Abstract: Disclosed are exendin-3 or exendin-4 derivatives modified with biotin, a preparation method thereof and a pharmaceutical composition containing the same. More specifically, disclosed are exendin-3 or exendin-4 derivatives in which the lysine residue of exedin is modified with biotin. The disclosed exendin-3 or exendin-4 derivatives modified with biotin show biological activity similar to that of native exendin and at the same time, have increased in vivo stability and are easily absorbed through the mucosa. Thus, biotin-modified exendin-3 or exendin-4 derivatives are useful for treating diseases, which can be caused by the excessive secretion of insulin, the lowering of plasma glucose, the inhibition of gastric or intestinal motility, the inhibition of gastric or intestinal emptying or the inhibition of food intake. Particularly, the biotin-modified exendin-3 or exendin-4 derivatives are useful for the treatment of diabetes, obesity and irritable bowel syndromes.

Abstract: Disclosed are exendin-3 or exendin-4 derivatives modified with biotin, a preparation method thereof and a pharmaceutical composition containing the same. More specifically, disclosed are exendin-3 or exendin-4 derivatives in which the lysine residue of exedin is modified with biotin. The disclosed exendin-3 or exendin-4 derivatives modified with biotin show biological activity similar to that of native exendin and at the same time, have increased in vivo stability and are easily absorbed through the mucosa. Thus, biotin-modified exendin-3 or exendin-4 derivatives are useful for treating diseases, which can be caused by the excessive secretion of insulin, the lowering of plasma glucose, the inhibition of gastric or intestinal motility, the inhibition of gastric or intestinal emptying or the inhibition of food intake. Particularly, the biotin-modified exendin-3 or exendin-4 derivatives are useful for the treatment of diabetes, obesity and irritable bowel syndromes.