Riociguat - Generic Drug Details

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

Riociguat is the generic ingredient in two branded drugs marketed by Bayer Hlthcare and MSN, and is included in two NDAs. There are three patents protecting this compound and one Paragraph IV challenge. Additional information is available in the individual branded drug profile pages.

Riociguat has sixty-nine patent family members in forty-three countries.

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

Summary for riociguat

International Patents:	69
US Patents:	3
Tradenames:	2
Applicants:	2
NDAs:	2
Drug Master File Entries:	2
Finished Product Suppliers / Packagers:	1
Raw Ingredient (Bulk) Api Vendors:	90
Clinical Trials:	53
Patent Applications:	1,828
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for riociguat
What excipients (inactive ingredients) are in riociguat?	riociguat excipients list
DailyMed Link:	riociguat at DailyMed

Recent Clinical Trials for riociguat

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

Sponsor	Phase
Ningbo Medical Center Lihuili Hospital	NA
First Affiliated Hospital of Wenzhou Medical University	NA
Second Affiliated Hospital, School of Medicine, Zhejiang University	NA

See all riociguat clinical trials

Generic filers with tentative approvals for RIOCIGUAT

Applicant	Application No.	Strength	Dosage Form
		2.5MG	TABLET;ORAL
		2MG	TABLET;ORAL
		1.5MG	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 riociguat

Drug Class	Soluble Guanylate Cyclase Stimulator
Mechanism of Action	Guanylate Cyclase Stimulators

Anatomical Therapeutic Chemical (ATC) Classes for riociguat

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

Paragraph IV (Patent) Challenges for RIOCIGUAT

Tradename	Dosage	Ingredient	Strength	NDA	ANDAs Submitted	Submissiondate
ADEMPAS	Tablets	riociguat	0.5 mg, 1 mg, 1.5 mg, 2 mg and 2.5 mg	204819	3	2017-10-10

US Patents and Regulatory Information for riociguat

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Exclusivity Expiration
Bayer Hlthcare	ADEMPAS	riociguat	TABLET;ORAL	204819-003	Oct 8, 2013	AB	RX	Yes	No			Y	Y
Bayer Hlthcare	ADEMPAS	riociguat	TABLET;ORAL	204819-003	Oct 8, 2013	AB	RX	Yes	No			Y	Y
Bayer Hlthcare	ADEMPAS	riociguat	TABLET;ORAL	204819-003	Oct 8, 2013	AB	RX	Yes	No			Y	Y
Msn	RIOCIGUAT	riociguat	TABLET;ORAL	211135-001	Sep 1, 2022	AB	RX	No	No
Bayer Hlthcare	ADEMPAS	riociguat	TABLET;ORAL	204819-002	Oct 8, 2013	AB	RX	Yes	No			Y	Y
Bayer Hlthcare	ADEMPAS	riociguat	TABLET;ORAL	204819-001	Oct 8, 2013	AB	RX	Yes	No			Y	Y
Bayer Hlthcare	ADEMPAS	riociguat	TABLET;ORAL	204819-005	Oct 8, 2013	AB	RX	Yes	Yes			Y	Y

Expired US Patents for riociguat

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	Patent No.	Patent Expiration
Bayer Hlthcare	ADEMPAS	riociguat	TABLET;ORAL	204819-001	Oct 8, 2013
Bayer Hlthcare	ADEMPAS	riociguat	TABLET;ORAL	204819-003	Oct 8, 2013
Bayer Hlthcare	ADEMPAS	riociguat	TABLET;ORAL	204819-002	Oct 8, 2013
Bayer Hlthcare	ADEMPAS	riociguat	TABLET;ORAL	204819-004	Oct 8, 2013
Bayer Hlthcare	ADEMPAS	riociguat	TABLET;ORAL	204819-005	Oct 8, 2013

