Sitagliptin - Generic Drug Details

What are the generic drug sources for sitagliptin and what is the scope of patent protection?

Sitagliptin is the generic ingredient in three branded drugs marketed by Zydus Lifesciences, Azurity, and Merck Sharp Dohme, and is included in three NDAs. There are four patents protecting this compound. Additional information is available in the individual branded drug profile pages.

Sitagliptin has four patent family members in four countries.

There are thirty-five drug master file entries for sitagliptin. Two suppliers are listed for this compound. There are twenty-four tentative approvals for this compound.

Summary for sitagliptin

International Patents:	4
US Patents:	4
Tradenames:	3
Applicants:	3
NDAs:	3
Drug Master File Entries:	35
Finished Product Suppliers / Packagers:	2
Raw Ingredient (Bulk) Api Vendors:	103
Clinical Trials:	466
Patent Applications:	6,759
Drug Prices:	Drug price trends for sitagliptin
What excipients (inactive ingredients) are in sitagliptin?	sitagliptin excipients list
DailyMed Link:	sitagliptin at DailyMed

See drug prices for sitagliptin

DrugPatentWatch^® Estimated Loss of Exclusivity (LOE) Date for sitagliptin

Dosage:

TABLET;ORAL

^*The generic entry opportunity date is the latter of the last compound-claiming patent and the last regulatory exclusivity protection. Many factors can influence early or later generic entry. This date is provided as a rough estimate of generic entry potential and should not be used as an independent source.

Recent Clinical Trials for sitagliptin

Identify potential brand extensions & 505(b)(2) entrants

Sponsor	Phase
Case Comprehensive Cancer Center	PHASE2
Khyber Medical College, Peshawar	PHASE3
Fundacin para la Investigacin del Hospital Clnico de Valencia	PHASE4

See all sitagliptin clinical trials

Generic filers with tentative approvals for SITAGLIPTIN

Applicant	Application No.	Strength	Dosage Form
		100MG	TABLET;ORAL
		50MG	TABLET;ORAL
		25MG	TABLET;ORAL

The 'tentative' approval signifies that the product meets all FDA standards for marketing, and, but for the patents / regulatory protections, it would approved.

Pharmacology for sitagliptin

Drug Class	Dipeptidyl Peptidase 4 Inhibitor
Mechanism of Action	Dipeptidyl Peptidase 4 Inhibitors

Anatomical Therapeutic Chemical (ATC) Classes for sitagliptin

A10BH	Dipeptidyl peptidase 4 (DPP-4) inhibitors
A10B	BLOOD GLUCOSE LOWERING DRUGS, EXCL. INSULINS
A10	DRUGS USED IN DIABETES
A	Alimentary tract and metabolism

US Patents and Regulatory Information for sitagliptin

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Exclusivity Expiration
Zydus Lifesciences	ZITUVIO	sitagliptin	TABLET;ORAL	211566-003	Oct 18, 2023		RX	Yes	Yes			Y
Azurity	BRYNOVIN	sitagliptin hydrochloride	SOLUTION;ORAL	219122-001	Jan 16, 2025		RX	Yes	Yes			Y
Merck Sharp Dohme	JANUVIA	sitagliptin phosphate	TABLET;ORAL	021995-001	Oct 16, 2006		RX	Yes	No					Y
Zydus Lifesciences	ZITUVIO	sitagliptin	TABLET;ORAL	211566-002	Oct 18, 2023		RX	Yes	No			Y

