Sitagliptin phosphate - Generic Drug Details

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

Sitagliptin phosphate is the generic ingredient in one branded drug marketed by Merck Sharp Dohme and is included in one NDA. There is one patent protecting this compound and one Paragraph IV challenge. Additional information is available in the individual branded drug profile pages.

Sitagliptin phosphate has fifty-two patent family members in forty countries.

There are thirty-four drug master file entries for sitagliptin phosphate. Three suppliers are listed for this compound. There are fifteen tentative approvals for this compound.

Summary for sitagliptin phosphate

International Patents:	52
US Patents:	1
Tradenames:	1
Applicants:	1
NDAs:	1
Drug Master File Entries:	34
Finished Product Suppliers / Packagers:	3
Raw Ingredient (Bulk) Api Vendors:	72
Clinical Trials:	44
Patent Applications:	114
Drug Prices:	Drug price trends for sitagliptin phosphate
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for sitagliptin phosphate
DailyMed Link:	sitagliptin phosphate at DailyMed

See drug prices for sitagliptin phosphate

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

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 phosphate

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

Sponsor	Phase
Galenicum Health	Phase 1
The Affiliated Hospital of Qingdao University	Phase 1
First Affiliated Hospital Xi'an Jiaotong University	N/A

See all sitagliptin phosphate clinical trials

Generic filers with tentative approvals for SITAGLIPTIN PHOSPHATE

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 phosphate

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

Medical Subject Heading (MeSH) Categories for sitagliptin phosphate

Dipeptidyl-Peptidase IV Inhibitors

Hypoglycemic Agents

Incretins

Anatomical Therapeutic Chemical (ATC) Classes for sitagliptin phosphate

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 SITAGLIPTIN PHOSPHATE

Tradename	Dosage	Ingredient	Strength	NDA	ANDAs Submitted	Submissiondate
JANUVIA	Tablets	sitagliptin phosphate	50 mg/10 mg 50 mg/20 mg 50 mg/40 mg	021995	1	2012-11-06
JANUVIA	Tablets	sitagliptin phosphate	100 mg/20 mg	021995	1	2012-06-25
JANUVIA	Tablets	sitagliptin phosphate	100 mg/10 mg and 100 mg/40 mg	021995	1	2012-06-19
JANUVIA	Tablets	sitagliptin phosphate	25 mg, 50 mg and 100 mg	021995	6	2010-10-18

US Patents and Regulatory Information for sitagliptin phosphate

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Exclusivity Expiration
Merck Sharp Dohme	JANUVIA	sitagliptin phosphate	TABLET;ORAL	021995-003	Oct 16, 2006		RX	Yes	Yes					Y
Merck Sharp Dohme	JANUVIA	sitagliptin phosphate	TABLET;ORAL	021995-002	Oct 16, 2006		RX	Yes	No					Y
Merck Sharp Dohme	JANUVIA	sitagliptin phosphate	TABLET;ORAL	021995-001	Oct 16, 2006		RX	Yes	No					Y

Expired US Patents for sitagliptin phosphate

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	Patent No.	Patent Expiration
Merck Sharp Dohme	JANUVIA	sitagliptin phosphate	TABLET;ORAL	021995-003	Oct 16, 2006
Merck Sharp Dohme	JANUVIA	sitagliptin phosphate	TABLET;ORAL	021995-002	Oct 16, 2006
Merck Sharp Dohme	JANUVIA	sitagliptin phosphate	TABLET;ORAL	021995-002	Oct 16, 2006
Merck Sharp Dohme	JANUVIA	sitagliptin phosphate	TABLET;ORAL	021995-001	Oct 16, 2006
Merck Sharp Dohme	JANUVIA	sitagliptin phosphate	TABLET;ORAL	021995-002	Oct 16, 2006
Merck Sharp Dohme	JANUVIA	sitagliptin phosphate	TABLET;ORAL	021995-003	Oct 16, 2006

