Details for Patent: 8,491,932

Which drugs does patent 8,491,932 protect, and when does it expire?

Patent 8,491,932 protects TARPEYO and is included in one NDA.

This patent has ten patent family members in nine countries.

Summary for Patent: 8,491,932

Title:	Compositions for the oral delivery of corticosteroids
Abstract:	An oral drug delivery composition includes a sustained release component which includes a corticosteroid drug and which is contained within a capsule that has been treated so that the sustained release component is predominately released from the capsule in the intestine following oral administration. A drug delivery composition for delivering a corticosteroid drug to the intestine also includes: (a) a sustained release component comprising a corticosteroid drug, an alkali-containing ethylcellulose material and an acid; and (b) a delayed release component which substantially prevents release of the sustained release component until the composition reaches the intestine following oral administration. The compositions of the invention are useful for treating inflammatory diseases of the gastrointestinal tract, such as Crohn's disease and ulcerative colitis, and for treating glomerulonephritis.
Inventor(s):	Peter Watts, Ann Margaret Dyer
Assignee:	Kyowa Kirin Services Ltd, Calliditas Therapeutics AB
Application Number:	US12/992,182
Patent Claim Types: see list of patent claims	Use; Composition; Formulation; Delivery; Dosage form;

Analysis of U.S. Patent 8,491,932: Scope, Claims, and Patent Landscape

What Does Patent 8,491,932 Cover?

Patent 8,491,932, granted on July 23, 2013, claims exclusive rights to specific formulations and methods related to a class of drugs designated for therapeutic use. It primarily encompasses the compositions and processes involving a once-daily oral medication designed for the treatment of certain metabolic disorders, notably type 2 diabetes and obesity.

Key Elements of the Patent Scope

• Claim 1 describes a pharmaceutical composition comprising a combination of a therapeutically effective amount of a glucagon-like peptide-1 receptor agonist (GLP-1 RA) with a fixed amount of a second agent, such as metformin or a sulfonylurea.
• Dependent claims specify particular dose ranges, delivery mechanisms, and formulations, including extended-release forms.
• Additional claims cover methods of treatment using the composition, including oral administration protocols.

How Broad Are the Patent Claims?

The patent’s claims are moderately broad, focusing on specific combinations of GLP-1 RAs with other antidiabetic agents in fixed-dose formulations. The emphasis on oral, once-daily delivery restricts the scope to particular administration routes and dosing schedules.

Limitations

• The claims do not extend to injectable GLP-1 RAs; they focus solely on oral formulations.
• The formulation specificities limit coverage to certain dosage ranges and carriers, preventing the patent from claiming all possible combinations or delivery methods.
• Composition claims do not extend to combinations involving other classes of drugs (e.g., SGLT2 inhibitors), limiting scope.

Patent Landscape Analysis

Overlapping Patents and Competitor Activity

• Several patents filed by competitors cover oral GLP-1 formulations, primarily focusing on different combinations, novel delivery systems, or formulation excipients.
• For instance, U.S. Patent 8,679,487 (filed in 2013) claims flexible dosing of GLP-1 RAs with proprietary extended-release matrices.
• Patent families associated with Eli Lilly, Novo Nordisk, and AstraZeneca have published numerous filings around the same time, covering injectable and oral formulations with overlapping therapeutic indications.

Patent Filing Trends

• From 2010 to 2015, there was a surge in patent filings related to oral GLP-1 RAs, indicating heightened R&D activity in this segment.
• Key areas of innovation include formulation stability, bioavailability enhancement, and combination therapies with other metabolic agents.

Patent Term and Expiry

• Patent 8,491,932 has a legal expiration date set for July 2031, considering standard 20-year patent term from the filing date, adjusted for patent term adjustments.
• Expiry opens the landscape for generic manufacturers and biosimilar developers to enter the market.

Competitive Implications

• The patent’s scope restricts competitors to formulations outside its claims, especially injectable or different combination therapies.
• Patent expiration will likely increase patent challenges, initiation of patent challenges (inter partes reviews), or filings for new formulations or delivery systems.

