Extension of the group of incretin-targeted preparations: Saxagliptin – a new dipeptidyl peptidase-4 inhibitor

A new selective incretin-targeted dipeptidyl peptidase-4 inhibitor was registered in the Russian Federation in August 2010. The enzyme dipeptidyl peptidase-4 inactivates glucagon-like peptide-1 (GLP-1). A rise of GLP-1 concentration in blood plasma is known to result in the glucose-dependent stimulation of insulin secretion by pancreatic beta-cells and suppression of glucagon release. Saxagliptin is readily absorbed in the gastrointestinal tract and remains active within 24 hours after oral intake. It allows the drug to be taken once during 24 hours. Clinical studies have demonstrated that saxagliptin improves glycemic control when used as both monotherapy and in combination with other antidiabetic medicines (metformin, sulfonylureas, and thiazolidinediones). The use of saxagliptin leads to a reduction of fasting and postprandial plasma glucose level and thereby to the clinically significant decrease in glycated hemoglobin (HbA1c) concentration. The low risk of hypoglycemia following saxagliptin intake is due to the glucose-dependent mechanism of its action. The results of clinical investigations indicate that saxagliptin is safe and well tolerated by the patients and has no significant influence on their body weight; its dose does not need to be corrected for the sex and age of the patients or the presence of concomitant hepatic disorders.