VEGF Antagonist Formulations for Intravitreal Administration
AssigneeRegeneron Pharmaceuticals, Inc.
InventorsEric FURFINE, Daniel DIX, Kenneth GRAHAM, Kelly FRYE
Life of this patent
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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 an amino acid sequence of SEQ ID NO:4.
Claims19
An ophthalmic formulation of a vascular endothelial growth factor (VEGF) antagonist, comprising
- (a) 1-100 mg/ml a VEGF antagonist;
- (b) 0.01-5% of one or more organic co-solvent(s) which is one or more of polysorbate, polyethylene glycol (PEG), and propylene glycol;
- (c) 30-150 mM of a tonicity agent selected from sodium chloride or potassium chloride;
- and,
- (d) 5-40 mM of sodium phosphate buffer,
- wherein the VEGF antagonist consists of a dimer of two polypeptides consisting of amino acids 27-457 of SEQ ID NO:4.
A lyophilizable formulation of a vascular endothelial growth factor (VEGF) antagonist, comprising
- (a) 5-50 mg/ml of the VEGF antagonist;
- (b) 5-25 mM of sodium phosphate buffer, pH about 5.8-7.0;
- (c) 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,
- (d) 1-10% of a stabilizing agent selected from the group consisting of sucrose, sorbitol, glycerol, trehalose, and mannitol,
- wherein the VEGF antagonist consists of a dimer of two polypeptides consisting of amino acids 27-457 of SEQ ID NO:4.
A lyophilizable formulation of a vascular endothelial growth factor (VEGF) antagonist, comprising
- (a) 5-50 mg/ml of the VEGF antagonist;
- (b) 5-25 mM of a phosphate buffer, pH about 5.8-7.0;
- (c) 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
- (d) 20-150 mM of a tonicity agent,
- wherein the VEGF antagonist consists of a dimer of two polypeptides consisting of amino acids 27-457 of SEQ ID NO:4.
Dependencies are inferred from the claim text.