Detailed Analysis of the Scope and Claims of United States Patent 10,442,847: Glucagon Analogues
Introduction
The United States Patent 10,442,847, assigned to Zealand Pharma A/S, pertains to glucagon analogues and their medical applications, particularly in the treatment of hypoglycemia. This patent is a crucial component of the intellectual property portfolio protecting Zegalogue, a drug developed by Zealand Pharma.
Patent Overview
Publication and Issuance
The patent was issued on October 15, 2019, and is identified by the publication number US10442847B2. It is part of a broader family of patents related to glucagon analogues[4].
Scope of the Invention
Medical Use
The patent primarily focuses on glucagon analogues designed for the treatment of hypoglycemia. However, the scope extends to other conditions associated with excess body weight, such as obesity, metabolic syndrome, insulin resistance, glucose intolerance, type-2 diabetes, hypertension, and various cardiovascular diseases[1][4].
Chemical Structure
The glucagon analogues described in the patent have a specific amino acid sequence derived from the native human glucagon sequence. These analogues include at least four amino acid substitutions or deletions at specific positions. The sequence is defined as:
- His-Ser-Gln-Gly-Thr-Phe-Thr-Ser-Asp-Tyr-Ser-Lys-Tyr-Leu-Asp-Ser-Arg-Arg-Ala-Gln-Asp-Phe-Val-Gln-Trp-Leu-Glu-Asn-Thr
- With substitutions and deletions allowed at positions 2, 3, 4, 9, 10, 15, 16, 17, 20, 21, 24, 28, and 29[4].
Substitutions and Deletions
The patent specifies various options for substitutions and deletions, including:
- X2: Aib or Ala
- X3: His, Pro, Dab(Ac), Dap(Ac), or Gln(Me)
- X4: DAla
- X9: Glu
- X10: Val, Leu, N-Me-Tyr, or N-Me-DTyr
- X15: Glu
- X16: Aib, Lys, Glu, Leu, Val, DVal, Phe, His, Arg, Pro, DPro, N-Me-Ser, or N-Me-DSer
- X17: Ala or Ser
- X20: Glu or Lys
- X21: Glu, Lys, or Ser
- X24: Lys, Ser, Glu, or Ala
- X28: Ser, Glu, Lys, or absent
- X29: Ser, Ala, or absent[4].
Improved Properties
The glucagon analogues in this patent exhibit improved solubility and stability compared to native human glucagon, making them more suitable for liquid formulations[4].
Patent Claims
Compound Claims
The patent claims cover the glucagon analogue peptides themselves, as well as their salts and solvates. These claims are broad enough to encompass a range of modifications while ensuring the compounds retain glucagon agonist activity[4].
Method Claims
The patent also includes method claims related to the use of these glucagon analogues in medical treatments. This includes methods for treating hypoglycemia and other conditions associated with excess body weight[1][4].
Composition Claims
The patent covers compositions comprising the glucagon analogue peptides, nucleic acids encoding these peptides, expression vectors, and host cells containing these nucleic acids or expression vectors. These compositions are formulated with carriers suitable for administration[1].
Patent Landscape
Exclusivities and Patent Protection
Zegalogue, the drug protected by this patent, is covered by multiple U.S. patents, including US10442847B2 and US11795204B2. These patents are active and will expire in 2035 and 2034, respectively. Additionally, Zegalogue benefits from New Chemical Entity (NCE) exclusivity until March 22, 2026, which further delays the potential launch of generic versions[2].
Generic Launch
The estimated generic launch date for Zegalogue is February 3, 2035, based on the patent expiration dates and exclusivities. However, this date can be influenced by legal activities such as patent term extensions, amendments, or challenges to the patents[2][5].
Strategic Implications
Market Protection
The broad scope of the patent claims and the multiple layers of protection (patents and exclusivities) ensure that Zealand Pharma maintains market exclusivity for Zegalogue for an extended period. This protection is crucial for recouping investment in research and development and for maintaining a competitive edge in the market[2][3].
Competitive Landscape
Understanding the patent landscape is essential for competitors looking to enter the market. Identifying weaker patent protection in certain jurisdictions or exploring design-around strategies can provide opportunities for generic or bioequivalent products[3].
Key Takeaways
- Broad Scope of Claims: The patent covers a wide range of glucagon analogues with specific substitutions and deletions, ensuring broad protection.
- Improved Properties: The analogues exhibit improved solubility and stability, making them more viable for medical use.
- Extended Market Exclusivity: The combination of patents and exclusivities delays the generic launch until 2035.
- Strategic Importance: The patent is a critical component of Zealand Pharma's intellectual property strategy, protecting their investment and market position.
FAQs
What is the primary use of the glucagon analogues described in US10442847B2?
The primary use is in the treatment of hypoglycemia, although the scope extends to other conditions associated with excess body weight.
When does the patent US10442847B2 expire?
The patent expires on February 3, 2035.
What are the key improvements in the glucagon analogues described in the patent?
The analogues have improved solubility and stability compared to native human glucagon.
How does the New Chemical Entity (NCE) exclusivity affect the generic launch of Zegalogue?
The NCE exclusivity delays the generic launch until March 22, 2026, in addition to the patent protection.
Can competitors design around the patent claims to avoid infringement?
Yes, but the broad scope of the claims makes it challenging. Competitors must ensure their products do not infringe on the protected amino acid sequences and their allowed substitutions and deletions[3].
Sources
- US8642540B2 - Glucagon analogues - Google Patents
- Zegalogue patent expiration - Pharsight
- Eviscerating Patent Scope - DigitalCommons@NYLS
- US10442847B2 - Glucagon analogues - Google Patents
- Generic Zegalogue Availability - Drugs.com
