IP Library Granted Patent US 11,008,394
Granted Patent B2
US 11,008,394 · App. 16/390,197 · Granted May 18, 2021

High concentration antibody-containing liquid formulation

Inventors: Toshiyuki Morichika (Tokyo, JP); Daisuke Kameoka (Tokyo, JP); Yoshimi Imaeda (Tokyo, JP); Terutoshi Maeda (Tokyo, JP); Oliver Boris Stauch (Freiburg, DE)
Assignees: CHUGAI SEIYAKU KABUSHIKI KAISHA; F. HOFFMANN-LA ROCHE AG
C07K16/2866A61K39/3955A61K39/39591A61K47/183A61K47/20A61K47/26C07K1/14A61K9/0019A61K2039/505C07K2317/24C07K2317/76
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Quick Facts
Patent No.
US 11,008,394
App. No.
16/390,197
Granted
May 18, 2021
Kind
B2
Abstract

The problem to be solved is to provide an antibody-containing formulation which is stable and suited for subcutaneous administration, wherein dimerization and deamidation is prevented during long-term storage. The present application is directed to a stable antibody-containing liquid formulation characterized by containing arginine and methionine.

Claims (16)

1. A method of inhibiting deamidation of a humanized anti-IL-6 receptor antibody MRA in a concentrated liquid formulation of 150 to 200 mg/mL of the antibody, comprising including in the liquid formulation 50 to 300 mM arginine and histidine buffer, pH 6.0.

2. The method of claim 1 , wherein dimerization is also inhibited.

3. The method of claim 1 , wherein the arginine concentration is selected from the group consisting of 50 mM, 1.00 mM, 150 mM, 200 mM, and 300 mM.

4. The method of claim 3 , wherein the arginine concentration is 100 mM.

5. The method of claim 1 , wherein the antibody concentration in the formulation is 180 mg/mL.

6. The method of claim 1 , wherein the formulation further comprises polysorbate 20 or polysorbate 80 at a concentration from 0.005 to 3%.

7. A method of inhibiting deamidation of a humanized anti-IL-6 receptor antibody MRA in a concentrated liquid formulation of 150 to 200 mg/mL, of the antibody, comprising including in the liquid formulation 50 to 300 mM arginine, 0.005 to 3% polysorbate 80, and histidine buffer, pH 6.0.

8. The method of claim 7 , wherein dimerization is also inhibited.

9. The method of claim 7 , wherein the arginine concentration is 100 mM.

10. The method of claim 7 , wherein the antibody concentration in the formulation is 180 mg/mL.

11. A method for formulating humanized anti-IL-6 receptor antibody MRA for use for subcutaneous administration, comprising combining 150 to 200 mg/mL of the antibody with 50 to 300 mM arginine and a histidine buffer pH 6.0 to prepare a liquid formulation, wherein the arginine inhibits dimerization or deamidation of the antibody in the formulation.

12. The method of claim 11 , wherein the arginine concentration is 100 mM.

13. The method of claim 11 , wherein the antibody concentration is 180 mg/mL.

14. A method for formulating humanized anti-IL-6 receptor antibody MRA for use for subcutaneous administration, comprising combining 150 to 200 mg/mL of the antibody with 50 to 300 mM arginine, 0.005 to 3% polysorbate 80 and a histidine buffer pH 6.0 to prepare a liquid formulation, wherein the arginine inhibits dimerization or deamidation of the antibody in the formulation.

15. The method of claim 14 , wherein the arginine concentration is 100 mM.

16. The method of claim 14 , wherein the antibody concentration is 180 mg/mL.

Assignments (2)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 9, 2021
From: F. HOFFMANN-LA ROCHE AG
To: HOFFMANN-LA ROCHE INC.
Reel/Frame 058058/0023 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Apr 30, 2021
From: MORICHIKA, TOSHIYUKI; KAMECKA, DAISUKE; IMAEDA, YOSHIMI; MAEDA, TERUTOSHI; STAUCH, OLIVER BORIS
To: CHUGAI SEIYAKU KABUSHIKI KAISHA; F. HOFFMANN - LA ROCHE AG
Reel/Frame 056091/0490 →
Priority Claims (1)
JP 2007-336310 · Dec 27, 2007 · national
Continuity (4)
Division 14963414 · Dec 9, 2015
Division 14017013 · Sep 3, 2013
Division 12810938
Related Publication 20200079857A1 · Mar 12, 2020