Preclinical Assessment of Ezetimibe Combined with Curcumin in Colorectal Cancer Models

Purpose

The Ezetimibe-curcumin combination (Ezercumin™) is a new anticancer drug developed from the approved drug ezetimibe, combined with curcumin as a protein kinase inhibitor. Ezetimibe is an FDA-approved orally administered drug that blocks intestinal cholesterol uptake, thereby reducing plasma cholesterol levels. Previous studies in our lab showed that ezetimibe binds the MDM2-p53 binding domain and may reactivate p53 in cancers. However, ezetimibe is rapidly metabolized via glucuronidation, limiting its anticancer potential. Curcumin, a known kinase inhibitor, was evaluated for its ability to preserve ezetimibe's active form and enhance its antitumor effect.