TRACLEER Drug Patent Profile

Which patents cover Tracleer, and when can generic versions of Tracleer launch?

Tracleer is a drug marketed by Actelion and is included in two NDAs. There are two patents protecting this drug and one Paragraph IV challenge.

This drug has twenty-eight patent family members in twenty-three countries.

The generic ingredient in TRACLEER is bosentan. There are nineteen drug master file entries for this compound. Six suppliers are listed for this compound. Additional details are available on the bosentan profile page.

DrugPatentWatch^® Litigation and Generic Entry Outlook for Tracleer

A generic version of TRACLEER was approved as bosentan by SUN PHARM on April 26^th, 2019.

Summary for TRACLEER

International Patents:	28
US Patents:	2
Applicants:	1
NDAs:	2
Finished Product Suppliers / Packagers:	1
Raw Ingredient (Bulk) Api Vendors:	85
Clinical Trials:	44
Patent Applications:	5,801
Drug Prices:	Drug price information for TRACLEER
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for TRACLEER
What excipients (inactive ingredients) are in TRACLEER?	TRACLEER excipients list
DailyMed Link:	TRACLEER at DailyMed

See drug prices for TRACLEER

Recent Clinical Trials for TRACLEER

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

Sponsor	Phase
Humanis Saglık Anonim Sirketi	PHASE1
City of Hope Medical Center	Phase 1
National Cancer Institute (NCI)	Phase 1

See all TRACLEER clinical trials

Pharmacology for TRACLEER

Drug Class	Endothelin Receptor Antagonist
Mechanism of Action	Cytochrome P450 2C9 Inducers Cytochrome P450 3A Inducers Endothelin Receptor Antagonists

Paragraph IV (Patent) Challenges for TRACLEER

Tradename	Dosage	Ingredient	Strength	NDA	ANDAs Submitted	Submissiondate
TRACLEER	for Oral Suspension	bosentan	32 mg	209279	1	2019-02-08

US Patents and Regulatory Information for TRACLEER

TRACLEER is protected by two US patents.

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Exclusivity Expiration
Actelion	TRACLEER	bosentan	TABLET, FOR SUSPENSION;ORAL	209279-001	Sep 5, 2017	AB	RX	Yes	Yes			Y
Actelion	TRACLEER	bosentan	TABLET;ORAL	021290-002	Nov 20, 2001	AB	RX	Yes	Yes
Actelion	TRACLEER	bosentan	TABLET, FOR SUSPENSION;ORAL	209279-001	Sep 5, 2017	AB	RX	Yes	Yes			Y
Actelion	TRACLEER	bosentan	TABLET;ORAL	021290-001	Nov 20, 2001	AB	RX	Yes	No

Expired US Patents for TRACLEER

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	Patent No.	Patent Expiration
Actelion	TRACLEER	bosentan	TABLET;ORAL	021290-001	Nov 20, 2001
Actelion	TRACLEER	bosentan	TABLET;ORAL	021290-002	Nov 20, 2001

EU/EMA Drug Approvals for TRACLEER

Company	Drugname	Inn	Product Number / Indication	Status	Generic	Biosimilar	Orphan	Marketing Authorisation	Marketing Refusal
Janssen-Cilag International N.V.	Tracleer	bosentan	EMEA/H/C/000401Treatment of pulmonary arterial hypertension (PAH) to improve exercise capacity and symptoms in patients with WHO functional class III.Efficacy has been shown in:, , , Primary (idiopathic and familial) PAH;, PAH secondary to scleroderma without significant interstitial pulmonary disease;, PAH associated with congenital systemic-to-pulmonary shunts and Eisenmenger's physiology., , , Some improvements have also been shown in patients with PAH WHO functional class II., , Tracleer is also indicated to reduce the number of new digital ulcers in patients with systemic sclerosis and ongoing digital ulcer disease.,	Authorised	no	no	no	2002-05-14

International Patents for TRACLEER

When does loss-of-exclusivity occur for TRACLEER?

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

Canada

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 TRACLEER around the world.

Country	Patent Number	Title	Estimated Expiration
Russian Federation	2086544	BENZENESULFONAMIDE DERIVATIVES OF PYRIMIDINE OR THEIR SALTS, PHARMACEUTICAL COMPOSITION FOR TREATMENT OF DISEASES ASSOCIATED WITH ENDOTHELIN ACTIVITY
South Africa	9204126
Israel	187383	DISPERSIBLE BOSERTAN TABLET
Hungary	T63152
Japan	4219399
Mexico	9202747	NUEVAS SULFONAMIDAS Y PROCEDIMIENTOS PARA SU PREPARACION.
Austria	197044

