COMPOSITION COMPRISING A GLP-1 RECEPTOR AGONIST AND A GLUCAGON RECEPTOR AGONIST, AND USE THEREOF Russian patent published in 2020 - IPC A61K38/17 A61K38/26 A61K45/06 A61K47/60 A61P1/16 A61P3/04 A61P3/06 A61P3/10 

Abstract RU 2719144 C2

FIELD: medicine; pharmaceuticals.

SUBSTANCE: what is offered is a pharmaceutical composition for preventing or treating non-alcoholic fatty liver disease, losing weight, reducing blood sugar, reducing lipids, inhibiting appetite in a subject, reducing the total serum cholesterol level and/or reducing the triglyceride content in the liver, its version, the composition and use of said compositions. Said pharmaceutical composition contains a pharmaceutically effective amount of a GLP-1 receptor agonist and a glucagon receptor agonist. GLP-1 receptor agonist and the glucagon receptor agonist each independently form a conjugate with a hydrophilic polymer, a molar ratio of the conjugate, including a GLP-1 receptor agonist, to a conjugate comprising a glucagon receptor agonist ranges from 1:1 to 1:15. In the above composition, the GLP-1 receptor agonist is selected from exendin-4, exendin-3 and GLP-1, and the glucagon receptor agonist is glucagon and the hydrophilic polymer is polyethylene glycol. Variant of the pharmaceutical composition comprises an agent selected from a group consisting of: a combination of PB-721 and PB-119, a combination of PB-722 and PB-119 and a combination of PB-708 and PB-120, where PB-721 is mPEG-23KD-ppMAL-PB-740, where PB-740 has an amino acid sequence SEQ ID NO: 5; PB-722 is mPEG-23KD-ppMAL-PB-741, where PB-741 has the amino acid sequence SEQ ID NO: 6, in which the "-CO-NH2" side chain of glutamine in 24 position is modified in "-CO-NH-CH2CH2-SH"; PB-119 is mPEG-23KD-ppMAL-PB-105, where PB-105 has the amino acid sequence SEQ ID NO: 1; PB-120 is mPEG-25KD-ppMAL-PB-105, where PB-105 has the amino acid sequence SEQ ID NO: 1; and PB-708 is mPEG-25KD-ppMAL-PB-703, where PB-703 has the amino acid sequence SEQ ID NO: 4. What is also presented is a kit for preventing or treating non-alcoholic fatty liver disease, losing weight, reducing blood sugar, lowering lipids, inhibiting appetite in the individual, reducing total serum cholesterol and/or reducing triglycerides in the liver, comprising the composition.

EFFECT: composition and variant thereof can be used for preparing a drug for preventing or treating non-alcoholic fatty liver disease, losing weight, reducing lipids and/or reducing blood sugar, as well as for preparing a drug for suppressing appetite in a subject, reducing the level of total cholesterol in the serum and/or reducing the content of triglycerides in the liver.

11 cl, 40 dwg, 3 tbl, 21 ex

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RU 2 719 144 C2

Authors

Syuj Min

Lv Vej

Chzhan Inkhoj

Lo Syaosu

Dates

2020-04-17Published

2016-12-28Filed