METFORMIN HYDROCHLORIDE; SITAGLIPTIN PHOSPHATE - Generic Drug Details

What are the generic sources for metformin hydrochloride; sitagliptin phosphate and what is the scope of freedom to operate?

Metformin hydrochloride; sitagliptin phosphate is the generic ingredient in three branded drugs marketed by Msd Sub Merck and Ph Health, and is included in three NDAs. There are two patents protecting this compound and three Paragraph IV challenges. Additional information is available in the individual branded drug profile pages.

Metformin hydrochloride; sitagliptin phosphate has sixty-one patent family members in forty countries.

Two suppliers are listed for this compound.

Summary for METFORMIN HYDROCHLORIDE; SITAGLIPTIN PHOSPHATE

International Patents:	61
US Patents:	2
Tradenames:	3
Applicants:	2
NDAs:	3
Finished Product Suppliers / Packagers:	2
Clinical Trials:	10
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for METFORMIN HYDROCHLORIDE; SITAGLIPTIN PHOSPHATE
DailyMed Link:	METFORMIN HYDROCHLORIDE; SITAGLIPTIN PHOSPHATE at DailyMed

Recent Clinical Trials for METFORMIN HYDROCHLORIDE; SITAGLIPTIN PHOSPHATE

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

Sponsor	Phase
Zhibin Xu	PHASE4
Nanfang Hospital, Southern Medical University	PHASE4
University of Lahore Teaching Hospital	PHASE3

See all METFORMIN HYDROCHLORIDE; SITAGLIPTIN PHOSPHATE clinical trials

Pharmacology for METFORMIN HYDROCHLORIDE; SITAGLIPTIN PHOSPHATE

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

Anatomical Therapeutic Chemical (ATC) Classes for METFORMIN HYDROCHLORIDE; SITAGLIPTIN PHOSPHATE

A10BA	Biguanides
A10B	BLOOD GLUCOSE LOWERING DRUGS, EXCL. INSULINS
A10	DRUGS USED IN DIABETES
A	Alimentary tract and metabolism

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

Paragraph IV (Patent) Challenges for METFORMIN HYDROCHLORIDE; SITAGLIPTIN PHOSPHATE

Tradename	Dosage	Ingredient	Strength	NDA	ANDAs Submitted	Submissiondate
JANUMET XR	Extended-release Tablets	metformin hydrochloride; sitagliptin phosphate	100 mg/1000 mg	202270	1	2012-10-22
JANUMET XR	Extended-release Tablets	metformin hydrochloride; sitagliptin phosphate	50 mg/500 mg and 50 mg/1000 mg	202270	1	2012-03-16
JANUMET	Tablets	metformin hydrochloride; sitagliptin phosphate	50 mg/500 mg and 50 mg/1000 mg	022044	5	2010-10-18

US Patents and Regulatory Information for METFORMIN HYDROCHLORIDE; SITAGLIPTIN PHOSPHATE

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Exclusivity Expiration
Msd Sub Merck	JANUMET	metformin hydrochloride; sitagliptin phosphate	TABLET;ORAL	022044-002	Mar 30, 2007		RX	Yes	Yes	8,414,921*PED				Y
Msd Sub Merck	JANUMET	metformin hydrochloride; sitagliptin phosphate	TABLET;ORAL	022044-001	Mar 30, 2007		RX	Yes	No	7,326,708*PED				Y
Msd Sub Merck	JANUMET	metformin hydrochloride; sitagliptin phosphate	TABLET;ORAL	022044-002	Mar 30, 2007		RX	Yes	Yes	7,326,708*PED				Y
Ph Health	SITAGLIPTIN AND METFORMIN HYDROCHLORIDE	metformin hydrochloride; sitagliptin phosphate	TABLET, EXTENDED RELEASE;ORAL	204144-001	Jun 4, 2025		DISCN	No	No
Msd Sub Merck	JANUMET	metformin hydrochloride; sitagliptin phosphate	TABLET;ORAL	022044-001	Mar 30, 2007		RX	Yes	No	8,414,921*PED				Y

