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Drug interactions between the immunosuppressant tacrolimus and the cholesterol absorption inhibitor ezetimibe in healthy volunteers.

Author(s): Oswald S, Nassif A, Modess C, Keiser M, Ulrich A, Runge D, Hanke U, Lutjohann D, Engel A, Weitschies W, Siegmund W

Affiliation(s): Department of Clinical Pharmacology, University of Greifswald, Greifswald, Germany. stefan.oswald@uni-greifswald.de

Publication date & source: 2011-04, Clin Pharmacol Ther., 89(4):524-8. Epub 2011 Mar 2.

Publication type: In Vitro; Randomized Controlled Trial; Research Support, Non-U.S. Gov't

Immunosuppressive therapy is frequently associated with hypercholesterolemia, calling for lipid-lowering treatment without adverse drug interactions. One option is treatment with the cholesterol absorption inhibitor ezetimibe. We have shown in vitro that ezetimibe and tacrolimus may interact in competition for intestinal UGT1A1 and ABCB1 at concentrations reached in gut lumen after oral administration. However, this clinical study in healthy volunteers showed that the expected pharmacokinetic interaction between ezetimibe and tacrolimus is not of clinical relevance.

Page last updated: 2011-12-09

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