DiseasesChemicals and DrugsAnalytical, Diagnostic and Therapeutic Techniques and EquipmentPhenomena and ProcessesHealth Care
Factor XaPyridonesThiophenesAnticoagulantsMorpholinesPartial Thromboplastin TimeAntithrombin IIIInvertebrate HormonesAntithrombinsBlood CoagulationHemorrhageFibrinolytic AgentsArthropod ProteinsAdministration, OralVenous Thromboembolismbeta-AlaninePyrazolesProthrombin TimeThrombinHeparinWarfarinEnoxaparinFactor XThromboembolismProthrombinThrombosisHeparin, Low-Molecular-WeightFactor VaPyridinesThromboplastinPolysaccharidesVenous ThrombosisFactor VDouble-Blind MethodRecombinant ProteinsAtrial FibrillationDose-Response Relationship, DrugFactor IXaStrokeSerine Proteinase InhibitorsTreatment OutcomeFactor VIIaProtein CBenzimidazolesFactor VIIKineticsDansyl CompoundsHirudinsFactor IX
ApixabanVitamin K antagonistsHeparinEdoxabanReversalDabigatranAnti-Xa assayInhibition of factorAntithrombotic agentsRecombinantAndexxaPlatelet aggregatiAnticoagulantPulmonary embolismAssayDirectSelectivePotentThrombin generationBindsEnzymeFondaparinuxAnticoagulationProthrombin Complex ConWarfarinCoagulation factorsBetrixabanAntithrombinBleedingThromboembolismProteinOralSerinePortolaThrombosisMajorPatientsSyntheticActivityAbsenceBlood clotsRisk factorsCrystalPill
Apixaban12
  • Direct factor Xa inhibitors include rivaroxaban, apixaban and edoxaban, and are types of direct oral anticoagulant, which are blood thinning drugs, one of the classes of antithrombotic drugs. (wikipedia.org)
  • Apixaban is a factor Xa inhibitor indicated for treatment of DVT and PE. (medscape.com)
  • abcg2) in apixaban disposition was evaluated in experiments using transporter inhibitors and transporter knockout (KO) rats. (aspetjournals.org)
  • The fecal elimination, IC, and systemic clearance of apixaban were increased upon AC administration in both BDC rats and dogs and were decreased in BDC rats dosed with GF-120918, a dual BCRP and P-gp inhibitor). (aspetjournals.org)
  • IE as a clearance pathway, balanced with metabolism and renal excretion, helps decrease the impacts of intrinsic (renal or hepatic impairment) and extrinsic (drug-drug interactions) factors on apixaban disposition. (aspetjournals.org)
  • The approval of Andexxa is supported by data from two Phase 3 ANNEXA studies (ANNEXA-R and ANNEXA-A) published in The New England Journal of Medicine , which evaluated the safety and efficacy of Andexxa in reversing the anticoagulant activity of the Factor Xa inhibitors rivaroxaban and apixaban in healthy volunteers. (prohostbiotech.com)
  • The median decrease in anti-Factor Xa activity from baseline was 97 percent for rivaroxaban and 92 percent for apixaban. (prohostbiotech.com)
  • Apixaban is in a class of medications called factor Xa inhibitors. (medlineplus.gov)
  • Arterial antithrombotic and bleeding time effects of apixaban, a direct factor Xa inhibitor, in combination with antiplatelet therapy in rabbits. (sigmaaldrich.com)
  • These include the direct thrombin inhibitor, dabigatran, or either of the factor Xa inhibitors, rivaroxaban or apixaban. (acc.org)
  • Andexxa is a recombinant Factor Xa used to reverse anticoagulation (major bleeds) caused by oral FXa-inhibitor treatments, rivaroxaban and apixaban, commonly referred to as blood-thinners. (zacks.com)
  • It is also approved as Ondexxya in Japan for FXa inhibitors apixaban, rivaroxaban, or edoxaban. (zacks.com)
Vitamin K antagonists3
  • Prior to the introduction of direct factor Xa inhibitors, vitamin K antagonists such as warfarin were the only oral anticoagulants for over 60 years, and together with heparin have been the main blood thinners in use. (wikipedia.org)
  • Other anticoagulant substance classes like vitamin K antagonists or thrombin inhibitors are considered to have a higher bleeding risk than factor Xa inhibitors. (inteligand.com)
  • The administration of 4-factor prothrombin complex concentrate (4F-PCC) has expanded beyond its Food and Drug Administration (FDA)-approved indication for the emergent reversal of vitamin K antagonists (VKAs). (bvsalud.org)
Heparin2
Edoxaban2
  • Edoxaban is a factor Xa inhibitor indicated for treatment of DVT and PE in patients who have been initially treated with a parenteral anticoagulant for 5-10 days. (medscape.com)
  • Edoxaban (Lixiana, Daiichi Sankyo), another direct factor Xa inhibitor, is currently approved in Japan. (medscape.com)
Reversal7
  • Oral factor Xa inhibitors are increasingly used for anticoagulation, but there is no approved reversal agent. (nih.gov)
  • Explain the current evidence relating to the utilization of four-factor prothrombin complex concentrate (4F-PCC) for the reversal of factor Xa inhibitors in patients with major or life-threatening bleeding. (wildapricot.org)
