NESINA Drug Patent Profile

When do Nesina patents expire, and when can generic versions of Nesina launch?

Nesina is a drug marketed by Takeda Pharms Usa and is included in one NDA. There are two patents protecting this drug and one Paragraph IV challenge.

This drug has sixty-nine patent family members in thirty-seven countries.

The generic ingredient in NESINA is alogliptin benzoate. There are ten drug master file entries for this compound. Five suppliers are listed for this compound. Additional details are available on the alogliptin benzoate profile page.

DrugPatentWatch^® Generic Entry Outlook for Nesina

Nesina was eligible for patent challenges on January 25, 2017.

By analyzing the patents and regulatory protections it appears that the earliest date for generic entry will be July 27, 2026. This may change due to patent challenges or generic licensing.

There have been five patent litigation cases involving the patents protecting this drug, indicating strong interest in generic launch. Recent data indicate that 63% of patent challenges are decided in favor of the generic patent challenger and that 54% of successful patent challengers promptly launch generic drugs.

There are two tentative approvals for the generic drug (alogliptin benzoate), which indicates the potential for near-term generic launch.

Indicators of Generic Entry

Summary for NESINA

International Patents:	69
US Patents:	2
Applicants:	1
NDAs:	1
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for NESINA

Paragraph IV (Patent) Challenges for NESINA

Tradename	Dosage	Ingredient	Strength	NDA	ANDAs Submitted	Submissiondate
NESINA	Tablets	alogliptin benzoate	6.25 mg, 12.5 mg and 25 mg	022271	5	2017-01-25

US Patents and Regulatory Information for NESINA

NESINA is protected by two US patents and one FDA Regulatory Exclusivity.

This potential generic entry date is based on REVISIONS TO THE PEDIATRIC USE SUBSECTION OF LABELING TO INCLUDE THE RESULTS FROM CLINICAL STUDY SYR-322-309, CONDUCTED IN RESPONSE TO A PEDIATRIC WRITTEN REQUEST.

Generics may enter earlier, or later, based on new patent filings, patent extensions, patent invalidation, early generic licensing, generic entry preferences, and other factors.

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Exclusivity Expiration
Takeda Pharms Usa	NESINA	alogliptin benzoate	TABLET;ORAL	022271-001	Jan 25, 2013		RX	Yes	No	7,807,689		Y	Y
Takeda Pharms Usa	NESINA	alogliptin benzoate	TABLET;ORAL	022271-003	Jan 25, 2013		RX	Yes	Yes	7,807,689		Y	Y
Takeda Pharms Usa	NESINA	alogliptin benzoate	TABLET;ORAL	022271-002	Jan 25, 2013		RX	Yes	No	7,807,689		Y	Y
Takeda Pharms Usa	NESINA	alogliptin benzoate	TABLET;ORAL	022271-003	Jan 25, 2013		RX	Yes	Yes	8,697,125		Y

International Patents for NESINA

When does loss-of-exclusivity occur for NESINA?

Based on analysis by DrugPatentWatch, the following patents block generic entry in the countries listed below:

Argentina

Canada

Chile

Croatia

European Patent Office

Japan

Peru

Spain

Taiwan

Generics may enter earlier, or later, based on new patent filings, patent extensions, patent invalidation, early generic licensing, generic entry preferences, and other factors.

See the table below for additional patents covering NESINA around the world.

Country	Patent Number	Title	Estimated Expiration
Japan	2006298933	DIPEPTIDYL PEPTIDASE INHIBITORS
Canada	2819705	PROCEDE DE REGULATION DU METABOLISME DU GLUCOSE ET REACTIFS AFFERENTS (METHOD OF REGULATING GLUCOSE METABOLISM, AND REAGENTS RELATED THERETO)
Japan	4948298
Japan	2007191494	MEDICINE

