Rivaroxaban

 

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Zusammenfassung

Rivaroxaban (Xarelto®), ein neuartiger oraler, direkter Faktor-Xa-Hemmer, ist in klinischer Entwicklung zur Prävention und Behandlung thromboembolischer Erkrankungen. Rivaroxaban hemmt die Clot-assoziierte und die freie Faktor-Xa-Aktivität, die Prothrombinase, und die Thrombinbildung. In Tiermodellen verhinderte Rivaroxaban die Bildung und das Wachstum venöser und arterieller Thromben. Rivaroxaban hat eine hohe orale Bioverfügbarkeit, schnellen Wirkeintritt und vorhersagbare Pharmakokinetik. In Phase-II-Studien zur Prävention venöser Thromboembolien (VTE) nach großen orthopädischen Operationen und zur Behandlung tiefer Venenthrombosen war Rivaroxaban wirksam und gut verträglich. In einer Phase-III-Studie zeigte Rivaroxaban höhere Wirksamkeit als Enoxaparin zur Vorbeugung von VTEs bei Kniegelenkersatzoperationen bei vergleichbar niedrigen Blutungsraten. Rivaroxaban wird zudem zur Therapie und Sekundärprävention von VTEs, zur Schlaganfallprophylaxe bei Vorhofflimmern und zur Sekundärprävention bei Patienten mit akutem Koronarsyndrom geprüft. Rivaroxaban ist eine vielversprechende Alternative zur aktuellen Therapie mit Antikoagulanzien bei thromboembolischen Erkrankungen.

Summary

Rivaroxaban (Xarelto^®) is a novel, oral, direct Factor Xa (FXa) inhibitor in late-stage development for the prevention and treatment of thromboembolic disorders. Rivaroxaban inhibits clot-associated and free FXa activity, and prothrombinase activity, and reduces thrombin generation. In animal models, rivaroxaban prevented venous and arterial thrombosis, and was effective at treating venous thrombosis. Rivaroxaban has high oral bioavailability, a rapid onset of action and predictable pharmacokinetics. In phase II studies, rivaroxaban was effective and well tolerated for the prevention of venous thromboembolism (VTE) after major orthopaedic surgery, and for the treatment of deep vein thrombosis. In a phase III study, rivaroxaban demonstrated significantly superior efficacy to enoxaparin for thromboprophylaxis after total knee arthroplasty, with similar low bleeding. Rivaroxaban is also being assessed for the treatment and secondary prevention of VTE, prevention of stroke in patients with atrial fibrillation and secondary prevention in patients with acute coronary syndrome. Rivaroxaban is a promising alternative to current pharmacological agents for thromboembolic disorders.

• References

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