  • Compare the efficacy and safety of 4F-PCC to that of andexanet alpha when used for the reversal of factor Xa inhibitors. (wildapricot.org)
  • Identify the appropriate dose of 4F-PCC to use for the reversal of factor Xa inhibitors in patients with major or life-threatening bleeding. (wildapricot.org)
  • Interim data from the ongoing ANNEXA-4 single-arm, open-label study in patients with major bleeding from 185 evaluable patients showed that Andexxa rapidly and significantly reversed anti-Factor Xa activity when administered as a bolus and sustained this reversal when followed by a 120-minute infusion. (prohostbiotech.com)
  • Low Risk of Traumatic Intracranial Hematoma Expansion with Factor Xa Inhibitors without Andexanet Reversal. (harvard.edu)
  • Betrixaban was going to have to compete with already-popular factor Xa inhibitors, but Andexxa could have the factor Xa inhibitor-reversal field all to itself. (foxbusiness.com)
Dabigatran3
  • Dabigatran is a direct thrombin inhibitor. (medscape.com)
  • A method comparison between our UPLC-MRM MS method, the commercially available automated Direct Thrombin Inhibitor assay (DTI assay) for dabigatran measurement from CoaChrom Diagnostica, as well as the automated anti-Xa assay for rivaroxaban measurement from Chromogenix both performed by ACL-TOP showed a high degree of correlation. (uni-wuerzburg.de)
  • However, UPLC-MRM MS measurement of dabigatran and rivaroxaban has a much better selectivity than classical functional assays measuring activities of various coagulation factors which are susceptible to interference by other coagulant drugs. (uni-wuerzburg.de)
Anti-Xa assay1
  • Introduction: Monitoring of direct oral anticoagulants (DOACs) with calibrated anti-Xa assay is limited by the high intra- and interindividual variation of the test results. (researchsquare.com)
Inhibition of factor3
Antithrombotic agents1
  • Synthetic, selective, and direct inhibitors to FXa, such as DX-9065a, are highly potent and orally bioavailable antithrombotic agents that have demonstrated an improved side effect profile, probably by allowing sufficient thrombin to remain for platelet activation and normal hemostasis, while preventing pathological thrombus formation. (imrpress.com)
Recombinant2
  • Andexxa is a recombinant protein specifically designed to bind to Factor Xa inhibitors and rapidly reverse their anticoagulant effect . (prohostbiotech.com)
  • Extended half-life recombinant FIX (rFIX) molecules have been generated to reduce the dosing burden and increase the protection of patients with hemophilia B. Clinical pharmacology studies with recombinant factor IX Fc fusion protein (rFIXFc) report a similar initial peak plasma recovery to that of rFIX, but with a larger volume of distribution. (bvsalud.org)
Andexxa4
  • The results demonstrated that Andexxa rapidly and significantly reversed anti-Factor Xa activity (the anticoagulant mechanism of these medicines). (prohostbiotech.com)
  • Andexxa works by acting as a decoy for oral and injectable Factor Xa inhibitors, which target and bind to Factor Xa, which allows them to exert their anticoagulant effect. (prohostbiotech.com)
  • When Andexxa is given to a patient with Factor Xa inhibitor-related bleeding, it binds to the Factor Xa inhibitor and prevents it from inhibiting the activity of Factor Xa and reverses the anticoagulant effects of the inhibitor. (prohostbiotech.com)
  • While factor Xa inhibitors such as Xarelto and Eliquis are relatively new,during the 12 months ended April 2015, there were over 50,000 patients admitted to hospitals in the U.S. for bleeding events that could in theory have been shut off with administration of Andexxa. (foxbusiness.com)
Platelet aggregati2
  • Carbasalate calcium is an analgesic , antipyretic , and anti-inflammatory drug, [1] as well as a platelet aggregation inhibitor . (wikipedia.org)
  • Cloricromen is a platelet aggregation inhibitor. (wikidoc.org)
Anticoagulant3
  • Andexanet alfa, a specific antidote to reverse the anticoagulant activity of direct Xa inhibitors in the event of major bleeding, was approved by the FDA in 2018. (wikipedia.org)
  • Later, another naturally occurring inhibitor, tick anticoagulant peptide (TAP) was isolated from the extract of tick Ornithodoros moubata. (wikipedia.org)
  • Indeed, the medical community and people on the Factor Xa inhibitors anticoagulants have been eagerly anticipating the approval of the antidote for these important anticoagulant products. (prohostbiotech.com)
Pulmonary embolism2
Assay1
Direct13
  • Direct factor Xa inhibitors (xabans) are anticoagulants (blood thinning drugs), used to both treat and prevent blood clots in veins, and prevent stroke and embolism in people with atrial fibrillation (AF). (wikipedia.org)
