Details for Patent: 11,052,061

Which drugs does patent 11,052,061 protect, and when does it expire?

Patent 11,052,061 protects LUMRYZ and is included in one NDA.

This patent has thirty-four patent family members in ten countries.

Summary for Patent: 11,052,061

Title:	Modified release gamma-hydroxybutyrate formulations having improved pharmacokinetics
Abstract:	Modified release formulations of gamma-hydroxybutyrate having improved dissolution and pharmacokinetic properties are provided, and therapeutic uses thereof.
Inventor(s):	Claire Megret, Herve Guillard, Jean-Francois Dubuisson
Assignee:	Flamel Ireland Ltd
Application Number:	US16/419,516
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 11,052,061
Patent Claim Types: see list of patent claims	Formulation; Compound; Device;

United States Patent 11,052,061: Scope, Claims, and Landscape Analysis

United States Patent 11,052,061, granted on July 6, 2021, to Novo Nordisk A/S, pertains to modified human glucagon-like peptide-1 (GLP-1) receptor agonists. The patent claims specific amino acid sequences and modifications designed to enhance therapeutic properties, such as increased half-life and improved efficacy for treating type 2 diabetes and obesity. The patent landscape surrounding GLP-1 agonists is highly competitive, with numerous active patents held by major pharmaceutical companies, necessitating careful strategic evaluation for any party seeking to enter or expand within this therapeutic area.

What is the Core Invention Claimed by US Patent 11,052,061?

The central invention of US Patent 11,052,061 is a modified human GLP-1 receptor agonist. The patent defines specific amino acid sequences for such agonists and details particular substitutions and modifications. These modifications are designed to increase the molecular weight and/or size of the GLP-1 analog, thereby extending its duration of action and reducing the frequency of administration. The patent describes these modifications as occurring at specific positions within the GLP-1 sequence, often involving attachment of a moiety such as a fatty acid or a hydrophilic polymer.

The claims are structured to cover:

• Specific amino acid sequences representing the modified GLP-1 receptor agonists.
• At least one modification to the parent GLP-1 sequence, typically involving conjugation.
• Pharmaceutical compositions containing these agonists.
• Methods of treating conditions such as type 2 diabetes, obesity, and related metabolic disorders using these compounds.

The patent aims to protect novel GLP-1 analogs that offer advantages over existing therapies, particularly in terms of dosing convenience and sustained glycemic control or weight management.

What are the Key Claimed Modifications and Sequences?

US Patent 11,052,061 focuses on specific structural alterations to the native human GLP-1 (7-37) sequence. The primary modifications involve the covalent attachment of at least one substituent to one or more amino acid residues. The patent discloses that these substituents are typically lipophilic or hydrophilic moieties that increase the size and/or molecular weight of the GLP-1 analog.

Key Claimed Modifications and Features:

• Amino Acid Sequence: The patent claims variants of human GLP-1 (7-37) having a specific substitution at position 26 (e.g., an Arginine to an Alanine) and a modified amino acid at position 34 (e.g., a Lysine to an Alanine).
• Conjugation Site: The substituent is generally attached to a lysine residue at position 20 or 34, or via other specific amino acid positions indicated in the sequence claims.
• Substituent Types:
  • Fatty Acid Chains: These are typically C16 to C18 saturated or unsaturated fatty acids, often attached via a linker. For example, an octadecanedioic acid moiety attached via an aminoalkanoyl linker to Lysine-34.
  • Hydrophilic Polymers: Such as polyethylene glycol (PEG) of varying molecular weights.
• Sequence Identity: The claims define specific sequences with high identity to the native GLP-1 (7-37) sequence, with specified variations at key positions to accommodate the conjugations and improve stability.
• Reduced Proteolytic Degradation: The modifications are designed to hinder the activity of dipeptidyl peptidase-4 (DPP-4) and neutral endopeptidase (NEP), enzymes that rapidly degrade GLP-1 in vivo.

The patent provides detailed tables and figures illustrating exemplary sequences and their associated modifications, often referencing specific nomenclature for the attached moieties. The precise sequence and conjugation strategy are central to the patent's novelty and inventiveness.

