LINZESS Drug Patent Profile

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

Linzess is a drug marketed by Abbvie and is included in one NDA. There are seven patents protecting this drug and two Paragraph IV challenges.

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

The generic ingredient in LINZESS is linaclotide. There are ten drug master file entries for this compound. One supplier is listed for this compound. Additional details are available on the linaclotide profile page.

DrugPatentWatch^® Generic Entry Outlook for Linzess

Linzess was eligible for patent challenges on August 30, 2016.

Annual sales in 2021 were $1.1bn, indicating a strong incentive for generic entry (peak sales were $1.5bn in 2020).

There have been eleven 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 is one tentative approval for the generic drug (linaclotide), which indicates the potential for near-term generic launch.

Indicators of Generic Entry

Summary for LINZESS

International Patents:	218
US Patents:	7
Applicants:	1
NDAs:	1
Finished Product Suppliers / Packagers:	1
Raw Ingredient (Bulk) Api Vendors:	21
Clinical Trials:	19
Patent Applications:	273
Drug Prices:	Drug price information for LINZESS
Drug Sales Revenues:	Drug sales revenues for LINZESS
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for LINZESS
What excipients (inactive ingredients) are in LINZESS?	LINZESS excipients list
DailyMed Link:	LINZESS at DailyMed

See drug prices for LINZESS

See drug sales revenues for LINZESS

Recent Clinical Trials for LINZESS

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

Sponsor	Phase
AbbVie	Phase 2
National Cancer Institute (NCI)	Early Phase 1
RenJi Hospital	Phase 4

See all LINZESS clinical trials

Pharmacology for LINZESS

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

Paragraph IV (Patent) Challenges for LINZESS

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 LINZESS

LINZESS is protected by fifteen US patents and one FDA Regulatory Exclusivity.

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	202811-003	Jan 25, 2017		RX	Yes	Yes	9,708,371		Y
Abbvie	LINZESS	linaclotide	CAPSULE;ORAL	202811-001	Aug 30, 2012		RX	Yes	Yes	8,802,628		Y
Abbvie	LINZESS	linaclotide	CAPSULE;ORAL	202811-003	Jan 25, 2017		RX	Yes	Yes	10,702,576
Abbvie	LINZESS	linaclotide	CAPSULE;ORAL	202811-001	Aug 30, 2012		RX	Yes	Yes	7,304,036		Y	Y
Abbvie	LINZESS	linaclotide	CAPSULE;ORAL	202811-002	Aug 30, 2012		RX	Yes	No	7,304,036		Y	Y
Abbvie	LINZESS	linaclotide	CAPSULE;ORAL	202811-001	Aug 30, 2012		RX	Yes	Yes
Abbvie	LINZESS	linaclotide	CAPSULE;ORAL	202811-002	Aug 30, 2012		RX	Yes	No	9,708,371		Y

Expired US Patents for LINZESS

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	Patent No.	Patent Expiration
Abbvie	LINZESS	linaclotide	CAPSULE;ORAL	202811-003	Jan 25, 2017	8,110,553
Abbvie	LINZESS	linaclotide	CAPSULE;ORAL	202811-003	Jan 25, 2017	7,745,409
Abbvie	LINZESS	linaclotide	CAPSULE;ORAL	202811-003	Jan 25, 2017	7,371,727
Abbvie	LINZESS	linaclotide	CAPSULE;ORAL	202811-003	Jan 25, 2017	8,080,526
Abbvie	LINZESS	linaclotide	CAPSULE;ORAL	202811-001	Aug 30, 2012	8,110,553
Abbvie	LINZESS	linaclotide	CAPSULE;ORAL	202811-002	Aug 30, 2012	8,080,526
Abbvie	LINZESS	linaclotide	CAPSULE;ORAL	202811-001	Aug 30, 2012	8,080,526

EU/EMA Drug Approvals for LINZESS

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 LINZESS

When does loss-of-exclusivity occur for LINZESS?

Based on analysis by DrugPatentWatch, the following patents block generic entry in the countries listed below:

Canada

China

Denmark

European Patent Office

Hungary

Japan

Mexico

Poland

Spain

Generics may enter earlier, or later, based on new patent filings, patent extensions, patent invalidation, early generic licensing, generic entry preferences, and other factors.

See the table below for additional patents covering LINZESS around the world.

