2018
DOI: 10.1007/s40265-018-0940-4
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Abstract: Intravenous andexanet alfa [coagulation factor Xa (recombinant), inactivated-zhzo; Andexxa®] is a first-in-class recombinant modified factor Xa protein that has been developed by Portola Pharmaceuticals as a universal antidote to reverse anticoagulant effects of direct or indirect factor Xa inhibitors. In May 2018, andexanet alfa received its first global approval in the USA for use in patients treated with rivaroxaban and apixaban, when reversal of anticoagulant effects is required in life-threatening or unco… Show more

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Cited by 90 publications
(65 citation statements)
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“…DOAC management continues to be an issue in the perioperative setting, as measuring the effects of the factor Xa (FXa) inhibitors is not always possible . Although andexanet alfa has been approved for FXa inhibitor reversal in the United States and European Union (for life‐threatening or uncontrolled bleeding only), the drug has not been studied in surgical or procedural patients and has a relatively short duration of effect of approximately 3 hours . For emergency surgery, only idarucizumab is approved in most countries for dabigatran reversal .…”
Section: Discussionmentioning
confidence: 99%
“…DOAC management continues to be an issue in the perioperative setting, as measuring the effects of the factor Xa (FXa) inhibitors is not always possible . Although andexanet alfa has been approved for FXa inhibitor reversal in the United States and European Union (for life‐threatening or uncontrolled bleeding only), the drug has not been studied in surgical or procedural patients and has a relatively short duration of effect of approximately 3 hours . For emergency surgery, only idarucizumab is approved in most countries for dabigatran reversal .…”
Section: Discussionmentioning
confidence: 99%
“…Andexanet alfa, a recombinant modified human factor Xa decoy protein, has been shown to reverse the effects of direct factor Xa inhibitors (apixaban, rivaroxaban) by binding with higher affinity to these small molecules compared to endogenous factor Xa . Within 2–5 minutes of bolus administration, the concentration of the factor Xa inhibitor is significantly reduced with subsequent reduction in anti–factor Xa activity . Similar to its mechanism of reversing direct factor Xa inhibitors, andexanet alfa binds and neutralizes antithrombin III bound indirect factor Xa inhibitors (UFH, enoxaparin, and fondaparinux) .…”
Section: Discussionmentioning
confidence: 99%
“…While it is possible to overcome the UFH unresponsiveness by administration of higher doses of UFH, this practice may lead to substantial risk of UFH accumulation due to saturation of binding sites and reliance on the slower non‐saturable mechanism of renal clearance . Though andexanet alfa has a pharmacokinetic half‐life of 5–7 hours, its pharmacodynamic half‐life is 1 hour, therefore a rebound UFH effect may be seen following discontinuation of the andexanet alfa infusion …”
Section: Discussionmentioning
confidence: 99%
“…The synthesis of novel triazoles were prepared by the 1,3-dipolar cycloaddition between the N-propargyl amines (11)(12)(13)(14) and the organic azide (24-26) catalyzed by copper nanoparticles supported on ZnO in tetrahydrofuran as solvent, triethylamine as base at 160 °C under microwave irradiation (Scheme 7) [93]. (27)(28)(29)(30)(31)(32)(33)(34)(35)(36)(37)(38) were obtained in good to excellent yield (73-93%) using a lower loading of catalyst and in shorter reaction time (15 min) than previously reported by assisted microwave methodologies.…”
Section: Synthesis Of 1h-123-triazole Derivativesmentioning
confidence: 99%
“…In recent years, several direct FXa inhibitors have become available in the marketplace, and others are in active development ( Figure 2) [33,34]. Although these new oral anticoagulants are more efficacious than warfarin for the prevention of strokes and systemic embolism in patients with atrial fibrillation, the reversal agent Andexanet alfa has only recently been approved [35,36]. The development of antidotes for oral direct FXa inhibitors are still in the pipeline, but their expected approval for therapeutic purposes will be further beneficial to anticoagulation therapy [37,38].…”
Section: Introductionmentioning
confidence: 99%