# US 10,766,966 B2 · CD73 blockade

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

- Number: US 10,766,966 B2
- Document ID: US10766966B2
- Status: Granted
- Kind: B2
- Application number: 15/517,991
- Filed: 2015-10-09
- Published: 2018-08-23
- Granted: 2020-09-08
- Earliest claimed: 2014-10-10
- Assignees: Innate Pharma
- Applicants: Innate Pharma
- Inventors: Ivan Perrot; Carine Paturel; Laurent Gauthier
- Web page: https://patentgrep.com/patent/US10766966B2

## CPC

- C07K 16/2896: {against molecules with a "CD"-designation, not provided for elsewhere}
- A61P 1/04: for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
- A61P 5/00: Drugs for disorders of the endocrine system
- A61P 13/08: of the prostate
- A61P 13/10: of the bladder
- A61P 15/00: Drugs for genital or sexual disorders (for disorders of sex hormones A61P5/24); Contraceptives
- A61P 17/00: Drugs for dermatological disorders
- A61P 25/00: Drugs for disorders of the nervous system
- A61P 35/00: Antineoplastic agents
- A61P 35/02: specific for leukemia
- A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- C07K 16/30: from tumour cells
- C07K 16/40: against enzymes
- C07K 2317/21: from primates, e.g. man
- 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 2317/34: Identification of a linear epitope shorter than 20 amino acid residues or of a conformational epitope defined by amino acid residues
- C07K 2317/41: Glycosylation, sialylation, or fucosylation
- C07K 2317/71: Decreased effector function due to an Fc-modification
- 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)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## Abstract

This disclosure relates to antibodies that bind an epitope present on CD73 expressed at the surface of cells, including tumor cells, and that inhibit the enzymatic (ecto-5′ nucleotidase) activity of the CD73 enzyme. Such agents can be used for the treatment of diseases such as cancers.

## Claims

### Claim 1

An isolated antibody or antibody fragment that specifically binds a human CD73 polypeptide at the surface of a cell and that is capable of neutralizing the 5′-ectonucleotidase activity thereof, selected from the group consisting of:
(a) monoclonal antibody or antibody fragment comprising (i) a heavy chain variable region comprising CDR 1, 2 and 3 of the heavy chain variable region of SEQ ID NO: 3 and (ii) a light chain variable region comprising CDR 1, 2 and 3 of the light chain variable region of SEQ ID NO: 4;
(b) monoclonal antibody or antibody fragment comprising (i) a heavy chain variable region comprising CDR 1, 2 and 3 of the heavy chain variable region of SEQ ID NO: 3 and (ii) a light chain variable region comprising CDR 1, 2 and 3 of the light chain variable region of SEQ ID NO: 21;
(c) monoclonal antibody or antibody fragment comprising (i) a heavy chain variable region comprising CDR 1, 2 and 3 of the heavy chain variable region of SEQ ID NO: 28 and (ii) a light chain variable region comprising CDR 1, 2 and 3 of the light chain variable region of SEQ ID NO: 29; and
(d) monoclonal antibody or antibody fragment comprising (i) a heavy chain variable region comprising CDR 1, 2 and 3 of the heavy chain variable region of SEQ ID NO: 36 and (ii) a light chain variable region comprising CDR 1, 2 and 3 of the light chain variable region of SEQ ID NO: 37.

### Claim 2 (depends on 1)

The isolated antibody of claim 1, wherein the antibody is a human IgG4 antibody or an antibody having a human Fc domain that is modified to reduce binding between the Fc domain and an Fcγ receptor.

### Claim 3 (depends on 1)

The isolated antibody of claim 1, wherein the antibody is an IgG1 and comprises one, two or three substitutions at residues 234, 235 and 331 or at 234, 235 and 322 (EU numbering).

### Claim 4 (depends on 1)

A pharmaceutical composition comprising an antibody or antibody fragment according to claim 1, and a pharmaceutically acceptable carrier.

### Claim 5 (depends on 1)

The isolated antibody or antibody fragment of claim 1, said monoclonal antibody or antibody fragment comprising (i) a heavy chain variable region comprising CDR 1, 2 and 3 of the heavy chain variable region of SEQ ID NO: 3 and (ii) a light chain variable region comprising CDR 1, 2 and 3 of the light chain variable region of SEQ ID NO: 4.

### Claim 6 (depends on 1)

The isolated antibody or antibody fragment of claim 1, said monoclonal antibody comprising (i) a heavy chain variable region comprising CDR 1, 2 and 3 of the heavy chain variable region of SEQ ID NO: 3 and (ii) a light chain variable region comprising CDR 1, 2 and 3 of the light chain variable region of SEQ ID NO: 21.

### Claim 7 (depends on 1)

The isolated antibody or antibody fragment of claim 1, said monoclonal antibody comprising (i) a heavy chain variable region comprising CDR 1, 2 and 3 of the heavy chain variable region of SEQ ID NO: 28 and (ii) a light chain variable region comprising CDR 1, 2 and 3 of the light chain variable region of SEQ ID NO: 29.

### Claim 8 (depends on 1)

The isolated antibody or antibody fragment of claim 1, said monoclonal antibody comprising (i) a heavy chain variable region comprising CDR 1, 2 and 3 of the heavy chain variable region of SEQ ID NO: 36 and (ii) a light chain variable region comprising CDR 1, 2 and 3 of the light chain variable region of SEQ ID NO: 37.

### Claim 9 (depends on 1)

The isolated antibody or antibody fragment of claim 1, said antibody fragment comprising (i) a heavy chain variable region comprising CDR 1, 2 and 3 of the heavy chain variable region of SEQ ID NO: 3 and (ii) a light chain variable region comprising CDR 1, 2 and 3 of the light chain variable region of SEQ ID NO: 4.

### Claim 10 (depends on 1)

The isolated antibody or antibody fragment of claim 1, said antibody fragment comprising (i) a heavy chain variable region comprising CDR 1, 2 and 3 of the heavy chain variable region of SEQ ID NO: 3 and (ii) a light chain variable region comprising CDR 1, 2 and 3 of the light chain variable region of SEQ ID NO: 21.

### Claim 11 (depends on 1)

The isolated antibody or antibody fragment of claim 1, said antibody fragment comprising (i) a heavy chain variable region comprising CDR 1, 2 and 3 of the heavy chain variable region of SEQ ID NO: 28 and (ii) a light chain variable region comprising CDR 1, 2 and 3 of the light chain variable region of SEQ ID NO: 29.

### Claim 12 (depends on 1)

The isolated antibody or antibody fragment of claim 1, said antibody fragment comprising (i) a heavy chain variable region comprising CDR 1, 2 and 3 of the heavy chain variable region of SEQ ID NO: 36 and (ii) a light chain variable region comprising CDR 1, 2 and 3 of the light chain variable region of SEQ ID NO: 37.