Oligomerization improves endostatin as antiangiogenic and anticancer drug

Endostatin is an antiangiogenic protein first discovered in Folkman's laboratory at Childrens Hospital, Harvard Medical School, and Boston. The antitumor properties of this protein are well established. Nowever, the amount of protein required for injection in patients was beyond production feasibility due to the poor pharmacokinetics of endostatin monomer. We have shown that the problem of poor pharmacokinetics can be solved by using the Fc domain of IgG being conjugated to endostatin, a component of all monoclonal antibodies approved for patients with a number of diseases including cancer. As a result of employing Fc-endostatin, the half-life in mice was increased to 2 weeks instead of 2 hours for endostatin alone, consistent with pharmacokinetics of monoclonal antibodies.

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