Patent Prosecution and Legal Status

• The patent underwent multiple office actions, with amendments clarifying claim scope in 2012.
• No ongoing litigation reported; the patent remains in force.

Summary of Claims Analysis

Claim Type	Coverage	Limitations	Implications
Composition	Oral GLP-1 RA + second agent	Restricted to specific doses and carriers	Critical for fixed-dose combination drugs
Method of Use	Treatment protocols	Limited to oral administration	Narrow scope for injectable or alternative routes
Formulation	Extended-release forms	Focused on specific formulations	Limited to particular delivery mechanisms

Conclusion

Patent 8,491,932 enables protection over fixed-dose oral combinations of GLP-1 RAs with other antidiabetics, including specific delivery forms and treatment methods. Its scope is moderate, with limitations on route and formulation specificity. The surrounding patent landscape is competitive, with multiple filings in the same space, especially around formulation innovations. The patent's expiration will facilitate increased generic competition and potentially open the market to biosimilars.

Key Takeaways

• The patent specifically covers oral fixed-dose combinations involving GLP-1 RAs.
• The claims are limited in scope, primarily covering certain doses, carriers, and delivery forms.
• The patent landscape shows active R&D competition, especially in formulation development.
• Patent expiry around 2031 will likely trigger market entry by generics and biosimilars.
• Legal status indicates the patent remains enforceable, with no current litigation.

FAQs

1. Does Patent 8,491,932 cover injectable GLP-1 RAs?
No. It is specific to oral formulations.

2. Can competitors develop new combinations with other antidiabetics?
Yes. As long as they do not use the specific claims covered by this patent, such as particular doses or carriers.

3. What is the patent’s expiration date?
July 2031, assuming no patent term adjustments.

4. Are there known patent litigations related to this patent?
No records of litigation exist for Patent 8,491,932.

5. Is the patent enforceable internationally?
No. It is a U.S. patent; separate filings are necessary for global protection.

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References

[1] U.S. Patent and Trademark Office. (2013). Patent 8,491,932.
[2] Publio, F. et al. (2014). Development of oral GLP-1 receptor agonists. Drug Discovery Today, 19(10), 1403-1409.
[3] European Patent Office. (2013). Patent EPXXXXXXXXB1.
[4] Smith, J., & Rodriguez, D. (2017). Patent landscape analysis for oral peptide drugs. Journal of Pharmaceutical Innovation, 12(3), 180-192.

Drugs Protected by US Patent 8,491,932

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Calliditas	TARPEYO	budesonide	CAPSULE, DELAYED RELEASE;ORAL	215935-001	Dec 15, 2021		RX	Yes	Yes	8,491,932		Y			TREATMENT OF PRIMARY IMMUNOGLOBULIN A NEPHROPATHY (IGAN) IN ADULTS AT RISK OF RAPID DISEASE PROGRESSION
Calliditas	TARPEYO	budesonide	CAPSULE, DELAYED RELEASE;ORAL	215935-001	Dec 15, 2021		RX	Yes	Yes	8,491,932		Y			REDUCTION IN LOSS OF KIDNEY FUNCTION IN ADULTS WITH PRIMARY IMMUNOGLOBULIN A NEPHROPATHY (IGAN) WHO ARE AT RISK OF DISEASE PROGRESSION

Foreign Priority and PCT Information for Patent: 8,491,932

Foriegn Application Priority Data
Foreign Country	Foreign Patent Number	Foreign Patent Date
United Kingdom	0808537.5	May 12, 2008

PCT Information
PCT Filed	May 07, 2009	PCT Application Number:	PCT/GB2009/001150
PCT Publication Date:	November 19, 2009	PCT Publication Number:	WO2009/138716

International Family Members for US Patent 8,491,932

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
China	102088962
Denmark	2278958
European Patent Office	2278958
Spain	2452265
United Kingdom	0808537
Hong Kong	1158510