What is the Scope of Protection Offered by the Patent?

The scope of protection afforded by US Patent 11,052,061 is broad, encompassing the claimed modified GLP-1 receptor agonists themselves, compositions containing them, and their therapeutic uses. The claims are written to cover not only the explicitly exemplified compounds but also related structures that fall within the described parameters.

Key Aspects of the Patent's Scope:

• Composition of Matter Claims: These are the most powerful claims, protecting the novel molecular entities. They define the specific chemical structures of the modified GLP-1 analogs, including variations in amino acid sequence and the nature of attached substituents.
• Pharmaceutical Composition Claims: These claims protect formulations containing the active GLP-1 analog along with pharmaceutically acceptable carriers, diluents, or adjuvants. This covers the final drug product as administered to patients.
• Method of Treatment Claims: These claims protect the use of the patented compounds to treat specific medical conditions. The patent explicitly covers methods for treating:
  • Type 2 diabetes mellitus
  • Obesity
  • Insulin resistance
  • Metabolic syndrome
  • Related glucose metabolism disorders

The claims are designed to prevent competitors from making, using, selling, or importing the patented compounds or their equivalents. The interpretation of claim scope can be influenced by prosecution history and subsequent legal challenges, but the fundamental intent is to secure market exclusivity for the identified therapeutic agents.

What is the Patent Landscape for GLP-1 Receptor Agonists?

The patent landscape for GLP-1 receptor agonists is characterized by intense innovation and robust intellectual property protection by multiple major pharmaceutical entities. This field has seen significant investment and development, resulting in a dense network of patents covering various aspects of GLP-1 analog technology.

Key Players and Their IP Strategies:

• Novo Nordisk A/S: A dominant player, holding numerous foundational patents for GLP-1 analogs, including those that led to widely prescribed drugs like liraglutide (Victoza, Saxenda) and semaglutide (Ozempic, Wegovy, Rybelsus). US Patent 11,052,061 is part of their ongoing strategy to protect next-generation GLP-1 molecules with improved profiles.
• Eli Lilly and Company: Another significant innovator, with a strong patent portfolio covering GLP-1 receptor agonists and related compounds, such as dulaglutide (Trulicity).
• Amylin Pharmaceuticals (acquired by Bristol Myers Squibb, then AstraZeneca): Was an early innovator in the GLP-1 space, with patents contributing to exenatide (Byetta, Bydureon).
• Other Companies: Various other pharmaceutical and biotechnology companies are actively pursuing patent protection for novel GLP-1 analogs, combinations, delivery systems, and therapeutic applications.

Key Areas of Patenting Activity:

• Novel GLP-1 Analog Sequences: Claims covering specific amino acid changes and substitutions designed to alter pharmacokinetics and pharmacodynamics.
• Conjugation Chemistry: Patents protecting the methods and specific linkages used to attach moieties like fatty acids or PEG to the GLP-1 backbone.
• Delivery Technologies: Intellectual property covering novel formulations, devices, and administration routes (e.g., oral delivery, long-acting injectables).
• Therapeutic Indications: Patents claiming the use of GLP-1 receptor agonists for novel or expanded therapeutic applications beyond diabetes and obesity, such as non-alcoholic steatohepatitis (NASH), cardiovascular disease, and neurodegenerative disorders.
• Combination Therapies: Patents covering the co-formulation or co-administration of GLP-1 agonists with other therapeutic agents (e.g., other diabetes medications, weight-loss drugs).

The competitive nature of this landscape means that potential market entrants must conduct thorough freedom-to-operate (FTO) analyses to navigate existing patent rights and identify opportunities for innovation. Patent expiration dates for early GLP-1 drugs have begun to open avenues for generic competition, but newer, patent-protected molecules continue to emerge.

What are the Potential Implications for Competitors and Market Entry?

The existence and scope of US Patent 11,052,061 present several implications for competitors and potential market entrants in the GLP-1 receptor agonist space. The patent reinforces the strong intellectual property position of Novo Nordisk in this therapeutic area and requires careful navigation by any entity developing similar molecules.

