Sitagliptin Phosphate Monohydrate CAS 654671-77-9

Sitagliptin phosphate is the first dipeptidyl peptidase IV (DDP-4) inhibitor drug developed by Merck & Co. of Germany and approved by the U.S. Food and Drug Administration for the treatment of type 2 diabetes. Sugar drugs can improve the body’s own ability to reduce excessive blood sugar levels, and by inhibiting the activity of this enzyme, it can relatively increase the levels of naturally occurring incretins, including glucagon-like peptide-1 and glucose-dependent insulinotropic peptides. Trigger the clinical effect of increasing insulin production by the pancreas and stopping glucose production by the liver, ultimately lowering blood glucose concentrations. The characteristics of this product are that it can reduce hunger while stimulating insulin secretion, and will not cause weight gain, and will not cause hypoglycemia and edema. It is suitable for diabetic patients with poor blood sugar control and frequent hypoglycemia. It has been clinically verified in 552 patients with mild to moderate type 2 diabetes mellitus. Taking sitagliptin phosphate once a day, 100 mg each time, can reduce glycated hemoglobin by 0.6%-1.1% after taking the drug for 12 weeks. The incidence of adverse reactions was similar to placebo, and the most commonly reported adverse reactions (incidence >5% and higher than placebo) were nasal congestion or runny nose, as well as sore throat, upper respiratory tract infection, and headache.

Clinical studies have shown that sitagliptin phosphate as a monotherapy in patients with type 2 diabetes can significantly reduce the level of glycated hemoglobin (HbA1c). When used in combination with metformin or TZDs, it has a significant adjunctive role in targeting the three major defects of type 2 diabetes: insulin resistance, beta-cell dysfunction (reduced insulin release), and alpha-cell dysfunction (uninhibited hepatic glucose generation) to function. However, the drug should not be used for the treatment of patients with type 1 diabetes or diabetic ketoacidosis.