Expired US Patents for METFORMIN HYDROCHLORIDE; SITAGLIPTIN PHOSPHATE

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	Patent No.	Patent Expiration
Msd Sub Merck	JANUMET XR	metformin hydrochloride; sitagliptin phosphate	TABLET, EXTENDED RELEASE;ORAL	202270-003	Feb 2, 2012	6,890,898
Msd Sub Merck	JANUMET XR	metformin hydrochloride; sitagliptin phosphate	TABLET, EXTENDED RELEASE;ORAL	202270-001	Feb 2, 2012	7,078,381
Msd Sub Merck	JANUMET	metformin hydrochloride; sitagliptin phosphate	TABLET;ORAL	022044-002	Mar 30, 2007	7,459,428
Msd Sub Merck	JANUMET XR	metformin hydrochloride; sitagliptin phosphate	TABLET, EXTENDED RELEASE;ORAL	202270-001	Feb 2, 2012	6,340,475
Msd Sub Merck	JANUMET XR	metformin hydrochloride; sitagliptin phosphate	TABLET, EXTENDED RELEASE;ORAL	202270-002	Feb 2, 2012	7,078,381

International Patents for METFORMIN HYDROCHLORIDE; SITAGLIPTIN PHOSPHATE

Country	Patent Number	Title	Estimated Expiration
Canada	2529400	SEL D'ACIDE PHOSPHORIQUE D'UN INHIBITEUR DE LA DIPEPTIDYL PEPTIDASE IV (PHOSPHORIC ACID SALT OF A DIPEPTIDYL PEPTIDASE-IV INHIBITOR)
Poland	1654263
Brazil	PI0411726	composto, monoidrato, sal, composição farmacêutica, método para o tratamento de diabetes tipo 2, processo para preparar o composto, uso do composto, e, processo para a preparação do monoidrato cristalino
Japan	2006516268
World Intellectual Property Organization (WIPO)	2005003135

Supplementary Protection Certificates for METFORMIN HYDROCHLORIDE; SITAGLIPTIN PHOSPHATE

Patent Number	Supplementary Protection Certificate	SPC Country	SPC Expiration	SPC Description
1412357	DO 77; 5006-2008	Slovakia		PRODUCT NAME: SITAGLIPTIN A METFORMIN; REGISTRATION NO/DATE: EU/1/08/455/001-014 20080716
1532149	C300569	Netherlands		PRODUCT NAME: LINAGLIPTINE, DESGEWENST IN DE VORM VAN EEN ZOUT, IN COMBINATIE MET METFORMINEHYDROCHLORIDE; REGISTRATION NO/DATE: EU/1/12/780/001-028 20120720
1412357	C300357	Netherlands		PRODUCT NAME: SITAGLIPTINE, DESGEWENST IN DE VORM VAN EEN FARMACEUTISCH AANVA ARDBAAR ZOUT, IN HET BIJZONDER HET MONOFOSFAAT, EN METFORMINE DESGEWENST IN DE VORM VAN EEN FARMACEUTISCH AANVAARDBAAR ZOUT, IN HET BIJZONDER HET HYDROCHLORIDE; REGISTRATION NO/DATE: EU/1/08/455/001-014 20080716
1412357	SPC/GB08/040	United Kingdom		PRODUCT NAME: SITAGLIPTIN OPTIONALLY IN THE FORM OF A PHARMACEUTICALLY ACCEPTABLE SALT, IN PARTICULAR THE MONOPHOSPHATE, PLUS METFORMIN OPTIONALLY IN THE FORM OF A PHARMACEUTICALLY ACCEPTABLE SALT, IN PARTICULAR THE HYDROCHLORIDE.; REGISTERED: CH 58450 01-03 20080408; UK EU/1/08/455/001 20080716; UK EU/1/08/455/002 20080716; UK EU/1/08/455/003 20080716; UK EU/1/08/455/004 20080716; UK EU/1/08/455/005 20080716; UK EU/1/08/455/006 20080716; UK EU/1/08/455/007 20080716; UK EU/1/08/455/008 20080716; UK EU/1/08/455/009 20080716; UK EU/1/08/455/010 20080716; UK EU/1/08/455/011 20080716; UK EU/1/08/455/012 20080716; UK EU/1/08/455/013 20080716; UK EU/1/08/455/014 20080716
1412357	132008901682802	Italy		PRODUCT NAME: SITAGLIPTIN/METFORMINA CLORIDRATO(JANUMET, VELMETIA, EFFICIB); AUTHORISATION NUMBER(S) AND DATE(S): JANUMET:EU/1/08/455/001... 014; VELMETIA:EU/1/08/456/001...014;EFFICIB: EU/1/08/457/001....014, 20080716;58450-01;58450-02; 58450-03, 20080408

