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Riociguat Oral Product
Riociguat is a soluble guanylate cyclase stimulator that increases cyclic GMP levels to promote vasodilation and reduce pulmonary vascular resistance.
Riociguat is a soluble guanylate cyclase stimulator that increases cyclic GMP levels to promote vasodilation and reduce pulmonary vascular resistance. Used for Pulmonary arterial hypertension (PAH), Chronic thromboembolic pulmonary hypertension (CTEPH).
At a glance
| Generic name | Riociguat Oral Product |
|---|---|
| Also known as | Ambrisentan Oral Product |
| Sponsor | University of Calgary |
| Drug class | Soluble guanylate cyclase stimulator |
| Target | Soluble guanylate cyclase (sGC) |
| Modality | Small molecule |
| Therapeutic area | Cardiovascular |
| Phase | FDA-approved |
Mechanism of action
Riociguat directly activates soluble guanylate cyclase (sGC) in vascular smooth muscle cells, leading to increased production of cyclic GMP (cGMP). This elevation in cGMP causes smooth muscle relaxation and vasodilation, reducing pulmonary vascular resistance and improving hemodynamics in pulmonary hypertension. The drug works independently of nitric oxide availability, making it effective even in patients with impaired endothelial function.
Approved indications
- Pulmonary arterial hypertension (PAH)
- Chronic thromboembolic pulmonary hypertension (CTEPH)
Common side effects
- Hypotension
- Headache
- Dizziness
- Dyspepsia
- Nausea
Key clinical trials
- Treatment of Exercise-Induced Pulmonary Vascular Dysfunction After Pulmonary Thromboendarterectomy or Balloon Pulmonary Angioplasty (PHASE2)
- Networked Drug REpurposing for Mechanism-based neuroPrOtection in Acute Ischaemic STROKE (PHASE2)
- THERAPY-HYBRID-BPA Trial (PHASE2)
- Study on the Safety of BAY 63-2521, How it is Tolerated and the Way the Body Absorbs, Distributes and Gets Rid of the Study Drug Given as a Single Oral Dose of 1 mg Tablet in Participants With Impaired Liver Function and Healthy Participants Matched for Age-, Gender-, and Weight (PHASE1)
- Study on the Safety of BAY 63-2521, How it is Tolerated and the Way the Body Absorbs, Distributes and Gets Rid of the Study Drug Given as a Single Oral Dose of 1 mg Tablet in Participants With Renal Impairment and Healthy Participants Matched for Age-, Gender-, and Weight (PHASE1)
- Upfront Combination Pulmonary Arterial Hypertension Therapy (PHASE4)
- Interaction With HIV Antiretroviral Agents (PHASE1)
- Efficacy Study of Riociguat and Its Effects on Exercise Performance and Pulmonary Artery Pressure at High Altitude (PHASE4)
Primary sources
Every claim on this page is sourced from regulatory or scientific primary sources. See our editorial policy for full methodology.
| