New anticoagulants

S. Haas; S. Schellong

doi:10.1055/s-0037-1616898

Hämostaseologie, Table of Contents

Hamostaseologie 2007; 27(01): 41-47
DOI: 10.1055/s-0037-1616898

Orginal Articles

Schattauer GmbH

New anticoagulants

From bench to bedsideNeue Antikoagulanzienvom Labor bis zur Klinik

S. Haas

¹Klinikum rechts der Isar, Technische Universität München

,

S. Schellong

²Universitätsklinikum Carl-Gustav-Carus, TU Dresden

› Author Affiliations

Abstract

Summary

Heparins and vitamin K antagonists have been the cornerstones of anticoagulation therapy for several decades. Although they are very effective at inhibiting the coagulation process, they have several practical limitations. This was a challenge for the development of therapies that will overcome these drawbacks while matching the efficacy of the two classes of anticoagulants. Advances were achieved in the development of safer, convenient, more specific treatments, which should provide predictable anticoagulant responses and substantially improve the prevention and management of thromboembolic disorders. In the search for new agents matching the ideal anticoagulant profile, different steps in the coagulation cascade have been targeted, including direct thrombin inhibition, and inhibition of factor Xa, factor IXa, the factor Vlla-tissue factor complex and the factor Va-factor Vllla complex. The most advanced clinical development has been achieved with direct factor Xa- and factor IIa-inhibitors which may replace conventional anticoagulants for long-term prevention and treatment of venous and arterial thromboembolic complications.

Zusammenfassung

Heparine und Vitamin-K-Antagonisten waren die tragenden Säulen der gerinnungshemmenden Therapie in den vergangenen Jahrzehnten. Diese Pharmaka sind zwar sehr wirksame Antikoagulanzien, haben jedoch einige Nachteile bei der praktischen Anwendung. Dies führte zur Entwicklung neuer gerinnungshemmender Medikamente, die im Vergleich zu den konventionellen eine mindestens ebenbürtige Wirksamkeit haben, jedoch ohne deren Limitierungen aufzuweisen. Fortschritte wurden hinsichtlich Verträglichkeit, einfacher Anwendung und spezifischer Wirkung erzielt, was zu Verbesserungen der Prädiktivität und des Thrombosemanagements führte. Auf der Suche nach einem Antikoagulans mit idealem Profil wurden verschiedene Stufen der Gerinnungskaskade gezielt gehemmt, z. B. Thrombin, Faktor X, Faktor IX sowie Komplexe von Faktor VIIa und Tissue-Faktor bzw. Faktor Va und Faktor VIIIa. Die klinische Entwicklung der direkten Faktor-Xa- und Faktor-IIa-Inhibitoren ist am weitesten vorangeschritten, was möglicherweise zum Ersatz der konventionellen Antikoagulanzien in der Langzeitprophylaxe und Therapie venöser und arterieller thromboembolischer Komplikationen führt.

Keywords

Anticoagulants - factor Xa inhibitors - factor IIa inhibitors - heparins - vitamin K antagonists

Schlüsselwörter

Antikoagulanzien - Faktor-Xa-Inhibitoren - Faktor-IIa-Inhibitoren - Vitamin-K-Antagonisten

Full Text

References

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