Expanding the clinical utility of therapeutic proteins: activated protein C variants with improved pharmacological properties

Proteins have emerged as viable treatments for a broad range of diseases, and their therapeutic applications have expanded considerably during the past decade. Although most biologics are administered in their native form to patients, engineering efforts to improve the properties of therapeutic proteins are becoming more prevalent. A recent study has shown that substantial improvements in the pharmacological profile of Xigris [R] can be achieved by mutations that diminish its inactivation by serpins, underscoring the importance of optimization efforts to create biologics with improved clinical profiles.