# US 12,257,290 B2 · PIC1 inhibition of myeloperoxidase oxidative activity in an animal model

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- Number: US 12,257,290 B2
- Document ID: US12257290B2
- Status: Granted
- Kind: B2
- Application number: 18/332,026
- Filed: 2023-06-09
- Published: 2023-10-12
- Granted: 2025-03-25
- Earliest claimed: 2018-01-09
- Assignees: Realta Holdings, LLC
- Applicants: Realta Holdings, LLC
- Inventors: Neel K. Krishna; Kenji Cunnion
- Web page: https://patentgrep.com/patent/US12257290B2

## CPC

- A61K 38/43: Enzymes; Proenzymes; Derivatives thereof
- 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 38/005: {Enzyme inhibitors (protease inhibitors A61K38/55)}
- A61K 38/08: Peptides having 5 to 11 amino acids {(A61K38/043 - A61K38/046 take precedence)}
- A61K 47/10: Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
- A61P 29/00: Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- A61P 37/06: Immunosuppressants, e.g. drugs for graft rejection
- C07K 14/005: from viruses
- C07K 14/4703: {Inhibitors; Suppressors}
- C12N 2770/00022: New viral proteins or individual genes, new structural or functional aspects of known viral proteins or genes
- C12N 2770/00033: Use of viral protein as therapeutic agent other than vaccine, e.g. apoptosis inducing or anti-inflammatory
- 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)
- C12N: MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA (microbiological testing media C12Q1/00)

## Abstract

A method of treating systemic lupus erythematosus in a subject is provided in which a therapeutically effective amount of PIC1 is administered to the subject. A method of treating transfusion-related acute lung injury is also provided where a therapeutically effective amount of PIC1 is administered to the subject. PIC1 can modulate immune complex activation of the complement system and NET formation in the subject. PIC1 can also inhibit myeloperoxidase (MPO) activity in the subject.

## Claims

### Claim 1

A method of reducing myeloperoxidase (MPO) levels in a subject, the method comprising:
administering a therapeutically effective amount of a PIC1 peptide to the subject in need thereof, wherein the PIC1 peptide comprises the sequence of IALILEPICCQERAA-dPEG24 (SEQ ID NO: 19),
wherein the PIC1 peptide is administered at a dose of from 5 to 160 mg/kg body weight of the subject.

### Claim 2 (depends on 1)

The method of claim 1, wherein the method is effective to inhibit inflammation in the subject.

### Claim 3 (depends on 1)

The method of claim 1, wherein the method is effective to inhibit inflammatory tissue damage in the subject.

### Claim 4 (depends on 1)

The method of claim 1, wherein the method is effective to preserve normal lung architecture in the subject.

### Claim 5 (depends on 1)

The method of claim 1, wherein the method is effective to inhibit one or more of lung damage, neutrophil invasion into lung tissue, and MPO activity.

### Claim 6 (depends on 5)

The method of claim 5, wherein the MPO activity is in lung tissue.

### Claim 7 (depends on 1)

The method of claim 1, wherein the method is effective to modulate immune complex activation of the complement system in the subject.

### Claim 8 (depends on 1)

The method of claim 1, wherein the PIC1 peptide is administered at a dose of from 5 to 100 mg/kg body weight of the subject.

### Claim 9 (depends on 1)

The method of claim 1, wherein the PIC1 peptide is administered intravenously.

### Claim 10 (depends on 1)

The method of claim 1, wherein the PIC1 peptide is administered at a dose of about 10 mg/kg body weight of the subject.