1. Pharmacology and Toxicology

2. Pharmacodynamic effect

3. Toxicity study

4. Treatment characteristics

5. Pharmacology and Toxicology

pharmacological action

Liraglutide is a GLP-1 analogue, which has 97% sequence homology with human GLP-1. Human GLP-1 can bind and activate GLP-1 receptor. GLP-1 receptor is the target of natural GLP-1. GLP-1 is an endogenous incretin hormone, which can promote the glucose concentration dependent secretion of insulin by pancreatic β cells. Different from Daran GLP-1, the pharmacokinetics and pharmacokinetic characteristics ofLiraglutide in human body are suitable for once a day administration. After subcutaneous injection, the mechanism of prolonging the action time includes: the self-linking effect of slowing absorption; binding with albumin; higher enzyme stability for DPP-IV and nep, thus having longer plasma half-life.

The activity of Liraglutide is mediated by its specific interaction with GLP-1 receptor, which leads to the increase of camp. Liraglutide can stimulate insulin secretion in a glucose concentration dependent mode, while reducing excessive pancreas in a glucose concentration dependent mode

The secretion of high glycogen. Therefore, when blood glucose increases, insulin secretion is stimulated and glucagon secretion is inhibited. In contrast, in hypoglycemia, Liraglutide can reduce insulin secretion without affecting glucagon secretion. The hypoglycemic mechanism of Liraglutide also includes slightly prolonging gastric emptying time. Liraglutide can reduce weight and body fat by reducing hunger and energy intake.

2. Pharmacodynamic effect

The effect of Liraglutidelasts for 24 hours, which can improve blood glucose control by reducing fasting and postprandial blood glucose in patients with type 2 diabetes.

In patients with type 2 diabetes, a single administration ofLiraglutide observed an increase in insulin secretion in a glucose concentration dependent pattern (Figure 4).

Fig. 4 after receiving 7.5 UG / kg (about 0.7mg) ofLiraglutide or placebo, the patients with type 2 diabetes (n = 10) were delivered step by step

Mean insulin secretion rate (ISR) and glucose concentration during increased glucose infusion

3. Toxicity study

Genotoxicity: according to genotoxicity research data, there is no special harm to human body caused by Liraglutide.

Reproductive toxicity: animal studies have not shown thatLiraglutide has a direct harmful effect on fertility, but at the highest dose it slightly increases early embryo mortality. In the second trimester, the administration of Liraglutide can lead to weight loss of the mother animal and slow growth of the fetus

With the unknown meaning of the rat ribs and rabbit bone variation. The growth of newborn rats slowed down after receiving Liraglutide, and this effect still existed in the high dose group after weaning. It is not clear that the growth retardation of newborn mice is caused by the direct GLP-1 effect

The decrease of milk quantity or the decrease of milk production due to the decrease of caloric intake.

Carcinogenicity: non lethal thyroid C-cell tumor was observed in two-year carcinogenicity test in rats and mice. In rats, NOAEL was not observed. These tumors were not observed in monkeys after 20 months of administration. Gnawing

These findings in rodents are due to a non genotoxic, GLP-1 receptor-mediated specific action, which is particularly sensitive in rodents. The correlation between this effect and human body may be low, but it can not be completely excluded. No other drug-related tumors were found.

4. Treatment characteristics

Intelligent hypoglycemic

The advantages of Novolin & reg; compared with traditional oral hypoglycemic drugs and insulin are reflected in its hypoglycemic mechanism: GLP-1 is a polypeptide synthesized by intestinal cells, which can adjust insulin secretion "on demand" according to the level of glucose in the body, just like a "switch" is installed for the pancreas. When the blood sugar in the body is too high, it will "turn on" this switch to release insulin; when the blood sugar reaches the normal range, it will "turn off" the switch to keep the blood sugar in a stable range and minimize the risk of hypoglycemia.

Protect β cell

The main advantages of Novolin & reg; are also reflected in its function of protecting islet β cells. The gradual failure of β cell function is the "culprit" for the continuous progress of diabetes. The existing oral antidiabetic drugs do not have the function of protecting β cell, which can not prevent the further development of diabetes. Lead studies in more than 4000 diabetic patients in more than 40 countries around the world have shown that Novolin & reg; can improve the quantity and quality of β cell insulin secretion, so it may delay the development of diabetes.

Only once a day

In addition to its excellent performance in lowering blood sugar, reducing hypoglycemic events, and protecting beta cell function, Novelli & reg; can also reduce weight. At the same time, because it can reduce systolic blood pressure, it also plays an advantage in reducing the risk of cardiovascular disease. This undoubtedly brings unexpected "surprises" to type 2 diabetes patients. In addition, Novelli & reg; provides the maximum flexibility of treatment, which only needs to be administered once a day, and can be administered at any time of the day, not limited by the dining time, so as to maximize the convenience of patients' medication.

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Chengdu Shengnuo Biotechnology Co., Ltd. has "Chengdu polypeptide drug engineering technology research center" in Chengdu, mainly engaged in polypeptide, polypeptide drug and beauty peptide research. Our zero defect has passed the FDA certification, and now it has become the first-class professional peptide drug and product development, technology transfer, technical service and peptide drug industry in the scale production and export of China's parks.