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Pharmaceutical composition comprising insulin and triple agonist having activity with respect to all of glucagon and glp-1 and gip receptor

A technology of glucagon and GLP-1, applied in the field of compound preparations, can solve the problems of combined use of combination preparations, etc., and achieve the effect of reducing side effects

Pending Publication Date: 2021-09-28
HANMI PHARMA
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, these have not been combined as combination preparations

Method used

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  • Pharmaceutical composition comprising insulin and triple agonist having activity with respect to all of glucagon and glp-1 and gip receptor
  • Pharmaceutical composition comprising insulin and triple agonist having activity with respect to all of glucagon and glp-1 and gip receptor
  • Pharmaceutical composition comprising insulin and triple agonist having activity with respect to all of glucagon and glp-1 and gip receptor

Examples

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example 1

[0693] Example 1: Preparation of triple agonists and long-acting conjugates thereof

[0694] (1) Preparation of triple agonist

[0695] Triple agonists exhibiting activity at all of the glucagon, GLP-1 and GIP receptors were prepared and their sequences are shown in Table 1 below.

[0696] Table 1

[0697]

[0698]

[0699]

[0700]

[0701] In the sequences shown in Table 1, amino acids marked with X represent aminoisobutyric acid (Aib), which is an unnatural amino acid, and underlined amino acids represent amino acids that form a loop together. In Table 1, CA represents 4-imidazole acetyl, and Y represents tyrosine.

[0702] (2) Preparation of triple agonist long-acting conjugates

[0703] In order to make 10kDa PEG with maleimide group and aldehyde group at its two ends, namely maleimide-PEG-aldehyde (10kDa, NOF, Japan) and triple agonist (SEQ ID NO:21 , 22, 42, 43, 50, 77 and 96) cysteine ​​residues PEGylated such that the triple agonist and maleimide-PEG...

example 2

[0713] Example 2: Preparation of native insulin long-acting conjugates

[0714] To pegylate 3.4K propion-ALD(2)PEG (3.4kDa PEG with one propionaldehyde group at each end, NOF, Japan) at the N-terminus of the B-chain of human native insulin (India, Biocon), natural Insulin and PEG were reacted at 25°C for 2 hours at a molar ratio of 1:4, where the native insulin concentration was 5 mg / mL. By adding 3 mM sodium cyanoborohydride (NaCNBH) as a reducing agent to a mixed solvent of 50 mM sodium citrate buffer (pH5. 3 ) to react. The reaction solution was purified using a SP-HP (GE Healthcare) column using a buffer containing sodium citrate (pH 3.0) and 45% EtOH and a KCl concentration gradient.

[0715] Next, in order to attach native insulin-linked PEG to the N-terminus of the immunoglobulin Fc fragment, the purified mono-PEGylated insulin and the immunoglobulin Fc fragment were reacted at a molar ratio of 1:1.2 at 25°C for 15 hours, At the same time, the total protein concent...

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Abstract

The present invention relates to a composition comprising insulin and a triple agonist having activity with respect to all of a glucagon receptor, GLP-1 receptor, and GIP receptor, and to a composite preparation comprising the composition.

Description

technical field [0001] The present invention relates to a composition containing insulin and a triple agonist active on glucagon, GLP-1 and GIP receptors and a composite preparation containing the composition. Background technique [0002] Insulin is a blood sugar-controlling hormone secreted by the human pancreas to transport excess glucose in the blood to the cells, thereby supplying the cells with an energy source and maintaining blood sugar levels within the normal range. However, in diabetics, insulin does not work properly due to insulin deficiency, insulin resistance and loss of beta-cell function. As a result, diabetic patients cannot utilize glucose in the blood as an energy source, and exhibit symptoms of hyperglycemia in which the blood sugar level is high, resulting in excretion of glucose in urine, which causes various complications. Therefore, diabetic patients with abnormal insulin production (type I) or insulin resistance (type II) require insulin therapy, a...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K38/28A61K38/22A61K47/68A61K47/60A61P3/10C07K14/62C07K14/605C07K14/575
CPCA61K38/28A61K47/60A61P3/10A61K47/68A61K38/26A61K2300/00A61K47/6811A61P3/04C07K14/62C07K14/605
Inventor 李钟锡金正国李相炖李钟守金尚允
Owner HANMI PHARMA
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