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 seventeen 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:	46
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
Nanfang Hospital, Southern Medical University	PHASE4
Zhibin Xu	PHASE4
University of Lahore	PHASE3

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	021995-001	Oct 16, 2006		RX	Yes	No					Y
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

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	021995-003	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
Iceland	2792
Australia	2004253889	Phosphoric acid salt of a dipeptidyl peptidase-IV inhibitor
Hong Kong	1095144	PHOSPHORIC ACID SALT OF A DIPEPTIDYL PEPTIDASE-IV INHIBITOR
Serbia	51873	SO FOSFORNE KISELINE I INHIBITORA DIPEPTIDIL PEPTIDAZE-IV (PHOSPHORIC ACID SALT OF A DIPEPTIDYL PEPTIDASE-IV INHIBITOR)
Taiwan	I347185
Montenegro	P60208	SO FOSFORNE KISJELINE I INHIBITORA DIPEPTIDIL PEPTIDAZE-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
1412357	CA 2008 00035	Denmark		PRODUCT NAME: SITAGLIPTIN VALGFRIT I FORM AF ET FARMACEUTISK ACCEPTABELT SALT, ISAER MONOPHOSPHAT, METFORMIN VALGFRIT I FORM AF ET FARMACEUTISK ACCEPTABELT SALT, ISAER HYDROCHLORID
1412357	C 2008 016	Romania		PRODUCT NAME: SITAGLIPTIN OPTIONAL SUB FORMA DE SARE ACCEPTABILAFARMACEUTIC IN SPECIAL MONOFOSFAT + METFORMIN OPTIONAL SUB FORMA DE SARE ACCEPTABILA FARMACEUTIC IN SPECIALCLORHIDRAT; NATIONAL AUTHORISATION NUMBER: RO EU/1/08/455/001 - RO EU/1/08/455/014; DATE OF NATIONAL AUTHORISATION: 20080716; NUMBER OF FIRST AUTHORISATION IN EUROPEAN ECONOMIC AREA (EEA): CH 58450 01, CH 58450 02, CH 58450 03; DATE OF FIRST AUTHORISATION IN EEA: 20080408
1412357	122008000046	Germany		PRODUCT NAME: SITAGLIPTIN, GEGEBENENFALLS IN FORM EINES PHARMAZEUTISCH ANNEHMBAREN SALZES, INSBESONDERE SITAGLIPTINPHOSPHAT- MONOHYDRAT, IN KOMBINATION MIT METFORMIN, GEGEBENENFALLS IN FORM EINES PHARMAZEUTISCH ANNEHMBAREN SALZES, INSBESONDERE DES HYDROCHLORIDS; NAT. REGISTRATION NO/DATE: EU/1/08/455/001-014 20080716 FIRST REGISTRATION: CH/LI 58450 01 58450 02 58450 03 20080408
1412357	2007/029	Ireland		PRODUCT NAME: SITAGLIPTIN, OPTIONALLY IN THE FORM OF A PHARMACEUTICALLY ACCEPTABLE SALT; REGISTRATION NO/DATE: EU/1/07/383/001-018 20070321
1084705	PA2014041	Lithuania		PRODUCT NAME: SITAGLIPTINUM; REGISTRATION NO/DATE: EU/1/07/383/001-024, 2007 03 21 EU/1/07/382/001-024 20070321
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

Last updated: July 27, 2025

rket Dynamics and Financial Trajectory for the Pharmaceutical Drug: Sitagliptin Phosphate

Introduction

Sitagliptin phosphate, marketed predominantly under the brand name Januvia among others, represents a significant evolution in the treatment of type 2 diabetes mellitus (T2DM). Since its regulatory approval in 2006, it has established a robust market presence driven by innovative pharmacotherapy, regulatory support, and escalating diabetes prevalence. This article examines the current market dynamics, financial trends, competitive positioning, and future outlook of sitagliptin phosphate within the global pharmaceutical landscape.

