Drug interactions between the immunosuppressant tacrolimus and the cholesterol absorption inhibitor ezetimibe in healthy volunteers.
Article Details
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Oswald S, Nassif A, Modess C, Keiser M, Ulrich A, Runge D, Hanke U, Lutjohann D, Engel A, Weitschies W, Siegmund W
Drug interactions between the immunosuppressant tacrolimus and the cholesterol absorption inhibitor ezetimibe in healthy volunteers.
Clin Pharmacol Ther. 2011 Apr;89(4):524-8. doi: 10.1038/clpt.2011.4. Epub 2011 Mar 2.
- PubMed ID
- 21368751 [ View in PubMed]
- Abstract
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.
DrugBank Data that Cites this Article
- Drug Enzymes
Drug Enzyme Kind Organism Pharmacological Action Actions Ezetimibe UDP-glucuronosyltransferase 1-1 Protein Humans UnknownSubstrateDetails Ezetimibe UDP-glucuronosyltransferase 1-3 Protein Humans UnknownSubstrateDetails - Drug Transporters
Drug Transporter Kind Organism Pharmacological Action Actions Ezetimibe Canalicular multispecific organic anion transporter 1 Protein Humans UnknownSubstrateDetails Ezetimibe P-glycoprotein 1 Protein Humans UnknownSubstrateDetails Ezetimibe Solute carrier organic anion transporter family member 1B1 Protein Humans UnknownSubstrateDetails