# US 12,215,170 B2 · Anti-TMPRSS6 antibodies and uses thereof

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- Number: US 12,215,170 B2
- Document ID: US12215170B2
- Status: Granted
- Kind: B2
- Application number: 17/916,008
- Filed: 2021-04-05
- Published: 2023-06-29
- Granted: 2025-02-04
- Earliest claimed: 2020-04-07
- Assignees: Mabwell Therapeutics, Inc.
- Applicants: Mabwell Therapeutics Inc.
- Inventors: Xin Du; Buxin Chen; Yu Jean Wang
- Web page: https://patentgrep.com/patent/US12215170B2

## CPC

- C07K 16/40: against enzymes
- A61P 7/06: Antianaemics
- C12N 15/63: Introduction of foreign genetic material using vectors; Vectors; Use of hosts therefor; Regulation of expression
- 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 2317/41: Glycosylation, sialylation, or fucosylation
- C07K 2317/565: Complementarity determining region [CDR]
- C07K 2317/71: Decreased effector function due to an Fc-modification
- C07K 2317/75: Agonist effect on antigen
- 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)
- 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

Antibodies and antigen-binding fragments thereof that bind type II transmembrane serine protease 6 (TMPRSS6) on the surface of a cell and increase hepcidin expression, and methods for treating disorders of iron metabolism using anti TMPRSS6 antibodies and fragments, are provided.

## Claims

### Claim 1

An anti-type II transmembrane serine protease 6 (TMPRSS6) antibody comprising a HC CDR1, a HC CDR2, and a HC CDR3 of a heavy chain variable region (VH) that comprises the amino acid sequence of SEQ ID NO: 21 or 51, and a LC CDR1, a LC CDR2, and a LC CDR3 of a light chain variable region (VL) of SEQ ID NO: 26 or 56.

### Claim 2 (depends on 1)

The anti-TMPRSS6 antibody of claim 1, wherein the HC CDR1, HC CDR2, HC CDR3, LC CDR1, LC CDR2, and LC CDR3 are defined by Kabat definition.

### Claim 3 (depends on 1)

The anti-TMPRSS6 antibody of claim 1, wherein the antibody is a humanized antibody.

### Claim 4 (depends on 3)

The anti-TMPRSS6 antibody of claim 3, wherein the HC CDR1, HC CDR2, HC CDR3, LC CDR1, LC CDR2, and LC CDR3 are grafted into a framework comprising variable regions derived from a human immunoglobulin framework.

### Claim 5 (depends on 1)

The anti-TMPRSS6 antibody of claim 1, wherein the antibody comprises a heavy chain variable region comprising the amino acid sequence of SEQ ID NO: 21 or 51.

### Claim 6 (depends on 1)

The anti-TMPRSS6 antibody of claim 1, wherein the antibody comprises a light chain variable region comprising the amino acid sequence of SEQ ID NO: 26 or 56.

### Claim 7 (depends on 5)

The anti-TMPRSS6 antibody of claim 5, wherein the antibody comprises a light chain variable region comprising the amino acid sequence of SEQ ID NO: 26 or 56.

### Claim 8 (depends on 1)

The anti-TMPRSS6 antibody of claim 1, wherein the antibody is a full-length antibody, a Fab fragment, or a single-chain variable fragment (scFv).

### Claim 9 (depends on 1)

The anti-TMPRSS6 antibody of claim 1, wherein the antibody comprises a heavy chain constant region of IgG1.

### Claim 10 (depends on 1)

The anti-TMPRSS6 antibody of claim 1, wherein the antibody comprises a heavy chain comprising the amino acid sequence of SEQ ID NO: 69 or 81.

### Claim 11 (depends on 1)

The anti-TMPRSS6 antibody of claim 1, wherein the antibody comprises a light chain comprising the amino acid sequence of SEQ ID NO: 71 or 83.

### Claim 12 (depends on 10)

The anti-TMPRSS6 antibody of claim 10, wherein the antibody comprises a light chain comprising the amino acid sequence of SEQ ID NO: 71 or 83.

### Claim 13 (depends on 1)

The anti-TMPRSS6 antibody of claim 1, wherein the antibody cross-reacts with at least one non-human TMPRSS6.

### Claim 14 (depends on 13)

The anti-TMPRSS6 antibody of claim 13, wherein the non-human TMPRSS6 is a mouse TMPRSS6 or a non-human primate TMPRSS6.

### Claim 15 (depends on 1)

The anti-TMPRSS6 antibody of claim 1, wherein the antibody specifically binds to human TMPRSS6.

### Claim 16 (depends on 1)

The anti-TMPRSS6 antibody of claim 1, wherein the antibody does not specifically bind to human matriptase-1 or human matriptase-3.

### Claim 17 (depends on 1)

A composition comprising the anti-TMPRSS6 of claim 1 and a pharmaceutically acceptable carrier.

### Claim 18 (depends on 1)

An isolated nucleic acid encoding the heavy chain variable region and/or the light chain variable region of the antibody of claim 1.

### Claim 19 (depends on 18)

A vector comprising the isolated nucleic acid of claim 18.

### Claim 20 (depends on 19)

A host cell comprising the vector of claim 19.