Overview of Sitagliptin Phosphate

Sitagliptin is a dipeptidyl peptidase-4 (DPP-4) inhibitor, enhancing endogenous incretin hormones such as GLP-1, thereby improving glycemic control in T2DM patients. Its once-daily oral administration offers a favorable safety profile compared to older agents, contributing to its widespread adoption. Developed by Merck & Co., it received FDA approval in 2006, revolutionizing the DPP-4 inhibitor class and expanding therapeutic options for diabetics.

Market Dynamics

Global Prevalence of T2DM and Market Drivers

The continuous rise in global T2DM cases underpins demand for effective pharmacotherapy. According to the International Diabetes Federation (IDF), approximately 537 million adults are living with diabetes worldwide as of 2021, projected to reach 643 million by 2030.[1] This escalating prevalence directly correlates with increased pharmaceutical sales, including sitagliptin.

In addition, the shift toward oral antidiabetic agents with better safety profiles over injectable therapies (e.g., insulin, GLP-1 receptor agonists) has favored sitagliptin's market position. Its once-daily dosing, minimal hypoglycemia risk, and weight neutrality bolster patient adherence and physician preferences, fueling sustained demand.

Competitive Landscape and Market Share

Sitagliptin competes primarily with other DPP-4 inhibitors such as saxagliptin, linagliptin, and alogliptin, as well as emerging incretin-based therapies. While initially dominant within the class, market share varies regionally owing to pricing, formulary placements, and regulatory approvals.

The entry of combination therapies, notably sitagliptin with metformin (JANUMET), has expanded market reach, addressing unmet needs for fixed-dose options. Such formulations contribute significantly to revenue streams, with Januvia and JANUMET representing a large proportion of Merck's diabetes portfolio.

Pricing and Reimbursement Policies

Pricing strategies influence sitagliptin's financial trajectory. Although initially premium-priced, competition, patent expirations, and payer negotiations have driven prices downward in some markets, especially in cost-sensitive regions such as Latin America and parts of Asia. Reimbursement policies in developed nations further affect sales volumes, with formulary placements determining accessibility.

Regulatory Environment and Patent Landscape

Patents protecting sitagliptin's formulation rights extended until 2022-2025 in various jurisdictions. Patent expirations often lead to generic entry, causing significant revenue erosion. Following patent losses, manufacturers resort to strategies like product differentiation, combination therapies, or geographical expansion to sustain revenues.

Financial Trajectory

Historical Sales Performance

Since launch, sitagliptin has demonstrated consistent growth. Merck's annual sales reports show that Januvia achieved peak global sales exceeding $7 billion in 2017, representing one of the top-selling antidiabetic agents worldwide.[2] Post-2017, sales plateaued or declined slightly, partially due to generics entering markets where patents expired and intensifying competition.

Impact of Patent Expiry and Generics

In the U.S., Merck's patent expiration in 2022 led to market entry of generic sitagliptin, resulting in significant price reductions and estimated sales erosion of up to 80% domestically. Globally, patent cliff effects varied, with some markets delaying generic penetration due to regulatory or pricing barriers.

Despite this, Merck continues to generate considerable revenues through brand extensions such as fixed-dose combinations and expansion into emerging markets. Moreover, the company's pipeline of next-generation DPP-4 inhibitors and novel incretin mimetics may mitigate the financial impact of generics on sitagliptin.

Growth Prospects and Revenue Forecasts

Forecasts project a gradual decline in global sitagliptin sales due to patent expirations, accompanied by a shift towards newer drug classes with superior efficacy or added benefits (e.g., SGLT2 inhibitors, GLP-1 receptor agonists). However, in markets with limited generic penetration, or where combination therapies dominate, revenues may remain stable or grow modestly through market expansion and formulary inclusions.

