Linagliptin - Generic Drug Details

What are the generic drug sources for linagliptin and what is the scope of freedom to operate?

Linagliptin is the generic ingredient in five branded drugs marketed by Invagen Pharms, Sunshine, Zydus Pharms, and Boehringer Ingelheim, and is included in eight NDAs. There are sixteen 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 sixty-two 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 six tentative approvals for this compound.

Summary for linagliptin

International Patents:	462
US Patents:	16
Tradenames:	5
Applicants:	4
NDAs:	8
Drug Master File Entries:	19
Finished Product Suppliers / Packagers:	3
Raw Ingredient (Bulk) Api Vendors:	93
Clinical Trials:	142
Patent Applications:	3,304
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
EMS	Phase 3
Diabetes & Endocrinology Foundation	N/A
Medanta, The Medicity, India	N/A

See all linagliptin clinical trials

Generic filers with tentative approvals for LINAGLIPTIN

Applicant	Application No.	Strength	Dosage Form
		5MG	TABLET;ORAL
		2.5MG; 1G	TABLET;ORAL
		2.5MG; 850MG	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	TRADJENTA	linagliptin	TABLET;ORAL	201280-001	May 2, 2011	AB	RX	Yes	Yes	8,846,695*PED				Y
Boehringer Ingelheim	JENTADUETO XR	linagliptin; metformin hydrochloride	TABLET, EXTENDED RELEASE;ORAL	208026-002	May 27, 2016		RX	Yes	Yes	8,673,927*PED				Y
Boehringer Ingelheim	JENTADUETO	linagliptin; metformin hydrochloride	TABLET;ORAL	201281-003	Jan 30, 2012	AB	RX	Yes	Yes	10,022,379*PED				Y
Boehringer Ingelheim	JENTADUETO XR	linagliptin; metformin hydrochloride	TABLET, EXTENDED RELEASE;ORAL	208026-002	May 27, 2016		RX	Yes	Yes	8,883,805*PED				Y
Boehringer Ingelheim	TRADJENTA	linagliptin	TABLET;ORAL	201280-001	May 2, 2011	AB	RX	Yes	Yes
Boehringer Ingelheim	JENTADUETO	linagliptin; metformin hydrochloride	TABLET;ORAL	201281-001	Jan 30, 2012	AB	RX	Yes	No
Boehringer Ingelheim	JENTADUETO XR	linagliptin; metformin hydrochloride	TABLET, EXTENDED RELEASE;ORAL	208026-001	May 27, 2016		RX	Yes	No	7,407,955*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	7,078,381
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	8,119,648
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	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/002110 Trajenta 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
Chile	2011000259	Uso de 1-[(4-metil-quinazolin-2-il)metil]-3-metil-7-(2-butin-1-il)-8-(3-(r)-amino-piperidin-1-il)-xantina, inhibidor de dpp-4 para tratar y/o prevenir enfermedades metabolicas en pacientes que no pueden ser tratados con metformina y/o que presentan deficiencias renales.
Chile	2012002527	Medio de aislamiento y conservación para islotes de langerhans o células beta, donde el medio que refuerza la vitalidad y la capacidad de secreción de las células contiene entre 1 nmol/l y 1 µmol/l de un inhibidor de dipeptidil peptidasa iv (dpp iv o cd26); procedimiento para reforzar la vitalidad y capacidad de secreción de islotes de langerhans o células beta durante la fase de aislamiento y transplante.
China	107674077	8‑[3‑氨基‑哌啶‑1‑基]‑黄嘌呤化合物，其制备方法及作为药物制剂的用途 (8-[3-AMINO-PIPERIDIN-1-YL]-XANTHINES, PRODUCTION THEREOF AND USE OF SAME AS MEDICAMENTS)
Japan	5734564
Mexico	2011003774	TRATAMIENTO DE LA DIABETES EN PACIENTES CON CONTROL GLUCEMICO INSUFICIENTE A PESAR DE LA TERAPIA CON UN FARMACO ORAL O NO ORAL ANTIDIABETICO. (TREATMENT FOR DIABETES IN PATIENTS WITH INSUFFICIENT GLYCEMIC CONTROL DESPITE THERAPY WITH AN ORAL OR NON-ORAL ANTIDIABETIC DRUG.)
Morocco	32539	علاج مرض السكري بالنسبة للمرضى الذين لايصلح لهم العلاج بالميتفورمين
Taiwan	201304782	8-[3-amino-piperidin-1-yl]-xanthines, the preparation thereof and their use as pharmaceutical compositions

