Detailed Analysis of the Scope and Claims of United States Patent 11,759,502
Introduction
United States Patent 11,759,502, owned by Novo Nordisk A/S, is a crucial component of the patent landscape surrounding the pharmaceutical product RYBELSUS® (semaglutide). This patent is part of a broader set of patents that protect various aspects of semaglutide, a GLP-1 receptor agonist used in the treatment of diabetes and obesity.
Patent Overview
The patent, titled "Compositions of GLP-1 Peptides and Preparation Thereof," was issued on September 19, 2023. It names Thomas Vilhelmsen, Helle Eliasen, and Tue Hansen as inventors, all of whom have assigned their rights to Novo Nordisk A/S[2][5].
Claims and Scope
The patent claims cover several key aspects of the pharmaceutical composition and its preparation:
Solid Dosage Pharmaceutical Composition
The patent claims a solid dosage pharmaceutical composition that includes:
- A salt of N-(8-(2-hydroxybenzoyl)amino)caprylic acid (salt of NAC).
- A granule, wherein the granule comprises semaglutide, a binder, and optionally other excipients such as lubricants and fillers[2][5].
Granule Composition
The granule composition is a critical part of the patent. It involves:
- Semaglutide, the active GLP-1 peptide.
- A binder to enhance the stability and cohesion of the granules.
- Optional excipients like lubricants and fillers to improve the manufacturing process and the final tablet properties[4].
Preparation Method
The patent describes a method for preparing these compositions, which includes steps such as:
- Mixing the GLP-1 peptide with fillers and/or binders.
- Dry granulation of the mixture.
- Mixing the granules with a composition comprising the salt of N-(8-(2-hydroxybenzoyl)amino)caprylic acid.
- Optionally adding further lubricants to the mixture[4].
Significance of the Salt of NAC
The inclusion of a salt of N-(8-(2-hydroxybenzoyl)amino)caprylic acid is significant because it enhances the stability and bioavailability of the GLP-1 peptide. This component is crucial for maintaining the efficacy of the drug when administered orally[4].
Bioavailability and Dissolution Properties
The inventors have found that the design of the granules significantly affects the dissolution properties and bioavailability of the GLP-1 peptide. The patent highlights that the bioavailability can be predicted from in vitro data, which is a valuable insight for optimizing the formulation[4].
Patent Landscape and Litigation
This patent is part of a larger set of patents (collectively known as the "Asserted Patents") that Novo Nordisk is using to defend against generic versions of RYBELSUS®. For instance, Apotex has filed an Abbreviated New Drug Application (ANDA) seeking approval for a generic version of RYBELSUS®, which has led to litigation. Novo Nordisk is asserting that Apotex's ANDA infringes on multiple patents, including the '502 Patent[2][5].
Exclusivity and Market Protection
The '502 Patent, along with other related patents, provides Novo Nordisk with exclusive rights to sell, distribute, and market RYBELSUS® in the United States until the patents expire. The earliest expiration date among the asserted patents is March 2026 for the '122 Patent, while the '502 Patent itself expires in 2033[1][2].
Industry Impact
The protection offered by this patent and others like it is crucial for Novo Nordisk's market dominance in the GLP-1 receptor agonist space. It allows the company to maintain its exclusive position in the market, ensuring that generic competitors cannot enter until the patents expire.
Conclusion
The United States Patent 11,759,502 is a vital component of Novo Nordisk's intellectual property strategy for RYBELSUS®. It protects key aspects of the drug's composition and preparation, ensuring the company's continued exclusivity in the market. The patent's focus on enhancing bioavailability and stability underscores the importance of formulation in pharmaceutical development.
Key Takeaways
- Patent Scope: Covers solid dosage pharmaceutical compositions and their preparation, including a salt of N-(8-(2-hydroxybenzoyl)amino)caprylic acid and semaglutide.
- Granule Composition: Includes semaglutide, binders, and optional excipients.
- Preparation Method: Involves mixing, dry granulation, and combining with the salt of NAC.
- Bioavailability: Granule design significantly affects bioavailability, which can be predicted from in vitro data.
- Patent Landscape: Part of the Asserted Patents defending against generic versions of RYBELSUS®.
- Exclusivity: Provides Novo Nordisk with exclusive market rights until patent expiration.
Frequently Asked Questions (FAQs)
Q: What is the main subject of United States Patent 11,759,502?
A: The patent covers compositions of GLP-1 peptides and their preparation, specifically focusing on semaglutide and its formulation.
Q: Who are the inventors listed on the patent?
A: The inventors are Thomas Vilhelmsen, Helle Eliasen, and Tue Hansen.
Q: What is the significance of the salt of N-(8-(2-hydroxybenzoyl)amino)caprylic acid in the patent?
A: This component enhances the stability and bioavailability of the GLP-1 peptide when administered orally.
Q: How does the granule design affect the drug's properties?
A: The granule design significantly affects the dissolution properties and bioavailability of the GLP-1 peptide, which can be predicted from in vitro data.
Q: What is the current status of the patent in terms of litigation?
A: The patent is part of ongoing litigation where Novo Nordisk is asserting that Apotex's ANDA infringes on multiple patents, including the '502 Patent.
Cited Sources
- Pharsight, Rybelsus patent expiration, Pharsight.
- Insight.rpxcorp.com, Case 1:24-cv-09729-RMB-AMD Document 17 Filed 12/11/24 Page, Insight.rpxcorp.com.
- Law.berkeley.edu, Software and Patent Scope: A Report from the Middle Innings, Law.berkeley.edu.
- Patents.google.com, *WO2013139694A1 - Compositions of glp-1 peptides and ..., Patents.google.com.
- Insight.rpxcorp.com, Case 1:24-cv-09729-RMB Document 1 Filed 10/10/24 Page, Insight.rpxcorp.com.
