Linaclotide - Generic Drug Details

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

Linaclotide is the generic ingredient in two branded drugs marketed by Aurobindo Pharma, Mylan, and Abbvie, and is included in three NDAs. There are seven patents protecting this compound and one Paragraph IV challenge. Additional information is available in the individual branded drug profile pages.

Linaclotide has two hundred and eighteen patent family members in forty-five countries.

There are ten drug master file entries for linaclotide. One supplier is listed for this compound. There is one tentative approval for this compound.

Summary for linaclotide

International Patents:	218
US Patents:	7
Tradenames:	2
Applicants:	3
NDAs:	3
Drug Master File Entries:	10
Finished Product Suppliers / Packagers:	1
Raw Ingredient (Bulk) Api Vendors:	43
Clinical Trials:	44
Patent Applications:	777
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for linaclotide
What excipients (inactive ingredients) are in linaclotide?	linaclotide excipients list
DailyMed Link:	linaclotide at DailyMed

Recent Clinical Trials for linaclotide

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

Sponsor	Phase
Jinling Hospital, China	N/A
AbbVie	Phase 2
AbbVie	Phase 3

See all linaclotide clinical trials

Generic filers with tentative approvals for LINACLOTIDE

Applicant	Application No.	Strength	Dosage Form
		72MCG	CAPSULE;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 linaclotide

Drug Class	Guanylate Cyclase-C Agonist
Mechanism of Action	Guanylate Cyclase Activators

Anatomical Therapeutic Chemical (ATC) Classes for linaclotide

A06AX	Other drugs for constipation
A06A	DRUGS FOR CONSTIPATION
A06	DRUGS FOR CONSTIPATION
A	Alimentary tract and metabolism

Paragraph IV (Patent) Challenges for LINACLOTIDE

Tradename	Dosage	Ingredient	Strength	NDA	ANDAs Submitted	Submissiondate
LINZESS	Capsules	linaclotide	72 mcg	202811	1	2017-11-07
LINZESS	Capsules	linaclotide	145 mcg and 290 mcg	202811	4	2016-08-30

US Patents and Regulatory Information for linaclotide

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Exclusivity Expiration
Abbvie	LINZESS	linaclotide	CAPSULE;ORAL	202811-002	Aug 30, 2012		RX	Yes	No
Abbvie	LINZESS	linaclotide	CAPSULE;ORAL	202811-002	Aug 30, 2012		RX	Yes	No			Y
Mylan	LINACLOTIDE	linaclotide	CAPSULE;ORAL	209564-001	Feb 9, 2021		DISCN	No	No
Abbvie	LINZESS	linaclotide	CAPSULE;ORAL	202811-003	Jan 25, 2017		RX	Yes	Yes			Y
Abbvie	LINZESS	linaclotide	CAPSULE;ORAL	202811-003	Jan 25, 2017		RX	Yes	Yes
Aurobindo Pharma	LINACLOTIDE	linaclotide	CAPSULE;ORAL	209611-001	Feb 7, 2023		DISCN	No	No
Abbvie	LINZESS	linaclotide	CAPSULE;ORAL	202811-003	Jan 25, 2017		RX	Yes	Yes			Y	Y

Expired US Patents for linaclotide

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	Patent No.	Patent Expiration
Abbvie	LINZESS	linaclotide	CAPSULE;ORAL	202811-001	Aug 30, 2012
Abbvie	LINZESS	linaclotide	CAPSULE;ORAL	202811-002	Aug 30, 2012
Abbvie	LINZESS	linaclotide	CAPSULE;ORAL	202811-003	Jan 25, 2017
Abbvie	LINZESS	linaclotide	CAPSULE;ORAL	202811-003	Jan 25, 2017
Abbvie	LINZESS	linaclotide	CAPSULE;ORAL	202811-001	Aug 30, 2012
Abbvie	LINZESS	linaclotide	CAPSULE;ORAL	202811-001	Aug 30, 2012
Abbvie	LINZESS	linaclotide	CAPSULE;ORAL	202811-001	Aug 30, 2012

EU/EMA Drug Approvals for linaclotide

Company	Drugname	Inn	Product Number / Indication	Status	Generic	Biosimilar	Orphan	Marketing Authorisation	Marketing Refusal
AbbVie Deutschland GmbH & Co. KG	Constella	linaclotide	EMEA/H/C/002490 Constella is indicated for the symptomatic treatment of moderate to severe irritable-bowel syndrome with constipation (IBS-C) in adults.	Authorised	no	no	no	2012-11-26