Country	Patent Number	Title	Estimated Expiration
World Intellectual Property Organization (WIPO)	2013025969
France	13C0030
Singapore	153824	METHODS AND COMPOSITIONS FOR THE TREATMENT OF GASTROINTESTINAL DISORDERS
Peru	20110543	FORMULACION SOLIDA ORAL QUE COMPRENDE LINACLOTIDA, CATION DE CALCIO Y LEUCINA
Lithuania	2603232
Hungary	E032237
Japan	2010222377	METHOD AND COMPOSITION FOR THE TREATMENT OF GASTROINTESTINAL DISORDER

Supplementary Protection Certificates for LINZESS

Patent Number	Supplementary Protection Certificate	SPC Country	SPC Expiration	SPC Description
1594517	SPC/GB13/032	United Kingdom		PRODUCT NAME: LINACLOTIDE; REGISTERED: UK EU/1/12/801/001 20121128; UK EU/1/12/801/002 20121128; UK EU/1/12/801/003 20121128; UK EU/1/12/801/004 20121128
1594517	132013902159410	Italy		PRODUCT NAME: LINACLOTIDE(CONSTELLA); AUTHORISATION NUMBER(S) AND DATE(S): EU/1/12/801/001-2-3-4, 20121128
2246360	CA 2013 00027	Denmark		PRODUCT NAME: LINACLOTID OG ENHVER TERAPEUTISK AEKVIVALENT FORM DERAF SOM ER BESKYTTET AF GRUNDPATENTET, HERUNDER DE ACCEPTABLE SALTE DERAF, INKLUSIVE SALTENE AF LINACLOTID; REG. NO/DATE: EU/1/12/801/001-004 20121128
1594517	1390024-6	Sweden		PRODUCT NAME: LINAKLOTID; FIRST MARKETING AUTHORIZATION NUMBER SE: EG EU/1/12/801, 2012-11-28
1594517	PA2013013	Lithuania		PRODUCT NAME: LINACLOTIDUM; REGISTRATION NO/DATE: EU/1/12/801/001 - EU/1/12/801/004 20121126
1594517	PA2013013,C1594517	Lithuania		PRODUCT NAME: LINAKLOTIDAS; REGISTRATION NO/DATE: EU/1/12/801/001 - EU/1/12/801/004 20121126
1594517	2013C/032	Belgium		PRODUCT NAME: LINACLOTIDE; AUTHORISATION NUMBER AND DATE: EU/1/12/801/001 20121128

Market Dynamics and Financial Trajectory for LINZESS

Introduction to LINZESS

LINZESS, developed by Ironwood Pharmaceuticals and marketed in collaboration with AbbVie Inc., is a prescription medication primarily used to treat constipation-predominant irritable bowel syndrome (IBS-C) and chronic idiopathic constipation (CIC). Here, we delve into the market dynamics and financial trajectory of LINZESS, highlighting its performance, challenges, and future prospects.

Market Demand and Growth

LINZESS has consistently demonstrated robust prescription demand growth. In the third quarter of 2024, total LINZESS prescription demand increased by 13% year-over-year, reaching 54 million capsules. This growth is attributed to both extended units and new-to-brand prescriptions, each increasing by 13% compared to the same period in 2023[1].

Financial Performance

U.S. Net Sales

Despite the strong prescription demand, LINZESS U.S. net sales in the third quarter of 2024 were $225.5 million, a 19% decrease compared to $279.0 million in the third quarter of 2023. This decline is largely due to pricing headwinds and higher-than-expected Medicaid utilization trends[1].

Revenue and Profit Sharing

Ironwood Pharmaceuticals and AbbVie share equally in the profits from U.S. LINZESS sales. In the third quarter of 2024, Ironwood's share of the net profits from LINZESS sales was $88.9 million, down from $110.1 million in the third quarter of 2023. The commercial margin for LINZESS was 65% in Q3 2024, compared to 72% in Q3 2023[1].

Total Revenue and Adjusted EBITDA

For the full year 2024, Ironwood has revised its guidance due to changes in gross-to-net estimates. Total revenue is now expected to be between $350 million and $375 million, with adjusted EBITDA projected to be over $75 million. This is a revision from the previous guidance of $405 million to $425 million in total revenue and adjusted EBITDA of over $120 million[3].

Market Dynamics

Competitive Landscape

The IBS treatment market is competitive, with LINZESS facing competition from other drugs such as Amitiza (Sucampo/Takeda/Abbott), plecanatide (Synergy), and tenapanor (AstraZeneca/Ardelyx). Despite this competition, LINZESS is expected to remain a leading treatment due to increased physician experience and continued marketing efforts[4].

