PTAB

PGR2026-00039

Biocon Biologics Inc v. Regeneron Pharmaceuticals Inc

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Petition
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1. Case Identification

2. Patent Overview

  • Title: Methods for Treating Angiogenic Eye Disorders with High Doses of VEGF Receptor Fusion Proteins
  • Brief Description: The ’036 patent discloses methods for treating angiogenic eye disorders by administering a high-concentration aqueous pharmaceutical formulation of a VEGF receptor fusion protein, such as aflibercept, via intravitreal injection. The claims require a specific protein concentration, administration volume, and formulation viscosity.

3. Grounds for Unpatentability

Ground 1: Claims 1 and 4-38 are obvious over Vitti, AU EYLEA Label, and Larson

  • Prior Art Relied Upon: Vitti (Application # 2016/0144025), AU EYLEA Label (a 2017 product label), and Larson (Application # 2015/0071920).
  • Core Argument for this Ground:
    • Prior Art Mapping: Petitioner argued that the combination discloses all limitations of the challenged claims. Vitti, a Regeneron application, taught stable, liquid aflibercept formulations with concentrations up to 115 mg/mL administered in volumes up to 100 µL for treating angiogenic eye disorders. The AU EYLEA Label disclosed that accidental overdoses of 8 mg of aflibercept were "generally well tolerated," teaching the claimed dosage. Larson taught that high-concentration protein formulations like aflibercept intended for injection should have a target viscosity of less than about 20 cP, and preferably less than 10 cP, which encompasses the claimed range of 5-15 cP.
    • Motivation to Combine: A Person of Ordinary Skill in the Art (POSA) would combine these references to reduce the high treatment burden associated with frequent, lower-dose eye injections. To achieve a longer duration of action and fewer injections, a POSA would increase the dose (as taught safe by the AU EYLEA Label) and thus the concentration (as taught by Vitti) for a small, safe injection volume. Larson provided the known, desired viscosity for such an injectable high-concentration formulation, making it a routine design consideration.
    • Expectation of Success: A POSA would have a reasonable expectation of success because Vitti already taught stable, high-concentration formulations of aflibercept. The AU EYLEA Label confirmed the safety and tolerability of the high dose, and Larson established that achieving the target viscosity for such formulations was a known and achievable objective for intravitreal administration.

Ground 2: Claims 1 and 4-38 are obvious over Furfine, Dix, AU EYLEA Label, and Fiedler in view of Larson

  • Prior Art Relied Upon: Furfine (Patent 7,608,261), Dix (Patent 8,921,316), AU EYLEA Label (a 2017 product label), Fiedler (Application # 2017/0232199), and Larson (Application # 2015/0071920).
  • Core Argument for this Ground:
    • Prior Art Mapping: This combination, consisting primarily of Regeneron's own prior art, also allegedly disclosed all claim limitations. Furfine and Dix taught stable, liquid formulations of aflibercept ("VEGF trap") at concentrations up to 100 mg/mL suitable for intravitreal injection. Fiedler taught pre-filled syringes for aflibercept administration in conventional volumes (e.g., 30-100 µL). The AU EYLEA Label again provided evidence that an 8 mg dose was well-tolerated. As in Ground 1, Larson supplied the target viscosity range for high-concentration injectables.
    • Motivation to Combine: The motivation was identical to Ground 1: to lessen the treatment burden by creating a higher-dose, higher-concentration aflibercept product. A POSA would naturally combine Regeneron’s own disclosures on high-concentration formulations (Furfine, Dix) with disclosures on administration devices and volumes (Fiedler) and safety at high doses (AU EYLEA Label). A POSA would then consult a reference like Larson to determine the routine and preferred viscosity for the resulting formulation.
    • Expectation of Success: Success was expected because Furfine and Dix already demonstrated the existence of stable 100 mg/mL aflibercept formulations. The known safety of the 8 mg dose (from the AU EYLEA Label) and the established formulation science for achieving target viscosities (from Larson and general knowledge) provided a clear and predictable path to the claimed invention.

Ground 3: Claims 1-38 are unpatentable for lack of written description under 35 U.S.C. §112

  • Core Argument for this Ground: Petitioner argued the ’036 patent specification fails to provide adequate written description to support the full scope of the claims. The claims recite a broad genus of formulations defined by functional results (e.g., a viscosity of 5-15 cP) and require only the VEGF fusion protein, but the specification provides only a few narrow examples that achieve these results. A key contention was that every formulation in the specification for which viscosity data is provided contains a buffer, and the data shows the type of buffer (e.g., histidine vs. phosphate) is critical to achieving the claimed viscosity. However, the claims are not limited to formulations containing a buffer, and thus claim subject matter (formulations without a buffer) that is not described or enabled by the specification. This disconnect between the narrow disclosure and the broad claims allegedly demonstrated that the inventors did not possess the full scope of the claimed invention at the time of filing.

  • Additional Grounds: Petitioner asserted additional obviousness challenges against claims 2 and 3 (Grounds 4 and 5), which added the 2011 EYLEA Clinical Review to the combinations of Grounds 1 and 2, respectively. The Clinical Review was used to teach that aflibercept does not cause a significant increase in blood pressure, a limitation recited in claims 2 and 3.

4. Relief Requested

  • Petitioner requests institution of Post Grant Review and cancellation of claims 1-38 of the ’036 patent as unpatentable.