MACITENTAN - Generic Drug Details

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

Macitentan is the generic ingredient in three branded drugs marketed by Alembic, Apotex, Aurobindo Pharma Ltd, Laurus, MSN, Sun Pharm, Torrent, Zydus Lifesciences, and Actelion, and is included in ten NDAs. There are five patents protecting this compound and one Paragraph IV challenge. Additional information is available in the individual branded drug profile pages.

Macitentan has ninety-nine patent family members in thirty-four countries.

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

Summary for MACITENTAN

International Patents:	99
US Patents:	5
Tradenames:	3
Applicants:	9
NDAs:	10
Drug Master File Entries:	10
Finished Product Suppliers / Packagers:	1
Raw Ingredient (Bulk) Api Vendors:	75
Clinical Trials:	61
Patent Applications:	1,716
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for MACITENTAN
What excipients (inactive ingredients) are in MACITENTAN?	MACITENTAN excipients list
DailyMed Link:	MACITENTAN at DailyMed

Recent Clinical Trials for MACITENTAN

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

Sponsor	Phase
Gachon University Gil Medical Center	PHASE4
China-Japan Friendship Hospital	EARLY_PHASE1
Humanis Saglık Anonim Sirketi	PHASE1

See all MACITENTAN clinical trials

Generic filers with tentative approvals for MACITENTAN

Applicant	Application No.	Strength	Dosage Form
		10MG	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 MACITENTAN

Drug Class	Endothelin Receptor Antagonist
Mechanism of Action	Endothelin Receptor Antagonists

Anatomical Therapeutic Chemical (ATC) Classes for MACITENTAN

C02KX	Antihypertensives for pulmonary arterial hypertension
C02K	OTHER ANTIHYPERTENSIVES
C02	ANTIHYPERTENSIVES
C	Cardiovascular system

Paragraph IV (Patent) Challenges for MACITENTAN

Tradename	Dosage	Ingredient	Strength	NDA	ANDAs Submitted	Submissiondate
OPSUMIT	Tablets	macitentan	10 mg	204410	11	2017-10-18

US Patents and Regulatory Information for MACITENTAN

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Exclusivity Expiration
Zydus Lifesciences	MACITENTAN	macitentan	TABLET;ORAL	211224-001	Apr 6, 2021		DISCN	No	No
Actelion	OPSUMIT	macitentan	TABLET;ORAL	204410-001	Oct 18, 2013	AB	RX	Yes	Yes	8,268,847*PED				Y
Torrent	MACITENTAN	macitentan	TABLET;ORAL	211107-001	Aug 5, 2024		DISCN	No	No
Sun Pharm	MACITENTAN	macitentan	TABLET;ORAL	211123-001	Aug 26, 2025	AB	RX	No	No
Actelion	OPSUMIT	macitentan	TABLET;ORAL	204410-001	Oct 18, 2013	AB	RX	Yes	Yes	7,094,781*PED				Y
Msn	MACITENTAN	macitentan	TABLET;ORAL	211136-001	Aug 20, 2025	AB	RX	No	No

EU/EMA Drug Approvals for MACITENTAN

Company	Drugname	Inn	Product Number / Indication	Status	Generic	Biosimilar	Orphan	Marketing Authorisation	Marketing Refusal
Janssen-Cilag International N.V.	Opsumit	macitentan	EMEA/H/C/002697Opsumit, as monotherapy or in combination, is indicated for the long-term treatment of pulmonary arterial hypertension (PAH) in adult patients of WHO Functional Class (FC) II to III.Efficacy has been shown in a PAH population including idiopathic and heritable PAH, PAH associated with connective tissue disorders, and PAH associated with corrected simple congenital heart disease.	Authorised	no	no	yes	2013-12-20

International Patents for MACITENTAN

Country	Patent Number	Title	Estimated Expiration
Russian Federation	2424805	СТАБИЛЬНЫЕ ФАРМАЦЕВТИЧЕСКИЕ КОМПОЗИЦИИ, ВКЛЮЧАЮЩИЕ ПИРИМИДИНСУЛЬФАМИД (STABLE PHARMACEUTICAL PYRIMIDINSULFAMIDE-INCLUDING COMPOSITIONS)
China	101262847
Japan	5208113
Denmark	1345920
Canada	2621273
Cyprus	1113395

Supplementary Protection Certificates for MACITENTAN

Patent Number	Supplementary Protection Certificate	SPC Country	SPC Expiration	SPC Description
1345920	300672	Netherlands		PRODUCT NAME: MACITENTAN, DESGEWENST IN DE VORM VAN EEN FARMACEUTISCH AANVAARDBAAR ZOUT; REGISTRATION NO/DATE: EU/1/13/893/001-003 20131220
1345920	122014000056	Germany		PRODUCT NAME: MACITENTAN; REGISTRATION NO/DATE: EU/1/13/893/001-003 20131220
1345920	2014/018	Ireland		PRODUCT NAME: MACITENTAN, THE STEREOISOMERS AND THE PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF.; REGISTRATION NO/DATE: EU/1/13/893 20131220
1345920	C01345920/01	Switzerland		PRODUCT NAME: MACITENTAN; REGISTRATION NO/DATE: SWISSMEDIC 61863 06.02.2014
1345920	502	Finland
1345920	1490025-2	Sweden		PRODUCT NAME: MACITENTAN; REG. NO/DATE: EU/1/13/893 20131220

Market Dynamics and Financial Trajectory for Macitentan

Last updated: November 26, 2025

Executive Summary

Macitentan, marketed under the brand name Opsumit, is a dual endothelin receptor antagonist primarily approved for the treatment of pulmonary arterial hypertension (PAH). Since its launch, the drug has carved a significant position in the niche but expanding PAH therapeutic market. This analysis explores the competitive landscape, regulatory environment, market drivers, financial performance, and projected trajectory for Macitentan over the next five years.

Introduction

Macitentan was developed by Sanofi and approved by the U.S. Food and Drug Administration (FDA) in 2013. The drug’s rapid adoption was driven by its superior efficacy and safety profile compared to predecessors like bosentan. Given the global rise in pulmonary hypertension cases, Macitentan's market is poised for sustained growth, contingent on regulatory, clinical, and geopolitical factors.

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Global Market Overview

Parameter	Value / Description
Global PAH Market (2022)	Estimated at $1.2 billion, expected to reach ~$2.0 billion by 2030[1]
Macitentan’s Market Share (2023)	Approx. 20-25%, with dominant position in U.S. & EU[2]
Number of PAH Patients (Global, 2023)	~70,000, projected growth at CAGR of 7% through 2030[3]
Top Competitors	Bosentan (Tracleer), Ambrisentan (Letairis), Macitentan (Opsumit)

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Market Drivers

1. Rising Incidence of Pulmonary Arterial Hypertension

• Increasing awareness and better diagnostic techniques have led to higher reported cases.
• PAH prevalence: 15-50 cases per million globally; higher in certain regions[4].

2. Efficacy and Safety Profile of Macitentan

• Superior binding affinity and reduced hepatotoxicity compared to bosentan[5].
• Once-daily dosing improves patient adherence.

3. Regulatory Approvals & Expanding Indications

• Additional approvals in Japan (2018) and other markets facilitate broader access.
• Ongoing trials for secondary indications like left-sided heart failure.

4. Patent and Exclusivity

• Patent protection until 2030; potential for extension based on clinical trials.

5. Pricing and Reimbursement Policies

• Generally favorable in developed markets.
• Variability in emerging markets impacts revenue streams.

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Market Challenges & Constraints

Challenge	Impact
High Cost of Therapy	Limits accessibility in low- and middle-income regions
Generic Competition Post-Expiry	Patent expiry forecast for 2030 may lead to price erosion
Limited Awareness & Diagnosis	Underdiagnosis hampers market penetration
Stringent Regulatory Environments	Lengthy approval processes in certain markets

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Financial Trajectory

Revenue Generation & Growth Estimates

Year	Estimated Revenue (USD million)	Notes
2023	~$370 million	Stable growth driven by U.S. and Europe markets
2025	~$500 million	Expected expansion with new market entries
2030	~$850 million	Propelled by increased market penetration and approvals

(Assuming a CAGR of approximately 12-15% from 2023 to 2030)

Profitability & Investment Overview

• Sanofi invests heavily in post-marketing surveillance and clinical trials.
• R&D pipeline for long-term growth focuses on combination therapies and novel endothelin antagonists.
• Margins are expected to improve as generic competition looms closer, though patent exclusivity till 2030 provides revenue buffers.

