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Last Updated: March 29, 2024

Claims for Patent: 7,608,261


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Summary for Patent: 7,608,261
Title:VEGF antagonist formulations suitable for intravitreal administration
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.
Inventor(s): Furfine; Eric (Concord, MA), Dix; Daniel (LaGrangeville, NY), Graham; Kenneth S. (Pleasant Valley, NY), Frye; Kelly (Pomona, NY)
Assignee: Regeneron Pharmacuticals, Inc. (Tarrytown, NY)
Application Number:11/818,463
Patent Litigation and PTAB cases: See patent lawsuits and PTAB cases for patent 7,608,261
Patent 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.

2. The ophthalmic formulation of claim 1, further comprising 1-7.5% of a stabilizing agent is selected from the group consisting of sucrose, sorbitol, glycerol, trehalose, or mannitol, pH between about 5.8-7.0.

3. The ophthalmic formulation of claim 2, comprising about 1-100 mg/ml of the VEGF antagonist, 10 mM sodium phosphate buffer, 40 mM NaCl, 0.03% polysorbate, and 5% sucrose, pH about 6.2-6.3.

4. The ophthalmic formulation of claim 3, comprising about 10-80 mg/ml of the VEGF antagonist.

5. The ophthalmic formulation of claim 4, comprising VEGF antagonist at a concentration selected from the group consisting of 10 mg/ml, 20 mg/ml, 40 mg/ml, and 80 mg/ml.

6. The ophthalmic formulation of claim 1, comprising 10-80 mg/ml VEGF antagonist, 10 mM sodium phosphate, 0.03% polysorbate, and 135 mM sodium chloride, pH about 6.2-6.3.

7. The ophthalmic formulation of claim 6, comprising VEGF antagonist at a concentration selected from the group consisting of 10 mg/ml, 20 mg/ml, 40 mg/ml, and 80 mg/ml.

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.

9. The lyophilizable formulation of claim 8, comprising about 20 mg/ml of the VEGF antagonist, about 10 mM sodium phosphate buffer, about 0.03% polysorbate, about 0.1% PEG and about 2.5% sucrose, pH about 6.2-6.3.

10. The lyophilizable formulation of claim 8, comprising about 20 mg/ml of the VEGF antagonist, about 5 mM sodium phosphate buffer, about 0.015% polysorbate, about 2.5% sucrose, and further comprising sodium chloride at about 20 mM, pH about 6.2-6.3.

11. The lyophilizable formulation of claim 8, comprising about 20 mg/ml of the VEGF antagonist, about 5 mM sodium phosphate buffer, about 0.015% polysorbate, and further comprising sodium chloride at about 67.5 mM, pH about 6.2-6.3.

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.

13. The lyophilizable formulation of claim 12, wherein the tonicity agent is sodium chloride at a concentration selected from the group consisting of 20 mM and 67.5 mM.

14. The lyophilizable formulation of claim 12, wherein the organic co-solvent is polysorbate at 0.015%.

15. The lyophilizable formulation of claim 12, wherein the VEGF antagonist is at a concentration selected from the group consisting of 5 mg/ml, 10 mg/ml, 20 mg/ml, and 40 mg/ml.

16. The lyophilizable formulation of claim 12, wherein the sodium phosphate buffer is at 5 mM.

17. A pre-filled syringe suitable for intravitreal administration comprising the formulation of claim 1.

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