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Sitagliptin, New Investigational Treatment for Type 2 Diabetes

Sep 20, 2005

The results from 2 Phase II studies show that sitagliptin a new class diabetes drugs called DPP-4 inhibitors, improved glycemic control with no significant weight gain and low risk of hypoglycemia.

In the Phase II studies of more than 1,000 patients, ”sitagliptin”, Merck Sharp & Dohme’s investigational medicine from a new class of diabetes treatments called dipeptidyl peptidase 4 (DPP-4) inhibitors, improved glycemic control in patients with type 2 diabetes and exhibited a safety and tolerability profile similar to placebo. In addition, patients taking sitagliptin experienced no significant weight gain and a low risk of hypoglycemia.

Results from a 12-week, double-blind, placebo-controlled, parallel group study in patients with type 2 diabetes showed that sitagliptin oral tablets significantly reduced HbA1c (A1C) from baseline as compared to placebo with an average reduction of 0.6 percent observed in the sitagliptin 100 mg once daily group (p<.001).

The majority of the patients in this study had mild to moderate hyperglycemia. The mean baseline A1C was approximately 7.7 with 28.8 percent of patients having a baseline A1C at or less than 7.0 percent. Observed differences in A1C between patients taking sitagliptin and patients administered placebo were greatest in those patients with a higher baseline A1C at randomization. In patients with a higher A1C baseline (i.e., between 8.5 and 10 percent), a 0.8 percent reduction, relative to placebo, was seen in patients randomized to the 100 mg once daily dose of sitagliptin using data carried forward, that is including patients whether they completed the study or not. A mean 1.1 percent reduction in A1C relative to placebo was observed in patients taking sitagliptin using data from patients who completed the study as per study protocol.

In this study, 552 type 2 diabetes patients, aged 30-74 years and with an HbA1C of 5.8 – 10.4% were randomized to one of five treatment groups: Placebo; sitagliptin (25 mg, 50 mg, or 100 mg) oral tablets once daily; or sitagliptin 50 mg oral tablets twice daily. Treatment with sitagliptin was generally well tolerated and resulted in no significant weight gain or incidence of GI related adverse events. Only one adverse event of hypoglycemia was reported in each of the four sitagliptin treatment groups, compared to no adverse events of hypoglycemia reported in the placebo group.

The second study presented was a randomized, double-blind, placebo-controlled study, which evaluated the efficacy and tolerability of sitagliptin in 743 patients with type 2 diabetes. The majority of the patients in this study had mild to moderate hyperglycemia (mean baseline A1C of 7.8 – 7.9 percent). Sitagliptin was generally well tolerated and resulted in no significant weight gain. Patients treated with glipizide had an average weight gain of 1.1 kilogram relative to placebo. Adverse event reports of hypoglycemia were observed in 4 percent of patients taking sitagliptin, 17 percent of patients taking glipizide and 2 percent of patients taking placebo.

Sitagliptin is an investigational medicine now under development by Merck & Co. for the treatment of type 2 diabetes. If approved, sitagliptin would be a member of a new class of antihyperglycaemic agents called DPP-IV inhibitors, which inhibit the DPP-4 enzyme that normally inactivates the incretin gut hormones GLP-1 and GIP. Sitagliptin is expected to lower blood glucose levels by increasing the level of active incretin hormones which increase insulin from pancreatic beta-cells and decrease glucagon from pancreatic alpha cells in a glucose-dependent manner (when blood glucose is elevated and not when blood glucose is low).

Reported at the European Association for the Study of Diabetes meeting, EASD.