# US 10,765,737 B2 · Methods for treating heart failure using glucagon receptor antagonistic antibodies

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- Number: US 10,765,737 B2
- Document ID: US10765737B2
- Status: Granted
- Kind: B2
- Application number: 15/757,352
- Filed: 2016-09-02
- Published: 2018-09-13
- Granted: 2020-09-08
- Earliest claimed: 2015-09-04
- Assignees: REMD Biotherapeutics, Inc.
- Applicants: REMD Biotherapeutics, Inc.
- Inventors: Hai Yan
- Web page: https://patentgrep.com/patent/US10765737B2

## CPC

- A61K 39/39533: {against materials from animals}
- A61K 9/0019: {Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner (non-active ingredients are additionally classified in A61K47/00)}
- A61K 38/26: Glucagons
- A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
- A61P 9/10: for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
- C07K 16/2869: {against hormone receptors (for antibodies against neuromediator receptors C07K16/286)}
- A61K 36/68: Plantaginaceae (Plantain Family)
- A61K 2039/505: {comprising antibodies}
- A61K 2039/57: {characterised by the type of response, e.g. Th1, Th2}
- C07K 2317/21: from primates, e.g. man
- C07K 2317/76: Antagonist effect on antigen, e.g. neutralization or inhibition of binding
- 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
- 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)

## Abstract

The present disclosure relates to methods for treating or preventing heart failure using a glucagon receptor blocking agent. In various embodiments, the present disclosure relates to methods for treating or preventing heart failure (e.g., post-myocardial infarction heart failure), diabetic cardiomyopathy heart failure), and lateral ventricular (LV) remodeling, using antigen binding and antagonizing proteins, e.g., fully human antibodies, that specifically bind to and antagonize the function of the human glucagon receptor.

## Claims

### Claim 1

A method for treating heart failure in a subject in need thereof comprising administering to the subject a therapeutically effective amount of an isolated antagonistic antigen binding protein that specifically binds to the human glucagon receptor (GCGR), wherein the antagonistic antigen binding protein is a human anti-GCGR antibody which comprises the amino acid sequence encoding the heavy chain of SEQ ID NO: 51 and the amino acid sequence encoding the light chain of SEQ ID NO: 52.

### Claim 2 (depends on 1)

A method according to claim 1, wherein the heart failure to be treated is selected from the group consisting of post-myocardial infarction heart failure and diabetic cardiomyopathy heart failure.

### Claim 3 (depends on 2)

A method according to claim 2, wherein the heart failure to be treated is post-myocardial infarction heart failure.

### Claim 4 (depends on 2)

A method according to claim 2, wherein the heart failure to be treated is diabetic cardiomyopathy heart failure.

### Claim 5 (depends on 1)

A method according to claim 1, wherein the therapeutically effective amount of the isolated antagonistic antigen binding protein is selected from: 0.001 to 100 mg/kg, 0.001 to 90 mg/kg, 0.001 to 80 mg/kg, 0.001 to 70 mg/kg, 0.001 to 60 mg/kg, 0.001 to 50 mg/kg, 0.001 to 40 mg/kg, 0.001 to 30 mg/kg, 0.001 to 20 mg/kg, 0.001 to 10 mg/kg, 0.001 to 5 mg/kg, 0.001 to 4 mg/kg, 0.001 to 3 mg/kg, 0.001 to 2 mg/kg, 0.001 to 1 mg/kg, 0.010 to 50 mg/kg, 0.010 to 40 mg/kg, 0.010 to 30 mg/kg, 0.010 to 20 mg/kg, 0.010 to 10 mg/kg, 0.010 to 5 mg/kg, 0.010 to 4 mg/kg, 0.010 to 3 mg/kg, 0.010 to 2 mg/kg, 0.010 to 1 mg/kg, 0.1 to 50 mg/kg, 0.1 to 40 mg/kg, 0.1 to 30 mg/kg, 0.1 to 20 mg/kg, 0.1 to 10 mg/kg, 0.1 to 5 mg/kg, 0.1 to 4 mg/kg, 0.1 to 3 mg/kg, 0.1 to 2 mg/kg, 0.1 to 1 mg/kg, 0.5 to 50 mg/kg, 0.5 to 40 mg/kg, 0.5 to 30 mg/kg, 0.5 to 20 mg/kg, 0.5 to 10 mg/kg, 0.5 to 5 mg/kg, 0.5 to 4 mg/kg, 0.5 to 3 mg/kg, 0.5 to 2 mg/kg, 0.5 to 1 mg/kg, 1 to 50 mg/kg, 1 to 40 mg/kg, 1 to 30 mg/kg, 1 to 20 mg/kg, 1 to 10 mg/kg, 1 to 5 mg/kg, 1 to 4 mg/kg, 1 to 3 mg/kg, 1 to 2 mg/kg, and 1 mg/kg body weight per week.

### Claim 6 (depends on 5)

A method according to claim 5, wherein the therapeutically effective amount of the isolated antagonistic antigen binding protein is 0.01 to 10 mg/kg body weight per week.

### Claim 7 (depends on 1)

A method according to claim 1, said method further comprising administering an anti-heart failure drug to the subject, wherein the ant-heart failure drug is selected from a group consisting of: angiotensin-converting enzyme (ACE) inhibitors, β-adrenergic blocking agents, angiotension II receptor blockers (ARBs), diuretics, and digitalis.

### Claim 8 (depends on 1)

A method according to claim 1, wherein the isolated antagonistic antigen binding protein is admixed with a pharmaceutically acceptable carrier to form a pharmaceutical composition for systemic administration to the subject.

### Claim 9 (depends on 8)

A method according to claim 8, wherein the systemic administration is selected from: intravenous injection, intramuscular injection, subcutaneous injection, intraperitoneal injection, transdermal injection, intraarterial injection, intrasternal injection, intrathecal injection, intraventricular injection, intraurethral injection, intracranial injection, intrasynovial injection or via infusions.

### Claim 10

A method of treating lateral ventricular (LV) remodeling comprising administration of a therapeutically effective amount of an isolated antagonistic antigen binding protein that specifically binds to the human glucagon receptor (GCGR), wherein the antagonistic antigen binding protein is a human anti-GCGR antibody which comprises the amino acid sequence encoding the heavy chain of SEQ ID NO: 51 and the amino acid sequence encoding the light chain of SEQ ID NO: 52.

### Claim 11 (depends on 10)

A method according to claim 10, said method further comprising administering an anti-heart failure drug to the subject, wherein the ant-heart failure drug is selected from a group consisting of: angiotensin-converting enzyme (ACE) inhibitors, β-adrenergic blocking agents, angiotension II receptor blockers (ARBs), diuretics, and digitalis.