EU/EMA Drug Approvals for sitagliptin

Company	Drugname	Inn	Product Number / Indication	Status	Generic	Biosimilar	Orphan	Marketing Authorisation	Marketing Refusal
Merck Sharp & Dohme B.V.	Xelevia	sitagliptin	EMEA/H/C/000762For adult patients with type-2 diabetes mellitus, Xelevia is indicated to improve glycaemic control:as monotherapy:in patients inadequately controlled by diet and exercise alone and for whom metformin is inappropriate due to contraindications or intolerance;as dual oral therapy in combination with:metformin when diet and exercise plus metformin alone do not provide adequate glycaemic control;a sulphonylurea when diet and exercise plus maximal tolerated dose of a sulphonylurea alone do not provide adequate glycaemic control and when metformin is inappropriate due to contraindications or intolerance;a peroxisome proliferator-activated receptor gamma (PPARγ) agonist (i.e. a thiazolidinedione) when use of a PPARγ agonist is appropriate and when diet and exercise plus the PPARγ agonist alone do not provide adequate glycaemic control;as triple oral therapy in combination with:a sulphonylurea and metformin when diet and exercise plus dual therapy with these medicinal products do not provide adequate glycaemic control;a PPARγ agonist and metformin when use of a PPARγ agonist is appropriate and when diet and exercise plus dual therapy with these medicinal products do not provide adequate glycaemic control.Xelevia is also indicated as add-on to insulin (with or without metformin) when diet and exercise plus stable dose of insulin do not provide adequate glycaemic control.	Authorised	no	no	no	2007-03-21
Merck Sharp & Dohme B.V.	Tesavel	sitagliptin	EMEA/H/C/000910For patients with type-2 diabetes mellitus, Tesavel is indicated to improve glycaemic control:as monotherapy:in patients inadequately controlled by diet and exercise alone and for whom metformin is inappropriate due to contraindications or intolerance;as dual oral therapy in combination with:metformin when diet and exercise plus metformin alone do not provide adequate glycaemic control;a sulphonylurea when diet and exercise plus maximal tolerated dose of a sulphonylurea alone do not provide adequate glycaemic control and when metformin is inappropriate due to contraindications or intolerance;a PPARγ agonist (i.e. a thiazolidinedione) when use of a PPARγ agonist is appropriate and when diet and exercise plus the PPARγ agonist alone do not provide adequate glycaemic control;as triple oral therapy in combination witha sulphonylurea and metformin when diet and exercise plus dual therapy with these agents do not provide adequate glycaemic control;a peroxisome-proliferator-activated-receptor-gamma (PPARγ) agonist and metformin when use of a PPARγ agonist is appropriate and when diet and exercise plus dual therapy with these agents do not provide adequate glycaemic control.Tesavel is also indicated as add on to insulin (with or without metformin) when diet and exercise plus stable dosage of insulin do not provide adequate glycaemic control.	Authorised	no	no	no	2008-01-10
Merck Sharp and Dohme B.V	Januvia	sitagliptin	EMEA/H/C/000722For adult patients with type-2 diabetes mellitus, Januvia is indicated to improve glycaemic control:as monotherapy:in patients inadequately controlled by diet and exercise alone and for whom metformin is inappropriate due to contraindications or intolerance;as dual oral therapy in combination with:metformin when diet and exercise plus metformin alone do not provide adequate glycaemic control;a sulphonylurea when diet and exercise plus maximal tolerated dose of a sulphonylurea alone do not provide adequate glycaemic control and when metformin is inappropriate due to contraindications or intolerance;a peroxisome-proliferator-activated-receptor-gamma (PPARγ) agonist (i.e. a thiazolidinedione) when use of a PPARγ agonist is appropriate and when diet and exercise plus the PPARγ agonist alone do not provide adequate glycaemic control;a PPARγ agonist (i.e. a thiazolidinedione) when use of a PPARγ agonist is appropriate and when diet and exercise plus the PPARγ agonist alone do not provide adequate glycaemic control;as triple oral therapy in combination with:a sulphonylurea and metformin when diet and exercise plus dual therapy with these medicinal products do not provide adequate glycaemic control;a PPARγ agonist and metformin when use of a PPARγ agonist is appropriate and when diet and exercise plus dual therapy with these medicinal products do not provide adequate glycaemic control.Januvia is also indicated as add-on to insulin (with or without metformin) when diet and exercise plus stable dose of insulin do not provide adequate glycaemic control.	Authorised	no	no	no	2007-03-20
Merck Sharp & Dohme B.V.	Ristaben	sitagliptin	EMEA/H/C/001234For adult patients with type-2 diabetes mellitus, Ristaben is indicated to improve glycaemic control:as monotherapy:in patients inadequately controlled by diet and exercise alone and for whom metformin is inappropriate due to contraindications or intolerance;as dual oral therapy in combination with:metformin when diet and exercise plus metformin alone do not provide adequate glycaemic control;a sulphonylurea when diet and exercise plus maximal tolerated dose of a sulphonylurea alone do not provide adequate glycaemic control and when metformin is inappropriate due to contraindications or intolerance;a peroxisome proliferator-activated-receptor-gamma (PPARγ) agonist (i.e. a thiazolidinedione) when use of a PPARγ agonist is appropriate and when diet and exercise plus the PPARγ agonist alone do not provide adequate glycaemic control;as triple oral therapy in combination with:a sulphonylurea and metformin when diet and exercise plus dual therapy with these medicinal products do not provide adequate glycaemic control;a PPARγ agonist and metformin when use of a PPARγ agonist is appropriate and when diet and exercise plus dual therapy with these medicinal products do not provide adequate glycaemic control.Ristaben is also indicated as add-on to insulin (with or without metformin) when diet and exercise plus stable dose of insulin do not provide adequate glycaemic control.	Authorised	no	no	no	2010-03-15

