US 12,331,099 B2
VEGF antagonist formulations suitable for intravitreal administration
Eric Furfine, Concord, MA (US); Daniel Dix, LaGrangeville, NY (US); Kenneth Graham, Pleasant Valley, NY (US); and Kelly Frye, Mendham, NJ (US)
Assigned to Regeneron Pharmaceuticals, Inc., Tarrytown, NY (US)
Filed by Regeneron Pharmaceuticals, Inc., Tarrytown, NY (US)
Filed on Oct. 23, 2024, as Appl. No. 18/924,707.
Application 12/560,885 is a division of application No. 11/818,463, filed on Jun. 14, 2007, granted, now 7,608,261, issued on Oct. 27, 2009.
Application 18/924,707 is a continuation of application No. 18/344,786, filed on Jun. 29, 2023.
Application 18/344,786 is a continuation of application No. 17/348,438, filed on Jun. 15, 2021, granted, now 11,732,024, issued on Aug. 22, 2023.
Application 17/348,438 is a continuation of application No. 16/582,486, filed on Sep. 25, 2019, granted, now 11,066,458, issued on Jul. 20, 2021.
Application 16/582,486 is a continuation of application No. 16/159,269, filed on Oct. 12, 2018, granted, now 10,464,992, issued on Nov. 5, 2019.
Application 16/159,269 is a continuation of application No. 15/879,294, filed on Jan. 24, 2018, granted, now 10,400,025, issued on Sep. 3, 2019.
Application 15/879,294 is a continuation of application No. 15/095,606, filed on Apr. 11, 2016, granted, now 9,914,763, issued on Mar. 13, 2018.
Application 15/095,606 is a continuation of application No. 14/330,096, filed on Jul. 14, 2014, granted, now 9,340,594, issued on May 17, 2016.
Application 14/330,096 is a continuation of application No. 13/914,996, filed on Jun. 11, 2013, granted, now 8,802,107, issued on Aug. 12, 2014.
Application 13/914,996 is a continuation of application No. 13/329,770, filed on Dec. 19, 2011, granted, now 8,481,046, issued on Jul. 9, 2013.
Application 13/329,770 is a continuation of application No. 12/833,417, filed on Jul. 9, 2010, granted, now 8,092,803, issued on Jan. 10, 2012.
Application 12/833,417 is a continuation of application No. 12/560,885, filed on Sep. 16, 2009, granted, now 7,807,164, issued on Oct. 5, 2010.
Claims priority of provisional application 60/814,484, filed on Jun. 16, 2006.
Prior Publication US 2025/0042972 A1, Feb. 6, 2025
This patent is subject to a terminal disclaimer.
Int. Cl. A61K 38/17 (2006.01); A61K 9/00 (2006.01); A61K 9/19 (2006.01); A61K 47/02 (2006.01); A61K 47/10 (2017.01); A61K 47/26 (2006.01); A61M 5/178 (2006.01); C07K 14/47 (2006.01); C07K 14/71 (2006.01)
CPC C07K 14/71 (2013.01) [A61K 9/0019 (2013.01); A61K 9/0048 (2013.01); A61K 9/19 (2013.01); A61K 38/179 (2013.01); A61K 38/1793 (2013.01); A61K 47/02 (2013.01); A61K 47/10 (2013.01); A61K 47/26 (2013.01); A61M 5/178 (2013.01); C07K 14/47 (2013.01); C07K 14/4705 (2013.01); C07K 2319/00 (2013.01); C07K 2319/30 (2013.01)] 30 Claims
 
1. A liquid ophthalmic formulation comprising:
40 mg/ml of a glycosylated vascular endothelial growth factor (VEGF) antagonist fusion protein comprising amino acids 27-457 of SEQ ID NO: 4;
water;
an organic co-solvent comprising polysorbate; and
a stabilizing agent,
wherein the liquid ophthalmic formulation has a pH of between 5.8 to 7.0,
wherein the liquid ophthalmic formulation is suitable for intravitreal administration,
wherein 90% or more of the weight of the VEGF antagonist fusion protein is not present as an aggregate, and
wherein the VEGF antagonist fusion protein is at least 95% free of protein contaminants.