulant that acts to limit the extent of clotting by cleaving and degrading factor V. Factor V Leiden is an ... which normally inhibits the pro-clotting activity of factor V) is not able to bind normally to Factor V, leading to a ...
*  Discovery and development of direct thrombin inhibitors
Most of those drugs are in the class of direct factor Xa inhibitors, but there is one DTI called AZD0837, which is a follow-up ... DTIs are still under development, but the research focus has shifted towards factor Xa inhibitors, or even dual thrombin and ... Nar, Herbert (2012). "The role of structural information in the discovery of direct thrombin and factor Xa inhibitors". Trends ... Thethi, Indermohan; Lewis, Bruce; Fareed, Jawed (1 January 2012). "Oral Factor Xa and Direct Thrombin Inhibitors". Journal of ...
*  Discovery and development of direct Xa inhibitors
Factors IIa, Xa, VIIa, IXa and XIa are all proteolytic enzymes that have a specific role in the coagulation cascade. Factor Xa ... Inhibition of factor Xa leads to antithrombotic effects by decreasing the amount of thrombin. Directly targeting factor Xa is ... Today there are three factor Xa inhibitors marketed: rivaroxaban, apixaban and edoxaban. Factor Xa was identified as a ... "Molecular model of an interaction between factor Xa and DX-9065a, a novel factor Xa inhibitor: Contribution of the ...
*  Thrombin
Xa). The activity of factor Xa is greatly enhanced by binding to activated Factor V (Va), termed the prothrombinase complex. ... Factor Xa with factor V as a cofactor leads to cleavage of the Gla and two Kringle domains (forming together a fragment called ... activated blood-coagulation factor II, blood-coagulation factor IIa, factor IIa, E thrombin, beta-thrombin, gamma-thrombin) is ... Heparin increases the affinity of antithrombin to thrombin (as well as factor Xa). The direct thrombin inhibitors, a newer ...
*  Protein C
Factor V, high-density lipoprotein, anionic phospholipids and glycosphingolipids. Factor Va binds to prothrombin and Factor Xa ... Factor VIIIa augments Factor X activation by a factor of around 200,000. Because of its importance in clotting, Factor VIII is ... It acts as a serine protease zymogen: APC proteolyses peptide bonds in activated Factor V and Factor VIII (Factor Va and Factor ... Protein S also binds to Factor Xa, inhibiting the latter from diminishing APC's inactivation of Factor Va. The inactivation of ...
*  Fondaparinux
Unlike direct factor Xa inhibitors, it mediates its effects indirectly through antithrombin III, but unlike heparin, it is ... Fondaparinux is a synthetic pentasaccharide factor Xa inhibitor. Apart from the O-methyl group at the reducing end of the ... selective for factor Xa. Fondaparinux is similar to enoxaparin in reducing the risk of ischemic events at nine days, but it ... and heparin sulfate this monomeric sequence is thought to form the high-affinity binding site for the anti-coagulant factor ...
*  Direct Xa inhibitor
Ex: Rivaro(Identifier)-xa(FactorXa)-ban(inhibitor) A naturally occurring inhibitor of factor Xa was first reported in 1971 by ... Direct Factor Xa Inhibitors as Anticoagulants , PharmaXChange.info - A review and presentation on the available factor Xa ... Direct factor Xa inhibitors ('xabans') are a class of anticoagulant drugs which act directly upon Factor X in the coagulation ... Direct factor Xa inhibitors are being used clinically. Clinical trials have shown promise for these compounds as substitutes ...
*  Idraparinux
... selectively blocks coagulation factor Xa. See Heparin: Mechanism of anticoagulant action for a comparison of the ...
*  Apixaban
... and reversible direct inhibitor of free and clot-bound factor Xa. Factor Xa catalyzes the conversion of prothrombin to thrombin ... It is a direct factor Xa inhibitor. Apixaban was approved in Europe in 2012. It was approved in the U.S. in 2014 for treatment ... "ELIQUIS® (apixaban) tablets Factor Xa Inhibitor" (PDF). FDA. August 2014. Retrieved 2014-11-02. Enriquez A, Lip GY, Baranchuk A ... Apixaban has no direct effect on platelet aggregation, but by inhibiting factor Xa, it indirectly decreases clot formation ...
