# US 12,180,303 B2 · Anti-human MASP-2 antibody, preparation method therefor and application thereof

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- Number: US 12,180,303 B2
- Document ID: US12180303B2
- Status: Granted
- Kind: B2
- Application number: 18/486,644
- Filed: 2023-10-13
- Published: 2024-02-08
- Granted: 2024-12-31
- Earliest claimed: 2021-04-15
- Assignees: Shanghai Mabgeek Biotech. Co., Ltd.
- Applicants: Shanghai Mabgeek Biotech. Co., Ltd.
- Inventors: Yipan Wu; Wei Dang; Chenghai Zhang; Lingqiao Zhu; Jinlin Guo; Yujing Yuan; Qiuling Zou; Yang Wang; Shun Hu
- Web page: https://patentgrep.com/patent/US12180303B2

## CPC

- C07K 16/40: against enzymes
- C07K 2317/24: containing regions, domains or residues from different species, e.g. chimeric, humanized or veneered
- C07K 2317/33: Crossreactivity, e.g. for species or epitope, or lack of said crossreactivity
- C07K 2317/76: Antagonist effect on antigen, e.g. neutralization or inhibition of binding
- C07K 2317/92: Affinity (KD), association rate (Ka), dissociation rate (Kd) or EC50 value
- 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

Disclosed are an antibody that can bind to human MASP-2, a preparation method therefor and an application thereof. The anti-human MASP-2 antibody of the present invention can specifically bind to human MASP-2, has good biological activity of inhibiting the cleavage of C4 and the generation of C3b, and can be applied in the treatment of MASP-2 related diseases, such as IgA nephropathy.

## Claims

### Claim 1

An antibody specifically binding to human MASP-2 or an antigen-binding fragment thereof, comprising a heavy chain variable region, wherein the heavy chain variable region comprises an HCDR3 sequence, an HCDR2 sequence and an HCDR1 sequence, wherein the HCDR3 sequence comprises an amino acid sequence as shown in SEQ IDS NO: 47; and, the HCDR2 sequence comprises an amino acid sequence as shown in SEQ ID NO: 46; and, the HCDR1 sequence comprises an amino acid sequence as shown in SEQ ID NO: 45;
and, the antibody or the antigen-binding fragment thereof further comprising a light chain variable region, wherein the light chain variable region comprises an LCDR1 sequence, an LCDR2 sequence, and an LCDR3 sequence, wherein the LCDR3 sequence comprises an amino acid sequence as shown in SEQ ID NO: 50; and, the LCDR2 sequence comprises an amino acid sequence as shown in SEQ ID NO: 49; and, the LCDR1 sequence comprises an amino acid sequence as shown in SEQ ID NO: 48.

### Claim 2 (depends on 1)

The antibody or the antigen-binding fragment thereof according to claim 1, wherein the antibody or the antigen-binding fragment thereof is a murine antibody or an antigen-binding fragment thereof.

### Claim 3 (depends on 2)

The antibody or the antigen-binding fragment thereof according to claim 2, wherein the murine antibody have a heavy chain variable region comprising an amino acid sequence as shown in SEQ ID NO: 11; wherein the murine antibody have a light chain variable region comprising an amino acid sequence as shown in SEQ ID NO: 12.

### Claim 4 (depends on 1)

The antibody or the antigen-binding fragment thereof according to claim 1, wherein the antibody or the antigen-binding fragment thereof is humanized to obtain a humanized antibody or an antigen-binding fragment thereof.

### Claim 5 (depends on 4)

The antibody or the antigen-binding fragment thereof according to claim 4, comprising a combination of a heavy chain variable region sequence as shown in SEQ ID NO: 70 and a light chain variable region sequence as shown in SEQ ID NO: 72.

### Claim 6 (depends on 1)

The antibody or the antigen-binding fragment thereof according to claim 1, wherein the antibody comprises a heavy chain sequence as shown in SEQ ID NO: 73 and a light chain sequence as shown in SEQ ID NO: 74.

### Claim 7 (depends on 1)

A DNA molecule encoding the antibody or the antigen-binding fragment thereof according to claim 1.

### Claim 8 (depends on 7)

A pharmaceutically acceptable expression vector comprising the DNA molecule according to claim 7.

### Claim 9 (depends on 7)

A host cell comprising the DNA molecule according to claim 7.

### Claim 10 (depends on 8)

A host cell comprising the expression vector according to claim 8.

### Claim 11 (depends on 1)

A pharmaceutical composition comprising the antibody or the antigen-binding fragment thereof according to claim 1, and a plurality of pharmaceutically acceptable excipients, diluents, or carriers.

### Claim 12 (depends on 1)

A method for treating MASP-2 related diseases in a subject in need of, comprising administering an effective amount of the antibody or the antigen-binding fragment thereof according to claim 1, wherein the disease is selected from the group consisting of IgA nephropathy, atypical hemolytic uremic syndrome, and hematopoietic stem cell transplantation-associated thrombotic microangiopathy.

### Claim 13 (depends on 11)

A method for treating MASP-2 related diseases in a subject in need of, comprising administering an effective amount of the pharmaceutical composition according to claim 11, wherein the disease is selected from the group consisting of IgA nephropathy, atypical hemolytic uremic syndrome, and hematopoietic stem cell transplantation-associated thrombotic microangiopathy.

### Claim 14 (depends on 1)

The antibody or the antigen-binding fragment thereof according to claim 1, wherein the antigen-binding fragment is selected from the group consisting of an Fab fragment, an Fab′ fragment, an F(ab′)2 fragment, an Fv fragment and an scFv fragment.

### Claim 15 (depends on 12)

The method according to claim 12, wherein the disease is IgA nephropathy.

### Claim 16 (depends on 13)

The method according to claim 13, wherein the disease is IgA nephropathy.
