# US 2006/0286104 A1 · Superagonistic anti-CD28 antibodies

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

- Number: US 2006/0286104 A1
- Document ID: US20060286104A1
- Status: Published application
- Kind: A1
- Application number: 11/433,080
- Filed: 2006-05-11
- Published: 2006-12-21
- Earliest claimed: 2005-05-11
- Assignees: Tegenero AG
- Inventors: Thomas Hanke; Martin Trischler; Christine Guntermann
- Web page: https://patentgrep.com/patent/US20060286104A1

## CPC

- C07K 16/2818: {against CD28 or CD152}
- A61P 3/10: for hyperglycaemia, e.g. antidiabetics
- A61P 17/06: Antipsoriatics
- A61P 19/02: for joint disorders, e.g. arthritis, arthrosis
- 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 31/14: for RNA viruses
- A61P 31/18: for HIV
- A61P 35/00: Antineoplastic agents
- A61P 35/02: specific for leukemia
- A61P 37/06: Immunosuppressants, e.g. drugs for graft rejection
- A61K 2039/505: {comprising antibodies}
- C07K 2317/24: containing regions, domains or residues from different species, e.g. chimeric, humanized or veneered
- C07K 2317/54: F(ab')2
- C07K 2317/56: variable (Fv) region, i.e. VH and/or VL
- C07K 2317/73: Inducing cell death, e.g. apoptosis, necrosis or inhibition of cell proliferation
- C07K 2317/732: Antibody-dependent cellular cytotoxicity [ADCC]
- C07K 2317/74: Inducing cell proliferation
- 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

The present invention relates to one or more nucleic acid(s) encoding a binding molecule specifically binding to a human CD28 molecule, comprising (a) a nucleic acid sequence encoding a VH region and a nucleic acid sequence encoding a VL region comprising CDRs in a human immunoglobulin framework, wherein (i) the CDRs of the VH region (CDR-H) comprise the amino acid sequences of SEQ ID NOS: 2 or 18 (CDR-H3), 4 or 20 (CDR-H2) and 6 or 22 (CDR-H1) or are encoded by the nucleic acid sequences of SEQ ID NOS: 1 or 17 (CDR-H3), 3 or 19 (CDR-H2) and 5 or 21 (CDR-H1); and (ii) the CDRs of the VL region (CDR-L) comprise the amino acid sequences of SEQ ID NOS: 8 or 24 (CDR-L3), 10 or 26 (CDR-L2) and 12 or 28 (CDR-L1) or are encoded by the nucleic acid sequences of SEQ ID NOS: 7 or 23 (CDR-L3), 9 or 25 (CDR-L2) and 11 or 27 (CDR-L1); and (b) a nucleic acid sequence encoding the constant region of a human IgG1 or IgG4 antibody.

## Claims

### Claim 1

Nucleic acid encoding a binding molecule specifically binding to a human CD28 molecule, comprising
(a) a nucleic acid sequence encoding a VH region and a nucleic acid sequence encoding a VL region comprising CDRs in a human immunoglobulin framework, wherein
(i) the CDRs of the VH region (CDR-H) comprise the amino acid sequences of SEQ ID NOS: 2 or 18 (CDR-H3), 4 or 20 (CDR-H2) and 6 or 22 (CDR-H1) or are encoded by the nucleic acid sequences of SEQ ID NOS: 1 or 17 (CDR-H3), 3 or 19 (CDR-H2) and 5 or 21 (CDR-H 1); and
(ii) the CDRs of the VL region (CDR-L) comprise the amino acid sequences of SEQ ID NOS: 8 or 24 (CDR-L3), 10 or 26 (CDR-L2) and 12 or 28(CDR-L1) or are encoded by the nucleic acid sequences of SEQ ID NOS: 7 or 23 (CDR-L3), 9 or 25 (CDR-L2) and 11 or 27 (CDR-L1); and
(b) a nucleic acid sequence encoding the constant region of a human IgG1 or IgG4 antibody.

### Claim 2 (depends on 1)

Nucleic acid according to claim 1, comprising a nucleic acid sequence encoding a VH region and a nucleic acid sequence encoding a VL region, wherein
(i) the nucleic acid sequence of the VH region comprises SEQ ID NO: 33 or 37 and/or encodes a (poly)peptide comprising the amino acid sequence SEQ ID NO: 34 or 38; and
(ii) the nucleic acid sequence of the V|_ region comprises SEQ ID NO: 35 or 39 and/or encodes a (poly)peptide comprising the amino acid sequence SEQ ID NO: 36 or 40.

### Claim 3 (depends on 1, 2)

Nucleic acid according to claim 1 or 2, comprising a nucleic acid sequence, wherein the nucleic acid sequence
(i) is SEQ ID NO: 13, 29, 41 or 45; and/or
(ii) encodes a (poly)peptide having the amino acid sequence SEQ ID NO: 14, 30, 42 or 46.

### Claim 4 (depends on 1, 2, 3)

Nucleic acid according to any one of claims 1 to 3, comprising a nucleic acid sequence, wherein the nucleic acid sequence
(i) is SEQ ID NO: 15, 31, 43 or 47; and/or
(ii) encodes a (poly)peptide having the amino acid sequence SEQ ID NO: 16, 32, 44 or 48.

### Claim 5 (depends on 1, 2, 3, 4)

Nucleic acid according to any one of claims 1 to 4, further comprising a nucleic acid sequence encoding a marker element or tag.

### Claim 6 (depends on 1, 2, 3, 4, 5)

Vector comprising the nucleic acid according to any one of claims 1 to 5.

### Claim 7 (depends on 6)

Host, transformed or transfected with a vector according to claim 6.

### Claim 8 (depends on 1, 2, 3, 4, 5, 7)

Method for preparing a binding molecule encoded by a nucleic acid according to any one of claims 1 to 5, comprising culturing the host according to claim 7 under suitable conditions; and isolating the binding molecule from the culture.

### Claim 9 (depends on 1, 2, 3, 4, 5, 6, 8)

Binding molecule encoded by a nucleic acid according to any one of claims 1 to 6; or prepared according to the method of claim 8.

### Claim 10 (depends on 9)

An antibody or fragment or derivative of an antibody comprising at least one binding molecule according to claim 9.

### Claim 11 (depends on 10)

Antibody according to claim 10, which is a monoclonal antibody.

### Claim 12 (depends on 1, 2, 3, 4, 5, 6, 7, 9, 10, 11)

Composition comprising the nucleic acid according to any one of claims 1 to 5, the vector according to claim 6, the host according to claim 7, the binding molecule according to claim 9, and/or the antibody or fragment or derivative of an antibody according to claim 10 or 11.

### Claim 13 (depends on 12)

Composition according to claim 12 which is a pharmaceutical composition and optionally further comprises a pharmaceutically acceptable carrier, a pharmaceutically acceptable excipient and/or a pharmaceutically acceptable diluent.

### Claim 14 (depends on 12)

Composition according to claim 12, which is a diagnostic composition.

### Claim 15 (depends on 12)

Composition according to claim 12, which is a kit comprising the nucleic acid, the vector, the host, the binding molecule and/or the antibody or fragment or derivative of an antibody in one or more containers.

### Claim 16 (depends on 1, 2, 3, 4, 5, 6, 7, 9, 10, 11)

Use of the nucleic acid according to any one of claims 1 to 5, the vector according to claim 6, the host according to claim 7, the binding molecule according to claim 9, and/or the antibody or fragment or derivative of an antibody according to claim 10 or 11 for the preparation of a pharmaceutical composition for the treatment of diseases associated with a faulty or deficient co-stimulability, function or number of T cells, of inflammatory diseases and/or autoimmune diseases.

### Claim 17 (depends on 1, 2, 3, 4, 5, 6, 7, 9, 10, 11)

Method for the treatment of diseases associated with a faulty co-stimulability, function or number of T cells, of inflammatory diseases, and/or of autoimmune diseases, comprising administering the nucleic acid according to any one of claims 1 to 5, the vector according to claim 6, the host according to claim 7, the binding molecule according to claim 9, and/or the antibody or fragment or derivative of an antibody according to claim 10 or 11.

### Claim 18 (depends on 16, 17)

Use according to claim 16 or method according to claim 17, wherein the disease associated with a faulty co-stimulability, function or number of T cells is selected from a group consisting of chronic lymphocytic leukemia of the B cell type (B-CLL), acute lymphoblastic leukemia (ALL), T-lymphopeny, solid tumors, HIV infection or HTLV infection.

### Claim 19 (depends on 16, 17)

Use according to claim 16 or method according to claim 17, wherein the inflammatory and autoimmune diseases are selected from the group consisting of rheumatoid arthritis (RA), diabetes mellitus type I, multiple sclerosis, psoriasis, Guillain-Barre syndrome, Crohn's disease, and diseases that are ascribed to undesirable T cell activation reactions, such as “graft-versus-host disease” (GvHD) or “host-versus-graft disease” (HvGD).

### Claim 20 (depends on 1, 2, 3, 4, 5, 6, 7, 9, 10, 11, 13)

Use of the nucleic acid according to any one of claims 1 to 5, of the vector according to claim 6, the host according to claim 7, the binding molecule according to claim 9, and/or of the antibody or fragment or derivative of an antibody according to claim 10 or 11 for the preparation of a diagnostic composition for in-vitro analysis of the responsitivity of a patient to a therapy with a pharmaceutical composition according to claim 13.