Saxagliptin A Highly Potent Dipeptidyl Peptidase - 4 Inhibitor

Saxagliptin is a highly potent dipeptidyl peptidase-4 inhibitor that selectively increases the levels of endogenous glucagon-like peptide-1 and glucose-dependent insulin-releasing peptides by selectively inhibiting DPP-4, Thereby regulating blood sugar.

Data show that the world's current nearly 290 million people suffering from diabetes, including type 2 diabetes accounted for 90% to 95%. If you do not prevent the spread of diabetes, the world's diabetes population will reach 440 million by 2030, diabetes has become the world's fourth largest cause of death. In 1932, the researchers found that the body naturally secreted by the intestinal pigment, which is fed by the small intestine endocrine cells in the secretion of hormones, by stimulating insulin secretion of pancreatic β cells to lower blood sugar. Chinese Ministry of Health diabetes counseling and cardiovascular disease prevention and control center expert committee of experts, general manager of the PLA General Hospital Pan Changyu said, and other simple promotion of insulin secretion of drugs, intestinal trypsin hypoglycemic agents because of its role is glucose-dependent , That is, only in the blood sugar when the "command" to produce insulin, so it has a protective effect on islet β cell function. A number of international studies have shown that pancreatic pancreatitis can not only promote insulin secretion of pancreatic β cells, lower blood sugar, but also reduce the apoptosis of β cells, thereby delaying the disease process, is expected to fundamentally curb the process of type 2 diabetes. Pancreatic trypsin unique hypoglycemic mechanism, accelerated the development of new drugs of diabetes. There are two types of drugs based on the mechanism of pancreatic and pancreatic action, but the mechanism of action is not exactly the same. A class of pancreatic trypsins supplemented with exogenous parenteral suppositories to enhance pancreatic pancreatitis in diabetic patients to stimulate beta cells to secrete insulin, known as exogenous enterotoxin. The other is the DPP-4 (dipeptidyl peptidase) inhibitor, called endogenous enterotoxin, represented by sagreline. DPP-4 inhibitor is by extending the role of the patient's own intestinal trypsin to achieve the purpose of hypoglycemic, and its side effects are very small, easy medication. Well-known large international research UKPDS data show that patients diagnosed with diabetes, the function of islet β cells has been lost in half. Professor Yang Wenying, vice president of the Asian Diabetes Association, pointed out that the long-term effective control of hyperglycemia is an important reason is that the existing treatment program is not yet effective and effective protection of human pancreatic β cells. Studies have shown that endogenous intestinal trypsin in the sustained hypoglycemic at the same time, can significantly improve pancreatic β-cell function. On the eve of the 2010 World Diabetes Day, Bristol-Myers Squibb and the United States AstraZeneca jointly announced that the world's first by the two global pharmaceutical companies jointly developed based on the mechanism of intestinal trypsin hypoglycemic drug sand Glentin has been approved by 46 countries, including the United States, India and the European Union, where China is still in the pre-IPO approval stage.

Use of saxagliptin

Oral, recommended dose 5mg once a day, medication time is not affected by the meal. Renal insufficiency patients: patients with mild renal insufficiency do not need to adjust the dose. Patients with moderate to severe renal insufficiency have limited experience in clinical studies and are not recommended for use in such patients. (See note and pharmacokinetics). Impaired liver function: mild to moderate liver damage. Ignorance No need to adjust the dose (see pharmacokinetics). This product is used for moderate liver damage caused by ignorance to be cautious, not recommended for patients with severe liver damage (see note). Potent Cytochrome P450 3A4 / 5 (CYP3A4 / 5) Inhibitors: potions with potent CYP3A4 / 5 inhibitors (eg ketoconazole, atazanavir, clarithromycin, itraconazole, nefazodone, Fenavir, ritonavir, saquinavir and telamycin) should be limited to 2.5mg / day.