Market Dynamics and Financial Trajectory for Metformin Hydrochloride and Sitagliptin Phosphate

Last updated: July 28, 2025

Introduction

The global pharmaceutical landscape is experiencing rapid evolution, driven by increasing prevalence of type 2 diabetes mellitus (T2DM), advancing biomedical technologies, and regulatory shifts. Central to this sector are antidiabetic agents, notably Metformin Hydrochloride and Sitagliptin Phosphate, which have solidified their positions within treatment protocols. This analysis examines the current market dynamics, growth drivers, competitive landscape, and future financial trajectories of these pivotal drugs.

Market Overview of Metformin Hydrochloride and Sitagliptin Phosphate

Metformin Hydrochloride

Metformin, a biguanide, remains the first-line therapy for T2DM globally, owing to its efficacy, safety profile, and cost-effectiveness. According to the International Diabetes Federation (IDF), over 537 million adults suffered from diabetes in 2021, with projections reaching 643 million by 2030[^1]. This exponential rise substantially fuels the demand for metformin.

Sitagliptin Phosphate

Sitagliptin, a DPP-4 inhibitor, developed by Merck & Co., emerged as a key second-generation oral antidiabetic agent approved in 2006. Its mechanism involves enhancing endogenous incretin hormones, leading to improved glycemic control. The drug's adoption is driven by patient preferences for oral medications with low hypoglycemia risk.

Market Dynamics

Drivers of Growth

Rising Prevalence of Diabetes

The escalating incidence of T2DM remains the primary catalyst. Sedentary lifestyles, obesity, aging populations, and urbanization exacerbate disease burden worldwide[^2]. As a result, the demand for both metformin and sitagliptin escalates.

Cost-Effectiveness of Metformin

Metformin's affordability, especially in low- and middle-income countries, sustains its massive prescriptions. WHO classifies it as an essential medicine, further supporting its widespread use[^3].

Innovation and Combinational Therapies

The advent of fixed-dose combinations (FDCs) integrating metformin with newer agents like sitagliptin boosts patient compliance and market penetration. Regulatory approvals for such FDCs expand treatment options, stimulating revenue streams[^4].

Regulatory Environment and Patent Dynamics

While sitagliptin's patent expired in various jurisdictions from around 2021, leading to generic options, metformin's patent is long expired, fostering universal availability. Patent cliffs encourage generic proliferation, influencing pricing and market competition.

Digital and Personalized Medicine Integration

Emerging digital health implementations, adherence monitoring, and personalized medicine approaches influence treatment regimens, indirectly affecting drug demand patterns.

Constraints and Challenges

Market Saturation and Competitive Pressures

The mature status of metformin and generic sitagliptin markets impedes significant revenue growth in established regions. Competitors offering alternative DPP-4 inhibitors or novel drug classes limit market expansion.

Regulatory and Safety Concerns

Reports of lactic acidosis associated with metformin, primarily in renal impairment, mandate guidelines and dosing adjustments, potentially impacting sales. Similarly, rare side effects of sitagliptin, such as pancreatitis, influence prescribing norms[^5].

Pricing Pressures

Price erosion due to generic competition and healthcare reimbursement reforms challenge profit margins, especially in cost-sensitive markets.

Emerging Opportunities

Growing Markets in Asia and Africa

Expanding healthcare infrastructure and increasing disease awareness in emerging markets provide substantial opportunities for market expansion.

Innovative Formulations and Delivery

Development of extended-release formulations, combination pills, and injectable forms further diversify product portfolios.

