IP Library › Granted Patent US 12,551,529
Granted Patent B2
US 12,551,529 · App. 18/173,549 · Granted Feb 17, 2026

Liquid formulation of a VEGF antagonist

Inventor: Rainer Sigl (Landsberg am Lech, DE)
Assignee: FORMYCON AG
A61K38/179A61K9/0019A61K9/0048A61K9/0051A61K47/02A61K47/10A61K47/22A61K47/26A61P27/10C07K16/22A61K9/08C07K14/71
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Quick Facts
Patent No.
US 12,551,529
App. No.
18/173,549
Granted
Feb 17, 2026
Kind
B2
Abstract

The present invention relates to liquid pharmaceutical compositions of a VEGF antagonist for intravitreal administration comprising a histidine buffer, an inorganic salt, a carbohydrate and a polysorbate.

Claims (15)

1 . A method of treating an intraocular neovascular disease comprising administering a liquid pharmaceutical composition comprising:

a) a histidine containing buffer at a concentration of from 8 mM to 15 mM, wherein the histidine-containing buffer is L-histidine/histidine hydrochloride,

b) a non-ionic surfactant at a concentration of 0.02% to 0.04% (w/v),

c) a VEGF antagonist, wherein said VEGF antagonist is aflibercept at a concentration of from 6 mg/mL to 45 mg/mL,

d) an inorganic salt at a concentration of from 35 to 45 mM, and

e) a carbohydrate at a concentration of from 3% to 20% (w/v).

2 . The method of claim 1 , wherein the pH of the composition is between 6.0 and 6.5.

3 . The method of claim 1 , wherein the histidine-containing buffer is present in a concentration of 10 mM.

4 . The method of claim 1 , wherein the non-ionic surfactant is polysorbate 20.

5 . The method of claim 1 , wherein the inorganic salt is NaCl.

6 . The method of claim 1 , wherein the carbohydrate is sucrose.

7 . The method of claim 1 , wherein the intraocular neovascular disease is age-related macular degeneration (AMD), visual impairment due to diabetic macular oedema (DME), visual impairment due to macular oedema secondary to retinal vein occlusion (branch RVO or central RVO), or visual impairment due to choroidal neovascularisation (CNV) secondary to pathologic myopia.

8 . The method of claim 1 , wherein the pH of the composition is between 6.2 and 6.5.

9 . A method of treating an intraocular neovascular disease comprising administering a liquid pharmaceutical composition consisting of histidine hydrochloride/L-histidine, polysorbate 20, NaCl, aflibercept, sucrose and water and having a pH of 6.2 or 6.5.

10 . The method of claim 9 , wherein the liquid pharmaceutical composition consists of 10 mM histidine hydrochloride/L-histidine, 0.03% polysorbate 20 (w/v), 40 mM NaCl, 40 mg/ml aflibercept, 5% sucrose and water and has a pH of 6.2 or 6.5.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 7, 2025
From: SIGL, RAINER
To: FORMYCON AG
Reel/Frame 072832/0370 →
Priority Claims (2)
EP 16152767 · Jan 26, 2016 · regional
EP 16199497 · Nov 18, 2016 · regional
Continuity (3)
Continuation 16742585 · Jan 14, 2020
Continuation 16072638
Related Publication 20230248806A1 · Aug 10, 2023
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