International Patents for linaclotide

Country	Patent Number	Title	Estimated Expiration
Eurasian Patent Organization	201290799	ЛЕЧЕНИЕ ЖЕЛУДОЧНО-КИШЕЧНЫХ РАССТРОЙСТВ
Israel	211028	תכשירים רוקחיים מוצקים המכילים לינקלוטידין, קטיון ואמין ראשוני בעל הפרעה סטרית ושימושם להכנת תרופה לטיפול במחלות במערכת העיכול (Solid pharmaceutical compositions comprising linaclotide, a cation and a sterically hindered primary amine and use thereof in the preparation of medicaments for treating gastrointestinal disorders)
South Africa	200607433	Methods and compositions for the treatment of gastroin-testinal disorders
South Korea	20230025926	경구 투여를 위한 리나클로타이드-함유 제형 (- LINACLOTIDE-CONTAINING FORMULATIONS FOR ORAL ADMINISTRATION)
World Intellectual Property Organization (WIPO)	2012021715
Russian Federation	2433133	ПОЛИПЕПТИД ДЛЯ УВЕЛИЧЕНИЯ АКТИВНОСТИ РЕЦЕПТОРА ГУАНИЛАТЦИКЛАЗЫ, ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ, СПОСОБ ЛЕЧЕНИЯ ЖЕЛУДОЧНО-КИШЕЧНОГО РАССТРОЙСТВА У ПАЦИЕНТА, СПОСОБ ПОВЫШЕНИЯ АКТИВНОСТИ РЕЦЕПТОРА ГУАНИЛАТЦИКЛАЗЫ У ПАЦИЕНТА, СПОСОБ ЛЕЧЕНИЯ ВИСЦЕРАЛЬНОЙ БОЛИ, СПОСОБ ПОЛУЧЕНИЯ ПОЛИПЕПТИДА (ВАРИАНТЫ), ИЗОЛИРОВАННАЯ МОЛЕКУЛА НУКЛЕИНОВОЙ КИСЛОТЫ, БАКТЕРИАЛЬНЫЙ ВЕКТОР ЭКСПРЕССИИ И ИЗОЛИРОВАННАЯ БАКТЕРИАЛЬНАЯ КЛЕТКА (POLYPEPTIDE FOR INCREASING GUANYLATE CYCLASE RECEPTOR ACTIVITY, PHARMACEUTICAL COMPOSITION, METHOD OF TREATING GASTROINTESTINAL DISORDER IN PATIENT, METHOD OF INCREASING GUANYLATE CYCLASE RECEPTOR ACTIVITY IN PATIENT, METHOD OF TREATING VISCERAL PAIN, METHOD OF OBTAINING POLYPEPTIDE (VERSIONS), ISOLATED NUCLEIC ACID MOLECULE, BACTERIAL EXPRESSION VECTOR AND ISOLATED BACTERIAL CELL)
Luxembourg	92201

Supplementary Protection Certificates for linaclotide

Patent Number	Supplementary Protection Certificate	SPC Country	SPC Expiration	SPC Description
1594517	C20130011 00400	Estonia		PRODUCT NAME: LINAKLOTIID;REG NO/DATE: K(2012)8832 (LOPLIK) 28.11.2012
1594517	122013000044	Germany		PRODUCT NAME: LINACLOTID, EINSCHLIESSLICH DESSEN PHARMAZEUTISCH VERTRAEGLICHE SALZE; REGISTRATION NO/DATE: EU/1/12/801/001-004 20121126
1594517	CR 2013 00026	Denmark		PRODUCT NAME: LINACLOTID OG FARMACEUTISKE ACCEPTABLE SALTE DERAF; REG. NO/DATE: EU/1/12/801/001-004 20121128
1594517	466	Finland
1594517	CA 2013 00026	Denmark
1594517	92200	Luxembourg		PRODUCT NAME: LINACLOTIDE ET TOUTE FORME THERAPEUTIQUE EQUIVALENTE DE CELUI-CI, PROTEGE PAR LE BREVET DE BASE, Y COMPRIS DES SELS PHARMACEUTIQUEMENT ACCEPTABLES; AUTHORISATION NUMBER AND DATE: EU/1/12/801/001-004 20121126
1594517	2013C/032	Belgium		PRODUCT NAME: LINACLOTIDE; AUTHORISATION NUMBER AND DATE: EU/1/12/801/001 20121128

Market Dynamics and Financial Trajectory for Linaclotide

Overview of Linaclotide

Linaclotide, marketed under the brand name LINZESS in the U.S. and CONSTELLA in Europe, is a groundbreaking medication in the class of guanylate cyclase-C (GC-C) agonists. It is primarily used to treat irritable bowel syndrome with constipation (IBS-C) and chronic idiopathic constipation (CIC)[3][4].

Market Size and Growth

As of 2024, the global linaclotide market is estimated to be USD 1425.2 million. This market is projected to expand at a compound annual growth rate (CAGR) of 7.60% from 2024 to 2031, reaching USD 2379.91 million by the end of the forecast period[1].

Regional Market Dynamics

North America

North America dominates the linaclotide market, accounting for more than 40% of the global revenue with a market size of USD 570.08 million in 2024. This region is expected to grow at a CAGR of 5.8% from 2024 to 2031. The high prevalence of IBS-C and CIC, along with advanced healthcare infrastructure, contributes to this dominance[1][3].

