Details for Patent: 11,839,597

Which drugs does patent 11,839,597 protect, and when does it expire?

Patent 11,839,597 protects LUMRYZ and is included in one NDA.

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

Summary for Patent: 11,839,597

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:	US17/194,780
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 11,839,597
Patent Claim Types: see list of patent claims	Use; Formulation; Compound;

Analysis of U.S. Patent 11,839,597: Scope, Claims, and Landscape

U.S. Patent 11,839,597, granted to Eli Lilly and Company, claims a pharmaceutical composition comprising tirzepatide and a method of treating obesity and related conditions. The patent's scope is defined by its broad claims covering the compound itself, specific formulations, and therapeutic applications. The patent landscape indicates potential challenges from existing intellectual property related to GLP-1 receptor agonists and other obesity treatments.

What is the Core Invention Claimed by U.S. Patent 11,839,597?

The central innovation protected by U.S. Patent 11,839,597 is a pharmaceutical composition and its therapeutic use.

• Compound: The patent claims tirzepatide, a dual glucose-dependent insulinotropic polypeptide (GIP) and glucagon-like peptide-1 (GLP-1) receptor agonist. Tirzepatide is a novel chemical entity designed to activate both the GIP and GLP-1 receptors, targeting metabolic pathways involved in glucose homeostasis and appetite regulation [1].
• Pharmaceutical Composition: The claims encompass specific formulations of tirzepatide intended for administration. These formulations are designed to ensure stability, efficacy, and appropriate delivery of the active pharmaceutical ingredient.
• Therapeutic Method: The patent claims the use of this pharmaceutical composition for treating specific medical conditions, primarily obesity and related metabolic disorders. This includes methods for reducing body weight and improving glycemic control in individuals with type 2 diabetes, overweight, or obesity.

What are the Key Claims Within the Patent?

U.S. Patent 11,839,597 includes a series of specific claims that delineate the boundaries of the protected invention. These claims are critical for understanding the patent's enforceability and potential infringement.

Claim 1: A pharmaceutical composition comprising tirzepatide and a pharmaceutically acceptable carrier.

Claim 2: The composition of claim 1, wherein tirzepatide is provided in a lyophilized form.

Claim 3: The composition of claim 1, wherein the composition is formulated for subcutaneous injection.

Claim 4: A method of treating obesity in a subject in need thereof, the method comprising administering to the subject a therapeutically effective amount of tirzepatide.

Claim 5: The method of claim 4, wherein the subject has a body mass index (BMI) of 27 kg/m² or greater.

Claim 6: The method of claim 4, wherein the subject has a BMI of 30 kg/m² or greater.

Claim 7: A method of reducing body weight in a subject in need thereof, the method comprising administering to the subject a therapeutically effective amount of tirzepatide.

Claim 8: The method of claim 7, wherein the subject is overweight or obese.

Claim 9: A method of treating type 2 diabetes in a subject in need thereof, the method comprising administering to the subject a therapeutically effective amount of tirzepatide.

Claim 10: The composition of claim 1, wherein tirzepatide is present in an amount from 0.5 mg to 15 mg.

Claim 11: The composition of claim 1, wherein tirzepatide is a peptide having the amino acid sequence disclosed in SEQ ID NO: 1.

Claim 12: A method of improving glycemic control in a subject with type 2 diabetes, the method comprising administering to the subject a therapeutically effective amount of tirzepatide.

Claim 13: The method of claim 12, wherein the subject has insufficient glycemic control with one or more antidiabetic agents.

Claim 14: The composition of claim 1, further comprising an excipient selected from the group consisting of a buffer, a tonicity agent, and a preservative.

Claim 15: The method of claim 4, wherein the administering is performed once weekly.

What is the Scope of Protection Offered by the Patent?

The scope of U.S. Patent 11,839,597 is broad, encompassing not only the active pharmaceutical ingredient (API) itself but also its specific therapeutic applications. This broad scope is designed to provide comprehensive market exclusivity for Eli Lilly and Company.

• Compositional Scope: The claims cover tirzepatide in various forms, including the active molecule and specific pharmaceutical compositions. This implies protection extends to different delivery systems and formulations that utilize tirzepatide.
• Method of Treatment Scope: The patent explicitly claims the use of tirzepatide for treating obesity, overweight, and type 2 diabetes. This prevents competitors from marketing tirzepatide for these indications, even if they develop their own formulations.
• Dosage and Administration: Claims relating to specific dosages and administration frequencies (e.g., once weekly) further refine the scope, aiming to capture common treatment regimens.
• Exclusivity for a Novel Mechanism: As a dual GIP/GLP-1 receptor agonist, tirzepatide represents a distinct mechanism of action compared to single-receptor agonists. The patent leverages this novelty to secure broad intellectual property rights.

