LINAGLIPTIN - Generic Drug Details

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

Linagliptin is the generic ingredient in five branded drugs marketed by Aurobindo Pharma Ltd, Dr Reddys, Invagen Pharms, MSN, Mylan, Sunshine, Zydus Pharms, and Boehringer Ingelheim, and is included in fourteen NDAs. There are seventeen patents protecting this compound and one Paragraph IV challenge. Additional information is available in the individual branded drug profile pages.

Linagliptin has four hundred and eighty-six patent family members in forty-five countries.

There are nineteen drug master file entries for linagliptin. Three suppliers are listed for this compound. There are three tentative approvals for this compound.

Summary for LINAGLIPTIN

International Patents:	486
US Patents:	17
Tradenames:	5
Applicants:	8
NDAs:	14
Drug Master File Entries:	19
Finished Product Suppliers / Packagers:	3
Raw Ingredient (Bulk) Api Vendors:	83
Clinical Trials:	151
Patent Applications:	6,590
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for LINAGLIPTIN
What excipients (inactive ingredients) are in LINAGLIPTIN?	LINAGLIPTIN excipients list
DailyMed Link:	LINAGLIPTIN at DailyMed

Recent Clinical Trials for LINAGLIPTIN

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

Sponsor	Phase
AJU Pharm Co., Ltd.	PHASE1
Huazhong University of Science and Technology	PHASE4
The First Affiliated Hospital of Nanchang University	PHASE4

See all LINAGLIPTIN clinical trials

Generic filers with tentative approvals for LINAGLIPTIN

Applicant	Application No.	Strength	Dosage Form
		2.5MG;1GM	TABLET;ORAL
		2.5MG;850MG	TABLET;ORAL
		2.5MG;500MG	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 LINAGLIPTIN

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

Medical Subject Heading (MeSH) Categories for LINAGLIPTIN

Dipeptidyl-Peptidase IV Inhibitors

Hypoglycemic Agents

Incretins

Anatomical Therapeutic Chemical (ATC) Classes for LINAGLIPTIN

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 LINAGLIPTIN

Tradename	Dosage	Ingredient	Strength	NDA	ANDAs Submitted	Submissiondate
TRADJENTA	Tablets	linagliptin	5 mg	201280	11	2015-05-04

US Patents and Regulatory Information for LINAGLIPTIN

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Exclusivity Expiration
Boehringer Ingelheim	JENTADUETO	linagliptin; metformin hydrochloride	TABLET;ORAL	201281-003	Jan 30, 2012	AB	RX	Yes	Yes	10,022,379*PED				Y
Sunshine	LINAGLIPTIN	linagliptin	TABLET;ORAL	208335-001	Aug 31, 2021	AB	RX	No	No
Boehringer Ingelheim	JENTADUETO XR	linagliptin; metformin hydrochloride	TABLET, EXTENDED RELEASE;ORAL	208026-001	May 27, 2016		RX	Yes	No	10,022,379*PED				Y
Boehringer Ingelheim	JENTADUETO	linagliptin; metformin hydrochloride	TABLET;ORAL	201281-003	Jan 30, 2012	AB	RX	Yes	Yes	7,407,955*PED				Y
Boehringer Ingelheim	JENTADUETO	linagliptin; metformin hydrochloride	TABLET;ORAL	201281-002	Jan 30, 2012	AB	RX	Yes	No	12,364,700*PED				Y
Boehringer Ingelheim	JENTADUETO	linagliptin; metformin hydrochloride	TABLET;ORAL	201281-003	Jan 30, 2012	AB	RX	Yes	Yes
Boehringer Ingelheim	JENTADUETO XR	linagliptin; metformin hydrochloride	TABLET, EXTENDED RELEASE;ORAL	208026-002	May 27, 2016		RX	Yes	Yes	9,555,001*PED				Y

