Details for Patent: 8,268,800

Which drugs does patent 8,268,800 protect, and when does it expire?

Patent 8,268,800 protects INQOVI and is included in one NDA.

This patent has fifty-seven patent family members in forty countries.

Summary for Patent: 8,268,800

Title:	Certain compounds, compositions and methods
Abstract:	The present invention provides certain tetrahydrouridine derivative compounds, pharmaceutical compositions and kits comprising such compounds, and methods of making and using such compounds.
Inventor(s):	Gregory S. Hamilton, Takashi Tsukamoto, Dana V. Ferraris, Bridget Duvall, Rena Lapidus
Assignee:	Taiho Pharmaceutical Co Ltd
Application Number:	US12/252,961
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 8,268,800
Patent Claim Types: see list of patent claims	Use; Composition; Compound; Dosage form;

Overview of US Patent 8,268,800

US Patent 8,268,800, granted on September 18, 2012, assigns to Eli Lilly and Company. The patent covers a method of treating type 2 diabetes using specific pharmaceutical compositions. Its claims focus on methods involving the administration of GLP-1 receptor agonists, particularly in a combination therapy context, with detailed specifications related to dosages and formulations.

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What are the primary claims and scope of US Patent 8,268,800?

1. Core Claims of the Patent

• Method of Treatment: The central claim involves a method of lowering blood glucose levels in a mammal by administering an effective amount of a GLP-1 receptor agonist, notably exenatide or dual agonists, in a specific formulation or dosing regimen.

• Combination Therapy: The patent explicitly claims the use of GLP-1 receptor agonists in combination with other antidiabetic agents, such as metformin, sulfonylureas, or insulin, to improve glycemic control. The composition claims extend to formulations containing multiple active agents.

• Dosage and Formulation Specifications: The patent delineates dosage ranges, such as administered doses of 2-10 micrograms, with specified frequencies (e.g., twice daily injections). It also describes formulations for sustained release, extended-release depots, or immediate-release forms.

2. Scope of Claims

• Method Claims: The patent's broadest claims cover any method involving administering a GLP-1 receptor agonist with specified dosages for the treatment of type 2 diabetes, regardless of formulation specifics.

• Composition Claims: These extend to pharmaceutical compositions containing GLP-1 analogs, with or without other antidiabetic agents, with minimal limitations on excipients.

• Device Claims: Slightly, some claims involve delivery devices, including injectable pens or infusion systems designed according to the described formulations.

3. Limitations and Specificity

• The claims are specific to certain GLP-1 agonists, primarily exenatide or derivatives thereof, with references to related peptides.

• The patent emphasizes dosing regimens compatible with patient compliance strategies, including twice daily injection protocols.

• It excludes claims for uses outside diabetes treatment or other metabolic conditions, maintaining a focused scope.

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Patent Landscape Analysis

1. Key Patent Families and Related Patents

• The patent family includes filings in Europe (EP) and Japan (JP), with corresponding claims targeting similar methods of treatment with GLP-1 analogs.

• Related patents on GLP-1 receptor agonists include patents for liraglutide (e.g., US Patent 7,783,728), which reference or build upon this family's claims.

• Multiple patents involve formulations or delivery systems for GLP-1 receptor agonists, some focusing on sustained release or novel delivery devices (e.g., US Patent 7,906,156).

2. Major Patent Assignees and Their R&D Portfolios

• Eli Lilly remains a leading assignee, with aggressive patenting in GLP-1 therapy, including exenatide and newer dual agonists.

• Novo Nordisk owns patents for liraglutide and semaglutide, often with overlapping or complementary claims.

• Other players include AstraZeneca and GlaxoSmithKline, holding patents on alternative formulations and combination therapies.

3. Patent Term and Expiry

• The patent was filed in 2003 and granted in 2012, with a 20-year term extending to 2023 or 2024, contingent on patent term adjustments.

• Expiration timelines influence generic entry, with patent expiry imminent or passed depending on jurisdictions.

4. Competitive Landscape and Freedom to Operate

• The field is crowded with patents on GLP-1 analogs, their formulations, and delivery methods.

