JANUVIA Drug Patent Profile

Which patents cover Januvia, and what generic alternatives are available?

Januvia is a drug marketed by Merck Sharp Dohme and is included in one NDA. There is one patent protecting this drug and four Paragraph IV challenges.

This drug has fifty-two patent family members in forty countries.

The generic ingredient in JANUVIA is sitagliptin phosphate. There are thirty-five drug master file entries for this compound. Three suppliers are listed for this compound. Additional details are available on the sitagliptin phosphate profile page.

DrugPatentWatch^® Generic Entry Outlook for Januvia

Januvia was eligible for patent challenges on October 16, 2010.

By analyzing the patents and regulatory protections it appears that the earliest date for generic entry will be May 24, 2027. This may change due to patent challenges or generic licensing.

Annual sales in 2021 were $8.9bn, indicating a strong incentive for generic entry (peak sales were $9.2bn in 2020).

There have been twenty-six 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 thirteen tentative approvals for the generic drug (sitagliptin phosphate), which indicates the potential for near-term generic launch.

Indicators of Generic Entry

Summary for JANUVIA

International Patents:	52
US Patents:	1
Applicants:	1
NDAs:	1
Finished Product Suppliers / Packagers:	3
Raw Ingredient (Bulk) Api Vendors:	82
Clinical Trials:	161
Patent Applications:	34
Drug Prices:	Drug price information for JANUVIA
Drug Sales Revenues:	Drug sales revenues for JANUVIA
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for JANUVIA
What excipients (inactive ingredients) are in JANUVIA?	JANUVIA excipients list
DailyMed Link:	JANUVIA at DailyMed

See drug prices for JANUVIA

See drug sales revenues for JANUVIA

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

NDA:

021995

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 JANUVIA

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

Sponsor	Phase
Hospital de Especialidades, Centro Medico Nacional "La Raza", Instituto Mexicano del Seguro Social	Phase 4
National Polytechnic Institute, Mexico	Phase 4
Peking University People's Hospital	Phase 2

See all JANUVIA clinical trials

Pharmacology for JANUVIA

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

Paragraph IV (Patent) Challenges for JANUVIA

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 JANUVIA

JANUVIA is protected by one US patents.

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
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	021995-002	Oct 16, 2006		RX	Yes	No					Y
Merck Sharp Dohme	JANUVIA	sitagliptin phosphate	TABLET;ORAL	021995-003	Oct 16, 2006		RX	Yes	Yes					Y

Expired US Patents for JANUVIA

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

See the table below for patents covering JANUVIA around the world.

Country	Patent Number	Title	Estimated Expiration
China	1132578
Dominican Republic	P2002000438	INHIBIDORES DE LA DIPETIDIL PEPTIDASA BETA-AMINO HETEROCÍCLICA PARA EL TRATAMIENTO O LA PREVENCIÓN DE LA DIABETES
Japan	3762407
Netherlands	300357
New Zealand	529833	Beta-amino tetrahydroimidazo (1, 2-A) pyrazines and tetrahydrotrioazolo (4, 3-A) pyrazines as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
Norway	335371

Supplementary Protection Certificates for JANUVIA

Patent Number	Supplementary Protection Certificate	SPC Country	SPC Expiration	SPC Description
1412357	106 4-2007	Slovakia		PRODUCT NAME: SITAGLIPTIN; REGISTRATION NO/DATE: EU/1/07/383/001 - EU/1/07/383/018 20070321
1412357	300287	Netherlands		PRODUCT NAME: SITAGLIPTINE, DESGEWENST IN DE VORM VAN EEN FARMACEUTISCH AANVAARDBAAR ZOUT, IN HET BIJZONDER SITAGLIPTINE FOSFAAT MONOHYDRAAT; REGISTRATION NO/DATE: EU/1/07/383/001-018 20070323
1412357	300357	Netherlands		300357, 20220705, EXPIRES: 20230715
1412357	343	Finland
1084705	C300708	Netherlands		PRODUCT NAME: LINAGLIPTIN; REGISTRATION NO/DATE: EU/1/11/707/001-011 20111224
1084705	CA 2014 00062	Denmark		PRODUCT NAME: SAXAGLIPTIN OG FARMACEUTISK SALTE DERAF, HERUNDER SAXAGLIPTIN HYDROCHLORID; REG. NO/DATE: EU/1/09/545/001-015 20091001

Market Dynamics and Financial Trajectory for JANUVIA

Introduction

JANUVIA, developed by Merck, is a dipeptidyl peptidase-4 (DPP-4) inhibitor used to improve glycemic control in patients with type 2 diabetes. Since its FDA approval in 2006, JANUVIA, along with its combination product JANUMET (sitagliptin and metformin), has been a significant player in the diabetes treatment market. Here, we delve into the market dynamics and financial trajectory of JANUVIA.

