Get our Free Patent Expiration Newsletter

Serving leading biopharmaceutical companies globally:

Medtronic
Baxter
Colorcon
Johnson and Johnson
Merck
Boehringer Ingelheim

Last Updated: October 18, 2019

DrugPatentWatch Database Preview

Claims for Patent: 7,608,261

See Plans and Pricing

« Back to Dashboard

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 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.

Details for Patent 7,608,261

Applicant Tradename Biologic Ingredient Dosage Form BLA Number Approval Date Patent No. Assignee Estimated Patent Expiration Status Orphan Source
Regeneron Pharmaceuticals EYLEA aflibercept INJECTABLE; INJECTION 125387 001 2011-11-18   Start Trial Regeneron Pharmacuticals, Inc. (Tarrytown, NY) 2036-04-30 RX company
>Applicant >Tradename >Biologic Ingredient >Dosage Form >BLA >Number >Approval Date >Patent No. >Assignee >Estimated Patent Expiration >Status >Orphan >Source

International Patent Family for US Patent 7,608,261

Make Better Decisions: Try a trial or see plans & pricing

Serving leading biopharmaceutical companies globally:

AstraZeneca
Express Scripts
Harvard Business School
Baxter
Johnson and Johnson
Moodys

Drugs may be covered by multiple patents or regulatory protections. All trademarks and applicant names are the property of their respective owners or licensors. Although great care is taken in the proper and correct provision of this service, thinkBiotech LLC does not accept any responsibility for possible consequences of errors or omissions in the provided data. The data presented herein is for information purposes only. There is no warranty that the data contained herein is error free. thinkBiotech performs no independent verifification of facts as provided by public sources nor are attempts made to provide legal or investing advice. Any reliance on data provided herein is done solely at the discretion of the user. Users of this service are advised to seek professional advice and independent confirmation before considering acting on any of the provided information. thinkBiotech LLC reserves the right to amend, extend or withdraw any part or all of the offered service without notice.