LINAGLIPTIN; METFORMIN HYDROCHLORIDE - Generic Drug Details

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

Linagliptin; metformin hydrochloride is the generic ingredient in three branded drugs marketed by Boehringer Ingelheim, Sunshine, and Zydus Pharms, and is included in four NDAs. There are eleven patents protecting this compound and two Paragraph IV challenges. Additional information is available in the individual branded drug profile pages.

Linagliptin; metformin hydrochloride has three hundred and eighty-nine patent family members in forty-five countries.

One supplier is listed for this compound. There are two tentative approvals for this compound.

Summary for LINAGLIPTIN; METFORMIN HYDROCHLORIDE

International Patents:	389
US Patents:	11
Tradenames:	3
Applicants:	3
NDAs:	4
Finished Product Suppliers / Packagers:	1
Clinical Trials:	61
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for LINAGLIPTIN; METFORMIN HYDROCHLORIDE
DailyMed Link:	LINAGLIPTIN; METFORMIN HYDROCHLORIDE at DailyMed

Recent Clinical Trials for LINAGLIPTIN; METFORMIN HYDROCHLORIDE

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

Sponsor	Phase
Medanta, The Medicity, India	N/A
Dong Wha Pharmaceutical Co. Ltd.	Phase 1
The First Affiliated Hospital with Nanjing Medical University	N/A

See all LINAGLIPTIN; METFORMIN HYDROCHLORIDE clinical trials

Generic filers with tentative approvals for LINAGLIPTIN; METFORMIN HYDROCHLORIDE

Applicant	Application No.	Strength	Dosage Form
		2.5MG; 1G	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; METFORMIN HYDROCHLORIDE

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

Anatomical Therapeutic Chemical (ATC) Classes for LINAGLIPTIN; METFORMIN HYDROCHLORIDE

A10BA	Biguanides
A10B	BLOOD GLUCOSE LOWERING DRUGS, EXCL. INSULINS
A10	DRUGS USED IN DIABETES
A	Alimentary tract and metabolism

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; METFORMIN HYDROCHLORIDE

Tradename	Dosage	Ingredient	Strength	NDA	ANDAs Submitted	Submissiondate
JENTADUETO XR	Extended-release Tablets	linagliptin; metformin hydrochloride	2.5 mg/1000 mg 5 mg/1000 mg	208026	1	2018-03-28
JENTADUETO	Tablets	linagliptin; metformin hydrochloride	2.5 mg/500 mg 2.5 mg/850 mg 2.5 mg/1000 mg	201281	8	2015-05-04

US Patents and Regulatory Information for LINAGLIPTIN; METFORMIN HYDROCHLORIDE

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 XR	linagliptin; metformin hydrochloride	TABLET, EXTENDED RELEASE;ORAL	208026-002	May 27, 2016		RX	Yes	Yes	9,415,016*PED				Y
Boehringer Ingelheim	JENTADUETO XR	linagliptin; metformin hydrochloride	TABLET, EXTENDED RELEASE;ORAL	208026-002	May 27, 2016		RX	Yes	Yes	10,022,379*PED				Y
Boehringer Ingelheim	JENTADUETO XR	linagliptin; metformin hydrochloride	TABLET, EXTENDED RELEASE;ORAL	208026-001	May 27, 2016		RX	Yes	No	9,415,016*PED				Y
Boehringer Ingelheim	JENTADUETO XR	linagliptin; metformin hydrochloride	TABLET, EXTENDED RELEASE;ORAL	208026-002	May 27, 2016		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
Boehringer Ingelheim	JENTADUETO	linagliptin; metformin hydrochloride	TABLET;ORAL	201281-001	Jan 30, 2012	AB	RX	Yes	No	10,973,827*PED				Y

