# US 2025/0367263 A9 · Therapeutic Regimens and Methods for Treatment of Cardiovascular Risk Factors using a GLP-1R and GCGR Agonist

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- Number: US 2025/0367263 A9
- Document ID: US20250367263A9
- Status: Published application
- Kind: A9
- Application number: 18/503,065
- Filed: 2023-11-06
- Published: 2025-12-04
- Earliest claimed: 2022-11-05
- Assignees: Spitfire Pharma LLC
- Applicants: Spitfire Pharma LLC
- Inventors: John Joseph Suschak, III; Bertrand Victor Gilbert Georges; Sarah K. Browne; Matthew Scott Harris; M. Scot Roberts; Maynara Lucca Andrade
- Web page: https://patentgrep.com/patent/US20250367263A9

## CPC

- A61K 38/26: Glucagons
- A61P 3/04: Anorexiants; Antiobesity agents
- A61P 3/06: Antihyperlipidemics
- A61P 3/08: for glucose homeostasis (pancreatic hormones A61P5/48)
- A61P 9/00: Drugs for disorders of the cardiovascular system
- C07K 14/605: Glucagons
- C07K 14/705: Receptors; Cell surface antigens; Cell surface determinants {(tumour specific antigens C07K14/4748)}
- 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

This disclosure relates to the once weekly dosing regimen of a dual GLP-1R and GCGR agonist, formulations, and methods of using the same for treatment of cardiovascular disease/disorder and/or reducing risk factors thereof by inducing reduction of pathogenic serum lipid mediators in a human being, wherein the human may or may not have other comorbidities such as obesity and/or type 2 diabetes. The dual GLP-1R and GCGR agonist includes the peptide product of SEQ ID NO. 1 (pemvidutide).

## Claims

### Claim at position 1

1-28. (canceled)

### Claim 29

A method of treating cardiovascular (CV) disease risk factors comprising:
administering a pharmaceutical composition comprising a therapeutically effective amount of SEQ ID NO: 1, or a pharmaceutically acceptable salt thereof to a patient in need thereof, wherein the patient is overweight, obese, has a body mass index (BMI kg/m2) of greater than or equal to 25, and/or has Type II diabetes and wherein the method reduces at least one CV disease risk factor as compared to baseline, the CV disease risk factor being selected from the group consisting of body weight, waist circumference, blood pressure, hyperglycemia, serum lipids, total cholesterol, triglycerides, HDL, LDL and/or VLDL particle concentration and/or diameter, phosphatidylethanolamines, phosphatidylcholines, lysophosphatidylethanolamines, sphingolipids and/or lysophosphatidylcholines.

### Claim 30 (depends on 29)

The method of claim 29, wherein the patient in need thereof is overweight.

### Claim 31 (depends on 29)

The method of claim 29, wherein the patient in need thereof is obese.

### Claim 32 (depends on 29)

The method of claim 29, wherein the patient in need thereof has a body mass index (BMI kg/m2) of greater than or equal to 25.

### Claim 33 (depends on 29)

The method of claim 29, wherein the patient in need thereof has Type II diabetes.

### Claim 34 (depends on 29)

The method of claim 29, wherein the pharmaceutical composition is administered once weekly in an amount of about 1.2 mg, about 1.8 mg, or about 2.4 mg.

### Claim 35 (depends on 29)

The method of claim 29, wherein the pharmaceutical composition is administered about once weekly in an amount of about 1.8 mg.

### Claim 36 (depends on 29)

The method of claim 29, wherein the pharmaceutical composition is administered about once weekly in an amount of about 2.4 mg.

### Claim 37 (depends on 29)

The method of claim 29, wherein a steady state dose is achieved after a dose escalating phase having a duration of about 2 weeks, about 3 weeks or about 4 weeks.

### Claim 38 (depends on 29)

The method of claim 29, wherein the pharmaceutical composition is administered once weekly for about five to 12 weeks.

### Claim 39 (depends on 29)

The method of claim 29, wherein the pharmaceutical composition is administered by parenteral injection.

### Claim 40

(canceled)

### Claim 41 (depends on 29)

The method of claim 29, wherein the pharmaceutical composition is administered from a liquid formulation comprising at least about 1.8 mg/ml pemvidutide.

### Claim 42 (depends on 29)

The method of claim 29, wherein the pharmaceutical composition is administered as a liquid pharmaceutical formulation comprising SEQ ID NO: 1 and about 0.20% (w/w) polysorbate 20, about 0.348% (w/w) arginine, and about 4.260% (w/w) mannitol in sterile water (pH 7.7±0.1).

### Claim 43

A method of treating cardiovascular (CV) disease risk factors comprising:
administering a pharmaceutical composition comprising a therapeutically effective amount of SEQ ID NO: 1, or a pharmaceutically acceptable salt thereof to a patient in need thereof, wherein the patient is overweight, obese, has a body mass index (BMI kg/m2) of greater than or equal to 25, and/or has Type II diabetes and wherein the method reduces at least one of plasma triglycerides, total plasma cholesterol, plasma LDL-cholesterol or plasma HDL-cholesterol levels by about any of 3%, 5% 7%, or 10% from baseline.

### Claim 44 (depends on 43)

The method of claim 43, wherein the plasma triglycerides are reduced from baseline.

### Claim 45 (depends on 43)

The method of claim 43, wherein the total plasma cholesterol is reduced from baseline.

### Claim 46 (depends on 43)

The method of claim 43, wherein the plasma LDL-cholesterol is reduced from baseline.

### Claim 47 (depends on 43)

The method of claim 43, wherein the plasma HDL-cholesterol is reduced from baseline.

### Claim 48

A method of reducing plasma lipids in a patient in need thereof, comprising administering a pharmaceutical composition comprising a therapeutically effective amount of SEQ ID NO: 1, or a pharmaceutically acceptable salt thereof to the patient in need thereof, wherein the patient has established cardiovascular disease and wherein the method reduces at least one of plasma triglycerides, total plasma cholesterol, plasma LDL-cholesterol or plasma HDL-cholesterol levels by 3%, 5%, 7%, or 10% from baseline.

### Claim at position 22

49-60. (canceled)

### Claim 61 (depends on 29)

The method of claim 29, wherein the pharmaceutical composition is administered as a liquid pharmaceutical formulation comprising SEQ ID NO: 1 and about 0.20% (w/w) polysorbate 20, about 0.348% (w/w) arginine, and about 4.260% (w/w) mannitol in sterile water (pH 7.7±0.1).