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Glucagon secretion: For patients with type 2 diabetes, exenatide can reduce glucagon secretion during hyperglycemia, reduce serum glucagon concentrations, reduce hepatic glucose output, and reduce insulin requirements. However, exenatide injection does not impair the normal glucagon response to hypoglycemia.

Gastric emptying: Exenatide injection can slow gastric emptying, thereby slowing the rate at which glucose from food enters the circulation.

Food intake: Administration of exenatide can reduce food intake in animals and humans.

Toxicology

A 104-week carcinogenicity study was conducted in male and female rats with subcutaneous rapid injection of 18, 70, and 250 µg/kg/day. Benign thyroid C-cell adenomas were observed in female rats in all exenatide dose groups. The incidence in female rats in the two control groups was 8% and 5%, and in the low, medium, and high dose groups was 14%, 11%, and 23%. According to the area under the curve (AUC), the systemic exposure of the low, medium and high dose groups is equivalent to 5, 22 and 130 times the exposure of the maximum recommended human dose of 20µg/day, respectively.

In the 104-week carcinogenicity study of mice with subcutaneous rapid injection of 18, 70 and 250µg/kg/day, no evidence of tumors was observed at a dose of 250µg/kg/day. According to AUC, the systemic exposure of this dose is equivalent to 95 times the exposure of the maximum recommended human dose of 20µg/day.

The results of the Ames bacterial mutagenicity test or the chromosome aberration test conducted with Chinese hamster ovary cells showed that exenatide was not mutagenic or teratogenic, whether with or without metabolic activation. The micronucleus test results of exenatide in mice were negative.