The discovery and development of rivaroxaban, an oral, direct factor Xa inhibitor.
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.
Global Therapeutic Research, Pharma R&D, Bayer HealthCare, Aprather Weg 18a, D-42096 Wuppertal, Germany.
This article was published in the following journal.
Name: Nature reviews. Drug discovery
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