US 11041149

US Patent 11,041,149: PH20 Polypeptide Variants, Formulations and Uses Thereof

Title: PH20 polypeptide variants, formulations and uses thereof

Assignee: Halozyme Inc. (original assignee); Halozyme Therapeutics Inc. (current assignee)

Inventors: Ge Wei, H. Michael Shepard, Qiping Zhao, Robert James Connor

Filing Date: March 19, 2020

Issue Date: June 22, 2021

Abstract: The patent describes modified PH20 hyaluronidase polypeptides, including variants that show increased stability and/or activity. It also covers related compositions, formulations, and their therapeutic applications.

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Plain-Language Overview of Independent Claims:

This patent includes several independent claims, focusing on modified PH20 polypeptides and their uses.

• Independent Claim 1: This claim covers a modified PH20 polypeptide that has increased stability, specifically resistance to denaturation under certain protein-denaturing conditions (like high temperature, agitation, low salt, or certain excipients). The modified polypeptide must retain hyaluronidase activity and show increased stability compared to an unmodified PH20 polypeptide (defined as SEQ ID NO: 7 or a similar C-terminal truncated fragment). The claim specifies that the PH20 polypeptide can be modified by glycosylation, and that increased stability can be shown by exhibiting higher hyaluronidase activity under denaturing conditions.

• Independent Claim 13: This claim is directed to a modified PH20 polypeptide that exhibits increased stability specifically in the presence of a phenolic preservative. This modified polypeptide must contain an amino acid replacement compared to an unmodified PH20 polypeptide (again, SEQ ID NO: 7 or a similar fragment), and the increased stability is measured by greater hyaluronidase activity in the presence of the preservative. The claim details various phenolic preservatives and their effective concentrations.

• Independent Claim 16: This claim covers a pharmaceutical composition containing any of the modified PH20 polypeptides described in Claim 13 (i.e., those with increased stability to phenolic preservatives) and also an insulin, such as a fast-acting insulin. The claim specifies effective amounts for both the modified PH20 polypeptide and the insulin, as well as potential pH ranges and additional components like salt, preservatives (including phenolic ones), surfactants, buffering agents, antioxidants, and zinc.

• Independent Claim 19: This claim describes a method for identifying or selecting a modified hyaluronan-degrading enzyme (like PH20) that shows stability under denaturing conditions. The method involves comparing the activity of the modified enzyme in the presence of a denaturing agent/condition to its activity in the absence of that agent/condition. An enzyme is selected if its activity in the denaturing condition is at least 5% of its activity without the denaturing condition.

• Independent Claim 22: This claim also outlines a method for identifying or selecting a modified hyaluronan-degrading enzyme with increased stability under denaturing conditions. This method compares the activity of a modified enzyme in a denaturing condition to the activity of a corresponding unmodified enzyme in the same denaturing condition. An enzyme is selected if it exhibits greater activity than the unmodified enzyme.

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CAFC 2026 Dockets:

As of April 26, 2026, there are no dockets for patent 11041149 specifically listed in the CAFC 2026 dockets based on the provided information. However, the patent explicitly notes related litigation:

• PTAB Case IPR2026-00313: This Inter Partes Review (IPR) case was filed with the Patent Trial and Appeal Board (PTAB) and is currently pending.
• US Case in New Jersey District Court: A litigation case, 2:25-cv-03179, has been filed in the New Jersey District Court.

It is important to note that PTAB and District Court cases are not dockets of the Court of Appeals for the Federal Circuit (CAFC). Appeals from PTAB decisions or District Court judgments would be filed with the CAFC. While these existing cases indicate ongoing legal challenges, they are not yet at the CAFC level.