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US 2011/0257601 A1Published application
Vegf antagonist formulations for intravitreal administration
AssigneeRegeneron Pharmaceuticals, Inc.
InventorsEric FURFINE, Daniel DIX, Kenneth S. GRAHAM, Kelly FRYE
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Abstract
Ophthalmic formulations of a vascular endothelial growth factor (VEGF)-specific fusion protein antagonist are provided suitable for intravitreal administration to the eye. The ophthalmic formulations include a stable liquid formulation and a lyophilizable formulation. Preferably, the protein antagonist has the amino acid sequence shown in SEQ ID NO:4.
Claims19
A stable liquid ophthalmic formulation of a vascular endothelial growth factor (VEGF) antagonist, comprising:
- (a) between 50 mg/ml to about 10 mg/ml of a VEGF antagonist of SEQ ID NO:4;
- (b) about 0.03% to about 0.1% polysorbate;
- (c) about 5-40 mM of sodium phosphate buffer, pH of about 5.8 to about 7.0;
- and
- (d) either:
- (i) about 5% sucrose and about 40 to about 50 mM NaCl, or
- (ii) about 135 mM NaCl,
- wherein at least 99% of the VEGF antagonist is present in native conformation following storage at 5° C. for 2 months as measured by size exclusion chromatography.
5 more elements
A non-liquid formulation of a vascular endothelial growth factor (VEGF) antagonist made according to the steps of:
- (a) combining in a liquid solution the following excipients:
- (i) about 5-50 mg/ml of the VEGF antagonist, comprising the amino acid sequence of SEQ ID NO:4;
- (ii) about 5-25 mM of sodium phosphate buffer, pH about 5.8-7.0;
- (iii) about 0.01-0.15% of an organic co-solvent, selected from the group consisting of polysorbate, polyethylene glycol (PEG), propylene glycol, and a combination thereof;
- and
- (iv) about 1-10% of a stabilizing agent selected from the group consisting of sucrose, sorbitol, glycerol, trehalose, and mannitol;
- and
- (b) lyophilizing the combination of step (a),
- wherein at least about 99% of the VEGF antagonist is present in native conformation as measured by size exclusion chromatography following storage at 5° C. for 2 months.
6 more elements
Dependencies are inferred from the claim text.