# US 12,180,264 B2 · IL1-R1 derived inhibitor of IL-1β and use thereof

> Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt

- Number: US 12,180,264 B2
- Document ID: US12180264B2
- Status: Granted
- Kind: B2
- Application number: 17/474,718
- Filed: 2021-09-14
- Published: 2021-12-30
- Granted: 2024-12-31
- Earliest claimed: 2020-05-22
- Applicants: R-Pharm Overseas, Inc.
- Inventors: Yan Lavrovsky; Alexey Repik; Mikhail Samsonov; Sergei Barbashov; Vasily Ignatiev
- Web page: https://patentgrep.com/patent/US12180264B2

## CPC

- C07K 14/7155: {for interleukins [IL]}
- 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)
- C07K 2319/30: Non-immunoglobulin-derived peptide or protein having an immunoglobulin constant or Fc region, or a fragment thereof, attached thereto
- 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)

## Abstract

A therapeutic composition is described that can be used for treating or prevention of diseases association with modulation of activity of human IL-1β. In certain aspects, the disclosed composition is based on engineering of a heterodimeric protein assembly that is capable of binding to human IL-1β and attenuating its function. The heterodimeric protein assembly comprises extracellular portions of human IL1-R1 and of human IL-1RAcP, or their functional fragments. Each, the IL1-R1 portion and the IL-1RAcP portion, is fused to a distinct mutant of Fc portion of the human Ig Gamma-1. The two distinct Fc mutants in the heterodimeric protein assembly are engineered as to favor the heteromeric dimer formation between the two Fc mutants over any homomeric assembly. The therapeutic composition has been formulated for administration into humans and animals.

## Claims

### Claim 1

A therapeutic composition, the composition comprising a heterodimeric protein composition capable of binding human IL-1β, said protein composition comprising:
a first polypeptide comprising amino acid sequence of SEQ ID NO. 8; and
a second polypeptide comprising amino acid sequence of SEQ ID NO. 9.

### Claim 2 (depends on 1)

The therapeutic composition of claim 1, further comprising about 6% (m/v) sucrose, about 3% (m/v) polyethylene glycol having an average molecular weight of 3350 Da, about 50 mM sodium chloride, and about 20 mM L-Histidine pH from about 4.5 to about 7.0.

### Claim 3 (depends on 2)

The therapeutic composition of claim 2, wherein said pH is about 6.5.

### Claim 4 (depends on 1)

The therapeutic composition of claim 1, further comprising about 1.2% (m/v) sucrose, about 0.09% (m/v) polysorbate 80, about 3% (m/v) D-mannitol, about 38 mM glycine, and about 15 mM TRIS-HCl, pH from about 6.5 to about 8.5.

### Claim 5 (depends on 4)

The therapeutic composition of claim 4, wherein said pH is about 7.5.