# US 2019/0169271 A1 · Use of a Long Acting GLP-1/Glucagon Receptor Dual Agonist for the Treatment of Non-Alcoholic Fatty Liver Disease

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- Number: US 2019/0169271 A1
- Document ID: US20190169271A1
- Status: Published application
- Kind: A1
- Application number: 16/267,880
- Filed: 2019-02-05
- Published: 2019-06-06
- Earliest claimed: 2014-09-16
- Assignees: Hanmi Pharm. Co., Ltd.
- Applicants: Hanmi Pharm. Co., Ltd.
- Inventors: Sang Youn Hwang; Jin Young Kim; Seung Su Kim; In Young Choi; Sung Youb Jung; Se Chang Kwon
- Web page: https://patentgrep.com/patent/US20190169271A1

## CPC

- C07K 16/00: Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies
- A61K 38/26: Glucagons
- A61K 47/60: the organic macromolecular compound being a polyoxyalkylene oligomer, polymer or dendrimer, e.g. PEG, PPG, PEO or polyglycerol
- A61K 47/6811: {the drug being a protein or peptide, e.g. transferrin or bleomycin}
- A61K 49/0008: {Screening agents using (non-human) animal models or transgenic animal models or chimeric hosts, e.g. Alzheimer disease animal model, transgenic model for heart failure}
- A61P 1/16: for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
- A61P 3/06: Antihyperlipidemics
- A61P 35/00: Antineoplastic agents
- C07K 2317/41: Glycosylation, sialylation, or fucosylation
- C07K 2317/53: Hinge
- C07K: PEPTIDES (peptides in foodstuffs A23; obtaining protein compositions for foodstuffs, working-up proteins for foodstuffs A23J; preparations for medicinal purposes A61K; peptides containing beta-lactam rings C07D; cyclic dipeptides not having in their molecule any other peptide link than those which form their ring, e.g. piperazine-2,5-diones, C07D; ergot alkaloids of the cyclic peptide type C07D519/02; macromolecular compounds having statistically distributed amino acid units in their molecules, i.e. when the preparation does not provide for a specific; but for a random sequence of the amino acid units, homopolyamides and block copolyamides derived from amino acids C08G69/00; macromolecular products derived from proteins C08H1/00; preparation of glue or gelatine C09H; single cell proteins, enzymes C12N; genetic engineering processes for obtaining peptides C12N15/00; compositions for measuring or testing processes involving enzymes C12Q; investigation or analysis of biological material G01N33/00)
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## Abstract

The present invention relates to a pharmaceutical composition for the prevention or treatment of non-alcoholic fatty liver disease including a long-acting GLP-1/glucagon receptor dual agonist, and a method for preventing or treatment of non-alcoholic fatty liver disease including administering the composition. The composition of the present invention either has no side effect of weight gain or reduces the side effect of weight gain, which is a side-effect of conventional therapeutic agents for non-alcoholic fatty liver disease, and reduces the amount of administrations of a long-acting GLP-1/glucagon receptor dual agonist, thus greatly improving patient's convenience. In addition, the long-acting GLP-1/glucagon receptor dual agonist of the present invention improves in vivo sustainability and stability.

## Claims

### Claim at position 1

1-18. (canceled)

### Claim 19

A method for preventing or treating liver inflammation in a subject, comprising administering a long-acting glucagon-like peptide-1 (GLP-1)/glucagon receptor dual agonist conjugate to the subject, wherein the subject is at high risk of or has the liver inflammation, wherein the long-acting GLP-1/glucagon receptor dual agonist conjugate comprises:
a GLP-1/glucagon receptor dual agonist comprising the amino acid sequence of any one of SEQ ID NOs: 2-23 or 27-34;
an immunoglobulin Fc region; and
a non-peptidyl polymer, wherein the non-peptidyl polymer covalently links the GLP-1/glucagon receptor dual agonist and the immunoglobulin Fc region.

### Claim 20 (depends on 19)

The method of claim 19, wherein the long-acting GLP-1/glucagon receptor dual agonist has no side effect of weight gain or reduces the side effect of weight gain.

### Claim 21 (depends on 19)

The method of claim 19, wherein the method reduces the expression or activity of tumor necrosis factor-α (TNF-α).

### Claim 22 (depends on 19)

The method of claim 19, wherein the long-acting GLP-1/glucagon receptor dual agonist simultaneously activates GLP-1 receptor and glucagon receptor.

### Claim 23 (depends on 19)

The method of claim 19, wherein the amino acids at positions 12 and 16 or 16 and 20 of the long-acting GLP-1/glucagon receptor dual agonist form a ring.

### Claim 24 (depends on 19)

The method of claim 19, wherein the non-peptidyl polymer comprises polyethylene glycol, polypropylene glycol, an ethylene glycol-propylene glycol copolymer, a polyoxyethylated polyol, polyvinyl alcohol, a polysaccharide, polyvinyl ethyl ether, a biodegradable polymer, a lipid polymer, hyaluronic acid, or a combination thereof.

### Claim 25 (depends on 24)

The method of claim 24, wherein the non-peptidyl polymer comprises polyethylene glycol.

### Claim 26 (depends on 24)

The method of claim 24, wherein the polysaccharide comprises dextran, a chitin, or a combination thereof.

### Claim 27 (depends on 19)

The method of claim 19, wherein the immunoglobulin Fc region is aglycosylated.

### Claim 28 (depends on 19)

The method of claim 19, wherein the immunoglobulin Fc region comprises a CH1 domain, CH2 domain, CH3 domain, CH4 domain, or a combination thereof.

### Claim 29 (depends on 28)

The method of claim 28, wherein the immunoglobulin Fc region further comprises a hinge region.

### Claim 30 (depends on 19)

The method of claim 19, wherein the immunoglobulin Fc region is derived from IgG, IgA, IgD, IgE, or IgM.

### Claim 31 (depends on 19)

The method of claim 19, wherein the immunoglobulin Fc region is a hybrid of domains from IgG, IgA, IgD, IgE, or IgM.