Saxagliptin

Abstract

Saxagliptin is a DPP‐4 inhibitor used to treat type 2 diabetes. The metabolism of saxagliptin in healthy human subjects was investigated. After an oral administration of saxagliptin over a dose range 2.5–50 mg, the hydroxylation metabolite 2 was the major metabolite observed in human plasma and urine. The plasma molar exposure to 2 was about three to seven folds higher than that of saxagliptin in human. In human urine, 7–21% and 16–51% of the dose were eliminated over 48 h as saxagliptin and 2 , respectively. After a single 50‐mg dose of [ 14 C]‐saxagliptin, 24, 36, and 75% of the dose were excreted in urine as saxagliptin, metabolite 2 , and total radioactivity, respectively. About 22% of the administered radioactivity was recovered in feces.