*  Betrixaban
It is potent, orally active and highly selective for factor Xa, being selected from a group of similar compounds for its low ... Piccini, J. P.; Lopes, R. D.; Mahaffey, K. W. (2010). "Oral factor Xa inhibitors for the prevention of stroke in atrial ... Betrixaban (INN; trade name Bevyxxa; development code PRT-054,021) is an anticoagulant drug which acts as a direct factor Xa ... "Merck Abandons Development of Factor Xa Inhibitor Betrixaban". CardioBrief. Retrieved 11 April 2014. "FDA approved betrixaban ( ...
*  Andexanet alfa
... is a biologic agent, a modified recombinant derivative of factor Xa (fXa). It acts as a decoy receptor - it has ... Andexanet alfa (trade name AndexXa) is a drug under investigation as a potential antidote for factor Xa inhibitors, a group of ... In 2015, the first randomized control trial showed that andexanet alfa reversed the effects of factor Xa inhibitor drugs ... March 2013). "A specific antidote for reversal of anticoagulation by direct and indirect inhibitors of coagulation factor Xa". ...
*  Edoxaban
Inhibition of factor Xa in the coagulation cascade reduces thrombin generation and thrombus formation. Factor Xa (FXa) is an ... including Factor X. In recent years, a new series of oral, direct acting inhibitors of Factor Xa have entered clinical ... Edoxaban (DU-176b, trade names Savaysa, Lixiana) is an oral anticoagulant drug which acts as a direct factor Xa inhibitor. It ... A number of anticoagulants inhibit the activity of Factor Xa. Unfractionated heparin (UFH), low molecular weight heparin (LMWH ...
*  Anti-apolipoprotein antibodies
AAHA interferes with factor Xa inhibition by Apo-H increasing factor Xa generation. However, like Apo-H the Lupus anticoagulant ... inhibits factor Xa generation. AAHA also inhibited the autoactivation of factor XII while at high AAHA concentrations, factor ... "Anticardiolipin antibodies block the inhibition by beta 2-glycoprotein I of the factor Xa generating activity of platelets". ... A synchronized inhibition of factor XII autoactivation by Apo-H and AHAA has been suggested. The haplotype HLA-DR4-DQ3 appears ...
*  Heparin
The activated AT then inactivates thrombin, factor Xa and other proteases. The rate of inactivation of these proteases by AT ... 2001). "Heparin enhances the specificity of antithrombin for thrombin and factor Xa independent of the reactive center loop ... Evidence for an exosite determinant of factor Xa specificity in heparin-activated antithrombin". J. Biol. Chem. 276 (18): 14961 ... as APTT is insensitive to alterations in factor Xa. Danaparoid, a mixture of heparan sulfate, dermatan sulfate, and chondroitin ...
*  Low molecular weight heparin
An anti-factor Xa activity may be useful for monitoring anticoagulation. Given its renal clearance, LMWH may not be feasible in ... LMWH has less of an effect on thrombin compared to heparin, but about the same effect on Factor Xa. Due to its renal clearance ... Heparin Antifactor Xa Assay Archived 2009-08-08 at Archive.is Page Updated: September 18, 2009 European Pharmacopedia ...
*  Rivaroxaban
It is the first available active direct factor Xa inhibitor which is taken by mouth. The maximum inhibition of factor Xa occurs ... Rivaroxaban inhibits both free Factor Xa and Factor Xa bound in the prothrombinase complex. It is a highly selective direct ... Factor Xa inhibitor with oral bioavailability and rapid onset of action. Inhibition of Factor Xa interrupts the intrinsic and ... The effects last approximately 8-12 hours, but factor Xa activity does not return to normal within 24 hours, so once-daily ...
