# US 12,178,873 B2 · High concentration antibody formulations

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- Number: US 12,178,873 B2
- Document ID: US12178873B2
- Status: Granted
- Kind: B2
- Application number: 17/326,725
- Filed: 2021-05-21
- Published: 2021-09-09
- Granted: 2024-12-31
- Earliest claimed: 2010-05-14
- Assignees: Amgen Inc.
- Applicants: Amgen Inc.
- Inventors: Timothy David Osslund
- Web page: https://patentgrep.com/patent/US12178873B2

## CPC

- A61K 47/14: Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
- 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 9/08: Solutions {(composition of solutions A61K47/00)}
- A61K 39/3955: {against proteinaceous materials, e.g. enzymes, hormones, lymphokines}
- A61K 39/39591: {Stabilisation, fragmentation}
- A61K 47/12: Carboxylic acids; Salts or anhydrides thereof
- A61K 47/24: containing atoms other than carbon, hydrogen, oxygen, halogen, nitrogen or sulfur, e.g. cyclomethicone or phospholipids
- A61P 1/02: Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
- A61P 19/00: Drugs for skeletal disorders
- A61P 19/08: for bone diseases, e.g. rachitism, Paget's disease
- A61P 19/10: for osteoporosis
- C07K 16/22: against growth factors {; against growth regulators}
- A61K 2039/505: {comprising antibodies}
- C07K 2317/76: Antagonist effect on antigen, e.g. neutralization or inhibition of binding
- 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

Discloses herein are high concentration antibody thrmulations comprising an anti-sclerostin immunoglobulin and an acetate salt and/or an acetate buffer and methods of use.

## Claims

### Claim 1

A sterile liquid formulation comprising:
(a) an anti-sclerostin immunoglobulin at a concentration of from about 70 mg/mL to about 120 mg/mL, wherein the immunoglobulin comprises a set of 6 CDRS set forth in amino acid sequences SEQ ID NOs: 73-78;
(b) calcium acetate, wherein the calcium acetate comprises calcium at a concentration ranging from about 5 mM to about 15 mM; and acetate at a concentration ranging from about 10 mM to about 90 mM; and
(c) a polyol in an amount ranging from about 4% w/v to about 6% w/v.

### Claim 2 (depends on 1)

The sterile liquid formulation of claim 1, that has a total osmolarity of less than about 350 mOsm/L.

### Claim 3 (depends on 1)

The sterile liquid formulation of claim 1, wherein the immunoglobulin is present at a concentration of at least 120 mg/mL.

### Claim 4 (depends on 1)

The sterile liquid formulation of claim 1, wherein the immunoglobulin is present at a concentration of 90 mg/mL.

### Claim 5 (depends on 1)

The sterile liquid formulation of claim 1, wherein the absolute viscosity of the formulation is about 10 cP or less.

### Claim 6 (depends on 1)

The sterile liquid formulation of claim 1, wherein the polyol is sucrose.

### Claim 7 (depends on 1)

The sterile liquid formulation of claim 1, wherein the formulation has a pH ranging from about 5 to about 5.5.

### Claim 8 (depends on 1)

The sterile liquid formulation of claim 1, further comprising (d) a surfactant.

### Claim 9 (depends on 1)

The sterile liquid formulation of claim 1, wherein the immunoglobulin comprises the amino acid sequences of SEQ ID NOs: 86 and 84.

### Claim 10 (depends on 1)

A method of treating osteoporosis in a patient in need thereof comprising administering the formulation of claim 1 to the patient.