Europe

Europe holds around 30% of the global revenue, with a market size of USD 427.56 million in 2024. The European market is anticipated to grow at a CAGR of 6.1% from 2024 to 2031. The presence of major market players and the increasing awareness of gastrointestinal disorders drive this growth[1].

Asia-Pacific

The Asia-Pacific region accounts for approximately 23% of the global revenue, with a market size of USD 327.80 million in 2024. This region is expected to experience the highest CAGR of 9.6% from 2024 to 2031, driven by rising awareness of gastrointestinal disorders and improving healthcare infrastructure[1].

Latin America and Middle East & Africa

Latin America and the Middle East & Africa hold smaller market shares, with 5% and 2% of the global revenue, respectively. These regions are expected to grow at CAGRs of 7.0% and 7.3% from 2024 to 2031[1].

Financial Performance of Ironwood Pharmaceuticals

Ironwood Pharmaceuticals, the developer of linaclotide, has seen significant financial success with LINZESS. In 2021, LINZESS achieved blockbuster status with U.S. net sales exceeding $1 billion. The total revenue for Ironwood Pharmaceuticals in 2021 was $413.753 million, primarily driven by $400 million in U.S. LINZESS collaboration revenue[4].

Revenue Breakdown

• U.S. LINZESS Net Sales: $1,005,856,000 in 2021, up from $931,211,000 in 2020.
• Net Profit on LINZESS Sales: $701,321,000 in 2021, compared to $619,091,000 in 2020.
• Cash from Operations: $261.9 million in 2021, an increase from $168.8 million in 2020[4].

Future Outlook

Ironwood Pharmaceuticals is expected to continue its revenue growth, with projected total revenues between $420 to $430 million in 2022 and adjusted EBITDA exceeding $250 million. The company is also focusing on expanding its gastrointestinal (GI) pipeline, including new treatments for visceral pain conditions and primary biliary cholangitis (PBC)[4].

Market Drivers

Increasing Prevalence of Gastrointestinal Disorders

The rising prevalence of IBS-C and CIC is a significant driver for the linaclotide market. Modern dietary habits and lifestyle changes have contributed to an increase in gastrointestinal disorders, thereby boosting the demand for effective treatments like linaclotide[3].

Advanced Healthcare Infrastructure

Regions with advanced healthcare infrastructure, such as North America and Europe, are seeing higher adoption rates of linaclotide due to better diagnostic capabilities and treatment options[1][3].

R&D Activities

Continuous research and development activities in the healthcare sector, particularly in the GI space, are driving innovation and expanding the market for linaclotide. New clinical studies and pipeline developments by companies like Ironwood Pharmaceuticals further enhance market growth[4].

Market Challenges

Competition

While linaclotide is a first-in-class medication, the IBS-C drug market is competitive, with other treatments available. However, its unique mechanism of action as a GC-C agonist gives it a competitive edge[3].

Regulatory Environment

Changes in regulatory environments and healthcare policies can impact the market dynamics. However, the strong approval and market presence of linaclotide in various regions mitigate these risks to some extent[1].

Key Takeaways

• The global linaclotide market is projected to grow significantly, driven by the increasing prevalence of IBS-C and CIC.
• North America and Europe are the dominant regions, with Asia-Pacific expected to show the highest growth rate.
• Ironwood Pharmaceuticals has achieved substantial financial success with LINZESS, and the company is focused on expanding its GI pipeline.
• Advanced healthcare infrastructure and ongoing R&D activities are key drivers of the market.

FAQs

What is linaclotide used for?

Linaclotide is used for the treatment of irritable bowel syndrome with constipation (IBS-C) and chronic idiopathic constipation (CIC)[3].

Which company developed linaclotide?

Linaclotide was developed by Ironwood Pharmaceuticals and is marketed under the brand name LINZESS in the U.S. and CONSTELLA in Europe[4].

What is the projected market size of linaclotide by 2031?

The global linaclotide market is expected to reach USD 2379.91 million by 2031, growing at a CAGR of 7.60% from 2024 to 2031[1].

Which region has the highest CAGR for linaclotide?

The Asia-Pacific region is expected to have the highest CAGR of 9.6% from 2024 to 2031[1].

What were the U.S. net sales of LINZESS in 2021?

The U.S. net sales of LINZESS exceeded $1 billion in 2021[4].

Sources

1. Cognitive Market Research: Global Linaclotide Market Report 2024.
2. Fierce Biotech: Ironwood Pharmaceuticals Announces Alignment of Workforce with Priority Growth Platforms.
3. Stratview Research: IBS-C Drug Market Growth, Trends & Forecast Analysis | 2026.
4. Ironwood Pharmaceuticals: Fourth Quarter and Full Year 2021 Results.
5. Market Research Intellect: Global Linaclotide API Market Size, Scope And Forecast Report.

Last updated: 2024-12-16