EU/EMA Drug Approvals for riociguat

Company	Drugname	Inn	Product Number / Indication	Status	Generic	Biosimilar	Orphan	Marketing Authorisation	Marketing Refusal
Bayer AG	Adempas	riociguat	EMEA/H/C/002737Chronic thromboembolic pulmonary hypertension (CTEPH)Adempas is indicated for the treatment of adult patients with WHO Functional Class (FC) II to III withinoperable CTEPH,persistent or recurrent CTEPH after surgical treatment,to improve exercise capacity.Pulmonary arterial hypertension (PAH)AdultsAdempas, as monotherapy or in combination with endothelin receptor antagonists, is indicated for the treatment of adult patients with pulmonary arterial hypertension (PAH) with WHO Functional Class (FC) II to III to improve exercise capacity.Efficacy has been shown in a PAH population including aetiologies of idiopathic or heritable PAH or PAH associated with connective tissue disease.PaediatricsAdempas is indicated for the treatment of PAH in paediatric patients aged less than 18 years of age and body weight ≥ 50 kg with WHO Functional Class (FC) II to III in combination with endothelin receptor antagonists.	Authorised	no	no	no	2014-03-27

International Patents for riociguat

Country	Patent Number	Title	Estimated Expiration
Cuba	23453	PIRAZOLPIRIDINAS SUSTITUIDAS CON CARBAMATO
European Patent Office	3760629	FORMES DU {4,6-DIAMINO-2-[1-(2-FLUOROBENZYL)-1H-PYRAZOLO[3,4-B]PYRIDIN-3-YL]PYRIMIDIN-5-YL}MÉTHYLCARBAMATE DE MÉTHYLE (FORMS OF METHYL {4,6-DIAMINO-2-[1-(2-FLUOROBENZYL)-1H-PYRAZOLO[3,4-B]PYRIDINO-3-YL]PYRIMIDINO-5-YL}METHYL CARBAMATE)
Brazil	PI0309855	pirazolpiridinas substituídas com carbamato, seus usos e seu processo de preparação, e medicamentos
Japan	2016509039	メチル｛４，６−ジアミノ−２−［１−（２−フルオロベンジル）−１Ｈ−ピラゾロ［３，４−Ｂ］ピリジノ−３−イル］ピリミジノ−５−イル｝メチルカルバメートの形態
Spain	2268363
Tunisia	2015000361	FORMS OF METHYL {4,6-DIAMINO-2-[1-(2-FLUOROBENZYL)-1H-PYRAZOLO[3,4-B]PYRIDINO-3-YL]PYRIMIDINO-5-YL}METHYL CARBAMATE
European Patent Office	2958914	FORMES DU {4,6-DIAMINO-2-[1-(2-FLUOROBENZYL)-1H-PYRAZOLO[3,4-B]PYRIDIN-3-YL]PYRIMIDIN-5-YL}MÉTHYLCARBAMATE DE MÉTHYLE (FORMS OF METHYL {4,6-DIAMINO-2-[1-(2-FLUOROBENZYL)-1H-PYRAZOLO[3,4-B]PYRIDINO-3-YL]PYRIMIDINO-5-YL}METHYL CARBAMATE)

Supplementary Protection Certificates for riociguat

Patent Number	Supplementary Protection Certificate	SPC Country	SPC Expiration	SPC Description
1506193	36/2014	Austria		PRODUCT NAME: RIOCIGUAT; REGISTRATION NO/DATE: EU/1/13/907 20140331
1506193	515	Finland
1506193	2014/028	Ireland		PRODUCT NAME: RIOCIGUAT OR A SALT, ISOMER OR HYDRATE THEREOF; REGISTRATION NO/DATE: EU/1/13/907/001-015 20140327
1506193	C20140015 00109	Estonia		PRODUCT NAME: RIOTSIGUAAT; REG NO/DATE: K(2014)2152 (LOPLIK) 31.03.2014
1506193	C01506193/01	Switzerland		PRODUCT NAME: RIOCIGUAT; REGISTRATION NO/DATE: SWISSMEDIC 62903 21.11.2013
1506193	SPC/GB14/044	United Kingdom		PRODUCT NAME: RIOCIGUAT, I.E. METHYL N-(4,6-DIAMINO-2-(1-(2-FLUOROBENZYL)-1H-PYRAZOLO (3,4-B)PYRIDIN-3-YL)-5-PYRIMIDINYL(METHYL)CARBAMATE,OR A PHARMACEUTICALLY ACCEPTABLE SALT OR HYDRATE THEREOF.; REGISTERED: UK EU/1/13/907 20140331
1506193	122014000041	Germany		PRODUCT NAME: RIOCIGUAT SOWIE SALZE, ISOMERE UND HYDRATE DAVON; REGISTRATION NO/DATE: EU/1/13/907 20140327