Financial Trajectory Forecast

Historical Financial Insights

Revenue for global metformin market surpasses $1.3 billion annually, with Asia-Pacific constituting the largest segment[^6]. Sitagliptin's franchise revenue peaked at over $2.8 billion in 2016 before patent expiry-induced decline[^7].

Projected Market Growth

Analyst estimates project the combined antidiabetic drug market to grow at a CAGR of approximately 7-9% through 2028, driven predominantly by emerging markets and aging populations[^8].

• Metformin: Although mature, steady growth persists, primarily through generic proliferation and niche formulations. Focus on improving formulations for renal impairment patients maintains relevance.

• Sitagliptin and DPP-4 inhibitors: Anticipated Compound Annual Growth Rate (CAGR) reaches 6-8%, fueled by incremental adoption, combination therapies, and pipeline innovations.

Impact of Patent Expiries

Patent expirations facilitate generic entry, diminishing per-unit revenue but expanding overall volume. Companies adapt through brand differentiation, biosimilars, and expanding indications to sustain margins.

Pipeline and Future Developments

Emerging drugs, such as SGLT2 inhibitors and GLP-1 receptor agonists, pose competitive challenges but also open avenues for combination regimens involving established agents like metformin and sitagliptin.

Scenario Analysis:

• Optimistic: Continued innovation, robust market expansion in emerging economies, and successful pipeline products support a 10%+ CAGR over the next five years.

• Conservative: Market saturation, pricing pressures, and safety concerns limit growth to 3-5% CAGR.

Competitive Landscape

Leading generic manufacturers (e.g., Teva, Mylan), branded pharmaceutical companies (e.g., Merck, Novartis), and regional players dominate supply. Strategic alliances, licensing, and pipeline investments are pivotal to maintaining market share.

Regulatory and Policy Impact

Stringent regulatory standards, especially post-pandemic, influence drug approval timelines and market access strategies. Reimbursement policies vary, with a trend towards value-based models incentivizing cost-effective therapies like metformin.

Key Takeaways

• The rise in global T2DM prevalence underpins sustained demand for metformin and sitagliptin.
• Patent expirations catalyze generics, shrinking revenues but expanding overall market volume.
• Combination therapies and novel formulations present growth avenues amid mature markets.
• Emerging markets likely drive future expansion, offsetting stagnation in mature regions.
• Competitive pressures necessitate continuous innovation, pipeline diversification, and strategic collaborations.

FAQs

1. How will patent expiries affect the profitability of sitagliptin?
Patent expiries open avenues for generics, typically leading to significant price reductions and eroded profit margins; however, volume increases and portfolio diversification can mitigate adverse effects.

2. Are there upcoming innovations in metformin formulations?
Yes, extended-release formulations and combination products aim to improve tolerability and adherence, potentially revitalizing interest and expanding indications.

3. What role do biosimilars and generics play in this market?
They dominate supply, drastically lowering prices and expanding access, which pressures branded product revenues but sustains market growth through higher volumes.

4. How might emerging therapies influence the demand for metformin and sitagliptin?
New drug classes like SGLT2 inhibitors and GLP-1 receptor agonists may replace or supplement existing therapies, prompting shifts in prescribing trends but also opportunities for combination regimens.

5. What are key strategic considerations for pharmaceutical companies in this sector?
Innovation in formulations and combinations, expansion into emerging markets, navigating patent landscapes, and investing in pipeline developments are critical for maintaining competitive advantage.

References

[^1]: International Diabetes Federation. IDF Diabetes Atlas, 2021.
[^2]: World Health Organization. Obesity and overweight statistics, 2020.
[^3]: World Health Organization. Essential medicines.
[^4]: MarketLine. Global Patent and Innovation Trends in Antidiabetic Drugs, 2022.
[^5]: FDA Drug Safety Communications. Risks associated with DPP-4 inhibitors.
[^6]: Grand View Research. Global Metformin Market Analysis, 2022.
[^7]: EvaluatePharma. Sitagliptin franchise revenue data, 2016.
[^8]: Mordor Intelligence. Antidiabetic drugs market forecast, 2022–2028.