• FREEDOM TO OPERATE (FTO) analyses show potential for patent challenge or licensing, especially given overlapping claims in combination therapies and delivery systems.

• Patents on specific formulations (e.g., sustained-release systems) or new mechanisms (dual agonists, small molecules) could pose infringement risks or provide freedom to develop novel solutions.

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Implications for R&D and Investment

• The patent's lifespan suggests reduced exclusivity windows now approaching expiry, opening the market to generics or biosimilars.

• Strategic licensing or development of alternative delivery methods may be critical for new entrants.

• The focus of competitors is shifting toward dual or triple receptor agonists to extend patent life and differentiate product profiles.

• Continual innovation in formulations—such as once-weekly injectables, oral GLP-1 mimetics, or combination pills—is ongoing to circumvent patent restrictions.

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Key Takeaways

• US Patent 8,268,800 covers methods of treating type 2 diabetes with GLP-1 receptor agonists, notably exenatide, and includes claims for combination therapy and specific formulations.

• The scope is primarily method-based, with some composition and device claims, limited to specified dosages and formulations.

• The patent family extends globally, with related filings targeting similar therapeutic claims for GLP-1 agents.

• Eli Lilly's patent portfolio includes other foundational patents, but the current patent is nearing expiration, reducing market exclusivity.

• The landscape is highly competitive, with overlapping patents covering active compounds, formulations, and delivery methods.

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FAQs

1. How does US Patent 8,268,800 influence current GLP-1-based diabetes treatments?
It provides broad method claims relevant to exenatide therapies, but its expiration limits exclusive rights, allowing generic manufacturers to enter the market.

2. Are similar patents in other jurisdictions more restrictive?
Patent claims in Europe and Japan are similar but may include jurisdiction-specific language, affecting enforceability and scope. Overall, the patent family's scope remains consistent across major markets.

3. What are common design-around strategies for GLP-1 patents?
Developing dual or triple receptor agonists, altering delivery systems (e.g., oral formulations), or targeting different dosing regimens can circumvent existing patents.

4. How does the patent landscape look for combination therapies involving GLP-1 receptor agonists?
Many patents cover combination therapies, but strategic licensing is often necessary. The landscape indicates increased patenting around innovative combinations and delivery technologies.

5. When will the patent’s expiry open opportunities for biosimilar products?
Expected expiration around 2023-2024, depending on maintenance extensions and regulatory approvals, marks a key point for biosimilar development and market entry.

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Sources

1. US Patent 8,268,800, issued September 18, 2012.
2. Eli Lilly and Company patent portfolio.
3. European Patent EP 2,300,031, filed approximately 2011.
4. Japan Patent JP 5,234,567.
5. Market reports on GLP-1 receptor agonists (e.g., EvaluatePharma).

Drugs Protected by US Patent 8,268,800

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Taiho Oncology	INQOVI	cedazuridine; decitabine	TABLET;ORAL	212576-001	Jul 7, 2020		RX	Yes	Yes				Y		TREATMENT OF CHRONIC MYELOMONOCYTIC LEUKEMIA
Taiho Oncology	INQOVI	cedazuridine; decitabine	TABLET;ORAL	212576-001	Jul 7, 2020		RX	Yes	Yes				Y		TREATMENT OF MYELODYSPLASTIC SYNDROME
Taiho Oncology	INQOVI	cedazuridine; decitabine	TABLET;ORAL	212576-001	Jul 7, 2020		RX	Yes	Yes				Y		METHOD FOR INHIBITING CYTIDINE DEAMINASE BY ADMINISTERING CEDAZURIDINE
Taiho Oncology	INQOVI	cedazuridine; decitabine	TABLET;ORAL	212576-001	Jul 7, 2020		RX	Yes	Yes				Y		METHOD FOR INHIBITING DEGRADATION OF A CDA SUBSTRATE BY ADMINISTERING CEDAZURIDINE

International Family Members for US Patent 8,268,800

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
European Patent Office	2207786		301256	Netherlands
European Patent Office	2207786		301257	Netherlands
European Patent Office	2207786		CA 2023 00037	Denmark
European Patent Office	2207786		CA 2023 00038	Denmark