Bisegliptin

Bisegliptin (KRP-104) is a small molecule compound with antidiabetic activity. Bisegliptin is metabolized mainly by converting the cyano group to the carboxylic acid form, and DPP-4 plays a partial role in its metabolism. The carboxylic acid metabolite of bisegliptin can be detected both in vivo and in vitro. In rat experiments, the plasma concentration of the carboxylic acid metabolite of bisegliptin was affected by other DPP inhibitors, showing the complexity of its metabolic process. The amide intermediate of bisegliptin was detected both in vivo and in vitro, and its conversion rate was significantly faster than that of the parent compound when incubated with DPP-4[1].