What Is Vildagliptin?

The chemical formula of vildagliptin is (-)-(2S) -1-[[(3-hydroxytricyclo [3.3.1.1 [3,7]] silane-1-yl) amino] acetyl] Pyrrolidine-2-carbonitrile, a clinical drug is another dipeptidyl peptidase-IV (DPP-IV) inhibitor after oral administration of sitagliptin. It is limited by Novartis Pharmaceuticals. The company was approved for listing in the European Union in 2008 for the treatment of type 2 diabetes.

Vigliptin

The chemical formula of vildagliptin is (-)-(2S) -1-[[(3-hydroxytricyclo [3.3.1.1 [3,7]] silane-1-yl) amino] acetyl] Pyrrolidine-2-carbonitrile, a clinical drug is another dipeptidyl peptidase-IV (DPP-IV) inhibitor after oral administration of sitagliptin. It is limited by Novartis Pharmaceuticals. The company was approved for listing in the European Union in 2008 for the treatment of type 2 diabetes.

Chinese name

Vigliptin

Foreign name

vildagliptin

Molecular weight

303.4

Molecular formula

C17H25N3O2

CAS number

274901-16-5

^[3]

Vigliptin is a selective, competitive, and reversible DPP24 inhibitor. Glucose-dependent insulinotropic polypeptide (GIP) and glucagon-like polypeptide 1 (GLP-1) are important hormones to maintain glucose concentration in the body, and both have intestinal insulinotropic effects. GIP's insulin secretion-promoting effect is impaired in type 2 diabetes patients. Only GLP-1 can exert islet-promoting hormone secretion. It promotes insulin secretion by acting on receptors on the islet -cell membrane. GLP-1 also inhibits glucagon secretion and suppresses gastric emptying to increase satiety (inhibit appetite). DPP24 binds to proteins and exists in many tissues, such as the brush border of kidney, liver, and small intestinal membranes, pancreatic ducts, lymphocytes, and endothelial cells. It can rapidly make GLP-1 by hydrolyzing the second N-terminal alanine of GLP-1. Inactivated. This product inhibits the activity of the enzyme by combining with DPP24 to form a DPP24 complex. While increasing the concentration of GLP-1, promoting islet cells to produce insulin, it also reduces the concentration of glucagon, thereby lowering blood glucose. No significant effect on body weight. ^[4-5]

Pharmacokinetic studies of healthy humans show that this product is rapidly absorbed after oral administration, with an absorption rate of 85%, a protein binding rate of 4% to 17%, and a _Tmax of 1 to 2 hours. When the dosage is 25 200mg, the blood concentration is linear with the dosage. The t _1/2 is 1.5 4.5 h. When administered in a single dose of 25 to 200 mg, the inhibition rate of DPP-IV in plasma can reach more than 90% within 30 to 60 minutes, but the duration of the inhibition is related to the dose. When the dose is 50 and 100 mg, The 12-hour inhibition rate of DPP-IV was 70% and 90%, while the 24-hour inhibition rate of DPP-IV in the 100 mg group was 40%. This product is mainly (55%) metabolized by hydrolyzing cyano groups. In addition, 22% of the drug is excreted by the kidney as the original drug, and a small part of the drug is metabolized by the cytochrome P450 enzyme. However, this product is neither an inhibitor of this enzyme nor Not an inducer. Drug accumulation did not occur when multiple doses were administered, patients with liver and kidney dysfunction did not need to adjust the dose, and pharmacokinetic results were not affected by food. ^[6]

1. The most common adverse reactions were headache, nasopharyngitis, cough, constipation, dizziness, and sweating. Very few patients have symptoms of hypertension, but the relationship with this drug is uncertain. Almost all studies have confirmed that the incidence of hypoglycemia with vitagliptin is similar to that with placebo.

2. Control experiments found that compared with thiazolidinediones, the incidence of adverse reactions such as headache and rash was similar in patients who used vitagliptin. The Ting group was low. ^[2]

   Colleen et al.

   In summary, vitagliptin has the effect of reducing fasting and postprandial blood glucose levels, postprandial glucagon secretion, and improving B cell function, providing a new option for the treatment of patients with type 2 diabetes. The safety and effectiveness of this drug in combination with other drugs, contraindications, and adverse reactions need to be observed in more clinical studies.