Trelagliptin Succinate

Trelagliptin inhibits the activity of dipeptidyl peptidase 4. After a person eats, glucagon-like peptide 1 (GLP-1) is secreted from the intestines into the blood, and this inhibition stops it from being inactivated. The GLP-1 concentration in the blood rises, and the pancreas then releases insulin depending on the blood glucose concentration.

DPP-4 Inhibition

Trelagliptin selectively inhibits human plasma DPP-4 activity (IC50 value: 4.2 nmol/l, in vitro). Trelagliptin and alogliptin were also compared for DPP-4 inhibitory action under similar conditions (in vitro), and their IC50 values (nmol/L) were 1.3 and 5.3 respectively. In a study, type 2 diabetes patients whose blood glucose was not controlled well enough by diet and exercise took 100 mg of Trelagliptin once weekly, before meal, for 12 weeks. The study was double blind, parallel group and placebo controlled. The average DPP-4 inhibition rate 7 days after the final treatment was 77.4% in the Trelagliptin 100 mg group.

Active Type GLP-1 Concentration Elevation

Type 2 diabetes patients whose blood glucose was not controlled well enough by diet and exercise took 100 mg of Trelagliptin orally, once weekly, before meal, for 12 weeks. This was also a double-blind, parallel group, placebo-controlled comparative study. Meal load tests done 12 weeks after administration showed GLP-1 concentrations that were significantly elevated compared with the placebo group.

Glucose Tolerance Improvement

A single oral dose of Trelagliptin was given to obese type 2 diabetic model organisms (Wister fatty rat) and to non-obese type 2 diabetic model organisms (N-STZ-1.5 rat) after 1 night of fasting. Glucose was then given orally 1 hour after the drug, as a glucose load test. The results showed that Trelagliptin improves glucose tolerance.