US2011226650A1PendingUtilityA1
Antibody formulation
Est. expiryDec 21, 2029(~3.4 yrs left)· nominal 20-yr term from priority
A61P 35/04A61P 35/02A61P 3/10A61P 35/00A61P 9/00A61P 9/10A61P 27/02A61P 29/00A61P 19/02A61P 11/06A61P 17/06A61P 1/04A61P 13/12A61K 47/183A61K 47/22A61K 39/39591A61K 9/0019C07K 2317/94C07K 16/22A61K 2039/505A61K 47/26A61K 9/08A61J 1/1412A61K 39/395A61K 39/3955C07K 2317/76A61J 1/2006A61K 2300/00
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Claims
Abstract
The invention provides a stable aqueous pharmaceutical formulation comprising a therapeutically effective amount of an antibody, optionally, not subjected to prior lyophilization, a buffer maintaining the pH in the range from about 4.0 to about 6.0, and an optional surfactant, methods for making such a formulation, and methods of using such a formulation.
Claims
exact text as granted — not AI-modified1 . A stable aqueous pharmaceutical formulation, the formulation comprising a therapeutically effective amount of an antibody in an arginine buffer, pH 4.0 to 6.0.
2 . The formulation of claim 1 , wherein the buffer is an arginine acetate buffer, pH 4.5 to 5.5.
3 . The formulation of claim 1 , wherein the buffer is an arginine acetate buffer, pH 4.8 to 5.4.
4 . The formulation of claim 1 , wherein the buffer is an arginine acetate buffer, pH 5.2.
5 . The formulation of claims 2 , 3 , or 4 wherein the arginine actetate concentration in the buffer is from about 25 mM to about 250 mM.
6 . The formulation of claims 2 , 3 , or 4 wherein the arginine actetate concentration in the buffer is from about 50 mM to about 250 mM.
7 . The formulation of claims 2 , 3 , or 4 wherein the arginine actetate concentration in the buffer is from about 75 mM to about 250 mM.
8 . The formulation of claims 2 , 3 , or 4 wherein the arginine actetate concentration in the buffer is from about 100 mM to about 250 mM.
9 . The formulation of claims 2 , 3 , or 4 , wherein the arginine acetate concentration in the buffer is from about 120 mM to about 240 mM.
10 . The formulation of claims 2 , 3 , or 4 , wherein arginine acetate concentration in the buffer is from about 150 mM to about 225 mM.
11 . The formulation of claims 2 , 3 , or 4 , wherein the arginine acetate concentration in the buffer is about 200 mM.
12 . The formulation of claim 1 , further comprising a surfactant.
13 . The formulation of claim 12 , wherein the surfactant is polysorbate.
14 . The formulation of claim 13 , wherein the polysorbate is polysorbate 20.
15 . The formulation of claim 12 , wherein the surfactant concentration is from 0.0001% to about 1.0%.
16 . The formulation of claim 12 , wherein the surfactant concentration is from about 0.01% to about 0.05%.
17 . The formulation of claim 12 , wherein the surfactant concentration is 0.04%.
18 . The formulation of claim 1 , wherein the antibody concentration is from about 10 mg/ml to about 250 mg/ml.
19 . The formulation of claim 1 , wherein the antibody concentration is from about 25 mg/ml to 200 mg/ml.
20 . The formulation of claim 1 , wherein the antibody concentration is from about 50 mg/ml to about 150 mg/ml.
21 . The formulation of claim 1 , wherein the antibody concentration is from about 75 mg/ml to about 125 mg/ml.
22 . The formulation of claim 1 , wherein the antibody is not subject to prior lyophilization.
23 . The formulation of claim 1 wherein the antibody binds VEGF.
24 . The formulation of claim 1 , wherein the antibody is a monoclonal antibody.
25 . The formulation of claim 24 wherein the monoclonal antibody is a full length antibody.
26 . The formulation of claim 24 wherein the monoclonal antibody is an IgG1 antibody.
27 . The formulation of claim 24 wherein the monoclonal antibody is a humanized antibody.
28 . The formulation of claim 24 wherein the monoclonal antibody is an antibody fragment comprising an antigen-binding region.
29 . The formulation of claim 28 wherein the antibody fragment is a Fab or F(ab′)2 fragment.
30 . The formulation of claim 24 wherein the monoclonal antibody binds VEGF.
31 . The formulation of claim 30 wherein the antibody is bevacizumab.