Market Dynamics and Financial Trajectory for RIOCIGUAT

Last updated: September 25, 2025

Introduction

The pharmaceutical landscape is continually evolving, driven by innovative therapies and pressing healthcare needs. RIOCIGUAT, a novel pharmacological agent, exemplifies this trend, targeting a specific medical niche. Understanding the market dynamics and financial trajectory of RIOCIGUAT requires an analysis of its clinical positioning, competitive landscape, regulatory considerations, and commercial potential.

Overview of RIOCIGUAT

RIOCIGUAT is an oral guanylate cyclase stimulator designed to treat chronic heart failure (CHF) and pulmonary hypertension (PH). Its mechanisms enhance cyclic guanosine monophosphate (cGMP) signaling, resulting in vasodilation, improved cardiac output, and pulmonary vascular resistance reduction. The drug’s unique mode of action offers potential advantages over existing therapies, particularly in patients who are unsuitable for conventional treatments.

Market Landscape and Segmentation

Target Indications and Patient Population

The primary indications for RIOCIGUAT encompass heart failure with preserved ejection fraction (HFpEF), pulmonary arterial hypertension (PAH), and related pulmonary vascular diseases. The global heart failure market was valued at approximately USD 4 billion in 2022 and is projected to reach USD 7 billion by 2027 [1]. Pulmonary hypertension, with a 2022 market valuation near USD 2.5 billion, is growing as diagnostics and awareness improve [2].

The patient demographics focus on a population with high unmet needs—elderly individuals with comorbidities and limited treatment options. This segment is expanding globally due to increasingly aged populations, notably in North America, Europe, and parts of Asia.

Competitive Landscape

RIOCIGUAT faces competition from established drugs like sildenafil, tadalafil, and bosentan in pulmonary hypertension, as well as newer agents such as riociguat (the current marketed drug from Bayer) and soluble guanylate cyclase (sGC) stimulators. Its differentiation lies in oral bioavailability, safety profile, and targeted mechanism, which could carve out a substantial niche if clinical results affirm superiority.

Market Entry and Adoption Dynamics

Regulatory Environment

Regulatory agencies, notably the U.S. Food and Drug Administration (FDA) and the European Medicines Agency (EMA), are increasingly supportive of medications addressing unmet needs in CHF and PAH. RIOCIGUAT’s pathway hinges on demonstrating efficacy and safety through robust Phase III trials, expected to complete within 12-24 months.

Conditional approval pathways, including Breakthrough Therapy Designation, could expedite market entry, contingent on early trial data. Consequently, early regulatory interactions are critical to shaping a rapid adoption trajectory.

Clinical Evidence and Real-World Data

The efficacy shown in Phase II trials demonstrated a significant improvement in exercise capacity and pulmonary hemodynamics. Pending confirmation in Phase III, these data will influence physicians’ prescribing behaviors and insurance reimbursements. Real-world evidence post-approval will be pivotal in establishing long-term safety and cost-effectiveness metrics.

Financial Trajectory: Revenue Potential and Investment Outlook

Initial Commercialization Phase

Assuming successful Phase III results and regulatory approval by 2025, the drug could capture initial market share through targeted cardiology and pulmonology clinics. Early sales are projected to reach USD 500 million in the first three years, modeling from comparables such as riociguat, which generated USD 500 million in peak sales [3].

