B&l Delipharm, Corp.

Theraly Pharmaceuticals, Inc.

Su Young Chae

Kang Choon Lee

Yu Seok Youn

Chan Woong Park

Sung Kwon Lee

Won Bae Kim

Cheng Hao Jin

Disclosed herein are an N-terminal modified PEG-TRAIL conjugate and a preparation method and use thereof. The PEG-TAIL conjugate has pharmaceutical activity identical or similar to that of native TRAIL (TNF-related apoptosis-inducing ligand) with extended in vivo half-life and enhanced stability. Compared to native TRAIL, the PEG-TAIL conjugate exhibits high solubility and solution stability, with highly improved pharmacokinetic profiles. Thus, the PEG-TAIL conjugate may be very useful for preventing and treating proliferative diseases and autoimmune diseases.

N-terminal modified PEG-TRAIL

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.

Exendin polypeptide linked to biotin, method for the preparation thereof and pharmaceutical composition comprising the same

Disclosed herein are exendin singly modified with polyethylene glycole or a derivative thereof, a method for the preparation of the same, and uses thereof. Exendin modified at lysine (27) with polyethylene glycol shows biological activity similar to that of natural exendin, but is improved in half life. In addition, the modification position and the number of PEG or its derivative are restricted so as to minimize the side effects caused by a variety of combinations of such factors. The exendin is useful in the prevention and treatment of diseases caused by the over-secretion of insulin, or diseases caused due to a decrease in plasma glucose level, the inhibition of gastric or intestinal motility, the promotion of satiety, or the inhibition of food intake, especially diabetes, obesity and irritable colon syndrome.

Mono modified exendin with polyethylene glycol or its derivatives and uses thereof

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Gwangju, South Korea

Su Young Chae