# US 12,187,774 B2 · Heterodimeric Relaxin fusions and uses thereof

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- Number: US 12,187,774 B2
- Document ID: US12187774B2
- Status: Granted
- Kind: B2
- Application number: 18/346,205
- Filed: 2023-07-01
- Published: 2024-01-25
- Granted: 2025-01-07
- Earliest claimed: 2020-06-17
- Assignees: MedImmune, LLC
- Applicants: Medimmune Limited
- Inventors: Isabelle Sermadiras; Monika Anna Papworth; Judy Christiane Paterson; Esther Marie Martin; Peng Ke
- Web page: https://patentgrep.com/patent/US12187774B2

## CPC

- C07K 14/64: Relaxins
- A61K 38/2221: {Relaxins}
- A61P 9/00: Drugs for disorders of the cardiovascular system
- A61P 9/04: Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
- C07K 19/00: Hybrid peptides {, i.e. peptides covalently bound to nucleic acids, or non-covalently bound protein-protein complexes}
- C12N 15/85: for animal cells
- 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 47/6811: {the drug being a protein or peptide, e.g. transferrin or bleomycin}
- C07K 2319/30: Non-immunoglobulin-derived peptide or protein having an immunoglobulin constant or Fc region, or a fragment thereof, attached thereto
- C07K 2319/31: fusions, other than Fc, for prolonged plasma life, e.g. albumin
- 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)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- C12N: MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA (microbiological testing media C12Q1/00)

## Abstract

The present invention relates to heterodimeric Relaxin fusion polypeptides, in particular to heterodimeric Relaxin 2 fusion polypeptides and uses thereof. Thus, the invention provides Relaxin fusion polypeptides, nucleic acid molecules, vectors, host cells, pharmaceutical compositions and kits comprising the same and uses of the same including methods of treatment. The polypeptides and compositions of the invention may be useful, in particular, in the treatment of cardiovascular diseases, for example for the treatment of heart failure.

## Claims

### Claim 1

A nucleic acid molecule encoding a heterodimeric fusion comprising:
(i) a polypeptide according to SEQ ID NO: 11; and
(ii) a polypeptide according to SEQ ID NO: 20;
wherein SEQ ID NO: 11 comprises a first heterodimerisation domain connected to a Relaxin A chain polypeptide;
wherein SEQ ID NO: 20 comprises a second heterodimerisation domain connected to a Relaxin B chain polypeptide;
wherein the first heterodimerisation domain heterodimerises with the second heterodimerisation domain, and wherein the heterodimeric fusion has Relaxin activity.

### Claim 2 (depends on 1)

The nucleic acid molecule of claim 1, wherein the Relaxin A chain polypeptide and the Relaxin B chain polypeptide are covalently bound by at least one inter-chain disulphide bond.

### Claim 3 (depends on 1)

The nucleic acid molecule of claim 1, wherein the Relaxin A chain polypeptide and the Relaxin B chain polypeptide are not covalently linked to each other by an amino acid linker.

### Claim 4 (depends on 1)

A vector comprising the nucleic acid molecule of claim 1.

### Claim 5 (depends on 1)

A host cell comprising the nucleic acid molecule of claim 1.

### Claim 6 (depends on 5)

A method of producing a heterodimeric fusion, the method comprising: culturing the host cell of claim 5, and collecting the heterodimeric fusion.