IP Library Granted Patent US 9,364,542
Granted Patent B2
US 9,364,542 · App. 13/662,281 · Granted Jun 14, 2016

Protein formulations containing amino acids

Inventor: Byeong Seon Chang (Sherman Oaks, CA)
Assignee: Excelse Bio, Inc.
A61K47/183A61K38/47A61K38/4846A61K38/57A61K39/39591C07K16/1027C07K16/22C07K16/241C07K16/2863C07K16/2866C07K16/2887C07K16/32
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Quick Facts
Patent No.
US 9,364,542
App. No.
13/662,281
Granted
Jun 14, 2016
Kind
B2
Abstract

Provided are stable protein formulations that contain at least one amino acid. In certain embodiments, amino acid combinations either at least two, or three, or four, or more amino acids are included. By virtue of inclusion of the amino acids, the formulation has low viscosity and a protein in the formulations is physically, chemically, and biological stable even at high concentrations. In further embodiments, by virtue of inclusion of the amino acids, a protein in the formulations is physically, chemically, and biological stable even at high concentrations.

Claims (26)

1. A stable liquid pharmaceutical formulation comprising:

an antibody, the antibody being adalimumab, alemtuzumab, alirocumab, basiliximab, bevacizumab, daratumumab, infliximab, panitumumab, ranibizumab, rituximab or trastuzumab;

one or more amino acids to stabilize the antibody in the formulation, the one or more amino acids to stabilize the antibody including serine, threonine, alanine, glycine and valine and one or more further amino acids selected from the group consisting of isoleucine, asparagine, glutamine and aspartic acid; and

one or more amino acids to reduce the viscosity of the formulation, the one or more amino acids to reduce viscosity of the formulation including proline,

wherein the viscosity of the formulation is less than 100 cP.

2. The formulation of claim 1 , wherein the one or more amino acids to stabilize the antibody are serine, threonine, alanine, glycine, valine and isoleucine.

3. The formulation of claim 1 , wherein the one or more amino acids to stabilize the antibody are serine, threonine, alanine, glycine, valine and asparagine.

4. The formulation of claim 1 , wherein the one or more amino acids to stabilize the antibody are serine, threonine, alanine, glycine, valine and glutamine.

5. The formulation of claim 1 , wherein the one or more amino acids to stabilize the antibody are serine, threonine, alanine, glycine, valine and aspartic acid.

6. The formulation of claim 1 , wherein the one or more amino acids to stabilize the antibody are serine, threonine, alanine, glycine, valine, glutamine and asparagine.

7. The formulation of claim 1 , wherein the one or more amino acids to stabilize the antibody are serine, threonine, alanine, glycine, valine, glutamine and isoleucine.

8. The formulation of claim 1 , wherein the one or more amino acids to stabilize the antibody are serine, threonine, alanine, glycine, valine, glutamine and aspartic acid.

9. The formulation of claim 1 , wherein the one or more amino acids to stabilize the antibody are serine, threonine, alanine, glycine, valine, asparagine and isoleucine.

10. The formulation of claim 1 , wherein the one or more amino acids to stabilize the antibody are serine, threonine, alanine, glycine, valine, asparagine and aspartic acid.

11. The formulation of claim 1 , wherein the one or more amino acids to stabilize the antibody are serine, threonine, alanine, glycine, valine, isoleucine and aspartic acid.

12. The formulation of claim 1 , wherein the one or more amino acids to stabilize the antibody and the one or more amino acids to reduce viscosity of the formulation are each present at a concentration of at least 0.1 mg/mL.

13. The formulation of claim 1 , wherein the concentration of proline is from about 1 mg/mL to about 20 mg/mL and, when present in the formulation, the concentration of each of serine, threonine, glycine, alanine, valine, isoleucine and/or asparagine is from about 1 mg/mL to about 20 mg/mL.

14. The formulation of claim 1 , wherein when present in the formulation, the concentration of each of glutamine and/or aspartic acid is from about 1.5 mg/mL to about 10 mg/mL.

15. The formulation of claim 14 , wherein the concentration of each of serine and/or glycine is at least about 20 mg/mL.

16. The formulation of claim 13 , wherein the concentration of each of serine, threonine, glycine, alanine, valine, and/or proline is at least 10 mg/mL.

17. The formulation of claim 13 , wherein the concentration of isoleucine is at least 7 mg/mL.

18. The formulation of claim 13 , wherein the concentration of asparagine is from about 3 mg/mL to about 8 mg/mL.

19. The formulation of claim 14 , wherein the concentration of glutamine is from about 3 mg/mL to about 8 mg/mL.

20. The formulation of claim 15 , wherein the concentration of each of serine and/or glycine is at least 25 mg/mL.

21. The formulation of claim 20 , wherein the concentration of each of serine and/or glycine is at least 30 mg/mL.

22. The formulation of claim 21 , wherein the concentration of serine is at least 35 mg/mL.

Assignments (6)
ASSIGNMENT OF SECURITY INTEREST IN INTELLECTUAL PROPERTY, RECORDED ON NOVEMBER 29, 2021, AT REEL/FRAME 058231/0086 Recorded Mar 17, 2025
From: BARCLAYS BANK PLC, AS EXISTING AGENT
To: APOLLO ADMINISTRATIVE AGENCY LLC, AS SUCCESSOR AGENT
Reel/Frame 070531/0865 →
CHANGE OF NAME Recorded Dec 7, 2023
From: EXCELSE BIO, INCORPORATED
To: CURIA BIO IP HOLDINGS, INC
Reel/Frame 065834/0452 →
SECURITY INTEREST Recorded Nov 29, 2021
From: LAKEPHARMA HOLDINGS, INC.; LAKEPHARMA, INC.; EXCELSE BIO, INCORPORATED
To: BARCLAYS BANK PLC, AS COLLATERAL AGENT
Reel/Frame 058231/0086 →
SECURITY INTEREST Recorded Nov 29, 2021
From: LAKEPHARMA HOLDINGS, INC.; LAKEPHARMA, INC.; EXCELSE BIO, INCORPORATED
To: WILMINGTON TRUST, NATIONAL ASSOCIATION, AS COLLATERAL AGENT
Reel/Frame 058231/0134 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 27, 2015
From: CHANG, BYEONG SEON
To: INTEGRITY BIO, INC.
Reel/Frame 035276/0850 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 27, 2015
From: INTEGRITY BIO, INC.
To: EXCELSE BIO, INC.
Reel/Frame 035277/0294 →
Continuity (2)
Provisional Application 61552688 · Oct 28, 2011
Related Publication 20140127227A1 · May 8, 2014