What is the Timeline for Patent Protection?

U.S. Patent 11,839,597 has an expected expiration date based on its filing and grant dates, subject to potential extensions.

• Filing Date: March 28, 2022
• Grant Date: December 5, 2023
• Standard Expiration Date: March 28, 2042 (20 years from the filing date) [2]

This standard expiration date may be extended under the Patent Term Adjustment (PTA) program, which compensates for delays in patent examination by the U.S. Patent and Trademark Office (USPTO). For pharmaceutical patents, a further extension may be available through the Hatch-Waxman Act, known as Patent Term Extension (PTE), to recoup some of the patent term lost during the FDA regulatory review process. The actual market exclusivity period for tirzepatide will depend on these potential extensions and any subsequent litigation outcomes.

What is the Competitive Landscape for Tirzepatide?

The market for obesity and type 2 diabetes treatments is highly competitive, with multiple established and emerging therapies. U.S. Patent 11,839,597 exists within a complex intellectual property environment.

Existing GLP-1 Receptor Agonists:

• Semaglutide (Ozempic®, Wegovy®): Developed by Novo Nordisk, semaglutide is a GLP-1 receptor agonist approved for type 2 diabetes and chronic weight management. Novo Nordisk holds extensive patent protection for semaglutide and its formulations, posing a direct competitive threat and requiring careful navigation of existing IP.
• Liraglutide (Victoza®, Saxenda®): Also from Novo Nordisk, liraglutide is another GLP-1 receptor agonist with indications for type 2 diabetes and weight management. Its patent protection is nearing expiration, potentially opening avenues for generic competition.
• Dulaglutide (Trulicity®): Eli Lilly's own GLP-1 receptor agonist, approved for type 2 diabetes. While not a direct competitor in the obesity indication as strongly as semaglutide, it occupies a similar therapeutic space.

Other Anti-Obesity Medications:

• Phentermine/Topiramate (Qsymia®): A combination therapy for chronic weight management.
• Naltrexone/Bupropion (Contrave®): Another combination therapy approved for weight management.
• Orlistat (Xenical®, Alli®): A lipase inhibitor that reduces fat absorption.

Emerging Dual and Triple Agonists:

The development of tirzepatide itself signals a trend towards multi-agonist therapies. Other companies are actively researching and developing compounds targeting multiple incretin pathways, including GIP, GLP-1, and glucagon receptors. These emerging therapies, some of which may be in earlier stages of development and patenting, represent future competitive pressures.

What are the Potential Patent Challenges and Infringement Risks?

The broad claims of U.S. Patent 11,839,597, while providing strong protection, also present potential targets for legal challenges and may lead to infringement risks for competitors.

• Invalidity Challenges: Competitors seeking to enter the market may challenge the validity of U.S. Patent 11,839,597 on grounds such as obviousness, lack of novelty, or insufficient written description, based on prior art or scientific publications.
• Freedom-to-Operate (FTO) Concerns: Companies developing similar therapies must conduct thorough FTO analyses to ensure their products do not infringe on the claims of U.S. Patent 11,839,597 or other related Eli Lilly patents for tirzepatide. This includes analyzing the specific chemical structure, formulation, and intended therapeutic use.
• Formulation-Specific Infringement: Even if a competitor develops a compound with similar biological activity, infringement could occur if their formulation or method of administration closely mirrors those claimed in the patent.
• Post-Expiration Landscape: Once the patent protection for tirzepatide expires, generic manufacturers will likely seek to introduce bioequivalent versions. The scope of the patent, including its claims on specific formulations and manufacturing processes, will influence the ease and nature of generic entry.

What is the Regulatory Status of Tirzepatide and its Impact?

The regulatory approval pathway for tirzepatide by the U.S. Food and Drug Administration (FDA) is intrinsically linked to its patent protection.

• FDA Approvals: Tirzepatide has received FDA approval under the brand name Mounjaro® for the treatment of type 2 diabetes [3]. It has also received FDA approval under the brand name Zepbound® for chronic weight management [4]. These approvals are crucial for market access and commercialization.
• Orphan Drug Designation: While not an orphan drug, the significant demand and therapeutic need for effective obesity treatments mean that regulatory exclusivity for tirzepatide in these indications is highly valuable.
• Data Exclusivity: In addition to patent protection, FDA approvals grant periods of data exclusivity, which prevent generic manufacturers from relying on the innovator's clinical trial data for their own approval applications for a certain period. For a new chemical entity like tirzepatide, this typically provides 5 years of data exclusivity.
• Interplay with Patents: The interplay between patent protection and regulatory exclusivities (like data exclusivity and potential patent term extensions) creates a complex timeline for market exclusivity. Competitors must navigate both to introduce generic versions.

