# US 9,750,752 B2 · Subcutaneously administered anti-IL-6 receptor antibody

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- Number: US 9,750,752 B2
- Document ID: US9750752B2
- Status: Granted
- Kind: B2
- Application number: 14/062,026
- Filed: 2013-10-24
- Published: 2014-02-27
- Granted: 2017-09-05
- Earliest claimed: 2010-11-08
- Assignees: Hoffmann-La Roche Inc.; Chugai Seiyaku Kabushiki Kaisha
- Applicants: Hoffmann-La Roche Inc.; Chugai Seiyaku Kabushiki Kaisha
- Inventors: Xiaoping Zhang; Kimio Terao; Olivier Alfred Harari
- Web page: https://patentgrep.com/patent/US9750752B2

## 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)}
- A61K 31/573: substituted in position 21, e.g. cortisone, dexamethasone, prednisone or aldosterone
- A61K 38/47: acting on glycosyl compounds (3.2), e.g. cellulases, lactases
- A61K 39/39533: {against materials from animals}
- A61K 39/3955: {against proteinaceous materials, e.g. enzymes, hormones, lymphokines}
- A61P 9/00: Drugs for disorders of the cardiovascular system
- A61P 9/14: Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers
- A61P 17/00: Drugs for dermatological disorders
- A61P 17/06: Antipsoriatics
- A61P 21/00: Drugs for disorders of the muscular or neuromuscular system
- A61P 37/00: Drugs for immunological or allergic disorders
- A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- C12Y 302/01035: Hyaluronoglucosaminidase (3.2.1.35), i.e. hyaluronidase
- A61K 2039/505: {comprising antibodies}
- A61K 2039/54: {characterised by the route of administration}
- A61K 2039/545: {characterised by the dose, timing or administration schedule}
- A61K 2300/00: Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
- A61P 19/02: for joint disorders, e.g. arthritis, arthrosis
- A61P 29/00: Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- A61P 37/06: Immunosuppressants, e.g. drugs for graft rejection
- C07K 2317/24: containing regions, domains or residues from different species, e.g. chimeric, humanized or veneered
- C07K 2317/76: Antagonist effect on antigen, e.g. neutralization or inhibition of binding
- C07K 2317/94: Stability, e.g. half-life, pH, temperature or enzyme-resistance
- 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
- C12Y: ENZYMES

## Abstract

The present application discloses methods for treating an IL-6-mediated disorder such as rheumatoid arthritis (RA), juvenile idiopathic arthritis (JIA), systemic JIA (sJIA), polyarticular course JIA (pcJIA), systemic sclerosis, or giant cell arteritis (GCA), with subcutaneously administered antibody that binds interleukin-6 receptor (anti-IL-6R antibody). In particular, it relates to identification of a fixed dose of anti-IL-6R antibody, e.g. tocilizumab, which is safe and effective for subcutaneous administration in patients with IL-6-mediated disorders. In addition, formulations and devices useful for subcutaneous administration of an anti-IL-6R antibody are disclosed.

## Claims

### Claim 1

A method of treating giant cell arteritis (GCA) in a patient comprising administering an anti-IL-6 receptor (IL-6R) antibody to the patient in an amount effective to treat the GCA, wherein the anti-IL-6R antibody is administered subcutaneously as a fixed dose of 162 mg per dose every week or every two weeks, and wherein the anti-IL-6R antibody comprises the light chain and heavy chain amino acid sequences of SEQ ID NOs. 1 and 2, respectively.

### Claim 2 (depends on 1)

The method of claim 1 wherein the fixed dose is administered every week.

### Claim 3 (depends on 1)

The method of claim 1 wherein the fixed dose is administered every two weeks.

### Claim 4 (depends on 1)

The method of claim 1 further comprising administering an initial course of corticosteroid to the patient.

### Claim 5 (depends on 1)

The method of claim 1 wherein the effective amount reduces GCA signs and symptoms, maintains clinical remission, and/or reduces or stops corticosteroid to be administered to the patient.

### Claim 6 (depends on 1)

The method of claim 1 wherein the GCA is new onset GCA.

### Claim 7 (depends on 1)

The method of claim 1 wherein the GCA is refractory GCA.

### Claim 8

A method of treating giant cell arteritis in a patient comprising administering tocilizumab to the patient, wherein the tocilizumab is administered subcutaneously as a fixed dose of 162 mg per dose every week or every two weeks.

### Claim 9 (depends on 8)

The method of claim 8 wherein the fixed dose is administered every week.

### Claim 10 (depends on 8)

The method of claim 8 wherein the fixed dose is administered every two weeks.

### Claim 11 (depends on 8)

The method of claim 8 further comprising administering an initial course of corticosteroid to the patient.

### Claim 12 (depends on 8)

The method of claim 8 wherein the treatment reduces giant cell arteritis signs and symptoms in the patient.

### Claim 13 (depends on 8)

The method of claim 8 wherein the treatment maintains clinical remission in the patient.

### Claim 14 (depends on 8)

The method of claim 8 wherein the treatment reduces or stops corticosteroid to be administered to the patient.

### Claim 15 (depends on 8)

The method of claim 8 wherein the giant cell arteritis (GCA) is new onset GCA.

### Claim 16 (depends on 8)

The method of claim 8 wherein the giant cell arteritis (GCA) is refractory GCA.