Supplementary Protection Certificates for linagliptin

Patent Number	Supplementary Protection Certificate	SPC Country	SPC Expiration	SPC Description
1532149	PA2011013,C1532149	Lithuania		PRODUCT NAME: LINAGLIPTINUM; REGISTRATION NO/DATE: EU/1/11/707/001, 2011-08-24 EU/1/11/707/002, 2011-08-24 EU/1/11/707/003, 2011-08-24 EU/1/11/707/004, 2011-08-24 EU/1/11/707/005, 2011-08-24 EU/1/11/707/006, 2011-08-24 EU/1/11/707/007, 2011-08-24 EU/1/11/707/008, 2011-08-24 EU/1/11/707/00 2011082
2187879	17C1016	France		PRODUCT NAME: COMBINAISON D'EMPAGLIFLOZINE ET DE LINAGLIPTINE OU L'UN DE SES SELS PHARMACEUTIQUEMENT ACCEPTABLES; REGISTRATION NO/DATE: EU/1/16/1146 20161115
2187879	PA2017014,C2187879	Lithuania		PRODUCT NAME: EMPAGLIFLOZINO IR LINAGLIPTINO ARBA JO FARMACINIU POZIURIU PRIIMTINOS DRUSKOS DERINYS; REGISTRATION NO/DATE: EU/1/16/1146/001 - EU/1/16/1146/018 20161111
1532149	C01532149/01	Switzerland		PRODUCT NAME: LINAGLIPTIN; REGISTRATION NO/DATE: SWISSMEDIC 61893 08.03.2012
1084705	CR 2014 00065	Denmark		PRODUCT NAME: LINAGLIPTIN; REG. NO/DATE: EU/1/11/707/001-011 20110830
1532149	CA 2011 00030	Denmark
1532149	PA2012022	Lithuania		PRODUCT NAME: LINAGLIPTINUM + METFORMINI HYDROCHLORIDUM; REGISTRATION NO/DATE: EU/1/12/780/001 - EU/1/12/780/034 20120720

Market Dynamics and Financial Trajectory of Linagliptin

Introduction to Linagliptin

Linagliptin, marketed under the brand name Tradjenta, is a dipeptidyl peptidase-4 (DPP-4) inhibitor used in the treatment of type 2 diabetes. It works by increasing the levels of incretin hormones, enhancing the release of insulin when glucose levels are elevated, and decreasing the release of glucagon by the liver.

Market Growth and Trends

The pharmaceutical grade linagliptin market has experienced rapid and substantial growth in recent years. Projections indicate a continued significant expansion from 2023 to 2031, driven by increasing demand for effective diabetes treatments and the rising prevalence of type 2 diabetes globally[1][4].

Segmentation and Market Size

The market is segmented based on type (purity ≥99%, purity <99%) and application (tablets, metformin tablets, metformin extended release tablets), as well as geographical regions (North America, Europe, Asia-Pacific, South America, and Middle-East and Africa). The purity ≥98% segment accounted for a noticeable share of the global linagliptin market in 2023 and is projected to experience significant growth in the near future[1][4].

Financial Performance

The financial trajectory of linagliptin is marked by steady growth. In Canada, for example, the spending on linagliptin has increased from $4 million in 2012 to $101 million in 2021. This trend reflects the increasing adoption of DPP-4 inhibitors in diabetes management[3].

Drivers of Growth

Several factors drive the growth of the linagliptin market:

• Increasing Prevalence of Diabetes: The rising number of patients with type 2 diabetes globally creates a larger market for antidiabetic drugs like linagliptin[1][4].
• Efficacy and Safety Profile: Clinical trials have demonstrated linagliptin's safety and efficacy, particularly its ability to reduce A1C levels with a low risk of hypoglycemia. This makes it a preferred option for many healthcare providers[5].
• Convenience and Simplicity: Linagliptin is available in a once-daily tablet form, which can be taken with or without food, making it a convenient option for patients[2].

Challenges and Restraints

Despite the growth, the market faces several challenges:

• Cost: Linagliptin is significantly more expensive than first-line therapies like metformin and sulfonylureas. A 30-day supply of linagliptin can cost around $250, which is a barrier for many patients[2].
• Generic Competition: As patents for DPP-4 inhibitors expire, generic competition is expected to increase, potentially impacting the market share of branded products like linagliptin[3].
• Alternative Therapies: The emergence of other antidiabetic drugs, such as GLP-1 receptor agonists, which have shown significant growth and additional indications beyond diabetes, poses a competitive threat to linagliptin[3].

