# US 2023/0054032 A1 · Compositions and methods for treating ocular disease

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- Number: US 2023/0054032 A1
- Document ID: US20230054032A1
- Status: Published application
- Kind: A1
- Application number: 17/442,682
- Filed: 2020-03-26
- Published: 2023-02-23
- Earliest claimed: 2019-03-26
- Assignees: AsclepiX Therapeutics, Inc.
- Applicants: Asclepix Therapeutics, Inc.
- Inventors: Niranjan B. PANDEY
- Web page: https://patentgrep.com/patent/US20230054032A1

## CPC

- A61K 38/39: Connective tissue peptides, e.g. collagen, elastin, laminin, fibronectin, vitronectin, cold insoluble globulin [CIG]
- C07K 14/78: Connective tissue peptides, e.g. collagen, elastin, laminin, fibronectin, vitronectin or cold insoluble globulin [CIG]
- 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 9/0048: {Eye, e.g. artificial tears}
- A61P 9/10: for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
- A61P 27/02: Ophthalmic agents
- A61P 27/06: Antiglaucoma agents or miotics
- A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- A61K 38/00: Medicinal preparations containing peptides (peptides containing beta-lactam rings A61K31/00; cyclic dipeptides not having in their molecule any other peptide link than those which form their ring, e.g. piperazine-2,5-diones, A61K31/00; ergot alkaloids of the cyclic peptide type A61K31/48; containing macromolecular compounds having statistically distributed amino acid units A61K31/74; medicinal preparations containing antigens or antibodies A61K39/00; medicinal preparations characterised by the non-active ingredients, e.g. peptides as drug carriers, A61K47/00)
- 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)
- 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)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## Abstract

In various aspects and embodiments, the invention provides methods and pharmaceutical compositions for treating ocular disease, including ocular disease involving ocular vascular permeability or ocular inflammation. In various aspects and embodiments, the invention comprises administering about 1 μg to about 1 mg of collagen IV-derived biomimetic peptide or salt thereof to a patient by intraocular injection. Injections are provided at a frequency of from about monthly to about once every two years. In various embodiments, the methods and compositions provide for potent action and long duration of action, with infrequent intravitreal injections of a small volume.

## Claims

### Claim 1

A method for preventing or treating a condition involving ocular vascular permeability or inflammation in a patient, comprising: administering a unit dose of a collagen IV-derived biomimetic peptide or salt thereof to said patient by intraocular injection at a frequency of no more than about once every month.

### Claim 2 (depends on 1)

The method of claim 1, wherein the unit dose comprises about 10 μg to about 1 mg of the peptide.

### Claim 3

(canceled)

### Claim 4 (depends on 1)

The method of claim 1, wherein the patient has a condition selected from diabetic macular edema, retinal vein occlusion, wet age-related macular degeneration (wet AMD), or background diabetic retinopathy.

### Claim 5 (depends on 1)

The method of claim 1, wherein the patient has acute or chronic inflammation of the eye.

### Claim at position 6

6-7. (canceled)

### Claim 8 (depends on 1)

The method of claim 1, wherein the unit dose comprises about 700 μg or less, or about 500 μg or less, of the peptide or salt thereof.

### Claim at position 8

9-10. (canceled)

### Claim 11 (depends on 1)

The method of claim 1, wherein the unit dose is administered by intraocular injection no more frequently than once every three months.

### Claim at position 10

12-17. (canceled)

### Claim 18 (depends on 1)

The method of claim 1, wherein the unit dose comprises about 10 μg to about 50 of the peptide or salt thereof, and is administered at a frequency of no more than about monthly.

### Claim 19 (depends on 18)

The method of claim 18, wherein the unit dose comprises about 25 μg of the peptide or salt thereof, and the unit dose is administered by intraocular injection about monthly.

### Claim 20 (depends on 1)

The method of claim 1, wherein the unit dose comprises about 50 to about 150 μg of the peptide or salt thereof, and the unit dose is administered by intraocular injection at a frequency of no more than once every third month.

### Claim at position 14

21-24. (canceled)

### Claim 25 (depends on 1)

The method of claim 1, wherein the unit dose comprises about 150 to about 250 μg of the peptide or salt thereof, and is administered at a frequency of no more than once every six months.

### Claim at position 16

26-27. (canceled)

### Claim 28 (depends on 1)

The method of claim 1, wherein the unit dose comprises from about 200 μg to about 250 of the peptide or salt thereof, and is administered at a frequency of once every six to twelve months.

### Claim 29 (depends on 1)

The method of claim 1, wherein the unit dose comprises from about 250 μg to about 700 μg of the peptide or salt thereof, and is administered at a frequency of no more than once every six months.

### Claim at position 19

30-33. (canceled)

### Claim 34 (depends on 1)

The method of claim 1, wherein the unit dose is administered at a frequency of once every six to eighteen months.

### Claim 35

(canceled)

### Claim 36 (depends on 1)

The method of claim 1, wherein the unit dose comprises about 700 to about 1 mg of the peptide or salt thereof, and the unit dose is administered at a frequency of no more than once every twelve months.

### Claim at position 23

37-40. (canceled)

### Claim 41 (depends on 1)

The method of claim 1, wherein the peptide or salt thereof is administered after unsuccessful VEGF blockade or inhibitor therapy.

### Claim 42

(canceled)

### Claim 43 (depends on 1)

The method of claim 1, wherein the peptide or salt thereof is administered as an alternative to VEGF blockade or inhibitor therapy.

### Claim 44

(canceled)

### Claim 45 (depends on 1)

The method of claim 1, wherein the peptide comprises the amino acid sequence of any one of SEQ ID NOs: 1 to 36.

### Claim at position 29

46-48. (canceled)

### Claim 49 (depends on 1)

The method of claim 1, wherein the peptide has the amino acid sequence LRRFSTAPFAFIDINDVINF (SEQ ID NO:1).

### Claim 50 (depends on 1)

The method of claim 1, wherein the unit dose has a volume in the range of about 1 μl to about 1 mL, or a volume in the range of about 10 μL to about 0.5 mL, or a volume in the range of about 10 μL to about 250 or a volume in the range of about 10 μL to about 50 μL.

### Claim at position 32

51-52. (canceled)

### Claim 53

A pharmaceutical composition suitable for intraocular injection, comprising about 1 μg to about 1 mg of a collagen IV-derived biomimetic peptide or salt thereof as a unit dose in a pre-filled syringe, the peptide being formulated in an aqueous solution without particle encapsulation.

### Claim at position 34

54-68. (canceled)

### Claim 69 (depends on 53)

The pharmaceutical composition of claim 53, wherein the unit dose has a volume in the range of about 1 μl to about 1 mL, or a volume in the range of about 10 μL to about 0.5 mL, or a volume in the range of about 10 μL to about 250 or a volume in the range of about 10 μL to about 50 μL.

### Claim at position 36

70-71. (canceled)

### Claim 72 (depends on 53)

The pharmaceutical composition of claim 53, wherein the peptide comprises the amino acid sequence of any one of SEQ ID NOs: 1 to 36 or a derivative thereof.

### Claim 73 (depends on 72)

The pharmaceutical composition of claim 72, wherein the peptide has the amino acid sequence of SEQ ID NO:1.

### Claim at position 39

74-75. (canceled)