Supplementary Protection Certificates for NESINA

Patent Number	Supplementary Protection Certificate	SPC Country	SPC Expiration	SPC Description
1084705	SPC/GB14/083	United Kingdom		PRODUCT NAME: ALOGLIPTIN; REGISTERED: UK EU/1/13/844 20130923
0861666	SPC/GB07/009	United Kingdom		SPC/GB07/009: 20070126
1084705	C01084705/01	Switzerland		PRODUCT NAME: SITAGLIPTIN; REGISTRATION NO/DATE: SWISSMEDIC 57863 18.04.2007
1084705	PA2014044	Lithuania		PRODUCT NAME: LINAGLIPTINUM; REGISTRATION NO/DATE: EU/1/11/707/001-011 20110824

NESINA: Patent Landscape and Investment Fundamentals Analysis

Last updated: February 19, 2026

NESINA (alogliptin) faces a complex patent environment with expiring primary patents in key markets. Its future market performance is contingent on the company's strategy for navigating these expirations, particularly through potential lifecycle management and new market entries.

What is NESINA's Current Patent Status?

The primary compound patents for alogliptin, the active pharmaceutical ingredient in NESINA, have expired or are nearing expiration in major markets.

• United States: The key patent covering alogliptin, U.S. Patent No. 6,436,957, expired on October 14, 2022. This patent was foundational to NESINA's market exclusivity.
• Europe: European Patent EP1067142, which also covers alogliptin, expired in September 2023.
• Japan: Japanese Patent JP3771233, relevant to alogliptin, expired in July 2023.
• Other Markets: Similar patent expiries have occurred or are imminent in other significant pharmaceutical markets.

What are the Key Applications of NESINA?

NESINA is a dipeptidyl peptidase-4 (DPP-4) inhibitor used for the treatment of type 2 diabetes mellitus. Its primary indication is to improve glycemic control.

• Mechanism of Action: NESINA inhibits the DPP-4 enzyme, which increases the levels of incretin hormones (GLP-1 and GIP). These hormones enhance insulin secretion and suppress glucagon release in a glucose-dependent manner, thereby lowering blood glucose levels.
• Therapeutic Use: It is used as monotherapy or in combination with other antidiabetic agents, such as metformin, sulfonylureas, or thiazolidinediones, to achieve target HbA1c levels.

What is NESINA's Market Performance and Competitive Landscape?

NESINA has established a market presence, but faces intense competition within the DPP-4 inhibitor class and from newer diabetes treatment modalities.

Sales Performance

• Historical Sales: Global sales for NESINA (marketed as Nesina in the U.S. and Vipidia in other regions) have shown a fluctuating trend. For example, in 2020, Takeda Pharmaceutical Co. Ltd. reported global sales of approximately $543 million for alogliptin. By 2022, global sales were reported around $413 million, indicating a decline [1, 2].
• Market Penetration: While NESINA has secured prescriptions, it competes with other established DPP-4 inhibitors like sitagliptin (Januvia), saxagliptin (Onglyza), and linagliptin (Tradjenta), which often hold larger market shares due to earlier market entry and broader clinical trial data.

Competitive Landscape

The diabetes market is highly dynamic with continuous innovation. NESINA competes with:

• Other DPP-4 Inhibitors:
  • Sitagliptin (Merck & Co.)
  • Saxagliptin (AstraZeneca)
  • Linagliptin (Boehringer Ingelheim)
  • Dapagliflozin (AstraZeneca)
  • Empagliflozin (Boehringer Ingelheim)
  • Canagliflozin (Janssen)
• Other Diabetes Drug Classes:
  • GLP-1 Receptor Agonists: Semaglutide (Novo Nordisk), Liraglutide (Novo Nordisk), Dulaglutide (Eli Lilly) – these have gained significant traction due to demonstrated cardiovascular and renal benefits.
  • SGLT2 Inhibitors: Dapagliflozin (AstraZeneca), Empagliflozin (Boehringer Ingelheim), Canagliflozin (Janssen) – these are also favored for their cardiovascular and renal protective effects, often positioning them ahead of DPP-4 inhibitors in treatment guidelines.
  • Insulin Therapies: A wide range of insulin products for basal and bolus needs.
  • Other Oral Hypoglycemics: Metformin, Sulfonylureas, Thiazolidinediones.

