# US 10,370,443 B2 · Method of treating autoimmune disease by administering antibodies to interleukin-6

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- Number: US 10,370,443 B2
- Document ID: US10370443B2
- Status: Granted
- Kind: B2
- Application number: 15/687,085
- Filed: 2017-08-25
- Published: 2017-12-21
- Granted: 2019-08-06
- Earliest claimed: 2012-10-22
- Assignees: Fountain Biopharma Inc.
- Applicants: Fountain Biopharma Inc.
- Inventors: Tong-Young Lee; Han-Chung Wu; Tanny Chen Tsao; Willie Lin
- Web page: https://patentgrep.com/patent/US10370443B2

## CPC

- C07K 16/248: {IL-6}
- A61K 31/282: Platinum compounds
- A61K 31/337: having four-membered rings, e.g. taxol
- A61K 31/7068: having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
- A61K 39/3955: {against proteinaceous materials, e.g. enzymes, hormones, lymphokines}
- A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
- A61P 1/00: Drugs for disorders of the alimentary tract or the digestive system
- A61P 1/02: Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
- A61P 1/04: for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
- A61P 9/00: Drugs for disorders of the cardiovascular system
- A61P 11/00: Drugs for disorders of the respiratory system
- A61P 13/08: of the prostate
- A61P 15/00: Drugs for genital or sexual disorders (for disorders of sex hormones A61P5/24); Contraceptives
- 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 35/00: Antineoplastic agents
- A61P 35/02: specific for leukemia
- A61P 35/04: specific for metastasis
- A61P 37/00: Drugs for immunological or allergic disorders
- A61P 37/02: Immunomodulators
- A61P 37/06: Immunosuppressants, e.g. drugs for graft rejection
- A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- A61K 2039/505: {comprising antibodies}
- 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 2317/54: F(ab')2
- C07K 2317/55: Fab or Fab'
- C07K 2317/565: Complementarity determining region [CDR]
- C07K 2317/622: Single chain antibody (scFv)
- C07K 2317/73: Inducing cell death, e.g. apoptosis, necrosis or inhibition of cell proliferation
- 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)
- 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)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## Abstract

The present disclosure provides antibodies that bind to human interleukin-6 (IL6). The antibodies can modulate IL6 signaling and thus used in treatment or prevention of IL6 associated diseases or disorders, particularly inflammatory disorder, rheumatoid arthritis (RA), angiogenesis, and cancer.

## Claims

### Claim 1

A method for treating an autoimmune disease associated with IL-6, comprising administering to a subject in need thereof a therapeutically effective amount of an antibody that binds human interleukin 6 (IL6), wherein the antibody comprises:
(a) a heavy chain variable region (VH), which comprises a heavy chain complementary determining region 1 (HC CDR1) of SEQ ID NO: 2, a heavy chain complementary determining region 2 (HC CDR2) of SEQ ID NO: 4, and a heavy chain complementary determining region 3 (HC CDR3) of SEQ ID NO: 6 or SEQ ID NO: 16; or
(b) a light chain variable region (VL), which comprises a light chain complementary determining region 1 (LC CDR1) of SEQ ID NO: 9, a light chain complementary determining region 2 (LC CDR2) of SEQ ID NO: 11, and a light chain complementary determining region 3 (LC CDR3) of SEQ ID NO: 13 or SEQ ID NO: 15.

### Claim 2 (depends on 1)

The method of claim 1, wherein the subject has an autoimmune disease, which is selected from the group consisting of rheumatoid arthritis, Crohn's disease, psoriatic arthritis and psoriasis.

### Claim 3 (depends on 2)

The method of claim 2, wherein the amount of the antibody is effective in reducing production of inflammatory cytokines in the subject.

### Claim 4 (depends on 2)

The method of claim 2, wherein the autoimmune disease is rheumatoid arthritis and the method further comprises administering to the subject a disease modifying anti-rheumatic drug (DMARD).

### Claim 5 (depends on 4)

The method of claim 4, wherein the DMARD is selected from the group consisting of methotrexate, azathioprine, chloroquine, hydroxychloroquine, cyclosporine A, and sulfasalazine.