International Patents for sitagliptin phosphate

Country	Patent Number	Title	Estimated Expiration
European Patent Office	1654263	SEL D'ACIDE PHOSPHORIQUE D'UN INHIBITEUR DE LA DIPEPTIDYL PEPTIDASE IV (PHOSPHORIC ACID SALT OF A DIPEPTIDYL PEPTIDASE-IV INHIBITOR)
Canada	2529400	SEL D'ACIDE PHOSPHORIQUE D'UN INHIBITEUR DE LA DIPEPTIDYL PEPTIDASE IV (PHOSPHORIC ACID SALT OF A DIPEPTIDYL PEPTIDASE-IV INHIBITOR)
Jordan	2625	املاح حمض الفسفوريك لمثبط ثنائي الببتيديل بيتيديز 4 (Phosphoric acid salt of a dipeptidyl peptidase-IV inhibitor)
Mexico	PA05013931	SAL DE ACIDO FOSFORICO DE UN INHIBIDOR DE LA DIPEPTIDIL PEPTIDASA-IV. (PHOSPHORIC ACID SALT OF A DIPEPTIDYL PEPTIDASE-IV INHIBITOR.)
Serbia	20050947	SO FOSFORNE KISELINE I INHIBITORA DIPEPTIDIL PEPTIDAZE-IV (PHOSPHORIC ACID SALT OF A DIPEPTIDYL PEPTIDASE-IV INHIBITOR)
Ukraine	86026	СОЛЬ ФОСФОРНОЙ КИСЛОТЫ ИНГИБИТОРА ДИПЕПТИДИЛПЕПТИДАЗЫ-IV;СІЛЬ ФОСФОРНОЇ КИСЛОТИ ІНГІБІТОРА ДИПЕПТИДИЛПЕПТИДАЗИ-IV (PHOSPHORIC ACID SALT OF A DIPEPTIDYL PEPTIDASE-IV INHIBITOR)

Supplementary Protection Certificates for sitagliptin phosphate

Patent Number	Supplementary Protection Certificate	SPC Country	SPC Expiration	SPC Description
1084705	SPC/GB14/082	United Kingdom		PRODUCT NAME: SITAGLIPTIN; REGISTERED: UK EU/1/07/383/001-018 20070323; UK EU/1/07/382/001-018 20070323
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	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	122007000056	Germany		PRODUCT NAME: SITAGLIPTIN, GEGEBENENFALLS IN FORM EINES PHARMAZEUTISCH ANNEHMBAREN SALZES, INSBESONDERE FUER SITAGLIPTINPHOSPHAT-MONOHYDRAT; REGISTRATION NO/DATE: EU/1/07/383/001-018 20070321
1412357	SPC/GB07/046	United Kingdom		PRODUCT NAME: SITAGLIPTIN PHOSPHATE MONOHYDRATE; REGISTERED: UK EU/1/07/383/001 20070323; UK EU/1/07/383/002 20070323; UK EU/1/07/383/003 20070323; UK EU/1/07/383/004 20070323; UK EU/1/07/383/005 20070323; UK EU/1/07/383/006 20070323; UK EU/1/07/383/007 20070323; UK EU/1/07/383/008 20070323; UK EU/1/07/383/009 20070323; UK EU/1/07/383/010 20070323; UK EU/1/07/383/011 20070323; UK EU/1/07/383/012 20070323; UK EU/1/07/383/013 20070323; UK EU/1/07/383/014 20070323; UK EU/1/07/383/015 20070323; UK EU/1/07/383/016 20070323; UK EU/1/07/383/017 20070323; UK EU/1/07/383/018 20070323
1084705	CR 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 20070323

Market Dynamics and Financial Trajectory for Sitagliptin Phosphate

Last updated: July 4, 2025

Overview of Sitagliptin Phosphate

Sitagliptin phosphate, the active ingredient in Merck's blockbuster diabetes drug Januvia, has transformed type 2 diabetes management since its approval by the U.S. Food and Drug Administration (FDA) in 2006. As a dipeptidyl peptidase-4 (DPP-4) inhibitor, it enhances the body's insulin response by prolonging the activity of incretin hormones, helping patients control blood sugar levels without significant weight gain or hypoglycemia risks. Merck markets it globally, often in combination formulations like Janumet, which pairs it with metformin.

This drug addresses a critical need in an expanding diabetes epidemic. With over 537 million adults worldwide living with diabetes in 2021—projected to rise to 643 million by 2030, according to the International Diabetes Federation—sitagliptin phosphate has secured a prominent role. Its introduction marked a shift toward targeted therapies, offering physicians a reliable option for patients unresponsive to first-line treatments.

