# US 12,178,915 B2 · High concentration formulations of anti-CSF1 and anti-CSF1R antibodies

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- Number: US 12,178,915 B2
- Document ID: US12178915B2
- Status: Granted
- Kind: B2
- Application number: 17/747,844
- Filed: 2022-05-18
- Published: 2022-11-24
- Granted: 2024-12-31
- Earliest claimed: 2020-12-14
- Assignees: AmMax Bio, Inc.
- Applicants: AmMax Bio, Inc.
- Inventors: Laman Alani; Chung-Chiang Hsu; Aihua Zhu; Kirk William Johnson; Michael Huang
- Web page: https://patentgrep.com/patent/US12178915B2

## CPC

- A61K 9/19: lyophilised {, i.e. freeze-dried, solutions or dispersions (lyophilised products with subsequent particle size reduction A61K9/14; granules or pellets made by lyphilisation A61K9/1682; solid oral dosage forms made by lyophilisation A61K9/2095; lyophilisation additives A61K47/00)}
- 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 39/39591: {Stabilisation, fragmentation}
- A61K 47/183: {Amino acids, e.g. glycine, EDTA or aspartame}
- A61K 47/26: Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
- C07K 16/243: {Colony Stimulating Factors}
- C07K 16/2866: {against receptors for cytokines, lymphokines, interferons}
- A61K 2039/545: {characterised by the dose, timing or administration schedule}
- 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)
- 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

Provided are high concentration stable formulations of anti-CSF1R/CSF1 antibodies. An example formulation includes 105 to 250 mg/mL of the antibody, 100 mM to 200 mM of arginine glutamate or arginine HCl, 10 mM to 50 mM histidine, and 0.015 to 0.035 w/v % of polysorbate 80, at a pH of 5.4 to 5.6. Also provided are methods of using the formulations for treating diseases.

## Claims

### Claim 1

An aqueous pharmaceutical composition comprising at least 105 mg/mL of an antibody, a salt of arginine selected from the group consisting of arginine glutamate, arginine aspartate, and arginine HCl, histidine, and polysorbate (PS) selected from the group consisting of PS 80 and PS 20, at a pH of 5.0-6.0, wherein the antibody comprises a heavy chain comprising the amino acid sequence of SEQ ID NO:7 and a light chain comprising the amino acid sequence of SEQ ID NO:8.

### Claim 2 (depends on 1)

The aqueous pharmaceutical composition of claim 1, wherein the pH is 5.45 to 5.6.

### Claim 3 (depends on 2)

The aqueous pharmaceutical composition of claim 2, which comprises at least 140 mg/mL of the antibody.

### Claim 4 (depends on 1)

The aqueous pharmaceutical composition of claim 1, wherein the salt of arginine is arginine HCl.

### Claim 5 (depends on 1)

The aqueous pharmaceutical composition of claim 1, wherein the arginine HCl is present at a concentration of 100 mM to 200 mM.

### Claim 6 (depends on 1)

The aqueous pharmaceutical composition of claim 1, wherein the histidine is present at a concentration of 10 mM to 50 mM.

### Claim 7 (depends on 1)

The aqueous pharmaceutical composition of claim 1, wherein the polysorbate is present at a concentration of 0.01 to 0.04 w/v %.

### Claim 8 (depends on 1)

The aqueous pharmaceutical composition of claim 1, which does not include lysine.

### Claim 9 (depends on 8)

The aqueous pharmaceutical composition of claim 8, which does not include any of sucrose, acetate, NaCl, citrate, sugar, polyol, succinate, proline, or sorbitol.

### Claim 10 (depends on 1)

A solid composition that is lyophilized from the aqueous pharmaceutical composition of claim 1, or that forms the aqueous pharmaceutical composition of claim 1 when admixed with water.