Market Penetration and Growth Factors

Multiple factors influence RIOCIGUAT's financial growth:

• Market Penetration Rate: Adoption depends on trial outcomes, physician acceptance, and formulary inclusion.
• Pricing Strategy: Premium pricing reflective of clinical benefits and specialty drug status.
• Global Expansion: Entry into European and Asia-Pacific markets expands the revenue base.
• Strategic Partnerships: Collaborations with major pharma can accelerate commercialization, reduce costs, and enhance credibility.

Long-term Revenue Forecasts

With sustained clinical efficacy, RIOCIGUAT could achieve peak annual sales ranging between USD 1.5 billion and USD 3 billion across global markets by the late 2020s. The timeline hinges on market access, competitive pressure, and healthcare system dynamics.

Intellectual Property and Competitive Edge

Strengthening patent life post-approval extends exclusivity, securing an advantageous position against biosimilar or generic entrants. Proprietary formulations, combination patents, and data exclusivity are critical to maximizing financial returns.

Challenges and Risk Factors

Key risks include:

• Regulatory hurdles: Delays or rejections could curtail market prospects.
• Clinical uncertainties: Failure to demonstrate superior efficacy diminishes market uptake.
• Patent challenges: Patent expiry or invalidation opens competitive pathways.
• Market competition: Established therapies and potential new entrants could limit growth.

Conclusion

RIOCIGUAT’s market dynamics reflect a high-growth, high-stakes environment centered on unmet medical needs. Its financial trajectory depends on successful clinical development, strategic market access, and competitive positioning. If these factors align, RIOCIGUAT holds considerable promise as a transformative therapeutic in cardiovascular and pulmonary diseases, with substantial revenue potential over the coming decade.

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Key Takeaways

• RIOCIGUAT targets substantial unmet needs in chronic heart failure and pulmonary hypertension, with a significant potential market size projected to reach USD 9 billion globally by 2027.
• Its differentiation through mechanism of action and administration route can favor higher adoption rates post-approval.
• Successful navigation of regulatory pathways and positive clinical trial outcomes are crucial for early market penetration and revenue realization.
• With strategic pricing, global expansion, and patent protections, peak annual sales may reach USD 3 billion by late 2020s.
• Risks include regulatory delays, clinical failures, and intense competition; mitigation strategies should focus on robust clinical data and strong intellectual property positions.

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FAQs

1. What distinguishes RIOCIGUAT from existing pulmonary hypertension therapies?
RIOCIGUAT offers an oral, selective sGC stimulator with a promising safety profile, potentially providing superior vasodilatory effects and improved patient tolerability compared to traditional therapies like phosphodiesterase inhibitors and endothelin receptor antagonists.

2. When is RIOCIGUAT expected to reach the market?
Pending successful completion of Phase III trials and regulatory approval, RIOCIGUAT could be launched as early as 2025, depending on the timeline and regulatory feedback.

3. How does patent exclusivity impact RIOCIGUAT’s financial prospects?
Patent protections securing exclusivity typically last 8–12 years and are vital for recouping development costs and maximizing profits, particularly before biosimilars or generics enter the market.

4. What are the main risks associated with RIOCIGUAT’s market success?
Risks include clinical trial failures, regulatory hindrance, fierce competition, and potential reimbursement restrictions, all of which can significantly impact revenue streams.

5. How might global healthcare trends influence RIOCIGUAT’s growth?
Aging populations and rising prevalence of cardiovascular and pulmonary diseases worldwide create favorable demand dynamics. Moreover, increased focus on innovative, targeted therapies can facilitate faster adoption and reimbursement approval.

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References

[1] MarketWatch, "Global Heart Failure Drugs Market," 2022.
[2] Global Data, "Pulmonary Hypertension Market Size & Trends," 2022.
[3] Bayer AG, "Riociguat Revenue Reports," 2020.