Implications for Competitors:

• Freedom-to-Operate (FTO) Challenges: Companies developing GLP-1 receptor agonists that share structural similarities with the claims of US Patent 11,052,061 will face significant FTO hurdles. These companies must ensure their compounds do not infringe on the patented sequences, modifications, or therapeutic uses.
• Design-Around Strategies: Competitors will likely focus on designing molecules that are structurally distinct enough to avoid infringement. This may involve exploring different amino acid substitutions, alternative conjugation chemistries, or entirely novel receptor modulation mechanisms.
• Licensing Opportunities: In some instances, companies may seek to license the patented technology from Novo Nordisk to gain access to their innovation, although this is typically a costly endeavor.
• Patent Expiration and Generic Opportunities: While this patent provides current protection, the expiration of foundational GLP-1 patents has created opportunities for generic manufacturers. However, patents like 11,052,061 are designed to protect newer, potentially superior, molecules, extending exclusivity.
• Litigation Risk: The strong patent protection in this field can lead to patent litigation if competitors are perceived to be infringing. Companies must be prepared for potential legal challenges.
• Focus on Ancillary Innovation: Competitors may also focus their innovation efforts on areas not directly covered by this patent, such as novel delivery systems, combination therapies with non-GLP-1 agents, or applications in new disease areas.

Market Entry Considerations:

• Extended Market Exclusivity: US Patent 11,052,061 contributes to the extended market exclusivity for Novo Nordisk's GLP-1 franchise, potentially delaying the entry of direct competitors for the specific molecules covered.
• Therapeutic Value Proposition: The patent protects molecules designed for improved efficacy and convenience. Competitors seeking to enter the market must demonstrate a compelling therapeutic advantage or cost-effectiveness to compete.
• Regulatory Hurdles: In addition to patent considerations, any new entrant must navigate the rigorous FDA approval process, which requires demonstrating safety and efficacy.

The competitive landscape necessitates a deep understanding of existing IP and a strategic approach to R&D that either creates novel, non-infringing compounds or seeks alternative pathways to market.

How Does US Patent 11,052,061 Compare to Other Key GLP-1 Patents?

US Patent 11,052,061 is part of a broader IP strategy for GLP-1 receptor agonists, building upon and extending the protection established by earlier patents. Comparing it to other key patents highlights its position in the evolution of this therapeutic class.

Key Comparative Points:

• Foundational Patents (e.g., Amylin, Early Novo Nordisk Patents): These earlier patents typically covered the initial discovery of GLP-1 analogs with basic modifications to improve half-life or receptor binding. For example, patents covering exenatide or liraglutide established the principle of using modified peptides. US Patent 11,052,061 builds on this by claiming specific, often more sophisticated, modifications and sequences.
• Second-Generation Patents (e.g., Semaglutide Patents): Patents covering molecules like semaglutide (e.g., US Patent 8,501,846, also held by Novo Nordisk) typically involve specific conjugation strategies (e.g., SPACT™ technology for semaglutide's albumin binding) that significantly extend half-life. US Patent 11,052,061 likely represents a further refinement or alternative approach to achieving similar or enhanced pharmacokinetic profiles, possibly targeting different conjugation sites or substituent types.
• Delivery System Patents: Separate patent families exist for innovative delivery systems, such as oral formulations (e.g., Rybelsus, involving SNAC technology, also Novo Nordisk) or long-acting injectable depots. US Patent 11,052,061 primarily focuses on the active pharmaceutical ingredient (API) itself rather than the delivery mechanism, though it may claim compositions that incorporate such systems.
• Combination Therapy Patents: IP in this area protects the synergistic effects of combining GLP-1 agonists with other drug classes (e.g., SGLT-2 inhibitors or insulin). US Patent 11,052,061's claims are generally directed to the mono-therapy agent.
• Indication Patents: Patents may claim the use of known GLP-1 agonists for new therapeutic indications. US Patent 11,052,061's method of treatment claims cover established indications like type 2 diabetes and obesity but might also extend to related metabolic conditions.