Historical Performance

JANUVIA has had a robust performance since its launch. By 2012, it had become Merck's best-selling product franchise, with global sales reaching $5.7 billion[3].

• The drug's success was attributed to its efficacy, marketing proficiency, and strong sales in both the US and international markets. In the US, sales grew by 15% in the fourth quarter of 2012, while international sales grew by 25% during the same period[3].

Market Share and Competition

JANUVIA and JANUMET have dominated the DPP-4 inhibitor market, holding over 70% of the global market share as of 2013[3].

• Despite competitive market forces and regulatory challenges, analysts have remained bullish on the JANUVIA franchise. The drug's ability to maximally inhibit DPP-4 has been a key factor in its market dominance[3].

Loss of Exclusivity

In late 2021, JANUVIA lost its exclusivity in Europe, marking a significant turning point in its market dynamics.

• Following the loss of exclusivity, generic versions of sitagliptin quickly gained traction. In France, for example, patient counts for JANUVIA declined from 290,300 in August 2022 to 75,000 a year later, with a corresponding increase in patients using generic sitagliptin[1].
• Similarly, JANUMET saw a decline in patient counts from 450,200 in March 2023 to 173,700 by August 2023, as generic versions of sitagliptin and metformin gained popularity[1].

Financial Impact

The loss of exclusivity has had a pronounced financial impact on Merck.

• In 2023, sales of JANUVIA and JANUMET declined by 25% and 23%, respectively, compared to the previous year. This decline was reflected in Merck's financial results, with total sales for these products dropping from $4.513 billion in 2022 to $3.366 billion in 2023[2].

Sales Statistics

Despite the decline, JANUVIA remains one of the top-selling diabetes drugs.

• In 2022, JANUVIA and JANUMET combined sales were $4.513 billion, although this was a 15% drop from the previous year due to issues such as nitrosamine contamination[4].

Regional Performance

JANUVIA's performance varies significantly across different regions.

• In Europe, the drug has faced significant competition from generics following the loss of exclusivity. However, in other regions such as Japan, Latin America, and the Middle East, JANUVIA continues to show robust growth[3].
• Merck has also focused on emerging markets, particularly in Asia, where the prevalence of diabetes is high. For example, China and India have large diabetic populations, and Merck has conducted additional studies to gain approval in these markets[3].

Future Outlook

The future of JANUVIA is influenced by several factors, including competition from generics, regulatory approvals, and emerging market opportunities.

• While the drug faces challenges from generic competition, Merck's clinical study database and ongoing research into new indications and formulations could support its continued relevance. For instance, the potential cardiovascular benefits of DPP-4 inhibitors, although not conclusive, could be a positive factor[3].

Challenges and Opportunities

JANUVIA has faced several challenges, including safety concerns and regulatory actions.

• In 2022, the drug was flagged for nitrosamine contamination, a potential carcinogen, which led to a decline in sales. However, Merck's proactive approach to addressing these issues and its strong clinical data have helped maintain confidence in the product[4].

Key Takeaways

• Market Dominance: JANUVIA has been a leading DPP-4 inhibitor, dominating the global market with over 70% share.
• Loss of Exclusivity: The loss of exclusivity in Europe has led to a significant decline in sales due to generic competition.
• Financial Impact: Sales of JANUVIA and JANUMET have declined by 25% and 23%, respectively, in 2023 compared to the previous year.
• Regional Performance: The drug continues to show growth in regions like Japan, Latin America, and the Middle East.
• Future Outlook: The future of JANUVIA depends on managing generic competition, leveraging clinical data, and exploring new market opportunities.

FAQs

Q: What is JANUVIA used for? A: JANUVIA is used to improve glycemic control in patients with type 2 diabetes in conjunction with diet and exercise.

Q: When did JANUVIA lose its exclusivity in Europe? A: JANUVIA lost its exclusivity in Europe at the end of 2021.

Q: How has the loss of exclusivity affected JANUVIA sales? A: The loss of exclusivity has led to a significant decline in sales as generic versions of sitagliptin and sitagliptin/metformin have gained traction.

Q: What are the key regions where JANUVIA continues to show growth? A: JANUVIA continues to show robust growth in regions such as Japan, Latin America, and the Middle East.

Q: What challenges has JANUVIA faced recently? A: JANUVIA has faced challenges including safety concerns such as nitrosamine contamination and increased competition from generic versions.

Sources

1. Clarivate: After loss of exclusivity, small-molecule generics bite quick and hard ...
2. Merck: Merck Announces Fourth-Quarter and Full-Year 2023 Financial Results
3. Pharmaceutical Executive: Brand of the Year: Januvia
4. Xtalks: Top 15 Diabetes Drugs in 2023 by 2022 Sales Statistics
5. Merck: Merck Announces Third-Quarter 2024 Financial Results