Expired US Patents for LINAGLIPTIN; METFORMIN HYDROCHLORIDE

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	Patent No.	Patent Expiration
Boehringer Ingelheim	JENTADUETO	linagliptin; metformin hydrochloride	TABLET;ORAL	201281-001	Jan 30, 2012	7,078,381
Boehringer Ingelheim	JENTADUETO	linagliptin; metformin hydrochloride	TABLET;ORAL	201281-002	Jan 30, 2012	6,890,898
Boehringer Ingelheim	JENTADUETO XR	linagliptin; metformin hydrochloride	TABLET, EXTENDED RELEASE;ORAL	208026-002	May 27, 2016	6,635,280
Boehringer Ingelheim	JENTADUETO	linagliptin; metformin hydrochloride	TABLET;ORAL	201281-002	Jan 30, 2012	8,178,541
Boehringer Ingelheim	JENTADUETO	linagliptin; metformin hydrochloride	TABLET;ORAL	201281-001	Jan 30, 2012	6,303,661
Boehringer Ingelheim	JENTADUETO	linagliptin; metformin hydrochloride	TABLET;ORAL	201281-002	Jan 30, 2012	7,078,381

EU/EMA Drug Approvals for LINAGLIPTIN; METFORMIN HYDROCHLORIDE

Company	Drugname	Inn	Product Number / Indication	Status	Generic	Biosimilar	Orphan	Marketing Authorisation	Marketing Refusal
Boehringer Ingelheim International GmbH	Jentadueto	linagliptin, metformin hydrochloride	EMEA/H/C/002279 Treatment of adult patients with type-2 diabetes mellitus:Jentadueto is indicated as an adjunct to diet and exercise to improve glycaemic control in adult patients inadequately controlled on their maximal tolerated dose of metformin alone, or those already being treated with the combination of linagliptin and metformin.Jentadueto is indicated in combination with a sulphonylurea (i.e. triple combination therapy) as an adjunct to diet and exercise in adult patients inadequately controlled on their maximal tolerated dose of metformin and a sulphonylurea.	Authorised	no	no	no	2012-07-19

International Patents for LINAGLIPTIN; METFORMIN HYDROCHLORIDE

Country	Patent Number	Title	Estimated Expiration
South Korea	20110107810	TREATMENT FOR DIABETES IN PATIENTS WITH INADEQUATE GLYCEMIC CONTROL DESPITE METFORMIN THERAPY COMPRISING A DPP-IV INHIBITOR
Hong Kong	1204548	抑制劑的用途 (USES OF DPP IV INHIBITORS DPP IV)
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)
South Korea	20140068267	METHOD FOR PRODUCING CHIRAL 8-(3-AMINO-PIPERIDIN-1-YL)-XANTHINES
Ecuador	SP11010971	TRATAMIENTO DE LA DIABETES EN PACIENTES CON CONTROL GLUCEMICO INSUFICIENTE A PESAR DE LA TERAPIA CON UN FÁRMACO ORAL O NO ORAL ANTIDIABÉTICO
Canada	2897719	UTILISATIONS D'INHIBITEURS DE L'ENZYME DPP IV (USE OF DPP IV INHIBITORS)

