Factor Xa inhibitors

E. Perzborn

doi:10.1055/s-0037-1617033

Hämostaseologie, Table of Contents

Hamostaseologie 2009; 29(03): 260-267
DOI: 10.1055/s-0037-1617033

Review

Schattauer GmbH

Factor Xa inhibitors

New anticoagulants for secondary haemostasisFaktor-Xa-InhibitorenNeue Antikoagulanzien der sekundären Hämostase

E. Perzborn

¹Cardiovascular Pharmacology, Pharma R&D Discovery Research, Bayer Schering Pharma AG, Wuppertal, Germany

› Author Affiliations

Abstract

Summary

Oral factor Xa (FXa) inhibitors are a promising alternative to current anticoagulants. This paper reviews the latest developments of oral direct FXa inhibitors and focuses on those which have been approved for the prevention of venous thromboembolism (VTE) after total hip or knee replacement or are in advanced development and have passed phase II (proof of principle) testing.

The most advanced drugs are apixaban, betrixaban, edoxaban, eribaxaban, rivaroxaban, LY517717, TAK-442, and YM150. Rivaroxaban (Xarelto^→) is the first direct FXa inhibitor which has recently been approved for the prevention of VTE in adult patients after elective hip or knee replacement in several countries, including the European Union and Canada. Rivaroxaban has a flat dose-dependent anticoagulant response with a wide therapeutic window and low potential for drug-drug and drug-food interactions. Rivaroxaban can be given in fixed doses without coagulation monitoring.

This review describes the pharmacodynamic and pharmacokinetic profiles and the results of clinical trials with FXa inhibitors in the prevention and treatment of thromboembolic disorders.

Zusammenfassung

Orale Faktor-Xa(FXa)-Hemmer sind viel versprechende Alternativen zu den gebräuchli-chen Antikoagulanzien. In diesem Artikel werden Neuentwicklungen im Bereich der oralen direkten FXa-Hemmer vorgestellt mit Schwerpunkt auf solchen, die zur Prävention venöser Thromboembolien (VTE) nach Hüft- oder Kniegelenkersatz zugelassen sind oder sich in einem fortgeschrittenen Entwicklungsstadium befinden und die Phase-II-Studien zum Nachweis der Wirksamkeit (proof of principle) durchlaufen haben.

Apixaban, Betrixaban, Edoxaban, Eribaxaban, Rivaroxaban, LY517717, TAK-442 und YM150 sind die am weitesten entwickelten FXa-Hemmer. Rivaroxaban (Xarelto^®) ist der erste direkte FXa-Hemmer, der u. a. in der Europäischen Union und in Kanada zur Prävention von VTE nach elektivem Hüft- oder Kniegelenksersatz bei Erwachsenen zugelassen ist. Für Rivaroxaban wurde eine flach verlaufende dosisabhängige antikoagulatorische Wirkung gezeigt. Sein breites therapeutisches Fenster und geringes Potenzial für Wechselwirkungen mit Pharmaka und Nahrungsmitteln erlaubt die Gabe in fixer Dosis ohne Überwachung der Blutgerinnung.

Diese Übersicht beschreibt das pharmakodynamische und pharmakokinetische Profil sowie die Ergebnisse klinischer Studien mit FXaHemmern zur Prävention und Behandlung von Thromboembolien.

Keywords

Factor Xa inhibitors - anticoagulants - thrombosis

Schlüsselwörter

Faktor-Xa-Hemmer - Antikoagulanzien - Thrombose

Full Text

References

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