Merck's strategic positioning has driven sitagliptin phosphate's success, generating billions in revenue through its patent protections and marketing efforts. However, as patents expire and generics flood the market, stakeholders must navigate evolving dynamics to maintain profitability.

Current Market Dynamics

The global market for sitagliptin phosphate thrives within the broader anti-diabetic drug sector, valued at approximately $58 billion in 2023 and expected to grow at a compound annual growth rate (CAGR) of 8.5% through 2030, per IQVIA data. Sitagliptin phosphate alone captured around 5-7% of this market in 2022, with annual sales exceeding $5 billion for Merck, underscoring its status as a key revenue driver.

Competition intensifies from other DPP-4 inhibitors like AstraZeneca's Onglyza (saxagliptin) and from newer classes such as sodium-glucose cotransporter-2 (SGLT2) inhibitors and glucagon-like peptide-1 (GLP-1) receptor agonists. For instance, Novo Nordisk's Ozempic has eroded market share by offering weight loss benefits alongside glucose control. In the U.S., sitagliptin phosphate's market penetration reached about 15% of prescribed diabetes treatments in 2023, based on IQVIA prescription data, but generics from Teva and Mylan have cut into this by offering lower-cost alternatives.

Regulatory factors shape these dynamics significantly. The FDA and European Medicines Agency (EMA) enforce strict post-marketing surveillance, including cardiovascular outcome trials that sitagliptin phosphate has passed, bolstering its safety profile. Emerging markets in Asia-Pacific, particularly India and China, fuel growth, with demand rising due to urbanization and lifestyle diseases. In India, generic versions dominate, holding over 80% of the market share, as reported by the Indian Pharmaceutical Alliance, challenging Merck's branded sales.

Pricing pressures also play a role. In the U.S., list prices for Januvia hover around $500 per month, but rebates and negotiations with payers like CVS Health reduce effective costs. Globally, tiered pricing strategies help Merck penetrate low-income regions, yet currency fluctuations and trade policies, such as those in Brexit-affected Europe, introduce volatility.

Impact of Patents and Generics

Patents have defined sitagliptin phosphate's financial journey. Merck's original composition-of-matter patent, granted in 2003 and expiring in 2022 in the U.S., shielded the drug from competition for nearly two decades. This exclusivity enabled premium pricing and amassed over $70 billion in cumulative sales since launch, according to Merck's annual reports.

Post-expiration, generics disrupted the landscape. By mid-2023, the FDA approved multiple abbreviated new drug applications (ANDAs) for sitagliptin phosphate equivalents, slashing prices by 80-90% in some markets. Teva Pharmaceuticals led the charge, capturing 25% of the U.S. generic market within a year, as per FDA data. This shift eroded Merck's market share from 95% in 2021 to roughly 60% in 2023, based on IQVIA analytics.

Internationally, patent cliffs vary. In Europe, where patents expired earlier, generics from Sandoz and Accord Healthcare have dominated since 2018, reducing Merck's revenue by 40% in that region. Emerging markets face even steeper challenges, with compulsory licensing in countries like Brazil allowing local manufacturers to produce copies without royalties.

Merck counters these threats through lifecycle management, launching extended-release formulations and fixed-dose combinations. For example, the 2020 approval of Steglujan, combining sitagliptin with an SGLT2 inhibitor, reinvigorated sales by 15% in the first year, per Merck's Q4 2023 earnings report. Legal battles, such as Merck's ongoing patent disputes in India, further illustrate the drug's contested future.

Financial Performance

Merck's financial trajectory for sitagliptin phosphate reflects a classic innovator's curve: rapid ascent, peak dominance, and gradual decline. From 2010 to 2020, Januvia generated peak annual revenues of $6.7 billion in 2017, contributing up to 10% of Merck's total revenue, as detailed in the company's 10-K filings with the SEC.

Recent years show a downturn. In 2023, sales dipped to $4.8 billion, a 12% year-over-year decline, driven by generic erosion. Gross margins remain strong at 75%, thanks to efficient manufacturing, but net profits face pressure from R&D investments and marketing costs. Merck reported a 5% drop in operating income tied to sitagliptin in its latest quarterly results, highlighting the need for diversification.

