US2015209431A1PendingUtilityA1

Antibody and protein formulations

69
Assignee: BAYER HEALTHCARE LLCPriority: Aug 31, 2012Filed: Aug 28, 2013Published: Jul 30, 2015
Est. expiryAug 31, 2032(~6.1 yrs left)· nominal 20-yr term from priority
Inventors:Xinghang MaJun Xiang
A61K 39/39591A61K 39/3955C07K 16/18C07K 2317/94A61P 7/04C07K 16/38A61K 47/22A61K 2039/505A61K 9/19A61K 47/183C07K 2317/41A61K 9/0019A61K 47/20A61K 39/395A61K 47/26
69
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Claims

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.

Claims

exact text as granted — not AI-modified
What is claimed is: 
     
         1 . A salt-free protein or 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. 0 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 antibody;   wherein said protein or 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 salt-free protein or antibody formulation of  claim 1  wherein said formulation has a viscosity ranging from 1 to 8 mPa-S at 22° C. 
     
     
         3 . The salt-free protein or antibody formulation of  claim 1  wherein said formulation has and osmolality ranging from 240 to 380 mmol/kg. 
     
     
         4 . The salt-free protein or antibody formulation of any of  claim 1  wherein said non-ionic surfactant is a polysorbate selected from polysorbate 20 and polysorbate 80. 
     
     
         5 . The salt-free protein or antibody formulation of  claim 1  wherein said sugar is sucrose. 
     
     
         6 . The salt-free protein or antibody formulation of  claim 1  comprising between 10 mM and 50 mM arginine. 
     
     
         7 . The salt-free protein or antibody formulation of  claim 1 , comprising:
 a. 30 mM histidine,   b. 100 ppm polysorbate 80,   c. 292 mM sucrose, and   d. 20 mg/ml protein or antibody;   wherein said protein or antibody formulation has a pH ranging from pH 5.0 to pH 6.0.   
     
     
         8 . The salt-free protein or antibody formulation of  claim 1 , comprising:
 a. 10 mM histidine,   b. 75 ppm polysorbate 80,   c. 234 mM sucrose,   d. 50 mg/ml protein or antibody;   wherein said protein or antibody formulation has a pH ranging from pH 5.0 to pH 6.0.   
     
     
         9 . The salt-free protein or antibody formulation of  claim 1 , comprising:
 a. 10 mM histidine,   b. 75 ppm polysorbate 80,   c. 234 mM sucrose, and   d. 100 mg/ml protein or antibody;   wherein said protein or antibody formulation has a pH ranging from pH 5.0 to pH 6.0.   
     
     
         10 . The salt-free protein or antibody formulation of  claim 1 , comprising:
 a. 10 mM histidine,   b. 75 ppm polysorbate 80,   c. 88 mM sucrose,   d. 133 mM glycine, and   e. 100 mg/ml protein or antibody;   wherein said protein or antibody formulation has a pH ranging from pH 5.0 to pH 6.0.   
     
     
         11 . The salt-free protein or antibody formulation of  claim 1 , comprising:
 a. 10 mM histidine,   b. 75 ppm polysorbate 20,   c. 88 mM sucrose,   d. 133 mM glycine, and   e. 100 mg/ml protein or antibody;   wherein said protein or antibody formulation has a pH ranging from pH 5.0 to pH 6.0.   
     
     
         12 . The salt-free protein or antibody formulation of  claim 1 , comprising:
 a. 10 mM histidine,   b. 200 ppm polysorbate 20,   c. 88 mM sucrose,   d. 133 mM glycine, and   e. 100 mg/ml protein or antibody;   wherein said protein or antibody formulation has a pH ranging from pH 5.0 to pH 6.0.   
     
     
         13 . The salt-free protein or antibody formulation of  claim 1 , comprising:
 a. 10 mM histidine,   b. 75 ppm polysorbate 80,   c. 88 mM sucrose, and   d. 100 mg/ml protein or antibody;   wherein said protein or antibody formulation has a pH ranging from pH 5.0 to pH 6.0.   
     
