Etanercept formulations stabilized with xylitol

Patent metadata

Field	Value
Publication number	US-10213508-B2
Application number	US-201715716005-A
Country	US
Kind code	B2
Filing date	Sep 26, 2017
Priority date	Oct 18, 2011
Publication date	Feb 26, 2019
Grant date	Feb 26, 2019

Abstract

The invention provides stabilized aqueous pharmaceutical etanercept compositions suitable for long-term storage of etanercept, methods of manufacture of these compositions, methods of administration, and kits containing same.

First claim

What is claimed is:

1. A stabilized aqueous pharmaceutical composition comprising
a) etanercept,
b) buffer, and
c) stabilizer comprising 6 to 10 weight % xylitol,
wherein the composition has a pH of 6.0 to 6.6, or a pH within 10 percent of 6.0 and 6.6 and is free or essentially free of arginine.

2. The composition of claim 1 , wherein the pH is 6.3 or a pH within 10 percent of 6.3.

3. The composition of claim 1 , comprising 25 to 75 mg/mL of etanercept.

4. The composition of claim 3 , further comprising up to 100 mM NaCl and up to 5 wt. % sucrose.

5. The composition of claim 1 , comprising xylitol in an amount of 10 wt. % of the composition.

6. The composition of claim 1 , comprising 25 to 75 mg/mL of etanercept.

7. The composition of claim 6 , comprising 50 mg/mL or a concentration within 10 percent of 50 mg/ml of etanercept.

8. The composition of claim 7 , comprising 10 wt. % xylitol.

9. The composition of claim 7 , comprising 6 wt. % xylitol.

10. The composition of claim 6 , further comprising up to 100 mM NaCl and up to 5 wt. % sucrose.

11. The composition of claim 1 , further comprising one or more additional components selected from a tonicity modifier and an excipient.

12. The composition of claim 1 , further comprising up to 100 mM NaCl.

13. The composition of claim 1 , further comprising up to 5 wt. % sucrose.

14. A stabilized aqueous pharmaceutical composition comprising
a) 25 to 75 mg/mL of etanercept,
b) buffer, and
c) stabilizer comprising xylitol in an amount of 6 to 10 wt. % of the composition,
wherein the composition has a pH of 6.3 or a pH within 10 percent of 6.3, and is free or essentially free of arginine.

15. The composition of claim 14 , comprising 50 mg/mL or a concentration within 10 percent of 50 mg/ml of etanercept.

16. The composition of claim 15 , further comprising up to 100 mM NaCl and up to 5 wt. % sucrose.

17. The composition of claim 14 , comprising 6 wt. % xylitol.

18. The composition of claim 14 , comprising 50 mg/mL or a concentration within 10 percent of 50 mg/ml of etanercept and 10 wt. % xylitol.

19. The composition of claim 14 , comprising 50 mg/mL or a concentration within 10 percent of 50 mg/ml of etanercept and 6 wt. % xylitol.

20. The composition of claim 14 , further comprising one or more additional components selected from a tonicity modifier and an excipient.

21. The composition of claim 14 , further comprising up to 100 mM NaCl.

22. The composition of claim 14 , further comprising up to 5 wt. % sucrose.

23. The composition of claim 14 , further comprising up to 100 mM NaCl and up to 5 wt. % sucrose.

24. The composition of claim 23 , wherein the composition has osmolality of 180 to 420 milliosmoles or an osmolality within 10 percent of 180 to 420 milliosmoles; the composition is suitable for administration to a subject as a single dose; and the dose contains 10-80 mg/dose etanercept.

Assignees

• Coherus Biosciences Inc

Inventors

• Manning Mark
• Murphy Brian

Classifications

• A61P43/00

  Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00 · CPC title

• A61P37/08

  Antiallergic agents (antiasthmatic agents A61P11/06; ophthalmic antiallergics A61P27/14) · CPC title

• A61P37/02

  Immunomodulators · CPC title

• A61P37/00

  Drugs for immunological or allergic disorders · CPC title

• A61P7/00

  Drugs for disorders of the blood or the extracellular fluid · CPC title