The discovery and development of rivaroxaban, an oral, direct factor Xa inhibitor.

05:57 EDT 20th September 2014 | BioPortfolio

Summary of "The discovery and development of rivaroxaban, an oral, direct factor Xa inhibitor."

The activated serine protease factor Xa is a promising target for new anticoagulants. After studies on naturally occurring factor Xa inhibitors indicated that such agents could be effective and safe, research focused on small-molecule direct inhibitors of factor Xa that might address the major clinical need for improved oral anticoagulants. In 2008, rivaroxaban (Xarelto; Bayer HealthCare) became the first such compound to be approved for clinical use. This article presents the history of rivaroxaban's development, from the structure-activity relationship studies that led to its discovery to the preclinical and clinical studies, and also provides a brief overview of other oral anticoagulants in advanced clinical development.

Affiliation

Global Therapeutic Research, Pharma R&D, Bayer HealthCare, Aprather Weg 18a, D-42096 Wuppertal, Germany.

Journal Details

This article was published in the following journal.

Name: Nature reviews. Drug discovery
ISSN: 1474-1784
Pages:

Links

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