OPSUMIT Drug Patent Profile

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

Opsumit is a drug marketed by Actelion and is included in one NDA. There are five patents protecting this drug and one Paragraph IV challenge.

This drug has ninety-four patent family members in thirty-two countries.

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

DrugPatentWatch^® Generic Entry Outlook for Opsumit

Opsumit was eligible for patent challenges on October 18, 2017.

There have been five 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 are three tentative approvals for the generic drug (macitentan), which indicates the potential for near-term generic launch.

Indicators of Generic Entry

Summary for OPSUMIT

International Patents:	94
US Patents:	5
Applicants:	1
NDAs:	1
Finished Product Suppliers / Packagers:	1
Raw Ingredient (Bulk) Api Vendors:	92
Clinical Trials:	17
Patent Applications:	451
Drug Prices:	Drug price information for OPSUMIT
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for OPSUMIT
What excipients (inactive ingredients) are in OPSUMIT?	OPSUMIT excipients list
DailyMed Link:	OPSUMIT at DailyMed

See drug prices for OPSUMIT

Recent Clinical Trials for OPSUMIT

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

Sponsor	Phase
Janssen, LP	Phase 4
American Heart Association	Phase 4
Janssen Pharmaceutical K.K.	Phase 3

See all OPSUMIT clinical trials

Pharmacology for OPSUMIT

Drug Class	Endothelin Receptor Antagonist
Mechanism of Action	Endothelin Receptor Antagonists

Paragraph IV (Patent) Challenges for OPSUMIT

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

US Patents and Regulatory Information for OPSUMIT

OPSUMIT is protected by five 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	OPSUMIT	macitentan	TABLET;ORAL	204410-001	Oct 18, 2013		RX	Yes	Yes	8,268,847
Actelion	OPSUMIT	macitentan	TABLET;ORAL	204410-001	Oct 18, 2013		RX	Yes	Yes	8,367,685		Y
Actelion	OPSUMIT	macitentan	TABLET;ORAL	204410-001	Oct 18, 2013		RX	Yes	Yes	9,265,762		Y
Actelion	OPSUMIT	macitentan	TABLET;ORAL	204410-001	Oct 18, 2013		RX	Yes	Yes	10,946,015		Y
Actelion	OPSUMIT	macitentan	TABLET;ORAL	204410-001	Oct 18, 2013		RX	Yes	Yes	7,094,781		Y	Y

EU/EMA Drug Approvals for OPSUMIT

Company	Drugname	Inn	Product Number / Indication	Status	Generic	Biosimilar	Orphan	Marketing Authorisation	Marketing Refusal
Janssen-Cilag International N.V.	Opsumit	macitentan	EMEA/H/C/002697 Opsumit, 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 OPSUMIT

When does loss-of-exclusivity occur for OPSUMIT?

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

Argentina

Australia

Brazil

Canada

Chile

China

Croatia

Cyprus

Denmark

European Patent Office

Hong Kong

Israel

Japan

Malaysia

Mexico

Morocco

New Zealand

Norway

Poland

Portugal

Russian Federation

Slovenia

South Africa

South Korea

Spain

Taiwan

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 OPSUMIT around the world.

Country	Patent Number	Title	Estimated Expiration
Morocco	30704	COMPOSITIONS THERAPEUTIQUES
Denmark	2059246
Norway	20032699
South Korea	100819668
South Korea	101473022

Supplementary Protection Certificates for OPSUMIT

Patent Number	Supplementary Protection Certificate	SPC Country	SPC Expiration	SPC Description
1345920	SPC/GB14/018	United Kingdom		PRODUCT NAME: MACITENTAN, WHICH IS N-(5-(4-BROMOPHENYL)-6-(2((5-BROMOPYRIMIDIN-2-YL)OXY)ETHOXY)PYRIMIDIN-4-YL)-N'-PROPYLSULFURIC DIAMIDE; REGISTERED: UK EU/1/13/893 20131220
1345920	14C0017	France		PRODUCT NAME: MACITENTAN ET SES SELS PHARMACEUTIQUEMENT ACCEPTABLES; REGISTRATION NO/DATE: EU/1/13/893 20131220
1345920	132014902244514	Italy		PRODUCT NAME: MACITENTAN(OPSUMIT); AUTHORISATION NUMBER(S) AND DATE(S): EU/1/13/893/001-002, 20131220
1345920	1490025-2	Sweden		PRODUCT NAME: MACITENTAN; REG. NO/DATE: EU/1/13/893 20131220
1345920	CA 2014 00012	Denmark		PRODUCT NAME: MACITENTAN OG FARMACEUTISK ACCEPTABLE SALTE HERAF; REG. NO/DATE: EU/1/13/893 20131220

OPSUMIT Market Analysis and Financial Projection Experimental

Market Dynamics and Financial Trajectory for Opsumit

Introduction

Opsumit, known generically as macitentan, is a pivotal drug in the treatment of Pulmonary Arterial Hypertension (PAH), a severe and progressive disease. Developed by Actelion, which is now part of Johnson & Johnson, Opsumit has been a market leader in the PAH treatment landscape since its FDA approval in December 2013.

