# US 2014/0193421 A1 · Anti-Human XCR1 Antibodies

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- Number: US 2014/0193421 A1
- Document ID: US20140193421A1
- Status: Published application
- Kind: A1
- Application number: 14/240,090
- Filed: 2012-08-30
- Published: 2014-07-10
- Earliest claimed: 2011-09-01
- Assignees: Eisai R&D Management Co., Ltd.
- Inventors: Yoshimasa Sakamoto; Miyuki Nishimura; Tetsu Kawano; Yukihisa Sawa; Toshio Imai
- Web page: https://patentgrep.com/patent/US20140193421A1

## CPC

- C07K 16/2866: {against receptors for cytokines, lymphokines, interferons}
- A61P 3/10: for hyperglycaemia, e.g. antidiabetics
- A61P 5/14: of the thyroid hormones, e.g. T3, T4
- A61P 17/00: Drugs for dermatological disorders
- A61P 17/04: Antipruritics
- A61P 17/06: Antipsoriatics
- A61P 17/14: for baldness or alopecia
- A61P 19/00: Drugs for skeletal disorders
- A61P 19/02: for joint disorders, e.g. arthritis, arthrosis
- A61P 21/00: Drugs for disorders of the muscular or neuromuscular system
- A61P 25/00: Drugs for disorders of the nervous system
- A61P 29/00: Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- A61P 37/00: Drugs for immunological or allergic disorders
- A61P 37/02: Immunomodulators
- A61K 2039/505: {comprising antibodies}
- C07K 2317/24: containing regions, domains or residues from different species, e.g. chimeric, humanized or veneered
- 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 2317/55: Fab or Fab'
- C07K 2317/76: Antagonist effect on antigen, e.g. neutralization or inhibition of binding
- C07K 2319/55: containing a fusion with a toxin, e.g. diphteria toxin
- 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
- 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)

## Abstract

An object of the present invention is to provide a monoclonal antibody binding to human XCR1, wherein the antibody binds to linear or discontinuous epitopes which comprise at least three amino acids selected from the group consisting of the 8th, 11th, 12th, 13th, 14th, 16th, 17th, 22nd, 23rd, 176th, and 177th amino acids in the amino acid sequence of SEQ ID NO: 91.

## Claims

### Claim 1

An antibody binding to human XCR1, wherein the antibody binds to linear or discontinuous epitopes which comprise at least three amino acids selected from the group consisting of the 8th, 11th, 12th, 13th, 14th, 16th, 17th, 22nd, 23rd, 176th, and 177th amino acids in the amino acid sequence of SEQ ID NO: 91.

### Claim 2 (depends on 1)

The antibody according to claim 1, wherein the antibody is:
the antibody comprising a heavy chain variable region comprising heavy chain CDRs 1 to 3 described in (g) to (i) below and a light chain variable region comprising light chain CDRs 1 to 3 described in (j) to (1) below;
the antibody comprising a heavy chain variable region comprising heavy chain CDRs 1 to 3 described in (m) to (O) below and a light chain variable region comprising light chain CDRs 1 to 3 described in (p) to (r) below; or
the antibody comprising a heavy chain variable region comprising heavy chain CDRs 1 to 3 described in (a) to (c) below and a light chain variable region comprising light chain CDRs 1 to 3 described in (d) to (f) below:
(a) a heavy chain CDR 1 consisting of the amino acid sequence of SEQ ID NO: 41,
(b) a heavy chain CDR 2 consisting of the amino acid sequence of SEQ ID NO: 42,
(c) a heavy chain CDR 3 consisting of the amino acid sequence of SEQ ID NO: 43;
(d) a light chain CDR 1 consisting of the amino acid sequence of SEQ ID NO: 44,
(e) a light chain CDR 2 consisting of the amino acid sequence of SEQ ID NO: 45, and
(f) a light chain CDR 3 consisting of the amino acid sequence of SEQ ID NO: 46;
(g) a heavy chain CDR 1 consisting of the amino acid sequence of SEQ ID NO: 17,
(h) a heavy chain CDR 2 consisting of the amino acid sequence of SEQ ID NO: 18,
(i) a heavy chain CDR 3 consisting of the amino acid sequence of SEQ ID NO: 19;
(j) a light chain CDR 1 consisting of the amino acid sequence of SEQ ID NO: 20,
(k) a light chain CDR 2 consisting of the amino acid sequence of SEQ ID NO: 21,
(l) a light chain CDR 3 consisting of the amino acid sequence of SEQ ID NO: 22;
(m) a heavy chain CDR 1 consisting of the amino acid sequence of SEQ ID NO: 29,
(n) a heavy chain CDR 2 consisting of the amino acid sequence of SEQ ID NO: 30,
(o) a heavy chain CDR 3 consisting of the amino acid sequence of SEQ ID NO: 31;
(p) a light chain CDR 1 consisting of the amino acid sequence of SEQ ID NO: 32,
(q) a light chain CDR 2 consisting of the amino acid sequence of SEQ ID NO: 33, and
(r) a light chain CDR 3 consisting of the amino acid sequence of SEQ ID NO: 34.

### Claim 3 (depends on 1)

The antibody according to claim 1, wherein the antibody comprises a heavy chain variable region comprising an amino acid sequence of SEQ ID NO: 60 or 64, and a light chain variable region comprising an amino acid sequence of SEQ ID NO: 68 or 72.

### Claim 4 (depends on 1)

The antibody according to claim 1, wherein the antibody comprises a heavy chain variable region comprising an amino acid sequence of SEQ ID NO: 60, and a light chain variable region comprising an amino acid sequence of SEQ ID NO: 68.

### Claim 5 (depends on 1)

The antibody according to claim 1, wherein the antibody comprises a heavy chain variable region comprising an amino acid sequence of SEQ ID NO: 64, and a light chain variable region comprising an amino acid sequence of SEQ ID NO: 72.

### Claim 6 (depends on 1)

The antibody according to claim 1, wherein the antibody comprises a human constant region.

### Claim 7 (depends on 1)

The antibody according to claim 1, wherein the antibody comprises a heavy chain comprising an amino acid sequence of SEQ ID NO: 59, and a light chain comprising an amino acid sequence of SEQ ID NO: 67.

### Claim 8 (depends on 1)

The antibody according to claim 1, wherein the antibody comprises a heavy chain comprising an amino acid sequence of SEQ ID NO: 63, and a light chain comprising an amino acid sequence of SEQ ID NO: 71.

### Claim 9 (depends on 1)

The antibody according to claim 1 comprising an Fc region, wherein the Fc region is mutated to induce a change in ADCC activity.

### Claim 10 (depends on 9)

The antibody according to claim 9, wherein the Fc region is mutated to lower ADCC activity.

### Claim 11 (depends on 1)

The antibody according to claim 1, wherein the antibody is conjugated to a cytotoxic molecule.

### Claim 12 (depends on 1)

The antibody according to claim 1, wherein the antibody inhibits interaction between human XCR1 and human XCL1.

### Claim 13 (depends on 1)

The antibody according to claim 1, wherein the antibody inhibits cell migration of dendritic cells.

### Claim 14 (depends on 1)

The antibody according to claim 1, wherein the antibody suppresses the activity of cytotoxic T lymphocytes.

### Claim 15 (depends on 1)

A pharmaceutical composition comprising the antibody according to claim 1 and a pharmaceutically acceptable carrier or additive.

### Claim at position 16

16-27. (canceled)
