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:	108
Clinical Trials:	49
Patent Applications:	1,005
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
University of Newcastle Upon-Tyne	Phase 4
Sheffield Teaching Hospitals NHS Foundation Trust	Phase 4
University of Glasgow	Phase 4

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
Msn	RIOCIGUAT	riociguat	TABLET;ORAL	211135-004	Sep 1, 2022	AB	RX	No	No
Msn	RIOCIGUAT	riociguat	TABLET;ORAL	211135-003	Sep 1, 2022	AB	RX	No	No
Msn	RIOCIGUAT	riociguat	TABLET;ORAL	211135-002	Sep 1, 2022	AB	RX	No	No
Bayer Hlthcare	ADEMPAS	riociguat	TABLET;ORAL	204819-004	Oct 8, 2013	AB	RX	Yes	No			Y	Y
Bayer Hlthcare	ADEMPAS	riociguat	TABLET;ORAL	204819-004	Oct 8, 2013	AB	RX	Yes	No			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	204819-004	Oct 8, 2013
Bayer Hlthcare	ADEMPAS	riociguat	TABLET;ORAL	204819-001	Oct 8, 2013
Bayer Hlthcare	ADEMPAS	riociguat	TABLET;ORAL	204819-005	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

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/002737 Chronic 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
Netherlands	300659
Norway	329105
Japan	2005531553
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)
European Patent Office	1506193	PYRAZOLOPYRIDINES A SUBSTITUTION CARBAMATE (CARBAMATE-SUBSTITUTED PYRAZOLOPYRIDINES)
Taiwan	I282792

Supplementary Protection Certificates for riociguat

Patent Number	Supplementary Protection Certificate	SPC Country	SPC Expiration	SPC Description
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	2014C/030	Belgium		PRODUCT NAME: RIOCIGUAT; AUTHORISATION NUMBER AND DATE: EU/1/13/907 20140331
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	PA2014018	Lithuania		PRODUCT NAME: ; REGISTRATION NO/DATE: EU/1/13/907/001 - EU/1/13/907/015 20140327
1506193	122014000041	Germany		PRODUCT NAME: RIOCIGUAT SOWIE SALZE, ISOMERE UND HYDRATE DAVON; REGISTRATION NO/DATE: EU/1/13/907 20140327
1506193	36/2014	Austria		PRODUCT NAME: RIOCIGUAT; REGISTRATION NO/DATE: EU/1/13/907 20140331