The increasing emphasis on cardiovascular and renal outcome benefits in diabetes treatment guidelines has favored newer drug classes like GLP-1 RAs and SGLT2 inhibitors, potentially limiting the growth trajectory of DPP-4 inhibitors like NESINA.

What are the Opportunities and Risks for NESINA Post-Patent Expiry?

The expiration of primary patents presents significant risks from generic competition but also opens avenues for strategic market plays.

Opportunities

• Lifecycle Management and New Formulations: Manufacturers may seek to develop and patent new formulations or combination therapies involving alogliptin to extend market exclusivity.
  • Combination Products: Patents on fixed-dose combinations (e.g., alogliptin with metformin) could offer continued protection. For instance, the patent for Nesina Met (alogliptin-metformin) in the U.S. has different expiry dates, with some components potentially expiring later than the alogliptin compound patent.
  • Extended-Release Formulations: Developing and patenting novel drug delivery systems or extended-release versions of alogliptin.
• Geographic Market Expansion: Exploring or expanding market access in regions where patent protection is longer or regulatory pathways are less mature. This could involve targeting emerging markets with lower generic penetration rates.
• Out-licensing and Partnerships: Licensing alogliptin for use in specific therapeutic areas or patient populations where it demonstrates particular efficacy, or partnering with companies to develop new applications.
• Post-Marketing Surveillance and Real-World Evidence: Generating robust real-world data demonstrating long-term safety, efficacy, and cost-effectiveness can support continued market access and prescribing, even in the face of generic competition.

Risks

• Generic Competition: The most immediate risk is the introduction of generic alogliptin. Generic manufacturers typically enter the market shortly after primary patent expiry, offering significantly lower-priced alternatives. This leads to rapid erosion of market share and revenue for the originator product.
  • Price Erosion: Generic entry can lead to a price reduction of 70-90% for the active ingredient.
  • Market Share Loss: The originator product can lose a substantial portion of its market share within months of generic launch.
• Shifting Treatment Paradigms: As noted, newer drug classes offer broader benefits beyond glycemic control, leading to their preferential inclusion in treatment guidelines and physician preference.
• Exclusivity Expirations on Related Patents: Beyond the core compound patent, patents covering specific manufacturing processes, polymorphs, or therapeutic uses also expire, further facilitating generic entry.
• Regulatory Hurdles for New Formulations: The development and approval process for new drug formulations or combinations can be lengthy and costly, with no guarantee of success.

What is the Intellectual Property Strategy for NESINA?

The intellectual property strategy for NESINA likely involves a multi-faceted approach focused on extending exclusivity through formulation, combination, and process patents, alongside geographical considerations.

Key Patent Types and Their Role

• Compound Patents: These are the most fundamental patents, covering the chemical entity itself (alogliptin). Their expiration is the primary driver of generic entry. U.S. Patent No. 6,436,957 is an example.
• Formulation Patents: These protect specific ways the drug is delivered (e.g., tablets, extended-release capsules, injectables). If a novel and inventive formulation is developed, it can be patented independently of the compound.
• Combination Patents: Patents can cover the co-administration or co-formulation of alogliptin with other active pharmaceutical ingredients. For NESINA, patents covering alogliptin combined with metformin are crucial. For example, U.S. Patent No. 9,453,001 covers a specific alogliptin-metformin tablet formulation. However, the term for such patents is also finite.
• Process Patents: These protect specific methods of manufacturing the drug substance or drug product. While a new process patent might offer some protection, it is often possible for generic manufacturers to find alternative synthesis routes.
• Polymorph Patents: If different crystalline forms (polymorphs) of alogliptin are discovered and shown to have advantageous properties, they may be patentable.

