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.
Publication types
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Randomized Controlled Trial
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Research Support, Non-U.S. Gov't
MeSH terms
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ATP Binding Cassette Transporter, Subfamily B
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ATP Binding Cassette Transporter, Subfamily B, Member 1 / metabolism
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Administration, Oral
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Adult
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Animals
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Anticholesteremic Agents / pharmacokinetics*
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Anticholesteremic Agents / pharmacology
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Azetidines / pharmacokinetics*
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Azetidines / pharmacology
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Cell Line
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Cross-Over Studies
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Dogs
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Drug Interactions
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Ezetimibe
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Female
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Glucuronosyltransferase / metabolism
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Humans
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Immunosuppressive Agents / pharmacokinetics*
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Immunosuppressive Agents / pharmacology
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In Vitro Techniques
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Male
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Tacrolimus / pharmacokinetics*
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Tacrolimus / pharmacology
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Young Adult
Substances
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ABCB1 protein, human
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ATP Binding Cassette Transporter, Subfamily B
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ATP Binding Cassette Transporter, Subfamily B, Member 1
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Anticholesteremic Agents
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Azetidines
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Immunosuppressive Agents
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UGT1A1 enzyme
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Glucuronosyltransferase
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Ezetimibe
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Tacrolimus