     
         14 . The salt-free protein or antibody formulation of  claim 1 , comprising:
 a. 10 mM histidine,   b. 75 ppm polysorbate 80,   c. 88 mM sucrose,   d. 10 mM arginine, and   e. 100 mg/ml protein or antibody;   wherein said protein or antibody formulation has a pH ranging from pH 5.0 to pH 6.0.   
     
     
         15 . The salt-free protein or antibody formulation of  claim 1 , comprising 5 mM to 10 mM methionine. 
     
     
         16 . The salt-free protein or antibody formulation of  claim 1 , comprising:
 a. 10 mM histidine,   b. 75 ppm polysorbate 80,   c. 88 mM sucrose,   d. 30 mM lysine, and   e. 100 mg/ml protein or antibody;   wherein said protein or antibody formulation has a pH ranging from pH 5.0 to pH 6.0.   
     
     
         17 . A salt-free anti-TFPI 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. 0 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 anti-TFPI antibody;   wherein said anti-TFPI antibody formulation has a pH of pH 4.0 to pH 6.0 and wherein said anti-TFPI antibody formulation contains substantially no inorganic salt.   
     
     
         18 . The salt-free anti-TFPI antibody formulation of  claim 17  wherein said formulation has a viscosity ranging from 1 to 8 mPa-S at 22° C. 
     
     
         19 . The salt-free anti-TFPI antibody formulation of  claim 17  wherein said formulation has and osmolality ranging from 240 to 380 mmol/kg. 
     
     
         20 . The salt-free anti-TFPI antibody formulation of  claims 17  wherein said non-ionic surfactant is a polysorbate selected from polysorbate 20 and polysorbate 80. 
     
     
         21 . The salt-free anti-TFPI antibody formulation of  claim 17  wherein said sugar is sucrose. 
     
     
         22 . The salt-free anti-TFPI antibody formulation of  claim 17 , comprising:
 a. 10 mM histidine,   b. 75 ppm Tween 80,   c. 234 mM sucrose,   d. 30 mM arginine, and   e. 10 mM methionine, and   f. 100 mg/ml anti-TFPI antibody;   wherein said anti-TFPI antibody formulation has a pH of 5.5.   
     
     
         23 . The salt-free anti-TFPI antibody formulation of  claim 17  wherein said anti-TFPI antibody is a human IgG 2  monoclonal antibody. 
     
     
         24 . The salt-free anti-TFPI antibody formulation of  claim 17  wherein said human IgG 2  monoclonal antibody comprises 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. 
     
     
         25 . A method for the treatment of a disorder in a patient, said method comprising administering to said patient a therapeutically effective amount of a protein or antibody formulation comprising between 10 mM and 30 mM histidine, between 50 ppm and 200 ppm polysorbate 80 or polysorbate 20, between 88 mM and 292 mM sucrose, between 0 mM and 50 mM arginine, between 0 mM and 50 mM lysine, between 0 mM and 133 mM glycine, between 0 mM and 10 mM methionine, and between 1 mg/ml and 150 mg/ml of a protein or antibody at a pH of between pH 4.0 and pH 6.0, wherein said protein or antibody formulation contains substantially no inorganic salt. 
     
     
         26 . The method of  claim 25  wherein said protein or antibody formulation is administered intravenously, subcutaneously, or intramuscularly. 
     
     
         27 . 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 anti-TFPI antibody formulation that contains between 10 mM and 30 mM histidine, between 50 ppm and 200 ppm polysorbate 80 or polysorbate 20, between 88 mM and 292 mM sucrose, between 0 mM and 50 mM arginine, between 0 mM and 50 mM lysine, between 0 mM and 133 mM glycine, between 0 mM and 10 mM methionine, and between 1 mg/ml and 150 mg/ml of a protein at a pH of between pH 4.0 and pH 6.0, and wherein said anti-TFPI formulation contains substantially no inorganic salt. 
     
     
         28 . The method of  claim 27  wherein said anti-TFPI antibody is a human IgG 2  
 monoclonal antibody. 
 
     
     
         29 . The method of  claim 28  wherein said human IgG 2  monoclonal antibody comprises 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. 
     
     
         30 . The method of  claim 27  wherein said anti-TFPI antibody formulation is administered intravenously, intramuscularly, or subcutaneously.

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