Supplementary Protection Certificates for TRACLEER

Patent Number	Supplementary Protection Certificate	SPC Country	SPC Expiration	SPC Description
0526708	300097	Netherlands
0526708	C300097	Netherlands		PRODUCT NAME: BOSENTAN, DESGEWENST IN DE VORM VAN EEN ZOUT OF EEN HYDRAAT OF IN DE VORM VAN EEN ESTER VAN DE HYDROXYLGROEP VAN DE 2-HYDROXYETHOXY REST MET EEN ZUUR MET DE FORMULE R5-OH, WAARIN R5 EEN C1-7-ALKANOYL, BENZOYL, OF HETEROCYCLYCARBONYL VOORSTELT; NATL. REGISTRATION NO/DATE: U/1/02/220/001 - 005 20020515; FIRST REGISTRATION: CH IKS 58841 01 - 02 20020228
0526708	02C0042	France		PRODUCT NAME: BOSENTAN MONOHYDRATE; NAT. REGISTRATION NO/DATE: EU/1/02/220/001 20020515; FIRST REGISTRATION: LI - 55841 20020228
0526708	SPC/GB02/030	United Kingdom		PRODUCT NAME: BOSENTAN 4-(1,1-DIMETHYLETHYL)-N-(6-(2-HYDROXYETHOXY)-5-(2-METHOXYPHENOXY)-2(PYRIMIDIN-2-YL)PYRIMIDIN-4-YL)BENZENESULFONAMIDE AND ITS PHARMACEUTICALLY ACCEPTABLE SALTS
0526708	0290017-3	Sweden		PRODUCT NAME: BOSENTAN ELLER ETT SALT DAERAV; NAT. REGISTZRATION NO/DATE: EU/1/02/220/001 20020515; FIRST REGISTRATION: CH 55841 01 20020228
0526708	CA 2002 00026	Denmark

Market Dynamics and Financial Trajectory for TRACLEER (Bosentan)

Last updated: July 27, 2025

Introduction

TRACLEER (bosentan) stands as a pioneering oral endothelin receptor antagonist (ERA) primarily approved for the treatment of pulmonary arterial hypertension (PAH). Since its initial approval by the U.S. Food and Drug Administration (FDA) in 2001, TRACLEER has influenced treatment paradigms for PAH and set a benchmark in targeted pulmonary therapies. This report delineates the evolving market dynamics and financial trajectory of TRACLEER, considering recent developments, regulatory shifts, competitive landscape, and the broader implications of pulmonary hypertension management.

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Market Overview and Historical Context

Therapeutic Significance of TRACLEER

PAH—a progressive condition characterized by increased pulmonary vascular resistance—poses significant morbidity and mortality risks. TRACLEER’s mechanism involves antagonizing endothelin-1, a potent vasoconstrictor and mitogen implicated in PAH pathogenesis. Its oral administration convenience positioned it as a preferred therapy among ERA drugs, alongside others such as ambrisentan and macitentan.

Initial Market Entry and Adoption

TRACLEER’s approval in 2001 marked a critical advancement. Early adoption correlated with expanded indications, including treatment for systemic sclerosis-associated PAH, thus broadening its market base. Its efficacy in improving exercise capacity, hemodynamics, and delaying clinical worsening fostered strong clinician confidence, enabling robust sales in established markets like the U.S., Europe, and Japan.

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Market Dynamics

Regulatory Environment and Safety Concerns

Despite its efficacy, TRACLEER’s market faced hurdles due to safety alerts over hepatotoxicity, including the need for regular liver function monitoring—a requisite that impacts prescribing patterns and patient compliance. These safety considerations led to navigating risks versus benefits, influencing market penetration and pricing strategies.

Patent Landscape and Generic Competition

TRACLEER’s patent life—originally expiring around 2017—saw subsequent patent extensions and market exclusivity hurdles. The entry of generics has exerted pressure on pricing, profit margins, and market share, although the product’s clinical positioning sustains demand, especially in specific PAH subpopulations.

Competitive Landscape

Today, TRACLEER competes with newer ERAs such as macitentan (Opsumit) and ambrisentan (Letairis). These agents claim improved safety profiles, simplified dosing, and less monitoring, challenging TRACLEER’s market share. Nonetheless, TRACLEER retains a niche for refractory cases or patients unresponsive to alternative therapies.

Reimbursement and Market Access

Reimbursement policies significantly influence TRACLEER’s financial trajectory. Cost considerations, monitored liver side effects, and adoption incentives from payers directly impact prescribing behaviors, with price negotiations and formulary placements influencing overall revenue.

Emerging Therapeutic Developments

The pipeline for PAH includes drugs targeting novel pathways such as prostacyclin mimetics and soluble guanylate cyclase stimulators. While these innovations may threaten TRACLEER’s market share, combination therapies and personalized medicine approaches could sustain or enhance its revenue streams through specialized indications.

