VEGF antagonist formulations suitable for intravitreal administration
First Claim
Patent Images
1. An ophthalmic formulation of a vascular endothelial growth factor (VEGF) antagonist, comprisinga) 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.
3 Assignments
0 Petitions
Accused Products
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.
64 Citations
17 Claims
-
1. 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. - View Dependent Claims (2, 3, 4, 5, 6, 7, 17)
- 4;
-
8. 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. - View Dependent Claims (9, 10, 11)
- 4;
-
12. 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. - View Dependent Claims (13, 14, 15, 16)
- 4;
Specification