What is dipeptidyl peptidase 4 inhibitor?

Dipeptidyl peptidase 4 inhibitors are a relatively common drug in medicine. Dipeptidyl peptidase 4 inhibitors can mainly treat human diabetes and control human blood sugar. They are a common drug for diabetic patients. Taking dipeptidyl peptidase 4 inhibitors can also promote the secretion of human pancreatic cells, have the effect of lowering human blood sugar, and have a certain therapeutic effect on the body.

What are dipeptidyl peptidase 4 inhibitors?

The inhibitors, namely dipeptidyl peptidase 4 inhibitors, are a class of drugs for the treatment of type 2 diabetes. This class of drugs can inhibit the inactivation of glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP), increase the levels of endogenous GLP-1 and GIP, promote the release of insulin from pancreatic β cells, and inhibit the secretion of glucagon from pancreatic α cells, thereby increasing insulin levels and lowering blood sugar, and are less likely to induce hypoglycemia and weight gain.

Incretins are a class of polypeptide hormones produced in the intestine that promote insulin secretion. In the human body, they mainly include glucagon-like peptide-1 and glucose-dependent insulin-secreting polypeptide. Among them, the characteristics of GLP-1 include:

① It is produced after a meal and promotes the secretion of insulin by pancreatic β cells in a glucose-dependent manner, thereby lowering blood sugar and not easily inducing hypoglycemia; ② It inhibits the secretion of glucagon by pancreatic α cells;

③ Delaying gastric emptying is beneficial to the control of postprandial blood sugar;

④Reduce appetite and reduce food intake;

⑤Inhibit intestinal lipoprotein secretion and may reduce postprandial hyperlipidemia, which is a risk factor for cardiovascular disease, thus having a cardioprotective effect;

⑥It can regulate the regeneration, proliferation and survival of pancreatic β cells in vitro.

DPP-4 is a cell surface serine protease. DPP-4 is most highly expressed in the intestine and is also expressed in the liver, pancreas, placenta, and thymus. DPP-4 can inactivate a variety of bioactive peptides, including GLP-1 and GIP. DPP-4 inhibitors can inactivate DPP-4, thereby preventing it from breaking down GLP-1. By increasing the level of GLP-1, they can control blood sugar and are currently one of the main treatment directions for diabetes.

The inhibition rates of DPP-4 by DPP-4 inhibitors (glitazones) at their respective therapeutic doses are generally similar. They all have high oral bioavailability and are not affected by food intake; they are absorbed quickly, and the peak time is usually 1 to 2 hours. Except for vildagliptin, which is administered twice a day, the other glitazones are administered once a day. Among the gliptins, only saxagliptin is mainly metabolized by CYP 3A4/A5, and the risk of drug interactions with other DPP-4 inhibitors is low. Except for linagliptin, which is excreted via the enterohepatic circulation, the rest are mainly excreted via the kidneys.

Diabetes is a common disease that has a great impact on the lives of patients and has become one of the major diseases that poses a greater threat to human health. The application of DPP-4 inhibitors brings new hope to the treatment of type 2 diabetes. With the continuous understanding of DPP-4 inhibitors, the development of new drugs with higher selectivity, safety, tolerability, long-acting and more perfect effects will be able to treat diabetes more safely and effectively, bringing health and hope to patients.