ezetimibe + tacrolimus

This is a combination of ezetimibe, a cholesterol absorption inhibitor, and tacrolimus, a calcineurin inhibitor immunosuppressant. Ezetimibe works by selectively inhibiting the absorption of cholesterol and phytosterol by the small intestine through targeting the Niemann-Pick C1-Like 1 (NPC1L1) protein. Tacrolimus reduces immune system activity by binding to the immunophilin FKBP-12, creating a complex that inhibits calcineurin, which in turn inhibits T-lymphocyte signal transduction and IL-2 transcription. Studies have shown that while these drugs may interact in vitro through competition for intestinal UGT1A1 and ABCB1 at concentrations reached in the gut lumen after oral administration, clinical studies in healthy volunteers demonstrated that this pharmacokinetic interaction is not of clinical relevance.