# US 11,896,667 B2 · Treatment for bone diseases

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

- Number: US 11,896,667 B2
- Document ID: US11896667B2
- Status: Granted
- Kind: B2
- Application number: 17/020,108
- Filed: 2020-09-14
- Published: 2021-03-04
- Granted: 2024-02-13
- Earliest claimed: 2012-07-05
- Assignees: UCB Pharma S.A.
- Applicants: Ucb Pharma, S.A.
- Inventors: Martyn K. Robinson
- Web page: https://patentgrep.com/patent/US11896667B2

## CPC

- A61K 39/3955: {against proteinaceous materials, e.g. enzymes, hormones, lymphokines}
- A61K 33/42: Phosphorus; Compounds thereof
- A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
- 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 1/14: Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
- A61P 1/16: for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
- A61P 3/00: Drugs for disorders of the metabolism (of the blood or the extracellular fluid A61P7/00)
- A61P 3/02: Nutrients, e.g. vitamins, minerals
- A61P 3/10: for hyperglycaemia, e.g. antidiabetics
- A61P 5/18: of the parathyroid hormones
- A61P 7/06: Antianaemics
- A61P 15/00: Drugs for genital or sexual disorders (for disorders of sex hormones A61P5/24); Contraceptives
- A61P 15/12: for climacteric disorders
- A61P 19/02: for joint disorders, e.g. arthritis, arthrosis
- A61P 19/08: for bone diseases, e.g. rachitism, Paget's disease
- A61P 19/10: for osteoporosis
- A61P 25/00: Drugs for disorders of the nervous system
- A61P 25/02: for peripheral neuropathies
- A61P 25/32: Alcohol-abuse
- A61P 29/00: Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- A61P 31/08: for leprosy
- A61P 35/00: Antineoplastic agents
- A61P 37/02: Immunomodulators
- A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- C07K 16/22: against growth factors {; against growth regulators}
- A61K 2039/505: {comprising antibodies}
- C07K 16/18: against material from animals or humans
- C07K 2317/94: Stability, e.g. half-life, pH, temperature or enzyme-resistance
- 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
- 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)

## Abstract

The invention relates to the treatment of bone disorders. In particular, the invention is directed to the use of a dosing holiday to help overcome the resistance to anti-sclerostin antibodies which develops over time when a plurality of doses of antibody are given to a subject. By giving the subject to be treated such a dosing holiday, the subject may subsequently display an increased response to a subsequent dose of the anti-sclerostin antibody. The subject may be given multiple cycles of a batch of at least two doses of anti-sclerostin antibody and a dosing holiday. In some instances, the subject may be monitored to help determine when to give the dosing holiday. Further, the subject may be given a different treatment for the bone disorder during the dosing holiday from the anti-sclerostin antibody.

## Claims

### Claim 1

A method for treating osteoporosis in a mammalian subject, which method comprises:
(a) administering a batch of at least five doses of an anti-sclerostin antibody to a subject in need of such treatment, wherein the doses in the batch are administered at intervals of three to six weeks, and wherein the anti-sclerostin antibody comprises a CDR-H1 of SEQ ID NO:245, a CDR-H2 of SEQ ID NO:246, a CDR-H3 of SEQ ID NO:247, a CDR-L1 of SEQ ID NO:78, a CDR-L2 of SEQ ID NO:79 and a CDR-L3 of SEQ ID NO: 80;
(b) allowing the subject a dosing holiday that is at least twelve months in length; and
(c) administering to the subject a further batch of at least five doses of the anti-sclerostin antibody after the dosing holiday of (b).

### Claim 2 (depends on 1)

The method of claim 1, wherein the batch of doses in
step (a) comprises from five to twelve doses of the anti-sclerostin antibody.

### Claim 3 (depends on 1)

The method of claim 1, wherein the batch of doses in step (a) comprises from five to seven doses of the anti-sclerostin antibody.

### Claim 4 (depends on 1)

The method of claim 1, wherein step (b) comprises administering a different treatment for osteoporosis during the dosing holiday.

### Claim 5 (depends on 4)

The method of claim 4, wherein the different treatment is an anti-resorptive.

### Claim 6 (depends on 1)

The method of claim 1, wherein the method further comprises:
(d) allowing the subject a further dosing holiday which is at least twelve months in length; and
(e) administering to the subject at least five further doses of the anti-sclerostin antibody; and
optionally repeating steps (d) and (e) one or more further times.

### Claim 7 (depends on 1)

The method of claim 1, wherein the anti-sclerostin antibody comprises heavy chains comprising SEQ ID NO: 378 and light chains comprising SEQ ID NO: 376.

### Claim 8 (depends on 1)

The method of claim 1, wherein the anti-sclerostin antibody comprises heavy chains of SEQ ID NO: 145 or SEQ ID NO: 392 and light chains of SEQ ID NO: 141.

### Claim 9 (depends on 1)

The method of claim 1, wherein the amount of anti-sclerostin antibody administered for each dose is from about 50 to 250 mg.

### Claim 10 (depends on 1)

The method of claim 1, wherein the amount of anti-sclerostin antibody administered for each dose is about 70 mg.

### Claim 11 (depends on 1)

The method of claim 1, wherein the amount of anti-sclerostin antibody administered for each dose is about 140 mg.

### Claim 12 (depends on 1)

The method of claim 1, wherein the amount of anti-sclerostin antibody administered for each dose is about 210 mg.

### Claim 13 (depends on 1)

The method of claim 1, wherein a dose of the anti-sclerostin antibody is administered via multiple injections.

### Claim 14 (depends on 1)

The method of claim 1, wherein the subject is female.

### Claim 15 (depends on 1)

The method of claim 1, wherein the subject is a postmenopausal woman.

### Claim 16

A method for treating osteoporosis in a postmenopausal woman, the method comprising:
(a) administering a batch of at least five doses of an anti-sclerostin antibody to the woman, wherein the doses in the batch are administered at intervals of from three to six weeks, and wherein the anti-sclerostin antibody comprises a CDR-H1 of SEQ ID NO:245, a CDR-H2 of SEQ ID NO:246, a CDR-H3 of SEQ ID NO:247, a CDR-L1 of SEQ ID NO:78, a CDR-L2 of SEQ ID NO:79 and a CDR-L3 of SEQ ID NO: 80;
(b) allowing the woman a dosing holiday of at least twelve months in length; and
(c) administering to the woman a further batch of at least five doses of the anti-sclerostin antibody after the dosing holiday.

### Claim 17 (depends on 16)

The method of claim 16, wherein step (b) further comprises administering a bisphosphonate or denosumab during the dosing holiday.

### Claim 18 (depends on 16)

The method of claim 16, wherein the amount of anti-sclerostin antibody administered for each dose is about 210 mg.

### Claim 19 (depends on 16)

The method of claim 16, wherein a dose of the anti-sclerostin antibody is administered via multiple injections.