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Financial Trajectory and Revenue Trends

Global Sales Performance

Historically, TRACLEER achieved peak annual sales exceeding $1 billion globally in the early 2010s, driven by extensive indications and strong clinical data. However, sales have since plateaued or slightly declined, influenced by generic penetration and market saturation.

Impact of Generics and Market Skepticism

Post-patent expiring in developed markets, generic versions eroded sales margins. While these generics increased accessibility, they also introduced price competition, attenuating revenue growth. Furthermore, safety concerns and monitoring requirements marginally constrained prescribing, especially in outpatient settings.

Profitability and Cost Management

Despite potential revenue erosion, TRACLEER remains financially significant for its manufacturer, Bayer. Cost management initiatives, market expansion efforts into emerging markets, and strategic repositioning aim to optimize profitability amidst increasing competition and patent expiration risks.

Emerging Licensing and Strategic Alliances

Recent licensing agreements, particularly in developing regions, facilitate broader access, potentially stabilizing revenue streams. Moreover, Bayer’s focus on research and development endeavors for combination therapies sustains longer-term financial viability.

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Market Outlook and Future Perspectives

Growth Drivers

• Unmet Clinical Needs: Patients with PAH refractory to existing therapies represent a niche where TRACLEER’s efficacy remains invaluable.
• Expanded Indications: Potential approval for additional conditions, such as other forms of pulmonary hypertension or systemic sclerosis-related complications, could reverse sales decline trends.
• Global Market Expansion: Emerging markets offer demographic and epidemiological opportunities, provided reimbursement and safety monitoring complexities are managed.

Challenges to Sustain Trajectory

• Safety and Monitoring Burdens: Liver toxicity concerns necessitate ongoing surveillance, limiting convenience and patient adherence.
• Competitive Alternatives: Novel drugs with better safety profiles, simplified dosing, or superior efficacy threaten TRACLEER’s market share.
• Pricing Pressures: Healthcare cost containment measures worldwide pressure drug prices, reducing revenue potential.

Innovation and Strategic Positioning

Continued innovation—such as combination therapies, personalized medicine approaches, or delivery system enhancements—may sustain TRACLEER’s relevance. Emphasizing safety profile improvements or exploring new indications could bolster its market standing.

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Key Takeaways

• Market Positioning: Despite initial dominance, TRACLEER faces significant competition from newer ERAs and generic versions, with clinical safety considerations influencing prescribing patterns.
• Revenue Trends: Peak revenues have plateaued or declined due to patent expirations, market saturation, and safety monitoring requirements, although strategic access expansion could mitigate declines.
• Regulatory and Safety Landscape: Liver toxicity and monitoring protocols remain central to its market viability, necessitating effective risk management strategies.
• Competitive Dynamics: Newly approved and pipeline drugs threaten its market share, emphasizing the need for differentiation through improved safety, efficacy, or indications.
• Future Outlook: Growth potential persists in niche populations, emerging markets, and potential label expansions, but long-term sustainability will depend on innovation and strategic repositioning.

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FAQs

1. How does TRACLEER compare to other therapies for pulmonary arterial hypertension?
TRACLEER is notable for its oral administration and efficacy in improving PAH symptoms. However, it’s associated with hepatotoxicity, requiring liver monitoring. Newer ERAs like macitentan and ambrisentan offer improved safety profiles and dosing convenience, influencing prescribing choices.

2. What are the primary safety concerns associated with TRACLEER?
Hepatotoxicity is the most significant concern, mandating regular liver function testing. Rare cases of severe liver injury led to black box warnings and caution in patient monitoring.

3. How have patent expirations affected TRACLEER's market share?
Patent expirations introduced generic competition, reducing prices and revenues. While generics increased accessibility, they also diminished Bayer’s profitability, prompting strategic adjustments.

4. Is TRACLEER being developed for new indications?
Currently, its main approved indication remains PAH. However, ongoing research explores its role in systemic sclerosis-related complications and other vascular disorders, which could broaden its clinical utility.

5. What strategic measures are Bayer implementing to sustain TRACLEER’s market relevance?
Bayer focuses on expanding access in emerging markets, exploring new indications, and optimizing combination therapy formulas. Maintaining safety profiles and educating clinicians about patient monitoring also underpin ongoing strategies.

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References

[1] Food and Drug Administration (FDA). TRACLEER (bosentan) prescribing information. 2001.
[2] Simonneau G, et al. "Update on Pulmonary Arterial Hypertension Management." Circulation Research, 2019.
[3] Bayer Healthcare. "TRACLEER (Bosentan) Product Overview." 2022.
[4] MarketWatch. “Pulmonary Arterial Hypertension Drug Market Trends.” 2023.
[5] GlobalData. “Pharmaceutical Market Analysis: PAH Therapies.” 2022.