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Competitive Positioning & Differentiation

Parameter	Macitentan (Opsumit)	Bosentan (Tracleer)	Ambrisentan (Letairis)
Approval Year	2013	2001	2007
Dosing	Once daily	Twice daily	Once daily
Safety Profile	Better hepatotoxicity profile	Hepatotoxicity risks	Similar to Macitentan
Cost	Premium pricing	Slightly lower	Similar or slightly lower

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Regulatory & Policy Framework

1. Key Approvals and Indications

• FDA (2013): PAH (WHO Group 1) in adult patients.
• EMA (2013): Same as FDA, with evaluations for pediatric use.
• Japan (2018): Additional indications for pulmonary hypertension associated with congenital heart disease.

2. Pricing & Reimbursement Policies

• Global reimbursement varies:
  • U.S.: Favorable, covered under most private and Medicare plans.
  • EU: Reimbursement dependent on national policies.
  • Emerging Markets: Price controls and budget caps influence uptake.

3. Patent Landscape & Biosimilar Entry

• Patent expiry near 2030 creates opportunities for biosimilars.
• Companies like Teva and Dr. Reddy’s already investing in generic endothelin receptor antagonists.

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Comparison With Similar Therapies

Parameter	Macitentan	Bosentan	Ambrisentan
Mechanism	Dual endothelin A and B receptor antagonist	Dual receptor antagonist	Selective endothelin A receptor antagonist
Bioavailability	High	Moderate	High
Dosing Frequency	Once daily	Twice daily	Once daily
Approval Year	2013	2001	2007
Estimated Market Share (2023)	20-25%	40-45%	10-15%

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Future Outlook & Forecasts

Growth Opportunities

• Expansion into New Markets: Asia-Pacific, Latin America, and Africa.
• Combination Therapies: Dual or triple combination with phosphodiesterase inhibitors and prostacyclins.
• Biomarker Development: To optimize patient selection and dosing.

Risks & Uncertainties

• Patent challenges and patent cliffs.
• Regulatory delays and market access hurdles.
• Emergence of biosimilars impacting pricing.

Projected Market Share & Revenue Trajectory (2023–2030)

Year	Market Share (%)	Projected Revenue (USD million)	Key Drivers
2023	20-25%	~$370	Established approval, current uptake
2025	25-30%	~$500	Broader access, clinical trial success
2027	30-35%	~$650	Competition mitigation, pipeline progress
2030	35-40%	~$850	Patent expiry, biosimilar entries

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Key Takeaways

• Market Position: Macitentan remains a leading drug in PAH management, with conservation of market share due to its efficacy and safety profile.
• Growth Catalysts: Increasing PAH prevalence, expanded indications, and geographic penetration will drive revenues.
• Challenges: Patent expiration risks and emerging biosimilars threaten margins; strategic pricing and patent strategies remain critical.
• Investment Outlook: Sanofi’s continued R&D focus and pipeline development reinforce long-term potential.
• Strategic Recommendations: Stakeholders should monitor patent timelines, regulatory changes, and emerging competitors to navigate potential market shifts effectively.

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FAQs

1. When does the patent for Macitentan expire, and how will it affect the market?
   Patent protection is expected until 2030, after which biosimilar entrants could drastically reduce prices and market shares.

2. What are the main advantages of Macitentan over other PAH therapies?
   Macitentan offers a once-daily dosing, a superior safety profile, especially regarding hepatotoxicity, and proven efficacy in delaying disease progression.

3. How is the global regulatory landscape evolving for PAH drugs like Macitentan?
   Most jurisdictions follow stringent approval processes, but ongoing efforts aim at broader indications and pediatric approvals, potentially expanding market access.

4. What role does pricing and reimbursement play in the drug’s market trajectory?
   Favorable reimbursement policies in developed regions support sales, whereas price controls in emerging markets may hinder uptake.

5. Are there upcoming clinical trials that might influence Macitentan’s market?
   Yes, trials investigating combination therapies, pediatric use, and new indications could bolster its market position, contingent on positive outcomes.

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References

1. MarketWatch: Pulmonary arterial hypertension drugs market size and forecasts, 2022.
2. Sanofi Regulatory Filings: Opsumit market data and patent information, 2023.
3. Global Burden of Disease Study: PAH prevalence data, 2023.
4. European Medicines Agency (EMA): Macitentan approval details, 2013.
5. Clinical Pharmacology Reviews: Comparative efficacy of endothelin receptor antagonists, 2021.

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Note: All projections and data points are estimates based on current market conditions and available literature as of 2023.