Prior art

US Patent 11084865, titled "VEGF antagonist formulations suitable for intravitreal administration," was issued on August 10, 2021, from an application filed on January 10, 2020, by Regeneron Pharmaceuticals Inc.. The patent describes ophthalmic formulations of a vascular endothelial growth factor (VEGF)-specific fusion protein antagonist, including stable liquid and lyophilizable formulations, particularly those with the protein antagonist having the amino acid sequence of SEQ ID NO:4.

Anticipation under 35 U.S.C. § 102 means that a claimed invention is not novel because every element of the claim is disclosed, either expressly or inherently, in a single prior art reference.

Here are some of the most relevant prior art documents cited in US11084865:

• US 7,608,261 B2

  • Full Citation: US 7,608,261 B2 to Regeneron Pharmaceuticals, Inc., titled "VEGF antagonist formulations suitable for intravitreal administration".
  • Publication/Filing Date: Issued on October 27, 2009, from an application filed on June 14, 2007. This patent is a direct antecedent to US11084865, claiming benefit from the same provisional application filed June 16, 2006.
  • Brief Description: This patent also describes VEGF antagonist formulations for intravitreal administration, including liquid and lyophilized forms of the VEGF trap protein (SEQ ID NO:4). It covers formulations with similar components (VEGF antagonist, buffer, organic co-solvent, tonicity agent, stabilizing agent) and pH ranges as US11084865.
  • Potential Anticipated Claim(s): Given that US11084865 is a continuation of a lineage tracing back to US 7,608,261, and both share a common priority date and subject matter, US 7,608,261 potentially anticipates many, if not all, of the claims of US11084865, particularly those directed to the general composition of stable liquid or lyophilized VEGF antagonist formulations for intravitreal administration and the specific components and concentrations. For example, claims 1 and 26 of US11084865, which broadly cover a vial or pre-filled syringe comprising an ophthalmic formulation with a VEGF antagonist, organic co-solvent, buffer, and stabilizing agent, where the VEGF antagonist is glycosylated and comprises amino acids 27-457 of SEQ ID NO:4 and exhibits specified stability, are likely anticipated by the earlier patent's disclosures of similar formulations and stability. Further, claims like 51, describing a specific formulation with 40 mg/ml of the VEGF antagonist, polysorbate, sodium phosphate buffer, and sucrose, might also be anticipated if this specific combination falls within the scope of the formulations taught in US 7,608,261.

• US 6,436,897 B1

  • Full Citation: US 6,436,897 B1 to Regeneron Pharmaceuticals, Inc., titled "Lyophilized and reconstituted protein formulations".
  • Publication/Filing Date: Issued on August 20, 2002, from an application filed on March 27, 2001.
  • Brief Description: This patent generally describes lyophilized protein formulations that are resistant to degradation, aggregation, oxidation, and other degenerative processes. It highlights the use of lyophilization for long-term storage of proteins.
  • Potential Anticipated Claim(s): US 6,436,897 B1 broadly teaches the concept of lyophilizing proteins to achieve stability. While it does not specifically mention VEGF antagonists or intravitreal administration, it lays the groundwork for stable lyophilized protein formulations. Therefore, this patent could potentially anticipate aspects of claims in US11084865 related to the lyophilizable nature of the formulation and the stability achieved through lyophilization (e.g., claims 1, 26, and 51 regarding the native conformation of the protein after storage, if the method of achieving that stability is generally disclosed in the earlier patent). Specifically, the general principle that "the lyophilized protein is substantially resistant to degradation, aggregation, oxidation, and other degenerative processes while in the freeze-dried state" as mentioned in US11084865, references US 6,436,897.

• Holash et al. (2002) Proc. Natl. Acad. Sci. USA 99:11393-8

  • Full Citation: Holash et al. (2002) "VEGF-Trap: A VEGF blocker with potent antitumor effects," Proc. Natl. Acad. Sci. USA 99:11393-8.
  • Publication/Filing Date: Published in 2002.
  • Brief Description: This publication describes the "VEGF trap," a soluble VEGF-specific fusion protein antagonist. The VEGF trap described is the fusion protein that is the active ingredient in the formulations of US11084865.
  • Potential Anticipated Claim(s): This publication likely anticipates the core component of the claimed formulations—the VEGF antagonist fusion protein itself, particularly the general concept of a "VEGF trap" and potentially the specific sequence (or highly similar sequences) of SEQ ID NO:4, which is explicitly mentioned as the preferred VEGF antagonist in US11084865. Therefore, claims 1, 26, and 51, to the extent they rely on the novelty of the VEGF antagonist per se, could be anticipated.

• Kim et al. (2002) Proc. Natl. Acad. Sci. USA 99:11399-404

  • Full Citation: Kim et al. (2002) "The VEGF Trap: A novel antiangiogenic agent that inhibits ocular neovascularization," Proc. Natl. Acad. Sci. USA 99:11399-404.
  • Publication/Filing Date: Published in 2002.
  • Brief Description: This publication, similar to Holash et al., also describes the VEGF trap and its use as an antiangiogenic agent, specifically mentioning its ability to inhibit ocular neovascularization.
  • Potential Anticipated Claim(s): Similar to Holash et al., this reference could anticipate the VEGF antagonist fusion protein (SEQ ID NO:4) and its application in treating ocular conditions. The application of VEGF antagonists for ocular conditions directly relates to the "ophthalmic formulation suitable for intravitreal administration" language in the claims. Therefore, claims 1, 26, and 51, if they depend on the novelty of the VEGF antagonist or its general use for ocular indications, could be anticipated.