# US 11,433,134 B2 · Aqueous formulation of erythropoiesis stimulating protein stabilised by antioxidants for parenteral administration

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- Number: US 11,433,134 B2
- Document ID: US11433134B2
- Status: Granted
- Kind: B2
- Application number: 14/305,450
- Filed: 2014-06-16
- Published: 2014-10-02
- Granted: 2022-09-06
- Earliest claimed: 2007-11-15
- Assignees: Amgen Inc.
- Applicants: Christopher James Sloey; Jason Ko; Tiansheng Li
- Inventors: Christopher James Sloey; Jason Ko; Tiansheng Li
- Web page: https://patentgrep.com/patent/US11433134B2

## CPC

- A61K 47/12: Carboxylic acids; Salts or anhydrides thereof
- 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 38/1816: {Erythropoietin [EPO]}
- A61K 39/3955: {against proteinaceous materials, e.g. enzymes, hormones, lymphokines}
- A61K 39/39591: {Stabilisation, fragmentation}
- A61K 47/22: Heterocyclic compounds, e.g. ascorbic acid, tocopherol or pyrrolidones
- A61P 7/00: Drugs for disorders of the blood or the extracellular fluid
- 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 invention relates to stable aqueous protein formulations. In particular, disclosed herein are therapeutic protein formulations suitable for parenteral administration having one or more antioxidants.

## Claims

### Claim 1

An aqueous formulation comprising (i) an IgG1 antibody and (ii) a concentration of an antioxidant wherein the antioxidant is p-hydroxybenzoic acid, sulisobenzone, vanillic acid, or syringic acid, or a pharmaceutically acceptable salt or ester thereof, or mixtures thereof;
when the antioxidant is sulisobenzone, the antioxidant is present in the aqueous formulation at a concentration of about 5 mM,
when the antioxidant is p-hydroxybenzoic acid, vanillic acid or syringic acid, the antioxidant is present in the aqueous formulation at a concentration of about 20 mM,
wherein the antibody exhibits less than about 10% degradation as determined by exposure for about 3 hours to a 8 watt mid UV lamp having a spectral distribution from 270 nm to 360 nm with a maximum energy emission of about 302 nm and
wherein the formulation is suitable for parenteral administration.

### Claim 2 (depends on 1)

The aqueous formulation of claim 1, wherein the antibody has a concentration of at least 0.1 mg/mL.

### Claim 3 (depends on 2)

The aqueous formulation of claim 2, wherein the antibody has a concentration of about 1 to about 250 mg/mL.

### Claim 4 (depends on 1)

The aqueous formulation of claim 1, wherein the antibody is a monoclonal antibody.

### Claim 5 (depends on 1)

The aqueous formulation of claim 1, wherein the antibody exhibits less than 2% degradation.

### Claim 6

An aqueous formulation comprising (i) an antibody and (ii) a concentration of an antioxidant wherein the antioxidant is vanillic acid or syringic acid, or a pharmaceutically acceptable salt or ester thereof, or mixtures thereof and the antibody has a concentration of a least 0.1 mg/mL,
wherein the antioxidant is present in the aqueous formulation at a concentration of about 20 mM,
wherein the antibody exhibits less than about 10% degradation as determined by exposure for about 3 hours to a 8 watt mid UV lamp having a spectral distribution from 270 nm to 360 nm with a maximum energy emission of about 302 nm, and
wherein the formulation is suitable for parenteral administration.

### Claim 7 (depends on 6)

The aqueous formulation of claim 6, wherein the antibody has a concentration of about 1 to about 250 mg/mL.

### Claim 8 (depends on 6)

The aqueous formulation of claim 6, wherein the antibody is a monoclonal antibody.

### Claim 9 (depends on 8)

The aqueous formulation of claim 8, wherein the antibody is an IgG1 antibody.

### Claim 10 (depends on 6)

The aqueous formulation of claim 6, wherein the antibody exhibits less than 2% degradation.