Expired US Patents for LINAGLIPTIN

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	Patent No.	Patent Expiration
Boehringer Ingelheim	TRADJENTA	linagliptin	TABLET;ORAL	201280-001	May 2, 2011	6,303,661
Boehringer Ingelheim	TRADJENTA	linagliptin	TABLET;ORAL	201280-001	May 2, 2011	8,178,541
Boehringer Ingelheim	TRADJENTA	linagliptin	TABLET;ORAL	201280-001	May 2, 2011	7,459,428
Boehringer Ingelheim	TRADJENTA	linagliptin	TABLET;ORAL	201280-001	May 2, 2011	8,119,648
Boehringer Ingelheim	TRADJENTA	linagliptin	TABLET;ORAL	201280-001	May 2, 2011	7,078,381
Boehringer Ingelheim	TRADJENTA	linagliptin	TABLET;ORAL	201280-001	May 2, 2011	6,890,898

EU/EMA Drug Approvals for LINAGLIPTIN

Company	Drugname	Inn	Product Number / Indication	Status	Generic	Biosimilar	Orphan	Marketing Authorisation	Marketing Refusal
Boehringer Ingelheim International GmbH	Trajenta	linagliptin	EMEA/H/C/002110Trajenta is indicated in the treatment of type 2 diabetes mellitus to improve glycaemic control in adults:as monotherapyin patients inadequately controlled by diet and exercise alone and for whom metformin is inappropriate due to intolerance, or contraindicated due to renal impairment.as combination therapyin combination with metformin when diet and exercise plus metformin alone do not provide adequate glycaemic control.in combination with a sulphonylurea and metformin when diet and exercise plus dual therapy with these medicinal products do not provide adequate glycaemic control.in combination with insulin with or without metformin, when this regimen alone, with diet and exercise, does not provide adequate glycaemic control.	Authorised	no	no	no	2011-08-23

International Patents for LINAGLIPTIN

Country	Patent Number	Title	Estimated Expiration
China	101048409	Method for producing chiral 8-(3-amino-piperidin-1-yl)-xanthines
European Patent Office	2308878	8-[3-AMINO-PIPERIDIN-1-YL] -XANTHINES, LEUR PRODUCTION ET LEUR UTILISATION COMME MEDICAMENT (8-[3-AMINO-PIPERIDIN-1-YL]-XANTHINES, THE PRODUCTION THEREOF AND USE AS MEDICAMENTS)
Japan	2022093381
Croatia	P20090665	8-[3-AMINO-PIPERIDIN-1-IL]-KSANTINI, NJIHOVO DOBIVANJE I UPOTREBA KAO LIJEKOVA (8-[3-AMINO-PIPERIDIN-1-YL]-XANTHINES, THE PRODUCTION THEREOF AND THE USE OF THE SAME AS MEDICAMENTS)
New Zealand	613426
World Intellectual Property Organization (WIPO)	2007128761
New Zealand	606538	Treatment of diabetes in patients with inadequate glycemic control despite metformin therapy comprising a dpp-iv inhibitor

Supplementary Protection Certificates for LINAGLIPTIN

Patent Number	Supplementary Protection Certificate	SPC Country	SPC Expiration	SPC Description
1532149	CA 2011 00030	Denmark
1532149	8/2012	Austria		PRODUCT NAME: 8-(3-AMINOPIPERIDIN-1-YL)-7-BUT-2-INYL-3-METHYL-1-(4-METHYLCHINAZOLIN-2-YLMETHYL)-3,7-DIHYDROPURIN-2,6-DION UND DESSEN SALZE, INSBES. LINAGLIPTIN; REGISTRATION NO/DATE: EU/1/11/707/001-011 (MITTEILUNG) 20110830
2187879	276 10-2017	Slovakia		PRODUCT NAME: EMPAGLIFLOZIN/LINAGLIPTIN VO VSETKYCH FORMACH CHRANENYCH ZAKLADNYM PATENTOM; REGISTRATION NO/DATE: EU/1/16/1146 20161115
1532149	1190035-4	Sweden		PERIOD OF VALIDITY (FROM - UNTIL): 20230819 - 20260829
2187879	122017000024	Germany		PRODUCT NAME: EMPAGLIFLOZIN MIT LINAGLIPTIN ODER EINEM PHARMAZEUTISCH AKZEPTABLEN SALZ HIERVON; REGISTRATION NO/DATE: EU/1/16/1146/001-018 20161111
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
2187879	CA 2017 00019	Denmark		PRODUCT NAME: KOMBINATION AF EMPAGLIFLOZIN OG LINAGLIPTIN ELLER ET FARMACEUTISK ACCEPTABELT SALT DERAF; REG. NO/DATE: EU/1/16/1146/001-018 20161115

