VEGF antagonist formulations suitable for intravitreal administration
AssigneeRegeneron Pharmacuticals, 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.
Claims17
An ophthalmic formulation of a vascular endothelial growth factor (VEGF) antagonist, comprising
- a) 1-100 mg/ml of a VEGF antagonist comprising the amino acid sequence of SEQ ID NO:4;
- 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.
A lyophilizable formulation of a vascular endothelial growth factor (VEGF) antagonist, comprising
- a) 5-50 mg/ml of the VEGF antagonist, comprising the amino acid sequence 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, 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.
A lyophilizable formulation of a vascular endothelial growth factor (VEGF) antagonist, comprising
- a) 5-50 mg/ml of the VEGF antagonist, comprising the amino acid sequence 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.
Dependencies are inferred from the claim text.