Journal
NATURE REVIEWS DRUG DISCOVERY
Volume 10, Issue 1, Pages 61-+Publisher
NATURE PUBLISHING GROUP
DOI: 10.1038/nrd3185
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Funding
- Bayer HealthCare
- Johnson & Johnson Pharmaceutical Research Development
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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.
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