PTAB

IPR2025-01024

EmPower Clinic Services LLC v. Eli Lilly & Co

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Petition
petition

1. Case Identification

2. Patent Overview

  • Title: GIP/GLP-1 Receptor Co-agonist Peptide Compounds
  • Brief Description: The ’780 patent is directed to a genus of chemically modified peptide compounds that function as dual agonists for the Glucose-dependent Insulinotropic Polypeptide (GIP) and Glucagon-like Peptide-1 (GLP-1) receptors, intended for therapeutic use in conditions such as type 2 diabetes.

3. Grounds for Unpatentability

Ground 1: Claims 1-7, 9-10, and 12-18 are obvious over the combination of the ’657, ’483, and ’537 Publications.

  • Prior Art Relied Upon: The ’657 Publication (WO 2011/119657), the ’483 Publication (WO 2013/164483), and the ’537 Publication (WO 2006/097537).
  • Core Argument for this Ground:

    • Prior Art Mapping: Petitioner argued that the claimed invention is an obvious combination of three distinct elements, each well-known in the prior art for its specific function.

      • 1. The Base Peptide Sequence: The ’657 Publication disclosed a promising GIP/GLP-1 dual agonist peptide (SEQ ID NO:1) that serves as a lead compound. This peptide shares its first 28 amino acid residues with the claimed sequence. The ’483 Publication taught improving such GIP analogues by replacing the C-terminal portion with the familiar, stability-enhancing exenatide C-terminal motif (GGPSSGAPPPS). Petitioner asserted that combining the N-terminal sequence from the ’657 lead compound with the C-terminal motif from the ’483 teachings results in the exact peptide backbone recited in claim 1 of the ’780 patent.
      • 2. The Albumin-Binding Moiety: The ’537 Publication disclosed the precise albumin-binding moiety recited in claim 1. This moiety was successfully used to prolong the duration of action of the GLP-1 agonist semaglutide, achieving once-weekly dosing. The claimed moiety falls squarely within the scope of what the ’537 Publication taught.
      • 3. The Conjugation Site: The ’483 Publication explicitly taught acylating GIP/GLP-1 dual agonists to prolong their half-life, specifically identifying the lysine residue at position 20 (Lys20) as a suitable conjugation site. The ’537 Publication also demonstrated conjugation at a corresponding lysine position. Petitioner argued that conjugating the known moiety from ’537 at the known Lys20 site of the peptide derived from ’657 and ’483 renders the final claimed compound obvious.

    • Motivation to Combine (for §103 grounds): Petitioner contended that a person of ordinary skill in the art (POSA) would have been motivated by clear reasons to combine these references. A POSA would first combine the teachings of the ’657 and ’483 Publications to create a more effective dual agonist. The ’657 publication provided a promising lead compound, and the ’483 publication offered a known strategy—substituting the C-terminus with the exenatide motif—to improve metabolic stability and reduce potential immunogenicity.

      Having created this improved peptide, a POSA would have been further motivated to address the well-known challenge of frequent dosing. To achieve a longer duration of action, the POSA would turn to proven techniques. The ’537 Publication provided a blueprint, demonstrating that its specific albumin-binding moiety successfully conferred once-weekly dosing to a similar therapeutic peptide. A POSA would therefore be motivated to apply this successful moiety to the improved dual agonist peptide to achieve the same benefit of protracted action.

    • Expectation of Success (for §103 grounds): Petitioner argued that a POSA would have had a reasonable expectation of success. The structure-activity relationships (SARs) for GIP and GLP-1 agonists were well-developed, making the outcome of the proposed modifications predictable. Substituting the C-terminus with the exenatide motif was a known method for improving stability. Likewise, conjugating the specific albumin-binding moiety from the ’537 Publication at the Lys20 position was a known technique for extending half-life. The combination represented the application of known solutions to known problems, with each component expected to function as it had previously.

4. Relief Requested

  • Petitioner requests the institution of an inter partes review (IPR) and the cancellation of claims 1-7, 9-10, and 12-18 of the ’780 patent as unpatentable under 35 U.S.C. §103.