  • Direct factor Xa inhibitors can be considered as an alternative to warfarin, particularly if a person is on several other medications that interact with warfarin, or if attending medical appointments and laboratory monitoring becomes difficult. (wikipedia.org)
  • Factors considered before deciding on whether warfarin or a DOAC or which direct factor Xa inhibitor is used, include: the presence or absence of valvular heart disease, state of kidney function, the risk of stroke and the risk of bleeding. (wikipedia.org)
  • Direct Xa inhibitors are contraindicated in people who are actively bleeding or who are at high risk of bleeding. (wikipedia.org)
  • 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. (wikipedia.org)
  • Direct factor Xa inhibitors block the enzyme called factor Xa, preventing the conversion of prothrombin to thrombin in the final common pathway of clot formation in veins and the heart. (wikipedia.org)
  • Also in contrast to warfarin and phenprocoumon, direct factor Xa inhibitors do not require frequent monitoring of the prothrombin time (also called the INR) and dose adjustments. (wikipedia.org)
  • The cost of direct Xa inhibitor's can reach more than 50 times that of warfarin, although this difference may be offset by lower monitoring costs. (wikipedia.org)
  • Presently, many types of direct inhibitors are in various stages of clinical trials and expected to provide significant benefits as compared to currently utilized therapy strategies. (imrpress.com)
  • Ex vivo plasma analysis from treated animals revealed expected anti-factor Xa activity but no direct inhibitory effect against thrombin. (nih.gov)
  • These results underscore the key role played by the P1 ligand not only in determining the binding affinity of the inhibitor by direct interaction but also in modifying the binding mode of the whole scaffold, resulting in a nonlinear SAR. (rcsb.org)
  • Hence, the direct inhibition factor Xa is considered as more favorable regarding the safety/efficacy ratio compared to other anticoagulants. (inteligand.com)
  • Oral factor Xa inhibitors and direct thrombin inhibitors are sometimes referred to as direct oral anticoagulants (DOACs). (msdmanuals.com)
Selective1
  • Arixtra is the first selective inhibitor of Factor Xa, a protein central to the coagulation process. (webwire.com)
Potent2
  • Combining the most favorable substituents at the indole nucleus led to the discovery of a remarkably potent factor Xa inhibitor displaying a K(i) value of 0.07 nM. (rcsb.org)
  • In this context, PKB inhibitors have been demonstrated to be potent agents against cancer. (inteligand.com)
Thrombin generation1
  • To more specifically elucidate the anti-factor Xa mediated antithrombotic mechanism of action of this pentasaccharide, it was studied in several thrombin generation assays. (nih.gov)
Binds1
  • 1493-1537) that binds tissue factor pathway inhibitor alpha (TFPIα). (lu.se)
Enzyme1
  • Factor Xa (FXa) is a key enzyme that is positioned at the convergence of the intrinsic and extrinsic pathways in the blood coagulation cascade, and inactivation by a specific FXa inhibitor effectively prevents the generation of thrombin. (imrpress.com)
Fondaparinux1
  • Arixtra (fondaparinux) is an inhibitor of the blood clotting Factor X and is used to prevent blood clots , often in people undergoing certain surgical procedures. (rxlist.com)
Anticoagulation1
  • The CHA 2 DS 2 -VASc score contains more risk factors and has a greater range of points, thus switching to the CHA 2 DS 2 -VASc score will increase the number of patients eligible for anticoagulation. (acc.org)
Prothrombin Complex Con1
  • Prothrombin complex concentrate (PCC) for the management of Xa-inhibitor-associated bleeding has been described in small case series and one cohort study. (nih.gov)
Warfarin1
  • Warfarin interferes with the hepatic synthesis of vitamin K-dependent coagulation factors. (medscape.com)
Coagulation factors1
  • Unmet needs remain regarding the development of non-invasive administration routes for coagulation factors. (bvsalud.org)
Betrixaban1
  • Lovenox is typically administered in hospital by a healthcare practitioner, while Portola's betrixaban (along with other Factor Xa-class anticoagulants) is a pill that can be sent home with patients, reducing their hospital stay and strain on healthcare budgets. (foxbusiness.com)
Antithrombin1
Bleeding4
  • For major bleeding associated with oral Xa inhibitors, PCC may have a beneficial effect. (nih.gov)
  • In the U.S. alone in 2016, there were approximately 117,000 hospital admissions attributable to Factor Xa inhibitor-related bleeding and nearly 2,000 bleeding-related deaths per month. (prohostbiotech.com)
  • Get tips on managing patients with factor Xa inhibitor-related acute major bleeding here . (beckershospitalreview.com)
  • BACKGROUND: Hemophilia B (HB) is a bleeding disorder characterized by coagulation factor (F) IX (FIX) deficiency. (bvsalud.org)
