Premium
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,
Lütjohann D,
Engel A,
Weitschies W,
Siegmund W
Publication year - 2011
Publication title -
clinical pharmacology and therapeutics
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.941
H-Index - 188
eISSN - 1532-6535
pISSN - 0009-9236
DOI - 10.1038/clpt.2011.4
Subject(s) - ezetimibe , tacrolimus , pharmacology , pharmacokinetics , clinical pharmacology , drug , medicine , drug interaction , adverse effect , absorption (acoustics) , calcineurin , oral administration , cholesterol , transplantation , physics , acoustics
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. Clinical Pharmacology & Therapeutics (2011) 89 4, 524–528. doi: 10.1038/clpt.2011.4