Competitive Scenario

The linagliptin market is competitive, with several key players including Honor Lab, Morepen, Tapi Teva, EstechPharma, and others. These companies are focusing on strategy building and expanding their product portfolios to maintain market share[4].

Regional Analysis

The market is geographically diverse, with significant growth observed in regions like North America, Europe, and Asia-Pacific. Each region has its unique market dynamics, influenced by local healthcare policies, patient demographics, and economic factors[1][4].

Market Outlook and Forecast

The global linagliptin market is expected to continue its upward trend, driven by the increasing demand for antidiabetic medications and the expanding patient base. The market size is projected to grow significantly from 2023 to 2031, with a compound annual growth rate (CAGR) that reflects robust growth rates during the forecast period[1][4].

Key Players and Their Strategies

Key players in the linagliptin market are adopting various strategies to strengthen their market position:

• Product Portfolio Expansion: Companies are focusing on expanding their product portfolios to include a range of antidiabetic medications.
• Geographical Expansion: Players are looking to expand their presence in emerging markets where the demand for diabetes treatments is increasing.
• Research and Development: Continuous investment in R&D to improve the efficacy and safety profile of linagliptin and to explore new indications[4].

Consumer Behavior and Preferences

Consumer behavior plays a crucial role in the linagliptin market. Patients and healthcare providers prefer medications that are convenient, effective, and have a favorable safety profile. The once-daily dosing of linagliptin and its low risk of hypoglycemia make it a preferred choice for many[2][5].

Technological and Regulatory Trends

Technological advancements and regulatory changes also impact the market. For instance, the implementation of biosimilar switching policies in some regions has led to cost savings in the insulin market, which could influence the adoption of other antidiabetic drugs like linagliptin[3].

ESG and PESTEL Analysis

Environmental, Social, and Governance (ESG) factors, as well as Political, Economic, Social, Technological, Environmental, and Legal (PESTEL) analysis, are crucial in understanding the broader landscape of the linagliptin market. These factors can influence market dynamics, regulatory environments, and consumer behavior[4].

COVID-19 Impact

The COVID-19 pandemic has had a mixed impact on the linagliptin market. While it has disrupted supply chains and affected healthcare services, it has also highlighted the importance of effective diabetes management, potentially increasing demand for antidiabetic medications[4].

Key Takeaways

• The linagliptin market is experiencing significant growth driven by increasing demand for antidiabetic treatments.
• The market is segmented by type and application, with the purity ≥98% segment and linagliptin tablets being key segments.
• Despite high costs, linagliptin's efficacy and safety profile make it a preferred option.
• Key players are focusing on product portfolio expansion and geographical growth.
• Regulatory and technological trends, along with consumer behavior, play critical roles in shaping the market.

FAQs

Q: What is the primary use of linagliptin? A: Linagliptin is primarily used in the treatment of type 2 diabetes to help lower blood sugar levels.

Q: How does linagliptin compare to other DPP-4 inhibitors in terms of cost? A: Linagliptin is comparable in cost to other DPP-4 inhibitors but is significantly more expensive than first-line therapies like metformin and sulfonylureas[2].

Q: What are the key drivers of the linagliptin market? A: The key drivers include the increasing prevalence of diabetes, the efficacy and safety profile of linagliptin, and its convenience of use[1][4].

Q: How does linagliptin affect A1C levels? A: Clinical trials have shown that linagliptin can reduce A1C levels by approximately 1.2% when used as monotherapy and by 0.7% when added to metformin or metformin plus sulfonylurea[5].

Q: What are the potential challenges facing the linagliptin market? A: The market faces challenges such as high costs, generic competition, and the emergence of alternative therapies like GLP-1 receptor agonists[2][3].

Cited Sources

1. Global Pharmaceutical Grade Linagliptin Market Size, Trends and ... - Market Research Intellect
2. Linagliptin (Tradjenta) for the Treatment of Diabetes Mellitus - American Academy of Family Physicians
3. Market Intelligence Report: Antidiabetic Drugs, 2012-2021 - Government of Canada
4. Linagliptin Market Report 2024 (Global Edition) - Cognitive Market Research
5. New Phase III Data and Pooled Analysis for Linagliptin Show ... - Eli Lilly and Company Investor Relations

Last updated: 2024-12-16