(R)-8-(3-Amino-piperidin-1-yl)-7-but-2-ynyl-3-methyl-1-(4-methyl-quinazolin-2-ylmethyl)-3

Linagliptin Linagliptin, developed by Boehringer Ingelheim, was approved by the FDA on May 2, 2011. It is used to combine diet and exercise to improve the control of blood glucose levels in people with type 2 diabetes. Linagliptin improves blood glucose control in patients by inhibiting dipeptidyl peptidase-4 (DPP-4).

Incretin (Incretin) has the effect of promoting the secretion of insulin by pancreatic islet B cells, mainly including glucose-dependent insulinotropic polypeptide (GIP) and glucagon-like polypeptide-1 (GLP-1). DDP-4 is a serine protease located on the surface of cells. It binds to proteins and is widely present in plasma and various tissues in the body (such as kidney, liver, small intestinal villi, endothelial cells, etc.). Linagliptin is a selective DPP-4 inhibitor that inhibits the activity of the enzyme by reversibly binding to DPP-4, delays the degradation of GLP-1, enhances the activity of GLP-1, and stimulates in a glucose-dependent manner Insulin secretes and reduces the level of glucagon in the circulation, thereby regulating the blood glucose level of patients with type 2 diabetes.

Compared with other DPP-4 inhibitors, the main advantages of Linagliptin are: it has excellent renal safety and can effectively reduce glycosylated hemoglobin. Linagliptin is mainly excreted in the feces in the prototype form. After oral administration, the renal excretion is only 5% of the administered amount. Even if it is administered intravenously, only 30.8% is excreted via the kidneys. Therefore, there is no need for patients undergoing treatment. Regularly check liver and kidney function and dose adjustment. All patients can uniformly fix the dose for easy prescription.
Common adverse reactions of Linagliptin are respiratory infection, nasal congestion, muscle pain, headache and sore throat.