Supplementary Protection Certificates for LINAGLIPTIN; METFORMIN HYDROCHLORIDE

Patent Number	Supplementary Protection Certificate	SPC Country	SPC Expiration	SPC Description
1084705	C300708	Netherlands		PRODUCT NAME: LINAGLIPTIN; REGISTRATION NO/DATE: EU/1/11/707/001-011 20111224
1532149	C01532149/01	Switzerland		PRODUCT NAME: LINAGLIPTIN; REGISTRATION NO/DATE: SWISSMEDIC 61893 08.03.2012
1532149	C20110018 00046	Estonia		PRODUCT NAME: TRAJENTA-LINAGLIPTIN; REG NO/DATE: FINAL 24.08.2011
1532149	CR 2011 00030	Denmark		PRODUCT NAME: LINAGLIPTIN OG SALTE DERAF; NAT. REG. NO/DATE: EU/1/11/707/001-011 20110830; FIRST REG. NO/DATE: EU EU/1/11/707/001-0011 20110830
1532149	CA 2013 00001	Denmark		PRODUCT NAME: 8-(3-AMINOPIPERIDIN-1-YL)-7-BUT-2-INYL-3-METHYL-1-(4-METHYLCHINAZOLIN-2-YLMETHYL)-3,7-DIHYDROPURIN-2,6-DION ENANTIOMERER OG SALTE DERAF - SAERLIGT LINAGLIPTIN - I KOMBINATION MED METFORMINHYDROCHLORID; REG. NO/DATE: EU/1/12/780/001-028 20120720
1532149	C 2012 003	Romania		PRODUCT NAME: 8-(3-AMINOPIPERIDIN-1-IL)-7-BUT-2-INIL-3-METIL-1-(4-METILCHINAZOLIN-2-ILMETIL)3,7-DIHIDROPURIN-2,6-DIONA, ENANTIOMERII SI SARURILE LOR IN SPECIAL LINAGLIPTIN - LINAGLIPTIN, ENANTIOMERIISI SARURILE ACCEPTABILE FARMACEUTIC; NATIONAL AUTHORISATION NUMBER: RO EU/1/11/707/001 - RO EU/1/11/707/011; DATE OF NATIONAL AUTHORISATION: 20110824; NUMBER OF FIRST AUTHORISATION IN EUROPEAN ECONOMIC AREA (EEA): EU/1/11/707/001 - EU/1/11/707/011; DATE OF FIRST AUTHORISATION IN EEA: 20110824

LINAGLIPTIN; METFORMIN HYDROCHLORIDE Market Analysis and Financial Projection Experimental

Market Dynamics and Financial Trajectory for Linagliptin and Metformin Hydrochloride

Introduction to Linagliptin and Metformin Hydrochloride

Linagliptin and metformin hydrochloride are two potent antidiabetic drugs often combined in a fixed-dose formulation to treat type 2 diabetes mellitus (T2DM). Linagliptin is a dipeptidyl peptidase-4 (DPP-4) inhibitor, while metformin is a biguanide that increases insulin sensitivity and decreases hepatic glucose production[1].

Mechanism of Action

Linagliptin

Linagliptin works by inhibiting the DPP-4 enzyme, which is responsible for the degradation of incretin hormones. These hormones play a crucial role in regulating glucose homeostasis. By inhibiting DPP-4, linagliptin increases the levels of incretin hormones, leading to improved glycemic control[1].

Metformin

Metformin enhances insulin sensitivity and reduces hepatic glucose production, thereby lowering blood glucose levels. It is one of the most widely prescribed oral antidiabetic medications due to its efficacy and safety profile[1].

Market Size and Growth

The market for linagliptin is experiencing significant growth, driven by several key factors:

Rising Incidence of Type 2 Diabetes

The global incidence of type 2 diabetes is increasing, which has led to a higher demand for effective oral hypoglycemic medications like linagliptin. This trend is expected to continue, driving market growth[3].

Combination Therapies

The use of combination therapies, such as linagliptin and metformin, is becoming more prevalent. This combination offers convenience for patients and is often more effective than monotherapy, contributing to the market's expansion[1][3].

Safety and Efficacy

Linagliptin's positive safety profile and efficacy make it a preferred choice among consumers and healthcare professionals. Clinical evidence supporting its advantages, including cardiovascular protection, further enhances its market attractiveness[3].

Expanding Healthcare Infrastructure

The growth of healthcare infrastructure in emerging nations is increasing access to these medications, thereby expanding the consumer base[3].

Financial Projections

Current Market Value

As of 2023, the linagliptin market was valued at USD 1.3 billion[3].

Future Projections

The market is expected to reach USD 3 billion by 2031, growing at a compound annual growth rate (CAGR) of 11.7% from 2024 to 2031. This robust growth is driven by the increasing demand for effective diabetes management and the expanding use of combination therapies[3].

Sales and Revenue Trends

Antidiabetic Drug Market

The overall antidiabetic drug market has seen significant growth, with new-generation drugs like linagliptin contributing substantially. For example, sales of other antidiabetic drugs, including those in combination with metformin, have shown steady growth over the years[4].

Specific Sales Data

While specific sales data for the linagliptin and metformin combination is not isolated, the sales of similar combination products, such as empagliflozin and metformin, provide insight into the market's potential. For instance, sales of empagliflozin and metformin combinations have increased significantly, reflecting the growing demand for such therapies[4].