### Claim 6 (depends on 1)

The method of claim 1, wherein the antibody comprises (i) a VH that comprises the HC CDR1 of SEQ ID NO: 2, the HC CDR2 of SEQ ID NO: 4, and the HC CDR3 of SEQ ID NO: 6; or (ii) a VH that comprises the HC CDR1 of SEQ ID NO: 2, the HC CDR2 of SEQ ID NO: 4, and the HC CDR3 of SEQ ID NO: 16.

### Claim 7 (depends on 1)

The method of claim 1, wherein the VH comprises the amino acid sequence of SEQ ID NO: 17 or SEQ ID NO: 18.

### Claim 8 (depends on 1)

The method of claim 1, wherein the antibody comprises (i) a VL that comprises the LC CDR1 of SEQ ID NO: 9, the LC CDR2 of SEQ ID NO: 11, and the LC CDR3 of SEQ ID NO: 13; or (ii) a VL that comprises the LC CDR1 of SEQ ID NO: 9, the LC CDR2 of SEQ ID NO: 11, and the LC CDR3 of SEQ ID NO: 15.

### Claim 9 (depends on 8)

The method of claim 8, wherein the VL comprises the amino acid sequence of SEQ ID NO: 19 or SEQ ID NO: 20.

### Claim 10 (depends on 1)

The method of claim 1, wherein the antibody is selected from the group consisting of:
(i) an antibody comprising a VH that comprises the HC CDR1 of SEQ ID NO: 2, the HC CDR2 of SEQ ID NO: 4, and the HC CDR3 of SEQ ID NO: 6; and a VL that comprises the LC CDR1 of SEQ ID NO: 9, the LC CDR2 of SEQ ID NO: 11, and the CDR3 of SEQ ID NO: 13;
(ii) an antibody comprising a VH that comprises the HC CDR1 of SEQ ID NO: 2, the HC CDR2 of SEQ ID NO: 4, and the HC CDR3 of SEQ ID NO: 16, and a VL that comprises the LC CDR1 of SEQ ID NO: 9, the LC CDR2 of SEQ ID NO: 11, and the CDR3 of SEQ ID NO: 13;
(iii) an antibody comprising a VH that comprises the HC CDR1 of SEQ ID NO: 2, the HC CDR2 of SEQ ID NO: 4, and the HC CDR3 of SEQ ID NO: 6, and a VL that comprises the LC CDR1 of SEQ ID NO: 9, the LC CDR2 of SEQ ID NO: 11, and the CDR3 of SEQ ID NO: 15; and
(iv) an antibody comprising a VH that comprises the HC CDR1 of SEQ ID NO: 2, the HC CDR2 of SEQ ID NO: 4, and the HC CDR3 of SEQ ID NO: 16, and a VL that comprises the LC CDR1 of SEQ ID NO: 9, the LC CDR2 of SEQ ID NO: 11, and the CDR3 of SEQ ID NO: 15.

### Claim 11 (depends on 10)

The method of claim 10, wherein the antibody is selected from the group consisting of:
(i) an antibody comprising a VH that comprises the amino acid sequence of SEQ ID NO: 17, and a VL that comprises the amino acid sequence of SEQ ID NO: 19;
(ii) an antibody comprising a VH that comprises the amino acid sequence of SEQ ID NO: 17, and a VL that comprises the amino acid sequence of SEQ ID NO: 20; and
(iii) an antibody comprising a VH that comprises the amino acid sequence of SEQ ID NO: 18, and a VL that comprises the amino acid sequence of SEQ ID NO: 19; and
(iv) an antibody comprising a VH that comprises the amino acid sequence of SEQ ID NO: 18, and a VL that comprises the amino acid sequence of SEQ ID NO: 20.

### Claim 12 (depends on 1)

The method of claim 1, wherein the antibody is a full-length antibody or an antigen-binding fragment thereof.

### Claim 13 (depends on 12)

The method of claim 12, wherein the antigen-binding fragment of the antibody is Fab or (Fab′)2.

### Claim 14 (depends on 1)

The method of claim 1, wherein the antibody is a single chain antibody.

### Claim 15 (depends on 1)

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