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Pharmaceutical composition comprising polypeptide

A composition and drug technology, applied in the field of pharmaceutical compositions containing polypeptides, can solve the problems of reduced yield, reduced peptide drug activity, poor reactivity, etc., and achieve the effects of promoting lipolysis, enhancing insulin secretion, and reducing side effects

Pending Publication Date: 2021-06-04
D&D PHARMATECH INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0018] However, the method using PEG has disadvantages in that PEGylation reduces the activity of peptide drugs and the yield decreases due to poor reactivity to peptides as the molecular weight of PEG increases.

Method used

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  • Pharmaceutical composition comprising polypeptide
  • Pharmaceutical composition comprising polypeptide
  • Pharmaceutical composition comprising polypeptide

Examples

Experimental program
Comparison scheme
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example 1

[0154] Polypeptide into which cysteine ​​is introduced (molecular weight: 3,509 Da; SEQ ID NO.2: H(Aib)QGTFTSDYSKYLD E QAA K EFVQWLMNTC).

[0155] Here, underlined and bold highlighted residues in the amino acid sequence of SEQ ID NO. 2 indicate that covalent loops are formed between the residues.

example 1

[0156] Preparative Example 1: Synthesis of Conjugates Comprising Polypeptides and Non-Peptide Polymers

[0157] To prepare a conjugate comprising a polypeptide and a non-peptidic polymer, a polypeptide (molecular weight: 3,509 Da; SEQ ID NO.2: H(Aib)QGTFTSDYSKYLD) with cysteine ​​introduced into the C-terminal region (at position 30) was used E QAA K EFVQWLMNTC) was used as the polypeptide.

[0158] Meanwhile, as listed in Table 2 below, maleimide-activated monomethoxy PEG (mPEG-MAL, NOF (Japan)) was used as the non-peptide polymer.

[0159] To prepare the conjugates of Examples 2 to 7, the polypeptides as listed in Table 2 below were prepared. In this case, each of the polypeptides was dissolved in dimethyl sulfoxide (DMSO), and mPEG-MAL was dissolved in 50 mM phosphate-buffered saline (pH 6).

[0160] [Table 2]

[0161]

[0162] In the amino acid sequences SEQ ID NO. 2 to 4 as listed in Table 2, the two residues underlined and highlighted in bold refer to residues with ...

experiment example 1

[0167] Experimental example 1: the measurement of the in vitro activity of example 2

[0168] In order to examine the preventive or therapeutic effect of the conjugate of Example 2 on obesity, diabetes and non-alcoholic fatty liver disease, using expression GLP-1 (glucagon derivative) receptor and glucagon receptor (GCGR ) cell line for this experiment.

[0169] To determine the activity on the GLP-1 receptor, HEK293 / CRE-Luc cells expressing the human glucagon GLP-1 receptor were purchased from GenScript and used. cells in 5x 10 4 cells / well were seeded in a 96-well plate, and the wells were then treated with: the polypeptide of Example 1 (0.001 to 300 nM), the conjugate of Example 2 (0.001 to 300 nM), native glucagon (SEQ ID NO.1: HSQGTFTS-DYSKYLDSRRAQDFVQWLMNT, 0.013 to 300 nM) and GLP-1 (SEQ ID NO. 6: HAEGTFTSDVSSYLEGQAAKEFIAWLVKGR, 0.001 to 300 nM). Thereafter, the cells in CO 2 The incubation was continued for 4 hours at a temperature of 37° C. in an incubator. Subse...

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Abstract

The present invention relates to a pharmaceutical composition including a polypeptide, and more particularly, to a pharmaceutical composition for preventing or treating obesity, diabetes, or non-alcoholic fatty liver disease. The pharmaceutical composition is safe without any side effects such as vomiting or nausea, and has effects of reducing food intake, enhancing insulin secretion, suppressing gastric emptying, promoting lipolysis, and lowering a level of triglycerides.

Description

technical field [0001] The present invention relates to a pharmaceutical composition comprising a polypeptide and its medical use eg in the treatment or prevention of obesity, diabetes or non-alcoholic fatty liver disease. Peptides have the effect of reducing food intake, enhancing insulin secretion, inhibiting gastric emptying, promoting lipolysis, and lowering triglyceride levels without side effects such as vomiting or nausea. Background technique [0002] Recently, with the development of the economy and the rapid growth of science and technology, the aging population is increasing and adult diseases are rapidly increasing. This is due to stress, poor eating habits, excess calorie intake and decreased physical activity. As complications accompanying obesity, heart disease and cerebrovascular disease rank first and second in terms of mortality, and obesity is considered to be a cause of various adult diseases such as diabetes and nonalcoholic fatty liver disease. [000...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K38/16A61K47/60A61P1/16A61P3/04A61P3/10
CPCA61P3/10A61P1/16A61K47/60A61P3/04A61K38/00C07K14/605A61K47/6941
Inventor K·C·李O·Y·朴H·T·安E·J·朴J·H·申S·M·林
Owner D&D PHARMATECH INC
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