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Glp-1-fc fusion protein formulation

A fusion protein and glp-1-fc technology, applied in peptide/protein components, drug combinations, medical preparations of non-active ingredients, etc., can solve problems such as unsuitable preparations

Inactive Publication Date: 2010-06-09
ELI LILLY & CO
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] In addition, the preparation may not be suitable if it is physically unstable when there is instability caused by host cell proteases under examination

Method used

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  • Glp-1-fc fusion protein formulation
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  • Glp-1-fc fusion protein formulation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment

[0026] In vitro GLP-1 receptor activation assay

[0027] Using the CRE-luciferase system, HEK-293 cells stably expressing the human GLP-1 receptor were seeded in 96-well plates at 30,000 cells / well / 80 μL DMEM F12 medium with low serum. One day after seeding, 20 [mu]L aliquots of test proteins dissolved in 0.5% BSA were mixed with cells and incubated for 5 hours. For each test protein, 12 dilutions containing 3pM to 3nM were prepared typically at a 5X concentration and added to the cells to generate a dose response curve from which the EC was determined. 50 value. After incubation, 100 μL of luciferase reagent was added directly to each plate and mixed gently for 2 minutes. The plate was placed in a Tri-lux luminometer and the light output due to luciferase expression was calculated.

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Abstract

The invention provides a stable solution formulation comprising a therapeutically effective amount of a GLP-1-Fc fusion protein at about pH 6.5 in citrate buffer with polysorbate-80 and mannitol. The formulation is useful in treating diabetes and obesity as well as a variety of other conditions or disorders.

Description

field of invention [0001] The present invention relates to commercially available formulations of glucagon-like peptide analogs fused to the Fc portion of an immunoglobulin. The formulation can be used to treat diabetes and obesity, as well as a variety of other conditions or disorders. Background of the invention [0002] Glucagon-like peptide-1 (GLP-1) analogs and derivatives are promising in clinical trials for the treatment of type 2 diabetes. GLP-1 induces various biological effects such as stimulation of insulin secretion, inhibition of glucagon secretion, inhibition of gastric emptying, inhibition of gastric or intestinal motility, and induction of weight loss. A distinctive feature of GLP-1 is its ability to stimulate insulin secretion without the associated risks of hypoglycemia seen with insulin therapy or certain types of oral therapy that act by increasing insulin expression. [0003] GLP-1(1-37) activity is very low, and GLP-1(7-37)OH and GLP-1(7-36)NH 2 The ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/08A61K47/26A61K38/26
CPCA61K9/0019A61K47/26A61K47/18A61K38/26A61K47/12A61P3/10A61P3/04
Inventor K·额
Owner ELI LILLY & CO
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