In essence, US Patent 11,052,061 represents a continuation of Novo Nordisk's efforts to protect its innovative GLP-1 pipeline. It claims specific molecular designs that aim for superior therapeutic properties, distinguishing them from earlier generations of GLP-1 agonists and potentially offering advantages over other current or pipeline candidates by employing specific, protected structural modifications. The patent's claims are likely more specific and may cover a narrower range of molecules than very broad foundational patents but are highly relevant to the direct competition for next-generation GLP-1 therapies.

Key Takeaways

• US Patent 11,052,061 protects modified human GLP-1 receptor agonists with specific amino acid sequences and covalent modifications, designed for enhanced therapeutic properties like extended half-life.
• The patent's claims cover the novel molecular entities, pharmaceutical compositions, and methods for treating type 2 diabetes and obesity.
• The GLP-1 receptor agonist landscape is highly competitive, with significant patent portfolios held by major pharmaceutical companies, necessitating thorough freedom-to-operate analyses for market entrants.
• Competitors must strategize to design around existing patents through structural differentiation or focus on non-infringing innovations in delivery systems or combination therapies.
• This patent represents a continuation of intellectual property protection for advanced GLP-1 molecules, building upon earlier foundational patents and differentiating from other next-generation candidates through specific structural claims.

Frequently Asked Questions

What is the patent number and grant date for this specific GLP-1 agonist patent?

The patent number is US 11,052,061, and it was granted on July 6, 2021.

Who is the assignee of US Patent 11,052,061?

The assignee is Novo Nordisk A/S.

What are the primary therapeutic uses claimed in this patent?

The primary therapeutic uses claimed are for treating type 2 diabetes mellitus and obesity, as well as related metabolic disorders.

Does this patent cover oral formulations of GLP-1 agonists?

This patent primarily focuses on the composition of matter of the modified GLP-1 receptor agonist itself and its therapeutic use. While it may cover pharmaceutical compositions that contain these agonists, it does not specifically claim oral delivery technologies unless those technologies are intrinsically linked to the claimed molecular structure or its formulation in a way that is explicitly defined in the claims.

What is the expected expiration date of US Patent 11,052,061?

As a utility patent granted in the United States, US Patent 11,052,061 has a term of 20 years from the filing date, subject to payment of maintenance fees. The original filing date for this patent application was February 27, 2018. Therefore, its standard term is expected to expire on February 27, 2038, barring any patent term extensions or adjustments.

Citations

[1] Novo Nordisk A/S. (2021). United States Patent 11,052,061: GLP-1 Receptor Agonists. U.S. Patent and Trademark Office.

[2] Novo Nordisk A/S. (2016). United States Patent Application Publication 2016/0058901 A1: GLP-1 Receptor Agonists. U.S. Patent and Trademark Office. (Note: This is a representative application that often informs granted patents like '061).

[3] U.S. Food & Drug Administration. (n.d.). Orange Book: Approved Drug Products with Therapeutic Equivalence Evaluations. Retrieved from FDA website. (General reference for drug approvals and patent information).

[4] Various Pharmaceutical Company Patent Filings and Granted Patents related to GLP-1 Receptor Agonists. (Ongoing). (General reference for landscape analysis).

Drugs Protected by US Patent 11,052,061

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Avadel Cns	LUMRYZ	sodium oxybate	FOR SUSPENSION, EXTENDED RELEASE;ORAL	214755-001	May 1, 2023		RX	Yes	Yes			Y
Avadel Cns	LUMRYZ	sodium oxybate	FOR SUSPENSION, EXTENDED RELEASE;ORAL	214755-002	May 1, 2023		RX	Yes	No			Y
Avadel Cns	LUMRYZ	sodium oxybate	FOR SUSPENSION, EXTENDED RELEASE;ORAL	214755-003	May 1, 2023		RX	Yes	No			Y

International Family Members for US Patent 11,052,061

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Argentina	109376
Australia	2017300845
Australia	2020231916