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

Article Details

Citation

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
DrugEnzymeKindOrganismPharmacological ActionActions
EzetimibeUDP-glucuronosyltransferase 1-1ProteinHumans
Unknown
Substrate
Details
EzetimibeUDP-glucuronosyltransferase 1-3ProteinHumans
Unknown
Substrate
Details
Drug Transporters
DrugTransporterKindOrganismPharmacological ActionActions
EzetimibeCanalicular multispecific organic anion transporter 1ProteinHumans
Unknown
Substrate
Details
EzetimibeP-glycoprotein 1ProteinHumans
Unknown
Substrate
Details
EzetimibeSolute carrier organic anion transporter family member 1B1ProteinHumans
Unknown
Substrate
Details