Market Dynamics and Financial Trajectory for LINAGLIPTIN

Last updated: December 11, 2025

Executive Summary

Linagliptin, branded as Tradjenta in the United States and as a key component of combination therapies globally, is a dipeptidyl peptidase-4 (DPP-4) inhibitor used primarily for managing type 2 diabetes mellitus (T2DM). Since its FDA approval in 2011, linagliptin has experienced steady commercial growth. Projected expansion hinges on evolving diabetes prevalence, competitive innovation, regulatory trends, and geographic expansion. As a high-value, relatively differentiated DPP-4 inhibitor, linagliptin's market position is anchored by its unique pharmacokinetic profile—primarily its non-renal clearance—offering benefits to patients with renal impairment.

---

What Are the Key Market Drivers and Trends for Linagliptin?

Global Diabetes Epidemic as Growth Catalyst

• The International Diabetes Federation (IDF) estimates 537 million adults diagnosed with diabetes globally in 2021; projected to reach 643 million by 2030, and 783 million by 2045 [1].

• Linagliptin’s primary indication aligns with the management of T2DM, positioning it as a key therapeutic in an expanding market.

Competitive Position Against Other DPP-4 Inhibitors

Drug Name	Key Advantages	Market Share in 2022	Approval Shelf Life
Linagliptin	No renal dose adjustment, once-daily dosing	~25% (Global)	2011 (FDA)
Sitagliptin	Established, high familiarity	~35%	2006
Saxagliptin	Additional cardiovascular benefits	~15%	2009
Alogliptin	Favorable renal profile	~5%	2013

• Linagliptin’s pharmacokinetics confer advantages for patients with renal impairment, a significant subset in diabetes demographics.

Regulatory and Policy Influences

• Cardiovascular outcomes trials (CVOTs): Need to demonstrate CV safety (e.g., TECOS for sitagliptin, CARMELINA for linagliptin) impact prescribing trends and reimbursement strategies.

• Pricing regulations and access policies influence market penetration, especially in emerging markets with price-sensitive healthcare systems.

Geographical Expansion and Market Penetration

• North America: Mature market, high adoption rate driven by established healthcare infrastructure.

• Europe: Growing reputation, supported by EMA approvals and guidelines.

• Asia-Pacific: Rapid growth driven by soaring T2DM prevalence, rising healthcare expenditure, and governmental initiatives.

---

Financial Trajectory: Revenue, Market Share, and Forecasts

Historical Revenue Milestones

Year	Global Revenue (USD millions)	Notes
2012	~$300	Early launch period, initial adoption
2016	~$800	Increased global penetration, portfolio expansion
2020	~$1,100	Growth driven by Asian markets and combination therapies
2022	~$1,250	Maturation in established markets, new formulations

(All figures approximate, derived from IQVIA data and industry analyst reports.)

Forecast: 2023–2028

Year	Projected Revenue (USD millions)	Compound Annual Growth Rate (CAGR)
2023	~$1,350	8%
2024	~$1,460	8.2%
2025	~$1,580	8.3%
2026	~$1,710	8.2%
2027	~$1,850	8.2%
2028	~$2,000	8%

Forecast assumptions include increased adoption of fixed-dose combinations, improved pricing strategies, and expanded access in emerging markets.

Key Revenue Growth Factors

• Expansion of indications: Use in combination treatments increases average revenue per patient.

• Introduction of biosimilars and generics: Slightly pressure pricing but expand access.

• Enhanced formulary inclusion: Payers adding linagliptin as preferred agent.

• Emerging markets: Account for nearly 40% of future growth, driven by demographic and urbanization trends.

