US 12168036

Summary of U.S. Patent 12,168,036

A review of U.S. Patent 12,168,036 indicates the patent is the subject of a Post-Grant Review (PGR) proceeding before the Patent Trial and Appeal Board (PTAB) as of April 2, 2026. A search for related 2026 dockets at the Court of Appeals for the Federal Circuit (CAFC) yielded no results.

Title: Methods for treating angiogenic eye disorders with high doses of VEGF receptor fusion proteins

Assignee: Regeneron Pharmaceuticals, Inc.

Inventors: Kenneth S. Graham, Saurabh Wadhwa

Filing Date: July 23, 2021

Issue Date: December 17, 2024

Abstract: The present invention provides ophthalmic formulations having high concentrations of vascular endothelial growth factor (VEGF) receptor fusion protein and high stability during storage. Methods for treating angiogenic eye disorders using the high concentration formulations are also provided.

Plain-Language Overview of Independent Claims

U.S. Patent 12,168,036 contains 38 claims in total. The independent claims are claims 1, 16, 21, 28, and 33.

• Claim 1: Describes a method for treating an angiogenic eye disorder. This is accomplished by injecting into the eye a specific pharmaceutical formulation. The formulation's key components are a high concentration of a VEGF receptor fusion protein (specifically aflibercept), a histidine-based buffer to maintain pH, sucrose for stability, a surfactant (polysorbate 20), and L-arginine monohydrochloride, which can help in reducing viscosity. The claim specifies the concentrations and pH range of this formulation.

• Claim 16: This claim also outlines a method for treating angiogenic eye disorders via intravitreal injection. It details a liquid formulation with a high concentration of aflibercept, a histidine buffer, sucrose, and polysorbate 20. A key aspect of this claim is the specific viscosity range of the formulation and the fact that it is packaged in a pre-filled syringe for direct administration.

• Claim 21: This claim focuses on the pharmaceutical formulation itself. It describes a stable, injectable liquid that contains a high concentration of aflibercept, a histidine buffer, sucrose, polysorbate 20, and L-arginine. The claim specifies the pH, viscosity, and osmolality (a measure of solute concentration) of the formulation, ensuring its suitability for injection into the eye. It also states that the formulation is stable, with minimal formation of high molecular weight species (a sign of protein degradation) when stored for up to 6 months at 2-8°C.

• Claim 28: This claim covers a pre-filled syringe as a product. The syringe is filled with a specific volume of the sterile pharmaceutical formulation described in claim 21, ready for intravitreal injection to treat an angiogenic eye disorder.

• Claim 33: This claim describes a method for manufacturing the pharmaceutical formulation. The process involves combining a high concentration of aflibercept with the other specified ingredients (histidine buffer, sucrose, polysorbate 20, and L-arginine) to create the formulation with the specific properties outlined in claim 21.