# US 12,590,151 B2 · Anti-human CD19 antibodies with high affinity

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- Number: US 12,590,151 B2
- Document ID: US12590151B2
- Status: Granted
- Kind: B2
- Application number: 18/052,526
- Filed: 2022-11-03
- Published: 2023-10-05
- Granted: 2026-03-31
- Earliest claimed: 2015-10-02
- Assignees: Hoffmann-La Roche Inc.
- Applicants: Hoffmann-La Roche Inc.
- Inventors: Thomas Hofer; Claudia Ferrara Koller; Ekkehard Moessner; Mi He
- Web page: https://patentgrep.com/patent/US12590151B2

## CPC

- C07K 16/2803: {against the immunoglobulin superfamily}
- A61P 35/00: Antineoplastic agents
- A61P 37/02: Immunomodulators
- C07K 16/3061: {Blood cells}
- C07K 2317/24: containing regions, domains or residues from different species, e.g. chimeric, humanized or veneered
- C07K 2317/31: multispecific
- C07K 2317/33: Crossreactivity, e.g. for species or epitope, or lack of said crossreactivity
- C07K 2317/56: variable (Fv) region, i.e. VH and/or VL
- C07K 2317/565: Complementarity determining region [CDR]
- 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

## Abstract

The present invention relates to antibodies against human CD19 (anti-human CD19 antibodies), methods for their production, pharmaceutical compositions containing these antibodies, and methods of using the same.

## Claims

### Claim 1

An antibody that specifically binds to human CD19, wherein the antibody comprises
(a) CDR-L1 comprising the amino acid sequence of SEQ ID NO: 43,
(b) CDR-L2 comprising the amino acid sequence of SEQ ID NO: 44,
(c) CDR-L3 comprising the amino acid sequence of SEQ ID NO: 45,
(d) CDR-H1 comprising the amino acid sequence of SEQ ID NO: 46,
(e) CDR-H2 comprising the amino acid sequence of SEQ ID NO: 47, and
(f) CDR-H3 comprising the amino acid sequence of SEQ ID NO: 48.

### Claim 2 (depends on 1)

The antibody of claim 1, wherein the antibody is a monoclonal antibody.

### Claim 3 (depends on 1)

The antibody of claim 1, wherein the antibody is a humanized or chimeric antibody.

### Claim 4 (depends on 1)

The antibody of claim 1, wherein the antibody is an antibody fragment that specifically binds to human CD19.

### Claim 5 (depends on 1)

The antibody of claim 1, wherein the antibody comprises a VH domain comprising an amino acid sequence of SEQ ID NO:99 and a VL domain comprising an amino acid sequence of SEQ ID NO:100.

### Claim 6 (depends on 1)

The antibody of claim 1, which is a full length IgG1 antibody.

### Claim 7 (depends on 1)

The antibody of claim 1, which is a full length IgG1 antibody with mutations L234A, L235A, and P329G, numbering accordingly to the EU index of Kabat.

### Claim 8 (depends on 1)

The antibody of claim 1, wherein the antibody is cross reactive for human and cynomolgus CD19.

### Claim 9 (depends on 1)

The antibody of claim 1, wherein said antibody is a bispecific antibody that specifically binds to human CD19 and to a second antigen.

### Claim 10 (depends on 1)

A polynucleotide encoding the antibody of claim 1.

### Claim 11 (depends on 10)

A vector comprising the polynucleotide according to claim 10.

### Claim 12 (depends on 11)

A host cell comprising the vector of claim 11.

### Claim 13 (depends on 1, 12)

A method of producing the antibody of claim 1, comprising the steps of (i) culturing the host cell of claim 12 under conditions suitable for expression of the antibody, and (ii) recovering the antibody.

### Claim 14 (depends on 1)

A pharmaceutical formulation comprising the antibody of claim 1 and a pharmaceutically acceptable carrier.

### Claim 15 (depends on 1)

A method of treating a disease in an individual, comprising
administering to the individual a therapeutically effective amount of the antibody of claim 1.

### Claim 16 (depends on 15)

The method of claim 15, wherein the disease is a B-cell cancer.

### Claim 17 (depends on 15)

The method of claim 15, wherein the disease is an autoimmune disease, rheumatoid arthritis, lupus, psoriasis, and a bone disease.

### Claim 18 (depends on 9)

A polynucleotide encoding the antibody of claim 9.

### Claim 19 (depends on 18)

A vector comprising the polynucleotide according to claim 18.

### Claim 20 (depends on 19)

A host cell comprising the vector of claim 19.

### Claim 21 (depends on 9, 12)

A method of producing the antibody of claim 9, comprising the steps of (i) culturing the host cell of claim 12 under conditions suitable for expression of the antibody, and (ii) recovering the antibody.

### Claim 22 (depends on 9)

A pharmaceutical formulation comprising the antibody of claim 9 and a pharmaceutically acceptable carrier.

### Claim 23 (depends on 10)

A method of treating a CD-19-expressing disease in an individual, comprising administering to the individual a therapeutically effective amount of the antibody of claim 10.

### Claim 24 (depends on 23)

The method of claim 23, wherein the disease is a B-cell cancer.

### Claim 25 (depends on 15)

The method of claim 15, wherein the disease is an autoimmune disease, rheumatoid arthritis, lupus, psoriasis, or a bone disease.
