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Protease resistant insulin analogues

一种胰岛素类似物、胰岛素的技术，应用在治疗糖尿病领域，能够解决低生物利用度、侵袭性、不方便等问题

Pending Publication Date: 2009-09-23
NOVO NORDISK AS
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] Oral administration of protein drugs such as insulin often results in very low bioavailability due to enzymatic and absorption barriers
The common route of peptide and protein delivery is parenteral administration, which is invasive and inconvenient

Method used

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  • Protease resistant insulin analogues
  • Protease resistant insulin analogues

Examples

Experimental program
Comparison scheme
Effect test

Embodiment approach 1

[0022] Embodiment 1. An insulin analog in which at least two hydrophobic amino acids are substituted with hydrophilic amino acids relative to the parent insulin, wherein the substitutions are located within or in close proximity to two or more protease cleavage sites of the parent insulin proximate, and wherein such insulin analog optionally further comprises one or more insertional mutations.

Embodiment approach 2

[0023] Embodiment 2. The insulin analog of embodiment 1, wherein stability relative to parent insulin is enhanced.

Embodiment approach 3

[0024] Embodiment 3. The insulin analog of any one of embodiments 1-2, wherein the A chain of the insulin analog comprises at least one mutation and the B chain of the insulin analog comprises at least one mutation relative to the parent insulin.

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PUM

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Abstract

The present invention relates to novel insulin analogues exhibiting resistance towards protease, wherein at least two amino acids are substituted and / or deleted relative to the parent insulin molecule. A method for the preparation of such insulin analogues, insulin preparations containing the insulin analogues of the invention and a method of treating diabetes mellitus using these insulin analogues is also provided.

Description

field of invention [0001] The present invention relates to novel insulin analogs exhibiting resistance to proteases, methods of preparing such insulin analogs, methods of preparing insulin preparations containing the insulin analogs of the invention, and methods of using these insulin analogs in the treatment of diabetes. Background of the invention [0002] The oral route is by far the most widely used route of administration and is generally accepted by patients, especially for chronic treatments. However, therapeutic peptides or proteins are often limited to parenteral administration due to several barriers such as enzymatic hydrolysis in the gastrointestinal (GI) tract, drug efflux pumps, insufficient and variable absorption in the intestinal mucosa, and first-pass metabolism in the liver, Oral administration is not preferred. Human insulin is absorbed in the stomach (pepsin), in the intestinal lumen (chymotrypsin, trypsin, elastase, carboxypeptidase, etc.) and in the m...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K14/62A61K38/28C12N15/17
CPCC07K14/62A61K38/00A61P3/10A61P3/04A61P3/06A61P43/00A61P5/50
Inventor P·K·尼尔森F·休巴莱克I·劳特鲁普-拉森S·卢德维格森U·里贝尔-马德森P·巴尔施米特P·诺加尔德S·哈夫伦
Owner NOVO NORDISK AS
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