A pharmaceutical composition for treating obesity-related disease comprising insulinotropic peptide conjugate

An insulin-stimulating and peptide-releasing technology, which is applied in drug combinations, active ingredients of artificially synthesized polymer materials, and metabolic diseases, can solve problems such as unrevealed efficacy and patient difficulties, and achieve the effects of inhibiting food intake and reducing body fat

Active Publication Date: 2010-11-03
HANMI SCI CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

For the treatment of chronic diseases such as obesity, patients need to inject the drug multiple times a day, which is still difficult for patients
Furthermore, the exendin derivatives described in said patent exhibit different potencies, dose-dependence and duration in individuals, and do not show superior potency over native exendin in inhibiting food intake

Method used

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  • A pharmaceutical composition for treating obesity-related disease comprising insulinotropic peptide conjugate
  • A pharmaceutical composition for treating obesity-related disease comprising insulinotropic peptide conjugate
  • A pharmaceutical composition for treating obesity-related disease comprising insulinotropic peptide conjugate

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0048] Example 1: Preparation of insulin-releasing peptide conjugate (CA-Exendin)

[0049] 3.4K PropionALD(2) PEG (PEG with two propionaldehyde groups, IDB Inc., Korea) and lysine residues of imidazo-acetyl Exendin-4 (Bachem, Swiss) were pegylated ( pegylation) by reacting the peptide with PEG at a molar ratio of 1:15 at 4°C overnight at a peptide concentration of 5 mg / ml. During this time, the reaction was carried out in a pH 7.5 buffer, to which 20 mM SCB (NaCNBH 3 ) for the reaction. Mono-PEGylated exendin and isomers were separated using SOURCE S (XK 16ml, Amersham Biosciences) under the following conditions.

[0050] Column: SOURCE S (XK 16ml, Amersham Biosciences)

[0051] Flow rate: 2.0ml / min

[0052] Gradient: A 0→100% 45 minutes B (A: 20mM citric acid pH 3.0; B: A+0.5MKCl)

[0053] The isolated mono-PEGylated CA-Exendin-4 was bound to immunoglobulin Fc. The reaction was carried out at a ratio of peptide:immunoglobulin Fc = 1:4 at 4°C for 16 hours wi...

Embodiment 2

[0060] Example 2: Weight loss effect of insulinotropic peptide conjugates in ob / ob mice

[0061] The well-known obesity animal model ob / ob mice (C57BL / 6JHamSlc-ob / bo, female, 8-9 weeks old) were divided into 4 groups (5 mice in each group), and then the vehicle and Byetta (Amylin- Lily, exendin-4, 45 μg / kg, subcutaneous injection every day) and the insulinotropic peptide conjugate prepared in Example 1 (45 μg or 100 μg / kg, subcutaneous injection once a week). Then, 28-day body weight changes were measured, and blood lipid metabolism parameters such as cholesterol and free fatty acid levels were measured after the administration was completed. After completion of the examination, the liver and adipose tissue were excised and weighed. The weight reducing effect of insulinotropic peptide conjugates in ob / ob mice is shown in Table 1.

[0062] Table 1

[0063]

[0064] as table 1 and figure 1 and figure 2As shown, the insulinotropic peptide conjugate showed the...

Embodiment 3

[0065] Example 3: Weight loss effect of insulinotropic peptide conjugates in DIO mice

[0066] The well-known obesity animal model DIO (diet-induced obesity) mouse mice (C57BL / 6NcrjBgi, male, 25 weeks old) were divided into 5 groups (5 mice per group), and then administered with vehicle and Byetta (100 μg / kg, injected subcutaneously every day) and the insulinotropic peptide conjugate prepared in Example 1 (20, 50, 100 μg / kg, injected subcutaneously once a week). Then, the body weight change in 2 weeks was measured. The body weight reducing effect of insulinotropic peptide conjugates in DIO mice is shown in Table 2.

[0067] Table 2

[0068]

[0069] as table 2 and image 3 As shown, the insulinotropic peptide conjugate showed a better weight loss effect than Byetta at 1 / 17.5 dose, and the effect was dose-dependent. In addition, weekly administration of the insulinotropic peptide conjugate maintains efficacy longer than daily administration of exendin-4.

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Abstract

The present invention relates to a composition for treating obesity-related diseases comprising an insulinotropic peptide conjugate, more particularly, to a composition for treating obesity-related diseases comprising a conjugate prepared by covalently linking the insulinotropic peptide with a carrier substance via a non-peptidyl linker, and a method for treating obesity-related diseases by using the same. In particular, the composition for treating obesity-related diseases according to the present invention remarkably improves the efficacy of suppressing food intake and its duration to reduce body weight and body fat, thereby being useful for the treatment of obesity-related diseases.

Description

technical field [0001] The present invention relates to a composition for treating obesity-related diseases comprising an insulin-stimulating peptide conjugate, in particular to a combination for treating obesity-related diseases comprising a conjugate prepared by covalently linking insulin-stimulating peptide and a carrier substance through a non-peptidyl linker Compositions, and methods of using the compositions to treat obesity-related diseases. Background technique [0002] Obesity is a chronic disease associated with high morbidity and mortality, resulting from the accumulation of adipose tissue due to energy imbalance or overnutrition. Obesity and obesity-related diseases are serious health problems in the United States and around the world. Over the past 7 years, the prevalence of obesity has increased from 22.9% to 30.6% in the general population of the United States. According to the results of the 1999-2002 National Health and Nutrition Examination Survey (NHANES...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K38/16A61P3/04A61K39/395
CPCA61K47/48369A61K38/22A61K38/2207A61K31/365A61K38/26A61K31/137A61K47/6889A61K47/6811A61K47/6835A61P1/00A61P1/16A61P3/00A61P3/04A61P3/06A61P5/50A61P9/00A61P3/10A61K2300/00A61K38/16A61K31/74
Inventor 宋大海金玫永朴永振姜殷姬郑圣烨权世昌李宽淳
Owner HANMI SCI CO LTD
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