(3,3-Difluoropyrrolidin-1-yl)[(2S,4S)-4-[4-(pyrimidin-2-yl)piperazin-1-yl]pyrrolidin-2-yl]methanone

The objectives of the present study are to characterize the metabolism, pharmacokinetics, and excretion of [¹⁴C] Gosogliptin in Sprague-Dawley (SD) rats, beagle dogs, and humans. A single dose of [¹⁴C] Gosogliptin is administered orally to intact SD rats (5 mg/kg), beagle dogs (5 mg/kg), and humans (20 mg). After a single oral dose of [¹⁴C] Gosogliptin to SD rats, an overall mean of 97.1% of the administered radioactivity is recovered in the urine, feces, and cage wash over a period of 168 h postdose. The mean cumulative dose recovered in feces is 66.0%. The mean cumulative excretion in the urine is 30.8%. Approximately 95% of the excreted radioactivity recovery occurred in the first 48 h. Mean total recoveries of dosed radioactivity from bile duct-cannulated rats are 29.5% in urine and 62.0% in bile. No gender-related differences are observed in the excretion pattern of radioactivity^[2].