Clinical Efficacy and Safety

Efficacy in Glycemic Control

Clinical trials have demonstrated the efficacy of the linagliptin and metformin combination in improving glycemic control. For example, a 24-week trial showed that the combination of linagliptin and metformin provided a numerically higher reduction in HbA1c compared to monotherapy with either drug[1].

Safety Profile

The combination has been shown to have a comparable safety profile to monotherapy, with adverse event rates similar across treatment groups. This includes a low incidence of hypoglycemic events, which is a significant advantage[1][5].

Market Dynamics

Consumer and Healthcare Professional Preferences

The convenience and efficacy of the linagliptin and metformin combination make it a preferred choice among both consumers and healthcare professionals. This preference is driven by the positive safety profile and the ease of use of the combination therapy[3].

Regulatory Approvals

The combination product has been approved in various regions, including the US, where it is marketed as an adjunct to diet and exercise to improve glycemic control in adults with T2DM. Regulatory approvals are crucial for market expansion and have facilitated the widespread adoption of this combination therapy[1].

Competitive Landscape

The antidiabetic drug market is highly competitive, with several new-generation drugs vying for market share. However, the linagliptin and metformin combination has carved out a significant niche due to its proven efficacy and safety. The market is also influenced by partnerships between drug manufacturers and medical professionals, which help in raising awareness and encouraging adherence to these medications[3].

Future Outlook

Innovative Research and Development

Innovative research and development efforts are expected to introduce new formulations and enhance the existing market. This includes potential new combinations and improved delivery systems, which will further bolster the market's growth[3].

Expanding Consumer Base

The consumer base for linagliptin and metformin is expected to expand due to rising healthcare costs and easier access to drugs in developing nations. This expansion will be driven by the growing awareness of diabetes management and the need for effective oral hypoglycemic medications[3].

Key Takeaways

• The linagliptin and metformin combination is a highly effective treatment for type 2 diabetes, offering improved glycemic control and a favorable safety profile.
• The market for linagliptin is expected to grow significantly, reaching USD 3 billion by 2031, driven by the rising incidence of type 2 diabetes and the increasing use of combination therapies.
• The combination's convenience, efficacy, and safety make it a preferred choice among consumers and healthcare professionals.
• Regulatory approvals and partnerships between drug manufacturers and medical professionals are key factors in the market's expansion.

FAQs

Q: What is the mechanism of action of linagliptin and metformin?

A: Linagliptin inhibits the DPP-4 enzyme, increasing incretin hormone levels, while metformin enhances insulin sensitivity and reduces hepatic glucose production.

Q: What are the key drivers of the linagliptin market growth?

A: The key drivers include the rising incidence of type 2 diabetes, the increasing use of combination therapies, and the positive safety and efficacy profile of linagliptin.

Q: What is the projected market value of linagliptin by 2031?

A: The linagliptin market is expected to reach USD 3 billion by 2031, growing at a CAGR of 11.7% from 2024 to 2031.

Q: How does the combination of linagliptin and metformin compare to monotherapy in terms of safety?

A: The combination has been shown to have a comparable safety profile to monotherapy, with adverse event rates similar across treatment groups.

Q: What role do regulatory approvals play in the market expansion of linagliptin and metformin?

A: Regulatory approvals are crucial for market expansion, facilitating the widespread adoption of this combination therapy.

Sources

1. FDA Clinical Pharmacology Review: "Linagliptin and Metformin Hydrochloride Fixed-Dose Combination Tablets" - accessdata.fda.gov
2. Diabetes Care Journal: "Empagliflozin as Add-on Therapy in Patients With Type 2 Diabetes" - diabetesjournals.org
3. Market Research Intellect: "Linagliptin Market Size and Forecast" - marketresearchintellect.com
4. Canada.ca: "Market Intelligence Report: Antidiabetic Drugs, 2012-2021" - canada.ca
5. Diabetes Care Journal: "Combination of Empagliflozin and Linagliptin as Second-Line Therapy" - diabetesjournals.org