*  Darexaban
Factor Xa (FXa) is an essential blood coagulation factor that is responsible for the initiation of the coagulation cascade. FXa ... Darexaban (YM150) is a direct inhibitor of factor Xa created by Astellas Pharma. It is an experimental drug that acts as an ... "A dose escalation study of YM150, an oral direct factor Xa inhibitor, in the prevention of venous thromboembolism in elective ... "Prevention of venous thromboembolism with an oral factor Xa inhibitor, YM150, after total hip arthoplasty. A dose finding study ...
*  Ancylostoma caninum
June 1995). "Ancylostoma caninum anticoagulant peptide: a hookworm-derived inhibitor of human coagulation factor Xa". PNAS. 92 ... which inhibit a range of blood coagulation factors such as Xa are utilised by A. caninum to help in the feeding process by ...
*  Serpin
Johnson DJ, Li W, Adams TE, Huntington JA (May 2006). "Antithrombin-S195A factor Xa-heparin structure reveals the allosteric ... The heparin pentasaccharide-bound form of antithrombin is, thus, a more effective inhibitor of thrombin and factor Xa. ... Domain-swaps occur when mutations or environmental factors interfere with the final stages of serpin folding to the native ... Andreu-Agulló C, Morante-Redolat JM, Delgado AC, Fariñas I (December 2009). "Vascular niche factor PEDF modulates Notch- ...
*  Protein Z
The main role of protein Z appears to be the degradation of factor Xa. This is done by protein Z-related protease inhibitor ( ... factors VII, IX, X and protein C. The carboxyglutamate residues (which require vitamin K) bind protein Z to phospholipid ... ZPI), but the reaction is accelerated 1000-fold by the presence of protein Z. Oddly, ZPI also degrades factor XI, but this ...
*  Apolipoprotein H
Apo-H also inhibits the generation of factor Xa in the presence of platelets. Apo-H also inhibits that activation of factor ... Since protein C is involved in factor Va degradation Apo-H indirectly inhibits the degradation of factor Va. This inhibitory ... "Anticardiolipin antibodies block the inhibition by beta 2-glycoprotein I of the factor Xa generating activity of platelets". ... Normally Apo-H assumes an anti-coagulation activity in serum (by inhibiting coagulation factors); however, changes in blood ...
*  Schrödinger (company)
"Role of the Active-Site Solvent in the Thermodynamics of Factor Xa Ligand Binding". J. Am. Chem. Sco. 130 (9): 2817-2831. doi: ...
*  Kunitz domain
... a factor Xa inhibitor from the tick Ornithodoros moubata". FEBS Lett. 352 (2): 251-7. doi:10.1016/0014-5793(94)00941-4. PMID ... This is a highly selective inhibitor of factor Xa in the blood coagulation pathways. TAP molecules are highly dipolar, and are ... and tissue factor pathway inhibitor (TFPI). Standalone Kunitz domains are used as a framework for the development of new ... tissue factor pathway inhibitor precursor; and Kunitz STI protease inhibitor contained in legume seeds. Kunitz domains are ...
*  Otamixaban
Guertin KR, Choi YM (2007). "The discovery of the Factor Xa inhibitor otamixaban: from lead identification to clinical ... Otamixaban (INN) is an experimental injectable anticoagulant direct factor Xa inhibitor that was investigated for the treatment ...
*  Euler-Mascheroni constant
... where the nth factor is the (n + 1)th root of ∏ k = 0 n ( k + 1 ) ( − 1 ) k + 1 ( n k ) . {\displaystyle \prod _{k=0}^{n}(k+1 ... x^{-a}} gives γ f a = ( a − 1 ) ζ ( a ) − 1 a − 1 {\displaystyle \gamma _{f_{a}}={\frac {(a-1)\zeta (a)-1}{a-1}}} where again ...
*  Danaparoid
... sodium (Orgaran) is an anticoagulant that works by inhibiting activated factor X (factor Xa). Danaparoid is a ...