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Multiple-Dose Administration of Sitagliptin, a Dipeptidyl Peptidase-4 Inhibitor, Does Not Alter the Single-Dose Pharmacokinetics of Rosiglitazone in Healthy Subjects

From Merck & Co, Inc, Whitehouse Station, New Jersey (Mr Mistry, Dr Bergman, Dr Luo, Dr Davies, Dr Gottesdiener, Dr Wagner, Dr Herman); Merck & Co, Inc, Brussels, Belgium (Ms Cilissen); and SGS Life Sciences Services, Antwerp, Belgium (Dr Haazen).

Sitagliptin, a dipeptidyl peptidase-4 inhibitor, is an incretin enhancer that is approved for the treatment of type 2 diabetes. Sitagliptin is mainly renally eliminated and not a potent inhibitor of CYP450 enzymes in vitro. Rosiglitazone, a thiazolidenedione, is an insulin sensitizer and mainly metabolized by CYP2C8. Since both agents may potentially be coadministered, the purpose of this study was to examine the effects of sitagliptin on rosiglitazone pharmacokinetics. In this open-label, randomized, 2-period, crossover study, 12 healthy normoglycemic subjects, 21 to 44 years, received single 4-mg doses of rosiglitazone alone in one period and coadministered with sitagliptin on day 5 following a multiple-dose regimen for sitagliptin (200 mg once daily x 5 days) in the other period. The geometric mean ratios and 90% confidence intervals ([rosiglitazone + sitagliptin]/rosiglitazone) for rosiglitazone AUC_0- and C_max were 0.98 (0.93, 1.02) and 0.99 (0.88, 1.12), respectively. In conclusion, sitagliptin did not alter the pharmacokinetics of rosiglitazone in healthy subjects.

Key Words: MK-0431 • sitagliptin • DPP-4 • pharmacokinetics • rosiglitazone

Address for reprints: Address for correspondence: Gary A. Herman, MD, Merck Research Laboratories, Mail Code RY34-A536, PO Box 2000, Rahway, NJ 07065-0900.

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