International Patents for sitagliptin

Country	Patent Number	Title	Estimated Expiration
World Intellectual Property Organization (WIPO)	2015128877
South Africa	201606075	PHARMACEUTICAL COMPOSITIONS OF SITAGLIPTIN
Philippines	12016501686	PHARMACEUTICAL COMPOSITIONS OF SITAGLIPTIN
India	651MU2014

Supplementary Protection Certificates for sitagliptin

Patent Number	Supplementary Protection Certificate	SPC Country	SPC Expiration	SPC Description
0896538	07C0035	France		PRODUCT NAME: SITAGLIPTIN; REGISTRATION NO/DATE IN FRANCE: EU/1/07/383/001 DU 20070321; REGISTRATION NO/DATE AT EEC: EU/1/07/383/001-018 DU 20070321
1084705	CA 2014 00063	Denmark		PRODUCT NAME: SITAGLIPTIN OG FARMACEUTISK SALTE DERAF, HERUNDER SITAGLIPTIN PHOSPHAT MONOHYDRAT; REG. NO/DATE: EU/1/07/383/001-024 AND EU/1/07/382/001-024 20070321
1412357	C 2007 091	Romania		PRODUCT NAME: (3R)-3-AMINO-1-[9-(TRIFLUOROMETIL)-1,4,7,8-TETRAZABICICLO[4.3.0]NONA-6,8-DIEN-4-IL]-4-(2,4,5-TRIFLUOROFENIL)BUTAN-1-ONA - SITAGLIPTIN; NATIONAL AUTHORISATION NUMBER: RO EU/1/07/383/001 - RO EU/1/07/383/018; DATE OF NATIONAL AUTHORISATION: 20070321; NUMBER OF FIRST AUTHORISATION IN EUROPEAN ECONOMIC AREA (EEA): EU/1/07/383/001 - EU/1/07/383/018; DATE OF FIRST AUTHORISATION IN EEA: 20070321
1412357	0790041-8	Sweden		PRODUCT NAME: SITAGLIPTINFOSFATMONOHYDRAT

Market Dynamics and Financial Trajectory for SITAGLIPTIN

Last updated: October 23, 2025

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Introduction

Sitagliptin, marketed primarily under the brand name Januvia, is a dipeptidyl peptidase-4 (DPP-4) inhibitor used in managing type 2 diabetes mellitus (T2DM). Approved by the FDA in 2006, sitagliptin has established itself as a key player in the oral antidiabetic market. The drug's unique pharmacological profile, early market entry, and ongoing pipeline developments have significantly influenced its market dynamics and financial trajectory. This report delineates the current landscape, key drivers, challenges, and future outlook for sitagliptin within the global pharmaceutical sector.

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Market Overview and Key Drivers

Global Diabetes Epidemic and Market Expansion

The rising prevalence of T2DM remains the central driver for sitagliptin's sustained market demand. The International Diabetes Federation estimates that approximately 537 million adults worldwide live with diabetes, projected to reach 643 million by 2030 [1]. This escalation fuels the need for oral hypoglycemics like sitagliptin, contributing to a robust compound annual growth rate (CAGR) for the broader anti-diabetic drug segment.

Positioning of Sitagliptin in the Therapeutic Arsenal

Sitagliptin's mechanism of action—enhancing incretin hormones to increase insulin secretion and decrease glucagon levels—offers a targeted approach with a favorable safety profile. Its once-daily oral administration provides convenience, encouraging adherence. It is often prescribed alongside other antidiabetic agents, especially metformin, amplifying its therapeutic footprint.

Competitive Landscape and Market Share

Sitagliptin faces competition from other DPP-4 inhibitors like saxagliptin (Onglyza), linagliptin (Tradjenta), and alogliptin (Nesina). Although initially the market leader, its share has been challenged by newer agents and combination therapies offering superior efficacy or convenience. Nonetheless, it remains a commercially significant drug, with its patent expiry approaching in key markets, prompting players to alter their strategies.

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Patent Expiry and Generic Competition

Patent Timeline and Patent Cliff

Sitagliptin’s original composition patent expired or is set to expire in various jurisdictions around 2022-2023 [2]. This expiration opens the door for generic manufacturers to enter the market, fostering price competition, eroding branded sales, and pressuring profit margins.

Impact on Revenue Streams

Prior to patent expiry, sitagliptin generated annual revenues exceeding $4 billion globally (2017 figures), reflecting its dominant market position. Post-expiry, revenue decline is anticipated, contingent on generic uptake, pricing strategies, and market penetration. This mirrors patterns observed with similar drugs upon patent expiration and necessitates strategic pivots for the original developer.

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Regulatory and Clinical Developments

Pipeline Enhancements and Combination Therapies

Pharmaceutical companies have pursued reformulations to sustain competitiveness, including fixed-dose combinations (FDCs) with metformin (e.g., Janumet), which bolster patient adherence and preserve market share. Ongoing research into triple combination therapies and novel formulations aims to extend patent life and deliver added value.

