This drug is a dipeptidyl peptidase -4(DPP-4) inhibitor, which can control the blood sugar level by protecting endogenous intestinal glucagon and enhancing its effect. Glucose-dependent insulinotropic peptide (GIP) and glucagon-like peptide -1(GLP-1) are intestinal hypoglycemic agents released for dietary intake.
GLP-1 and GIP can increase insulin synthesis and release from islet β cells through intracellular signaling pathway, and GLP-1 can also reduce glucagon secretion from islet α cells, thus reducing hepatic glucose production. However, both GLP-1 and GIP are rapidly metabolized by DPP-4, resulting in the loss of their insulin-promoting effects.
This drug can inhibit the degradation of intestinal glucagon by DPP-4, so it can enhance the functions of GLP-1 and GIP, increase insulin release and reduce the circulating glucagon level (this effect is glucose-dependent). This drug selectively inhibits DPP-4, but has no inhibitory activity on DPP-8 or DPP-9. 1-4 hours after oral administration, the drug reached the peak concentration of 95nmol in blood, the area under the curve was 8.52mmol·h, the absolute bioavailability was about 87%, the protein binding rate was 38%, and the distribution volume was about 198L L. It is rarely metabolized in the liver. The renal clearance rate is about 35ml/min, the renal excretion rate is 87%(79% is the original drug), and the elimination half-life is 12.4 hours. Hemodialysis is helpful to the clearance of this drug.