US 12,077,593 B2
Stabilized formulations containing anti-interleukin-6 receptor (IL-6R) antibodies
Daniel B. Dix, LaGrangeville, NY (US); Kenneth S. Graham, Pleasant Valley, NY (US); Douglas Kamen, Poughquag, NY (US); and Scott M. Walsh, Tarrytown, NY (US)
Assigned to Regeneron Pharmaceuticals, Inc., Tarrytown, NY (US)
Filed by Regeneron Pharmaceuticals, Inc., Tarrytown, NY (US)
Filed on Apr. 8, 2021, as Appl. No. 17/225,887.
Application 17/225,887 is a continuation of application No. 16/100,020, filed on Aug. 9, 2018, granted, now 11,098,127.
Application 16/100,020 is a continuation of application No. 14/861,565, filed on Sep. 22, 2015, granted, now 10,072,086.
Application 14/861,565 is a continuation of application No. 12/986,223, filed on Jan. 7, 2011, granted, now 9,173,880.
Claims priority of provisional application 61/293,227, filed on Jan. 8, 2010.
Prior Publication US 2021/0230283 A1, Jul. 29, 2021
This patent is subject to a terminal disclaimer.
Int. Cl. A61K 39/395 (2006.01); A61J 1/06 (2006.01); A61K 9/00 (2006.01); A61K 31/485 (2006.01); A61K 47/18 (2017.01); A61K 47/22 (2006.01); A61K 47/26 (2006.01); C07K 16/24 (2006.01); C07K 16/28 (2006.01); A61K 39/00 (2006.01)
CPC C07K 16/2866 (2013.01) [A61J 1/065 (2013.01); A61K 9/0019 (2013.01); A61K 31/485 (2013.01); A61K 39/3955 (2013.01); A61K 47/183 (2013.01); A61K 47/22 (2013.01); A61K 47/26 (2013.01); C07K 16/248 (2013.01); A61K 2039/505 (2013.01); C07K 2317/21 (2013.01); C07K 2317/515 (2013.01); C07K 2317/94 (2013.01)] 27 Claims
 
1. A pen delivery device containing a stable liquid pharmaceutical formulation comprising:
(i) a human antibody that specifically binds to human interleukin-6 receptor (hIL-6R), wherein the antibody is at a concentration of from about 5 mg/ml to about 200 mg/ml and comprises a heavy chain variable region having the amino acid sequence of SEQ ID NO: 18 and a light chain variable region having the amino acid sequence of SEQ ID NO:26;
(ii) histidine at a concentration of from about 10 mM to about 25 mM;
(iii) arginine at a concentration of from about 25 mM to about 50 mM;
(iv) sucrose in an amount of from about 5% to about 10% w/v; and
(v) polysorbate in an amount of from about 0.1% to about 0.2% w/v,
wherein the formulation has a pH of about 5.8, about 6.0, or about 6.2, and at least 90% of the native form of the antibody is recovered after 1 month of storage at 45° C., as determined by size exclusion chromatography.