Regulatory Challenges and Approvals

Regulatory agencies continuously evaluate sitagliptin’s safety profile. While generally well-tolerated, concerns regarding pancreatitis risk [3] and potential links to autoimmune conditions influence prescribing patterns and could impact future approvals or label modifications.

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Financial Trajectory and Strategic Considerations

Revenue Trends and Forecasts

Bringing together market growth, patent expiry, and competitive dynamics, financial projections indicate a declining revenue trajectory for sitagliptin by mid-2020s. Analysts forecast a compound annual decline rate (CADR) of approximately 8-10% post-patent expiry, driven by generic erosion and market saturation. However, revenue from combination therapies and repurposing efforts could mitigate some losses.

Mergers, Acquisitions, and Portfolio Diversification

Major pharmaceutical players, including Merck (original developer), have diversified portfolios into newer incretin-based therapies, sodium-glucose co-transporter 2 (SGLT2) inhibitors, and glucagon-like peptide-1 (GLP-1) receptor agonists. These diversifications aim to offset declining sitagliptin revenue and position for long-term growth.

Market Expansion Opportunities

Emerging markets, with expanding healthcare infrastructure and rising T2DM prevalence, offer growth opportunities for generic formulations and biosimilars. Strategic collaborations and licensing arrangements may facilitate market penetration in regions like Asia and Africa, bolstering financial performance amid patent challenges.

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Challenges and Future Outlook

Evolving Therapeutic Landscape

The future trajectory of sitagliptin hinges on its positioning relative to newer agents offering improved efficacy, weight loss benefits, or reduced cardiovascular risks—attributes demonstrated by some GLP-1 receptor agonists and SGLT2 inhibitors [4]. The paradigm shift toward personalized medicine and combination regimens necessitates continuous innovation.

Regulatory and Safety Concerns

Ongoing safety assessments could influence regulatory status or market acceptance. Any adverse event signals might restrict usage, impacting revenues. Conversely, real-world evidence supporting safety can extend market viability.

Research and Development Strategies

For sustained relevance, developers may leverage drug repositioning, explore novel indications, or develop next-generation DPP-4 inhibitors with improved profiles. Investing in biosimilars and tools that enhance patient compliance constitute critical strategic pathways.

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Key Takeaways

• The global diabetes epidemic presents persistent demand drivers for sitagliptin, despite increasing competition.
• Patent expiration around 2022-2023 is set to significantly impact revenue, emphasizing the importance of lifecycle management.
• The rise of combination therapies, biosimilars, and novel agents reshapes the competitive landscape.
• Market expansion in emerging economies offers growth avenues, even as Western markets soften post-patent expiry.
• Strategic diversification into new drug classes and collaboration will be pivotal for sustained profitability and market relevance.

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FAQs

1. How does sitagliptin compare to other DPP-4 inhibitors in terms of efficacy and safety?
Sitagliptin exhibits comparable efficacy and safety profiles to other DPP-4 inhibitors. It effectively lowers HbA1c with minimal risk of hypoglycemia and weight gain, positioning it as a preferred option within this class, although individual patient factors may influence choice.

2. What is the impact of patent expiry on sitagliptin’s market value?
Patent expiry typically leads to generic entry, resulting in significant revenue decline due to price competition. For sitagliptin, post-2022, analysts expect a 70-80% reduction in sales in mature markets, unless offset by new formulations or indications.

3. Are there ongoing efforts to develop next-generation sitagliptin formulations?
Yes. Strategies include fixed-dose combinations with other antidiabetics, extended-release formulations, and investigating additional indications such as obesity or cardiovascular conditions to extend patent life and market relevance.

4. How does the safety profile affect sitagliptin’s market outlook?
While generally safe, concerns regarding pancreatitis and autoimmune events have surfaced, prompting cautious prescribing and regulatory scrutiny. Positive long-term safety data could sustain its use, whereas safety issues may restrict or diminish its market.

5. What strategic moves should pharmaceutical companies consider post-patent expiry?
Companies should invest in biosimilars or generics, expand into emerging markets, develop combination therapies, and innovate within related drug classes to maintain revenue streams and market relevance.

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References

[1] International Diabetes Federation. IDF Diabetes Atlas, 9th Edition, 2019.
[2] U.S. Food & Drug Administration. Patent timelines for sitagliptin.
[3] Villanueva, et al. “Safety of DPP-4 inhibitors in type 2 diabetes: a systematic review and meta-analysis.” BMJ, 2019.
[4] Garvey, et al. “Comparative efficacy and safety of incretin-based therapies in type 2 diabetes.” Diabetes Care, 2021.