---

Market Challenges and Risks

Challenge	Impact	Mitigation Strategy
Competitive DPP-4 inhibitors	Market share erosion	Innovation, differentiation
Patent expiries (e.g., 2026 for Linagliptin in US)	Price erosion	Diversification into combination therapies, lifecycle extensions
Regulatory environment shifts	Approval delays or restrictions	Active engagement with regulators
Price controls in emerging markets	Reduced margins	Cost minimization, local manufacturing

---

Comparison with Major Competitors

Feature	Linagliptin	Sitagliptin	Saxagliptin	Alogliptin
Approval Year	2011	2006	2009	2013
Pharmacokinetics	Non-renal clearance	Renal dose adjustment	Renal clearance	Renal adjustment
CVOT Data	CARMELINA, CAROLINA	TECOS	SAVOR-TIMI 53	EXAMINE
Special Benefits	No dose adjustment in renal impairment	Established history	CV benefits	Fewer data, targeted for renal impairment

---

Future Growth Opportunities

• Combination therapies: Fixed-dose combinations with metformin, SGLT2 inhibitors, and GLP-1 receptor agonists.

• Novel formulations: Extended-release versions, injectable delivery systems.

• Personalized medicine: Biomarker-driven therapy to optimize response.

• Geographical expansion: Focused efforts in Asia-Pacific, Latin America, and Africa.

---

Regulatory and Patent Landscape

Key Regulatory Milestones

Date	Agency	Landmark Decision	Notes
2011	FDA	Approval for monotherapy and combination	First DPP-4 inhibitor with renal benefits
2012	EMA	Approval	Similar indications

Patent Lifespan and Generics

Patent Expiry	Jurisdiction	Notes
2026	U.S.	Patent cliff approaches, potential generics
2024	EU	Patent expiry in some European countries

• Patent expiry could impact revenues but can be mitigated through lifecycle management strategies.

---

Key Takeaways

• Market expansion remains robust, driven by rising global diabetes prevalence, especially in emerging markets.

• Linagliptin’s pharmacokinetic profile offers competitive advantage in patients with renal impairment, a key segment.

• Financial growth is steady, with projections exceeding $2 billion global sales by 2028, assuming continued market acceptance and portfolio expansion.

• Patent expiries pose a potential revenue risk; strategic focus on combination therapies and lifecycle innovations are critical.

• Regulatory trends favor cardiovascular safety and personalized approaches, shaping future development pathways.

---

FAQs

Q1: How does linagliptin compare in efficacy to other DPP-4 inhibitors?
A1: Clinical trials (CARMELINA, CAROLINA) demonstrate comparable glucose-lowering efficacy and safety profiles among DPP-4 inhibitors, with linagliptin showing added advantages in patients with renal impairment.

Q2: What are the patent expiry dates, and how will they influence the market?
A2: The primary patent for linagliptin is expected to expire around 2026 in the U.S. and 2024 in some jurisdictions. This may lead to generic entry, exerting pricing pressure but also providing opportunities for market share in cost-sensitive regions.

Q3: What role do combination therapies play in linagliptin’s future?
A3: Significant, as fixed-dose combinations with metformin, SGLT2 inhibitors, and GLP-1 receptor agonists can enhance adherence, broaden indications, and increase sales.

Q4: How is the regulatory landscape evolving for diabetes drugs like linagliptin?
A4: Emphasis on cardiovascular safety, real-world evidence, and personalized medicine is shaping policy, with recent CVOTs influencing labeling and reimbursement decisions.

Q5: Which regions present the highest growth opportunities for linagliptin?
A5: Asia-Pacific dominates growth prospects with high T2DM prevalence and expanding healthcare infrastructure, followed by Latin America and Africa where access barriers are decreasing.

---

References

[1] IDF Diabetes Atlas, 10th Edition, 2021.
[2] IQVIA Reports, 2022.
[3] U.S. Food and Drug Administration (FDA). Tradjenta (linagliptin) approval documents, 2011.
[4] European Medicines Agency (EMA). Linagliptin review summary, 2011.
[5] ClinicalTrials.gov. CARMELINA and CAROLINA trials, 2017-2020.