Emerging markets (e.g., China, India) are expected to significantly contribute to future sales, as economic growth, increasing T2DM prevalence, and improved healthcare access foster drug adoption. The International Diabetes Federation estimates that treatment of diabetes in emerging markets will account for more than 70% of the global market by 2030, providing long-term growth potential for sitagliptin-based therapies.[1]

Market Challenges and Opportunities

Challenges

• Patent Expirations: The primary threat to revenue stability involves generic entry post-patent expiry, leading to price erosion.
• Competitive Pressures: The rising popularity of SGLT2 inhibitors and GLP-1 receptor agonists, with demonstrated benefits beyond glycemic control (cardiovascular and renal protection), may limit DPP-4 inhibitor market share.
• Regulatory and Reimbursement Barriers: Variations in healthcare policies can hinder drug accessibility, especially in cost-sensitive regions.
• Market Saturation: Mature markets like North America and Europe face saturation, constraining growth prospects.

Opportunities

• Combination Therapies: Fixed-dose combinations enhance adherence and expand market share. Merck’s JANUMET remains a key revenue driver.
• Expansion into New Markets: Increasing urbanization and healthcare infrastructure development underpin growth in emerging economies.
• Pipeline Development: Innovations such as next-generation DPP-4 inhibitors with improved profiles can maintain Merck's competitive edge.
• Personalized Medicine: Biomarker-driven therapies and tailored treatment algorithms may optimize sitagliptin’s utilization within broader T2DM management strategies.

Future Outlook

The future of sitagliptin phosphate hinges on strategies that adapt to patent expirations and evolving market preferences. Continuous innovation, strategic licensing, and diversification into combination therapies and new indications (e.g., non-alcoholic fatty liver disease) can sustain revenues. Additionally, shifting focus towards integrated diabetes care models and expanding into underserved markets will fuel financial resilience.

Regulatory focus on safety, efficacy, and cardiovascular outcomes will shape sitagliptin’s repositioning amid competitive alternatives. As the global diabetes epidemic persists, sitagliptin remains a relevant component within multifaceted treatment paradigms, albeit with a need for strategic agility to navigate patent expirations and market evolution.

Key Takeaways

• Robust Market Foundation: Since its approval, sitagliptin has achieved significant market dominance, driven by safety, convenience, and brand recognition.
• Impact of Patent Expiry: The impending or recent patent expiration in key markets has led to sharp revenue declines, emphasizing the importance of innovation and portfolio diversification.
• Competitive Landscape Shift: Emergence of alternative drug classes like SGLT2 inhibitors and GLP-1 RAs dilutes sitagliptin's market share, particularly in high-income regions.
• Growth in Emerging Markets: Long-term opportunities reside in expanding access and adoption in Asia, Latin America, and Africa, benefiting from rising diabetes prevalence.
• Strategic Adaptation Needed: Continued innovation, combination therapy expansion, and market penetration efforts are critical for sustained financial performance.

FAQs

1. What factors contributed to the initial market success of sitagliptin?
Its oral route, favorable safety profile, once-daily dosing, and ability to be combined with other antidiabetic drugs facilitated rapid adoption. Regulatory approval and marketing by Merck further supported its market dominance.

2. How has patent expiry affected sitagliptin’s revenue?
Patent expiry led to the entry of generic competitors, resulting in significant price drops and revenue erosion—estimated at up to 80% in core markets like the U.S.—forcing Merck to shift focus toward combination therapies and emerging markets.

3. What competitive threats does sitagliptin face today?
Increased adoption of SGLT2 inhibitors and GLP-1 receptor agonists, which offer additional benefits like weight loss and cardiovascular protection, diminish sitagliptin’s market share, especially in high-income countries.

4. Are there new indications for sitagliptin beyond type 2 diabetes?
Current research is exploring sitagliptin’s potential in managing obesity, non-alcoholic fatty liver disease, and cardiovascular conditions, but these are not yet approved indications.

5. What strategies can Merck employ to sustain sitagliptin’s market relevance?
Investing in next-generation formulations, expanding combination therapies, targeting emerging markets, and exploring new indications can help sustain revenues amidst patent cliffs and competitive pressures.

References

[1] International Diabetes Federation. IDF Diabetes Atlas, 2021.
[2] Merck & Co. Annual Reports and Financial Filings, 2017-2022.