High concentration antibody and protein formulations

Patent metadata

Field	Value
Publication number	US-9849181-B2
Application number	US-201414457408-A
Country	US
Kind code	B2
Filing date	Aug 12, 2014
Priority date	Aug 31, 2012
Publication date	Dec 26, 2017
Grant date	Dec 26, 2017

Abstract

Provided are salt-free antibody and other protein formulations that are substantially isosmotic and of low viscosity. Also provided are methods for the treatment of diseases using the disclosed formulations.

First claim

What is claimed is:

1. A method for the treatment of a disorder in a patient, said method comprising administering to said patient a therapeutically effective amount of an antibody formulation comprising:
a. 10 mM to 30 mM histidine;
b. 50 ppm to 200 ppm of a non-ionic surfactant;
c. 88 mM to 292 mM of a sugar or sugar alcohol selected from mannitol, dextrose, glucose, trehalose, and sucrose;
d. 10 mM to 50 mM arginine;
e. 0 mM to 50 mM lysine;
f. 0 mM to 133 mM glycine or alanine;
g. 0 mM to 10 mM methionine; and
h. 1 mg/ml to 150 mg/ml of a protein or an chimeric, humanized, or human anti-TFPI IgG2 monoclonal antibody comprising a light chain comprising the amino acid sequence of SEQ ID NO: 1 and a heavy chain comprising the amino acid sequence of SEQ ID NO: 2;

wherein said antibody formulation has a pH ranging from pH 4.0 to pH 6.0 and wherein said protein formulation contains substantially no inorganic salt.

2. The method of claim 1 , wherein said antibody formulation is administered intravenously, subcutaneously, or intramuscularly.

3. A method for the treatment of hemophilia A or hemophilia B in a patient, said method comprising administering to said patient a therapeutically effective amount of an antibody formulation comprising:
a. 10 mM to 30 mM histidine;
b. 50 ppm to 200 ppm of a non-ionic surfactant;
c. 88 mM to 292 mM of a sugar or sugar alcohol selected from mannitol, dextrose, glucose, trehalose, and sucrose;
d. 10 mM to 50 mM arginine;
e. 0 mM to 50 mM lysine;
f. 0 mM to 133 mM glycine or alanine;
g. 0 mM to 10 mM methionine; and
h. 1 mg/ml to 150 mg/ml of a protein or an chimeric, humanized, or human anti-TFPI IgG2 monoclonal antibody comprising a light chain comprising the amino acid sequence of SEQ ID NO: 1 and a heavy chain comprising the amino acid sequence of SEQ ID NO: 2;

wherein said antibody formulation has a pH ranging from pH 4.0 to pH 6.0 and wherein-said protein formulation contains substantially no inorganic salt.

4. The method of claim 3 , wherein said antibody formulation is administered intravenously, intramuscularly, or subcutaneously.

Assignees

• Bayer Healthcare Llc

Inventors

• Xiang Jun
• Ma Xinghang

Classifications

• C07K16/38

  against protease inhibitors of peptide structure · CPC title

• A61K39/3955

  against proteinaceous materials, e.g. enzymes, hormones, lymphokines · CPC title

• C07K16/18

  against material from animals or humans · CPC title

• A61K47/183

  Amino acids, e.g. glycine, EDTA or aspartame · CPC title

• A61K2039/505

  comprising antibodies · CPC title