Market Leadership and Sales Performance

Opsumit has consistently demonstrated strong sales performance, solidifying its position as a market leader in the PAH market. In 2020, Opsumit achieved blockbuster sales of $1,639 million, making it one of the highest-selling products in its class[1].

Clinical Trials and Label Expansions

Opsumit, along with another Johnson & Johnson product, Uptravi, is being investigated in clinical trials to support potential label expansions to chronic thromboembolic pulmonary hypertension (CTEPH). This expansion could significantly broaden the treatment options for CTEPH patients, who currently have limited approved therapies[1].

Competitive Landscape

The PAH market is highly competitive, with several drug classes vying for market share. However, Opsumit has maintained its dominance due to its efficacy and the strong patent portfolio held by Actelion. This portfolio, which includes 55% of the total patents for macitentan, poses significant challenges for generic drug manufacturers attempting to enter the market[4].

Drug Classes and Market Share

• Endothelin Receptor Antagonists (ERAs): Historically, ERAs were the most commercially lucrative class, but they are now under threat from generics and the increasing use of prostacyclins in triple combination therapies[1].
• Phosphodiesterase Type 5 Inhibitors (PDE5is): This class has faced fierce generic competition, leading to a significant decline in market share from $817 million in 2018 to $301 million in 2019[1].
• Prostacyclins: This class has surpassed ERAs in sales, with total sales of $2,675 million in 2019 compared to $2,286 million for ERAs. Prostacyclins are expected to continue their growth trajectory, driven by their use in early polytherapy regimens[1].

Financial Performance

Initial Success

After its approval, Opsumit quickly gained traction. In the first quarter of 2015, it generated $99.5 million in sales, which rose to $390.2 million in the first half of 2016. This strong uptake was reflected in Actelion's financial performance, with product sales reaching CHF 1,008 million in the first half of 2015, driven largely by Opsumit's success[5].

Continued Growth

Actelion's financial reports highlighted the significant contribution of Opsumit to their revenue. By the end of June 2015, Opsumit had generated sales of 208 million Swiss francs, benefiting over 9,800 patients. This performance led to an upgrade in Actelion's financial guidance for the full year 2015[5].

Future Outlook

Market Growth Drivers

The PAH market is expected to continue growing, driven by label expansions into non-PAH subtypes and positive data on morbidity/mortality endpoints. Opsumit, along with other key products, is anticipated to play a crucial role in this growth, particularly as clinical trials support its use in broader patient populations[1].

Pipeline and Innovation

Johnson & Johnson's innovative medicine division, which includes Opsumit, is poised for robust growth. The company expects to deliver a compound annual growth rate (CAGR) of 5-7% from 2025 to 2030, driven by market share gains, new product launches, and expansions into new patient populations[3].

Challenges and Opportunities

Generic Competition

Despite the strong patent portfolio, the eventual expiration of patents will open the door to generic competition. However, the complexity of macitentan's formulation and the existing patent landscape will make it challenging for generic manufacturers to enter the market quickly[4].

Off-Label Use and Unmet Needs

The high rate of off-label use of PAH drugs for other forms of pulmonary hypertension (groups 2, 3, and 5) highlights a critical unmet need for approved therapies in these indications. Addressing these needs through label expansions and new clinical trials will be a key area of focus and growth for Opsumit and other PAH treatments[1].

Key Takeaways

• Market Leadership: Opsumit is the established market leader in the PAH treatment market.
• Strong Sales Performance: Opsumit achieved blockbuster sales of $1,639 million in 2020.
• Clinical Trials and Label Expansions: Ongoing trials aim to expand Opsumit's label to include CTEPH.
• Competitive Landscape: Opsumit faces competition from other drug classes, but its strong patent portfolio and efficacy maintain its market position.
• Financial Performance: Opsumit has significantly contributed to Actelion's and Johnson & Johnson's financial success.
• Future Outlook: The PAH market is expected to grow, driven by label expansions and positive clinical data.

FAQs

What is Opsumit used for?

Opsumit (macitentan) is used for the treatment of Pulmonary Arterial Hypertension (PAH), a severe and progressive disease.

How has Opsumit performed in the market?

Opsumit has been a market leader in the PAH treatment market, achieving blockbuster sales of $1,639 million in 2020.

What are the challenges for generic versions of Opsumit?

Generic manufacturers face challenges due to Actelion's strong patent portfolio, which includes 55% of the total patents for macitentan.

What are the future growth drivers for the PAH market?

The PAH market is expected to grow due to label expansions into non-PAH subtypes, positive data on morbidity/mortality endpoints, and the increasing use of prostacyclins in triple combination therapies.

How does Opsumit fit into Johnson & Johnson's overall strategy?

Opsumit is part of Johnson & Johnson's innovative medicine division, which is expected to drive robust growth through market share gains, new product launches, and expansions into new patient populations.

Sources

1. Global Pulmonary Arterial Hypertension Market Report 2021 - Globenewswire
2. Johnson & Johnson Reports Q4 and Full-Year 2023 Results - Johnson & Johnson Investor Relations
3. Innovative Medicine Presentation - Johnson & Johnson
4. Opsumit's Generic Drugs for PAH - A Hurdle before Pharma - GreyB
5. ACTELION DELIVERS EXCELLENT FIRST HALF 2015 RESULTS - FiercePharma