# US 2020/0399380 A1 · Compositions and methods for treating pain in subjects with rheumatoid arthritis

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- Number: US 2020/0399380 A1
- Document ID: US20200399380A1
- Status: Published application
- Kind: A1
- Application number: 16/891,984
- Filed: 2020-06-03
- Published: 2020-12-24
- Earliest claimed: 2019-06-04
- Assignees: Regeneron Pharmaceuticals, Inc.
- Applicants: Sanofi Biotechnology; Regeneron Pharmaceuticals, Inc.
- Inventors: Susan Boklage; Toshio Kimura; Stefano Fiore; Gregory St John; Wenhui Wei; Vivian Bykerk
- Web page: https://patentgrep.com/patent/US20200399380A1

## CPC

- C07K 16/2866: {against receptors for cytokines, lymphokines, interferons}
- A61K 9/0019: {Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner (non-active ingredients are additionally classified in A61K47/00)}
- A61P 29/00: Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- C07K 16/241: {Tumor Necrosis Factors}
- A61K 2039/505: {comprising antibodies}
- A61K 2039/545: {characterised by the dose, timing or administration schedule}
- C07K 2317/21: from primates, e.g. man
- C07K 2317/565: Complementarity determining region [CDR]
- C07K 2317/76: Antagonist effect on antigen, e.g. neutralization or inhibition of binding
- 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 relates to the use of an anti-IL6 receptor antibody for treating unacceptable pain in subjects with rheumatoid arthritis. Subjects with unacceptable pain can have, e.g., refractory pain or strict refractory pain.

## Claims

### Claim 1

A method for treating unacceptable pain (UP) in a subject in need thereof who has rheumatoid arthritis, comprising administration of a therapeutically effective dose of an antibody that specifically binds IL-6 receptor, wherein the antibody comprises a heavy chain variable region comprising complementarity determining regions HCDR1, HCDR2, and HCDR3 and a light chain variable region comprising complementary determining regions LCDR1, LCDR2, and LCDR3, wherein:
(a) HCDR1 comprises the amino acid sequence of SEQ ID NO: 3;
(b) HCDR2 comprises the amino acid sequence of SEQ ID NO: 4;
(c) HCDR3 comprises the amino acid sequence of SEQ ID NO: 5;
(d) LCDR1 comprises the amino acid sequence of SEQ ID NO: 6;
(e) LCDR2 comprises the amino acid sequence of SEQ ID NO: 7; and
(f) LCDR3 comprises the amino acid sequence of SEQ ID NO: 8.

### Claim 2 (depends on 1)

The method of claim 1, wherein the antibody that specifically binds to the IL-6 receptor comprises a heavy chain variable region sequence SEQ ID NO: 1 and a light chain variable region sequence of SEQ ID NO: 2.

### Claim 3 (depends on 1)

The method of claim 1, wherein the subject has refractory pain (RP) or strict RP.

### Claim 4

(canceled)

### Claim 5 (depends on 1)

The method of claim 1, wherein the subject experiences a reduction in visual analog scale (VAS) to less than 40 mm after 24 weeks of treatment.

### Claim 6

(canceled)

### Claim 7 (depends on 1)

The method of claim 1, wherein the subject has a Disease Activity Score (DAS) of from 3.2 to 5.1.

### Claim 8 (depends on 1)

The method of claim 1, wherein the subject has a DAS of greater than 5.1.

### Claim 9

(canceled)

### Claim 10 (depends on 1)

The method of claim 1, wherein the subject is administered subcutaneously at a dose of about 150 mg or about 200 mg of the antibody at least once every two weeks.

### Claim 11

(canceled)

### Claim 12 (depends on 1)

The method of claim 1, wherein inflammation in the subject has been reduced by a disease-modifying antirheumatic drug (DMARD), selected from one or more of methotrexate, etanercept, infliximab, adalimumab, golimumab and certolizumab pegol.

### Claim at position 13

13-20. (canceled)

### Claim 21 (depends on 1)

The method of claim 1, wherein the subject was previously ineffectively treated for rheumatoid arthritis, or is intolerant of one or more DMARDs, or wherein the subject is considered an inappropriate candidate for continued treatment with by administering at least one DMARD different from the antibody.

### Claim 22 (depends on 21)

The method of claim 21, wherein the DMARD is methotrexate or a TNF-α antagonist.

### Claim at position 16

23-29. (canceled)

### Claim 30

A method for treating unacceptable pain (UP) in a subject in need thereof, comprising
(i) selecting a subject who has rheumatoid arthritis and UP; and
(ii) administering to the subject a therapeutically effective dose of an antibody that specifically binds IL-6 receptor, wherein the antibody comprises a heavy chain variable region comprising complementarity determining regions HCDR1, HCDR2, and HCDR3 and a light chain variable region comprising complementary determining regions LCDR1, LCDR2, and LCDR3, wherein:
(a) HCDR1 comprises the amino acid sequence of SEQ ID NO: 3;
(b) HCDR2 comprises the amino acid sequence of SEQ ID NO: 4;
(c) HCDR3 comprises the amino acid sequence of SEQ ID NO: 5;
(d) LCDR1 comprises the amino acid sequence of SEQ ID NO: 6;
(e) LCDR2 comprises the amino acid sequence of SEQ ID NO: 7; and
(f) LCDR3 comprises the amino acid sequence of SEQ ID NO: 8.

### Claim 31 (depends on 30)

The method of claim 30, wherein the antibody that specifically binds to the IL-6 receptor comprises a heavy chain variable region sequence SEQ ID NO: 1 and a light chain variable region sequence of SEQ ID NO: 2.

### Claim 32 (depends on 30)

The method of claim 30, wherein the subject has refractory pain (RP) or strict RP.

### Claim 33

(canceled)

### Claim 34 (depends on 30)

The method of claim 30, wherein the subject experiences a reduction in visual analog scale (VAS) to less than 40 mm after 24 weeks of treatment.

### Claim 35

(canceled)

### Claim 36 (depends on 30)

The method of claim 30, wherein the subject has a Disease Activity Score (DAS) of from 3.2 to 5.1.

### Claim 37 (depends on 30)

The method of claim 30, wherein the subject has a DAS of greater than 5.1.

### Claim 38

(canceled)

### Claim 39 (depends on 30)

The method of claim 30, wherein the subject is administered a dose of about 150 mg or about 200 mg of the antibody at least once every two weeks, subcutaneously.

### Claim 40

(canceled)

### Claim 41 (depends on 30)

The method of claim 30, wherein the inflammation in the subject has been reduced by a disease-modifying antirheumatic drug (DMARD), wherein the DMARD is selected from one or more of methotrexate, etanercept, infliximab, adalimumab, golimumab and certolizumab pegol.

### Claim at position 29

42-49. (canceled)

### Claim 50 (depends on 41)

The method of claim 41, wherein the subject was previously ineffectively treated for rheumatoid arthritis or wherein the subject is considered an inappropriate candidate for continued treatment with one or more DMARDs or has an inadequate response to one or more DMARD different from the antibody.

### Claim 51 (depends on 50)

The method of claim 50, wherein the DMARD is methotrexate or a TNF-α antagonist.

### Claim at position 32

52-87. (canceled)