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.
Claims18
A method of producing a lyophilized formulation of a VEGF antagonist, comprising a step of subjecting to lyophilization a pre-lyophilized formulation, which comprises:
- (a) 5-50 mg/ml of a vascular endothelial growth factor (VEGF) antagonist, comprising the amino acids 27-457 of SEQ ID NO:4;
- (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, polythylene 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, to generate a lyophilized formulation.
A method of producing a lyophilized formulation of a VEGF antagonist, comprising the step of subjecting to lyophilization a prelyophilization formulation, which comprises
- a) 5-50 mg/ml of a vascular endothelial growth factor (VEGF) antagonist, comprising amino acids 27-457 of SEQ ID NO:4;
- (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, to generate a lyophilized formulation.
Dependencies are inferred from the claim text.