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Interaction of Single-Dose Ezetimibe and Steady-State Cyclosporine in Renal Transplant Patients

From Merck Research Laboratories, Rahway, New Jersey, and West Point, Pennsylvania (Dr Bergman, Ms Burke, Mr Larson, Dr Johnson-Levonas, Dr Murphy, Dr Gottesdiener, Dr Paolini); Schering-Plough Research Institute, Kenilworth, New Jersey (Dr Reyderman, Dr Statkevich, Dr Maxwell, Dr Kosoglu); and Christchurch Clinical Studies Trust, Christchurch, New Zealand (Dr Robson).

This open-label, single-period study evaluated the single-dose pharmacokinetics of ezetimibe (EZE) 10 mg in the setting of steady-state cyclosporine (CyA) dosing in renal transplant patients. A single 10-mg dose of EZE was coadministered with the morning dose of CyA (75-150 mg twice a day). Total EZE (sum of unconjugated, parent EZE and EZE-glucuronide; EZE-total) AUC_0-last and C_max were compared to values derived from a prespecified database of healthy volunteers. Geometric mean ratios (90% CIs) for (EZE + CyA)/EZE alone for EZE-total AUC_(0-last) and C_max were 3.41 (2.55, 4.56) and 3.91 (3.13, 4.89), respectively. Compared to healthy controls, EZE-total AUC_(0-last) was 3.4-fold higher in transplant patients receiving CyA; similar exposure levels were seen in a prior multiple-dose study in which EZE 50 mg was administered to healthy volunteers without dose-related toxicity. Because the long-term safety implications of both higher EZE exposures and undetermined effect on CyA are not yet understood, the clinical significance of this interaction is unknown.

Key Words: Ezetimibe • cyclosporine • interaction • renal • transplant

Address for reprints: Arthur J. Bergman, Clinical Drug Metabolism, Merck Research Laboratories, WP 75-100, Sumneytown Pike, PO Box 4, West Point, PA 19486.

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