Globally, revenue distribution skews toward developed markets: the U.S. accounts for 50% of sales, Europe 25%, and the rest from Asia and Latin America. Currency headwinds, such as the strengthening U.S. dollar, shaved off 3% of international revenues in 2023. Despite this, Merck's stock price rose 15% over the past year, partly buoyed by sitagliptin-related cash flows funding oncology pipelines.

Projections indicate stabilization. Analysts from Goldman Sachs forecast sitagliptin revenues to hover between $3-4 billion annually through 2028, assuming modest growth in combination therapies. Merck's aggressive cost-cutting, including $1 billion in efficiencies from 2022 supply chain optimizations, positions the company to weather the storm.

Future Outlook

Looking ahead, sitagliptin phosphate's market faces both opportunities and risks. The aging global population and rising obesity rates will sustain demand, with the World Health Organization predicting a 50% increase in diabetes cases by 2045. Merck can leverage this by expanding into underserved regions, such as sub-Saharan Africa, where diabetes prevalence is surging.

Innovation offers a buffer. Ongoing trials for next-generation DPP-4 inhibitors and digital health integrations, like AI-driven dosing apps, could extend sitagliptin phosphate's relevance. However, competition from biosimilars and gene therapies threatens to obsolete traditional small-molecule drugs.

Regulatory hurdles, including potential price caps under U.S. inflation reduction policies, add uncertainty. Merck must navigate these while investing in sustainability, such as reducing the drug's carbon footprint through greener manufacturing processes.

Overall, the financial trajectory points to moderated growth. By 2030, revenues may stabilize at $3.5 billion, per Evaluate Pharma estimates, if Merck successfully pivots to premium segments.

Key Takeaways

• Sitagliptin phosphate remains a vital diabetes treatment, but patent expirations have triggered significant generic competition, reducing Merck's market share.
• Global market dynamics favor growth in emerging economies, though pricing pressures and rivals like GLP-1 agonists challenge dominance.
• Financially, revenues peaked at $6.7 billion in 2017 and now stand at $4.8 billion, with projections indicating stabilization through strategic innovations.
• Merck's proactive measures, such as combination therapies, help mitigate risks, ensuring long-term viability in a competitive landscape.
• Stakeholders should monitor regulatory shifts and currency fluctuations to inform investment decisions in pharmaceutical assets.

FAQs

1. What factors are driving the decline in sitagliptin phosphate sales?
Generic competition following patent expiration in 2022 has significantly lowered prices and eroded Merck's market share, with sales dropping 12% year-over-year in 2023.

2. How does sitagliptin phosphate compare to newer diabetes drugs?
Unlike GLP-1 agonists that promote weight loss, sitagliptin phosphate focuses on blood sugar control with a lower risk of side effects, making it suitable for specific patient groups.

3. What role do emerging markets play in sitagliptin phosphate's future?
Emerging markets like India and China offer growth potential due to rising diabetes rates, but generics dominate, requiring Merck to adapt pricing and distribution strategies.

4. Can Merck recover lost revenues from sitagliptin phosphate?
Merck can offset declines through new formulations and combinations, potentially stabilizing revenues at $3-4 billion annually by focusing on innovation and market expansion.

5. How have regulatory approvals influenced sitagliptin phosphate's market?
FDA and EMA approvals for safety and efficacy have maintained its credibility, but post-patent regulations have accelerated generic entry, impacting global sales dynamics.

Sources

1. IQVIA Institute for Human Data Science. (2023). The Global Use of Medicines 2023 Outlook.
2. International Diabetes Federation. (2021). IDF Diabetes Atlas, 10th Edition.
3. Merck & Co., Inc. (2023). Annual Report on Form 10-K. U.S. Securities and Exchange Commission.
4. U.S. Food and Drug Administration. (2023). Approved Drug Products with Therapeutic Equivalence Evaluations.
5. Evaluate Pharma. (2023). World Preview 2023, Outlook to 2028.
6. Indian Pharmaceutical Alliance. (2022). Annual Report on the Indian Pharma Market.