Global Market Potential

The global therapeutics market for IBS is projected to grow significantly, from $589.6 million in 2013 to $1.5 billion by 2023, driven by rising IBS prevalence and the increasing uptake of LINZESS in the U.S., five European countries, and Japan. LINZESS is anticipated to contribute the highest revenues among IBS treatments, with approximately $307.2 million across these regions by 2023[4].

Challenges and Pricing Headwinds

Pricing Pressure

LINZESS has faced significant pricing headwinds throughout 2024, primarily due to higher-than-expected Medicaid utilization trends. This has impacted the revenue and commercial margin of the drug, despite the robust prescription demand[1][3].

Gross-to-Net Changes

Ironwood has experienced a gross-to-net change in estimate related to the year ended December 31, 2023, which has resulted in a reduction of collaborative arrangements revenue. This adjustment has influenced the company's revised financial guidance for 2024[2][3].

Pipeline and Future Prospects

Apraglutide

Beyond LINZESS, Ironwood is making progress with apraglutide, a drug in development for the treatment of short bowel syndrome. The company is on track to complete the New Drug Application (NDA) submission in the first quarter of 2025. Apraglutide is expected to be a significant addition to Ironwood's portfolio, potentially becoming the drug of choice for physicians treating adult patients with short bowel syndrome who are dependent on parenteral support[1].

Other Pipeline Candidates

Ironwood is also advancing other pipeline candidates, including CNP-104 and IW-3300. These developments are part of the company's strategic priorities to diversify its product portfolio and ensure long-term growth[3].

Financial Guidance and Outlook

Revised Guidance

Due to the pricing headwinds and gross-to-net changes, Ironwood has revised its 2024 financial guidance. The company now expects U.S. LINZESS net sales to be between $900 million and $950 million, with total revenue ranging from $350 million to $375 million. Adjusted EBITDA is projected to be over $75 million[3].

Cash Flow and Capital Structure

Despite the challenges, Ironwood maintains a strong cash flow generation from LINZESS and a supportive capital structure. This positions the company well to execute its strategic priorities, including the development and potential launch of new products like apraglutide[3].

Key Takeaways

• Robust Prescription Demand: LINZESS continues to see strong prescription demand growth, with a 13% increase in Q3 2024.
• Pricing Headwinds: Despite demand growth, LINZESS faces significant pricing pressure, impacting revenue and commercial margin.
• Competitive Market: The IBS treatment market is competitive, but LINZESS remains a leading treatment due to physician experience and marketing efforts.
• Global Market Potential: The global IBS therapeutics market is projected to grow substantially, with LINZESS expected to contribute significantly.
• Pipeline Developments: Ironwood is advancing apraglutide and other pipeline candidates to diversify its portfolio and ensure long-term growth.
• Revised Financial Guidance: Ironwood has revised its 2024 financial guidance due to pricing headwinds and gross-to-net changes.

FAQs

What is LINZESS used for?

LINZESS is a prescription medication used to treat constipation-predominant irritable bowel syndrome (IBS-C) and chronic idiopathic constipation (CIC).

How has LINZESS performed in terms of prescription demand?

LINZESS has shown robust prescription demand growth, with a 13% increase in the third quarter of 2024 compared to the same period in 2023.

What are the main challenges facing LINZESS?

LINZESS faces significant pricing headwinds and higher-than-expected Medicaid utilization trends, which have impacted its revenue and commercial margin.

What is the projected global market size for IBS treatments by 2023?

The global therapeutics market for IBS is projected to reach $1.5 billion by 2023, with LINZESS anticipated to contribute the highest revenues among IBS treatments[4].

What is apraglutide, and what is its potential impact on Ironwood's portfolio?

Apraglutide is a drug in development for the treatment of short bowel syndrome. If approved, it is expected to become a significant addition to Ironwood's portfolio and potentially the drug of choice for physicians treating adult patients with short bowel syndrome who are dependent on parenteral support[1].

Sources

1. Ironwood Pharmaceuticals Reports Third Quarter 2024 Results - Biospace
2. Ironwood Pharmaceuticals Q1 2024 Earnings Slides - Ironwood Pharmaceuticals
3. Ironwood Pharmaceuticals Reports Second Quarter 2024 Results - Ironwood Pharmaceuticals
4. Treatment Market for Irritable Bowel Syndrome Could Hit $1.5 Billion - Drug Development
5. Ironwood Pharmaceuticals Reports Fourth Quarter and Full Year 2023 Results - Ironwood Pharmaceuticals