History

Historical antecedents for the development of direct factor Xa inhibitors and the rationale for targeting factor Xa are discussed above. The success of fondaparinux has fueled the development of a large number of direct factor Xa inhibitors that are currently in various stages of clinical development (Table 4). Fondaparinux must be administered parenterally, which is inconvenient for long-term administration, and because the greatest clinical need for new anticoagulants is for a replacement for warfarin, the present focus of drug development is on oral direct factor Xa inhibitors.

To date no oral direct factor Xa inhibitors have been approved for clinical use. This section will focus on those agents that are most advanced in clinical development.

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