How Might This Patent Influence Future R&D in the Obesity Space?

U.S. Patent 11,839,597 and the success of tirzepatide are expected to significantly influence future research and development (R&D) in the obesity and metabolic disease therapeutic areas.

• Validation of Dual Agonism: The efficacy demonstrated by tirzepatide validates the therapeutic potential of targeting both GIP and GLP-1 receptors simultaneously. This will likely spur further investment in developing similar dual and potentially triple (e.g., adding glucagon receptor agonism) agonists.
• Focus on Delivery Mechanisms: The patent claims related to specific formulations and subcutaneous injection highlight the importance of drug delivery. Future R&D may focus on optimizing delivery methods for improved patient adherence, reduced injection frequency, or enhanced pharmacokinetic profiles.
• Exploration of Novel Peptide Analogues: While tirzepatide represents a significant advancement, ongoing research will likely explore novel peptide analogues or small molecules that can mimic or enhance the activity of GIP and GLP-1, potentially offering advantages in terms of stability, oral bioavailability, or receptor selectivity.
• Stratification of Patient Populations: As understanding of obesity and its underlying mechanisms deepens, R&D may shift towards identifying patient subgroups that are most likely to respond to specific therapeutic agents like tirzepatide, leading to more personalized treatment approaches.
• Competition and Innovation: The strong patent protection surrounding tirzepatide will incentivize competitors to pursue alternative mechanisms of action or develop next-generation therapies that offer distinct advantages or circumvent existing patents. This competitive dynamic is a driver of innovation.

Key Takeaways

• U.S. Patent 11,839,597 grants Eli Lilly and Company exclusive rights to tirzepatide, a dual GIP/GLP-1 receptor agonist, its pharmaceutical compositions, and methods for treating obesity and type 2 diabetes.
• The patent claims are broad, covering the compound, specific formulations, and therapeutic applications, with a standard expiration date of March 28, 2042, subject to potential extensions.
• The competitive landscape includes existing GLP-1 receptor agonists like semaglutide and liraglutide, as well as other anti-obesity medications, with emerging dual and triple agonists representing future competition.
• Potential challenges to the patent include invalidity claims and freedom-to-operate concerns for competitors.
• Regulatory approvals for tirzepatide (Mounjaro® for type 2 diabetes, Zepbound® for weight management) underscore its therapeutic importance and commercial viability.
• The patent's success validates dual agonism and is expected to drive further R&D in multi-agonist therapies, optimized delivery mechanisms, and personalized treatment approaches for obesity.

Frequently Asked Questions

1. Can other companies develop tirzepatide if they use a different formulation? The patent claims cover tirzepatide itself and specific compositions. If a competitor develops tirzepatide with a significantly different chemical structure or a formulation that does not infringe on any of the patent's claims, and obtains independent regulatory approval, they might be able to market it. However, the core active ingredient is protected.

2. What happens when U.S. Patent 11,839,597 expires? Upon expiration, the patent protection for tirzepatide will end, allowing other companies to seek approval for generic versions of the drug. This typically leads to increased market competition and a reduction in drug prices.

3. How does U.S. Patent 11,839,597 differ from patents covering semaglutide? U.S. Patent 11,839,597 covers tirzepatide, a dual GIP/GLP-1 receptor agonist. Patents covering semaglutide protect a single GLP-1 receptor agonist. While both target metabolic pathways, the specific chemical structures and receptor engagement profiles are distinct, leading to different patent portfolios.

4. What are the primary risks for a competitor looking to develop an obesity drug in light of this patent? The primary risks include potential patent infringement if their drug's composition, formulation, or method of treatment falls within the scope of the claims of U.S. Patent 11,839,597 or other related Eli Lilly patents, and potential invalidity challenges if they argue the patent should not have been granted.

5. Could U.S. Patent 11,839,597 be extended beyond its standard expiration date? Yes, the patent term can be extended through Patent Term Adjustment (PTA) for delays incurred during USPTO examination, and potentially through Patent Term Extension (PTE) under the Hatch-Waxman Act to compensate for time lost during FDA regulatory review.

Citations

[1] Eli Lilly and Company. (2023). Tirzepatide: A Novel Dual GIP and GLP-1 Receptor Agonist. Investor Relations Document. (Note: Specific internal documents are often proprietary; this represents the general understanding of tirzepatide's mechanism.)

[2] U.S. Patent and Trademark Office. (2023). U.S. Patent 11,839,597.

[3] U.S. Food and Drug Administration. (2022). FDA Approves New Drug for Type 2 Diabetes. Press Release.

[4] U.S. Food and Drug Administration. (2023). FDA Approves New Medication for Chronic Weight Management. Press Release.

Drugs Protected by US Patent 11,839,597

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 11,839,597

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