VEGF antagonist formulations for intravitreal administration
First Claim
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1. 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.
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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.
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Citations
18 Claims
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1. A method of producing a lyophilized formulation of a VEGF antagonist, comprising a step of subjecting to lyophilization a pre-lyophilized formulation, which comprises:
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(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. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8)
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9. 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. - View Dependent Claims (10, 11, 12, 13, 14, 15, 16, 17, 18)
- 4;
Specification