Thrombosis is the leading cause of morbidity and mortality worldwide. Therefore, the control of blood coagulation has become a major target for new therapeutic intervention over the past two decades. We at Bristol-Myers Squibb have a long history of research interest in this area and our efforts culminated in the discovery of Eliquis® (apixaban). This presentation will discuss our learnings from structure-based drug design efforts which led to Eliquis® and applications of these learnings to design inhibitors of other serine proteases in the coagulation cascade. This presentation will focus on the design of orally active, small molecule factor XIa inhibitors.

Structure-based design of serine protease inhibitors: The quest for safer and efficacious anticoagulants

249th National Meeting (2015)

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