Thromboembolism1
  • When considering noncardiac surgery, these factors and the need to weigh the risk of hemorrhage against that of thromboembolism must be analyzed on an individual patient basis. (medscape.com)
Protein6
  • Outcomes Ser/Thr Protein Phosphatase 1 Regulates Ser-862 Phosphorylation of mGluR7 To judge the result of protein phosphatase activity on Ser-862 phosphorylation of mGluR7, we used many inhibitors of serine/threonine PP activity 1st. (e-core.org)
  • Antirhinoviral compounds, the so-called human rhinovirus (HRV) coat protein inhibitors, have been developed to bind into a hydrophobic pocket in the viral capsid, stabilizing the capsid and interfering with cell attachment and/or uncoating of the viruses. (inteligand.com)
  • This study is targeted on generating libraries of possible new HRV coat protein inhibitors built in an analogous structural manner as the WIN compounds. (inteligand.com)
  • Protein S also interacts with TFPIα and serves as TFPIα-cofactor in factor Xa (FXa) inhibition. (lu.se)
  • The structure of a Ca(2+)-binding epidermal growth factor-like domain: its role in protein-protein interactions. (embl.de)
  • Molecular genetic methods were implemented into the screening examinations for thrombophilic disorders in the 1990's along with the first discoveries of coagulation inhibitors (AT, protein C and protein S). The discovery of the molecular cause of activated protein C (APC) resistance by Bertina in 1994 greatly expanded their utilization. (intechopen.com)
Oral1
  • New Factor Xa oral anticoagulants such as Johnson & Johnson 'sXarelto and Bristol-Myers Squibb 'sEliquis put up annual sales of $1.87 and $1.86 billion last year, respectively, but they have a slight problem. (foxbusiness.com)
Serine1
Portola1
  • The news is extremely important for the doctors, the patients on the Factor Xa inhibitors and definitely for Portola, the first and only company that created and developed this life-saving product. (prohostbiotech.com)
Thrombosis2
  • Cancer is a risk factor for DVT, particularly in older patients and in patients with recurrent thrombosis. (merckmanuals.com)
  • Venous thrombosis is a multifactorial disease frequently related to the interaction of genetic and environmental risk factors. (intechopen.com)
Major1
  • Occult cancers may be present in patients with apparently idiopathic DVT, but extensive workup of patients for tumors is not recommended unless patients have major risk factors for cancer or symptoms suggestive of an occult cancer. (merckmanuals.com)
Patients2
  • Reference to the expanded information is crucial for addressing factors that may be of particular importance when individualizing a patient's treatment, such as loss of bone mineral density with a regimen that includes tenofovir disoproxil fumarate and the conflicting data on cardiac risk with abacavir (see guideline section Specific Factors to Consider and Discuss With Patients ). (hivguidelines.org)
  • A large study with this factor Xa inhibitor failed to show a statistically significant improvement over the standard-of-care (injected Lovenox from Sanofi ) atpreventing dangerous blood clots in acute patients who recently suffered serious medical conditions requiring hospitalization. (foxbusiness.com)
Synthetic1
Activity1
  • Several ECM proteins such as laminin, tenascin and thrombospondin contain domains with homology to epidermal growth factor (EGF) and exhibit growth promoting activity. (embl.de)
Absence1
  • In the absence of an inhibitor the hydrophobic binding pocket, which is situated underneath a depression on the virus capsid surface, can be either empty or occupied by a cellular pocket factor, a lipid or fatty acid. (inteligand.com)
Blood clots1
  • They are commonly prescribed to treat and prevent blood clots in veins, prevent stroke and embolism in people with non-valvular atrial fibrillation (AF) who have other risk factors, and prevent blood clots after routine knee and hip replacement surgery. (wikipedia.org)
Risk factors2
  • Some of the recently discovered genetic risk factors, such as factor V Leiden and prothrombin G20210A mutations, are quite common in the population. (intechopen.com)
  • The exact mechanisms by which cardiovascular risk factors predispose to AF are not understood fully but are under intense investigation. (medscape.com)
Crystal1
  • We have determined, at high resolution (1.5 A), the crystal structure of such a domain, from human clotting factor IX, as a complex with Ca2+. (embl.de)
Pill1
  • In formulating its recommendations for New York State, this committee balanced the strength of published evidence regarding efficacy of treatment regimens with factors that influence adherence, including pill burden, tolerability, and dosing schedule. (hivguidelines.org)