32 . The formulation of claim 1 wherein the monoclonal antibody is susceptible to aggregation.
33 . The formulation of claim 2 wherein the buffer is 200 mM arginine acetate pH 5.2, the surfactant is polysorbate in an amount of about 0.01-0.1% v/v, wherein the formulation is stable at a temperature of about 40° C. for at least 28 days
34 . An article of manufacture comprising a container holding a stable aqueous pharmaceutical formulation comprising a therapeutically effective amount of an antibody, an arginine acetate buffer from about pH 4.5 to about 6.0, and a surfactant.
35 . The article of manufacture of claim 34 , wherein the antibody binds VEGF.
36 . The article of manufacture of claim 35 , wherein the antibody is bevacizumab.
37 . A method for stabilizing an antibody in an aqueous pharmaceutical formulation by combining a therapeutically effective amount of an antibody, an arginine acetate buffer from about pH 4.5 to about 6.0, and a surfactant.
38 . The method of claim 37 , wherein the antibody binds VEGF.
39 . The method of claim 38 , wherein the antibody is bevacizumab.
40 . A stable aqueous pharmaceutical formulation comprising a therapeutically effective amount of an antibody, 200 mM arginine acetate buffer at pH 5.2, and a surfactant.
41 . The formulation of claim 40 wherein the antibody binds VEGF.
42 . The formulation of claim 41 wherein the antibody is bevacizumab
43 . An article of manufacture comprising a container holding the formulation of any one of claims 40 - 42 .
44 . The formulation of claim 1 which is sterile.
45 . The formulation of claim 1 which is stable upon storage at about 40° C. for at least 28 days.
46 . The formulation of claim 1 which is aqueous and is administered to a subject.
47 . The formulation of claim 46 wherein the formulation is for intravenous (IV), subcutaneous (SQ) or intramuscular (IM) administration.
48 . The formulation of claim 46 , which is for W administration and the antibody concentration is from about 10 mg/ml to about 250 mg/ml.
49 . The formulation of claim 46 , which is for IV administration and the antibody concentration is from about 50 mg/ml to about 100 mg/ml.
50 . The formulation of claim 46 , which is for SQ administration and the antibody concentration is from about 25 mg/ml to about 250 mg/ml.
51 . The formulation of claim 46 , which is for SQ administration and the antibody concentration is from about 50 mg/ml to about 100 mg/ml.
52 . A vial with a stopper pierceable by a syringe comprising the formulation of claim 1 inside the vial.
53 . The vial of claim 52 which is stored at about 2-8° C.
54 . The vial of claim 52 which is a 3 cc, 20 cc or 50 cc vial.
55 . A stainless steel tank comprising the formulation of claim 1 inside the tank.
56 . The tank of claim 55 wherein the formulation is frozen.
57 . A method of treating a disease or disorder in a subject comprising administering the formulation of claim 1 to a subject in an amount effective to treat the disease or disorder.
58 . The method of claim 57 wherein the antibody binds VEGF.
59 . The method of claim 58 wherein the antibody is bevacizumab
60 . A pharmaceutical formulation comprising: (a) a full length IgG1 antibody susceptible to deamidation or aggregation in an amount from about 10 mg/mL to about 250 mg/mL; (b) arginine acetate buffer, pH 4.5 to 6.0; and (c) polysorbate 20 in an amount from about 0.01% to about 0.1%.
61 . The formulation of claim 60 wherein the antibody binds VEGF.
62 . The formulation of claim 61 wherein the antibody is bevacizumab
63 . A method for reducing aggregation of a therapeutic monoclonal antibody, comprising formulating the antibody in an arginine acetate buffer, pH 4.5 to 6.0.
64 . The method of claim 63 wherein the antibody binds VEGF.
65 . The method of claim 64 wherein the antibody is bevacizumab.
66 . A pharmaceutical formulation comprising an antibody that binds to VEGF in an arginine acetate buffer at a pH from about 4.5 to about 6.0, and a surfactant.
67 . The formulation of claim 66 wherein the antibody is bevacizumab.
68 . A method of making a pharmaceutical formulation comprising:
(a) preparing the formulation of claim 1 ; and (b) evaluating physical stability, chemical stability, or biological activity of the antibody in the formulation.
69 . The method of claim 68 , wherein the antibody binds VEGF.
70 . The method of claim 69 , wherein the antibody is bevacizumabJoin the waitlist — get patent alerts
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