Patent Expiry Timeline Summary

Patent Type	Example Patent No.	Expiry Date (Approximate)	Market
Compound (Alogliptin)	US 6,436,957	October 2022	United States
Compound (Alogliptin)	EP1067142	September 2023	Europe
Compound (Alogliptin)	JP3771233	July 2023	Japan
Combination (Alogliptin/Metformin)	US 9,453,001	September 2030	United States

(Note: Expiry dates are subject to patent term adjustments, extensions, and ongoing litigation. This table provides a general overview.)

The patent for the alogliptin-metformin combination provides a longer period of exclusivity for this specific product. However, alogliptin itself is now exposed to generic competition.

What are the Key Investment Considerations?

The investment thesis for NESINA hinges on the strategic response to patent expiries and the potential for continued revenue generation through lifecycle management.

Investment Factors

• Genericization Risk: The primary driver of investment risk is the imminent and ongoing impact of generic alogliptin. Investors must model the projected decline in NESINA sales due to price erosion and market share loss.
• Lifecycle Management Efficacy: The success of any strategy to extend NESINA's commercial life (e.g., new formulations, combinations) is critical. The market exclusivity afforded by patents on these new entities will determine their revenue-generating potential.
• Pipeline Strength: For the originating company (Takeda Pharmaceutical Co. Ltd.), the overall pipeline of new drug candidates is paramount. Diversification into therapeutic areas beyond diabetes can mitigate risks associated with individual product patent expiries.
• Market Share Resilience: The ability of NESINA (and its branded combinations) to retain some market share, particularly in specific patient segments or geographies, will influence its terminal value. Factors such as physician loyalty, patient convenience, and cost-effectiveness relative to generics can play a role.
• Competitive Dynamics: The ongoing innovation and market entry of new diabetes therapies (GLP-1 RAs, SGLT2 inhibitors) continue to shift the competitive landscape, potentially pressuring the market position of older drug classes.
• Patent Litigation: While primary patents have expired, ongoing or potential litigation related to secondary patents or generic challenges can create uncertainty and impact market dynamics.

Key Takeaways

NESINA's market exclusivity, driven by its compound patents, has expired in major territories, exposing it to significant generic competition. While alogliptin-metformin combination patents offer a reprieve until later dates, the originator product faces a substantial revenue decline. Investment considerations must prioritize the efficacy of lifecycle management strategies and the broader portfolio strength of the originating company.

Frequently Asked Questions

What is the projected impact of generic alogliptin entry on NESINA sales?

Generic entry is projected to cause a rapid and substantial decline in NESINA sales, potentially exceeding 70% within the first year of generic availability due to significant price reductions and market share shift.

Are there any remaining patents that could extend NESINA's exclusivity?

Yes, patents covering specific fixed-dose combinations, such as alogliptin with metformin (e.g., U.S. Patent No. 9,453,001), are still in effect and provide exclusivity for those specific formulations until their respective expiry dates, projected around September 2030 in the U.S.

What is Takeda's strategy to mitigate NESINA patent expiry?

Takeda's strategy typically involves maximizing the value of existing assets through lifecycle management, including developing and promoting combination products and exploring potential new indications or formulations, while also focusing on pipeline development for future revenue streams.

How do newer diabetes drug classes affect NESINA's market position post-patent expiry?

Newer classes like GLP-1 receptor agonists and SGLT2 inhibitors offer benefits beyond glycemic control, such as cardiovascular and renal protection, which are increasingly prioritized in treatment guidelines. This trend will continue to challenge the market position of DPP-4 inhibitors like NESINA, even in the generic market.

What is the typical market share erosion for a drug like NESINA after patent expiry?

For a widely prescribed drug like NESINA, a significant portion of market share, often ranging from 70% to over 90%, can be lost to generic competitors within 12-24 months of generic launch, depending on market dynamics, physician adoption, and payer policies.

Citations

[1] Takeda Pharmaceutical Co., Ltd. (2021). Takeda Reports Full-Year Fiscal Year 2020 Results. [Press release]. [2] Takeda Pharmaceutical Co., Ltd. (2023). Takeda Reports Full-Year Fiscal Year 2022 Results. [Press release].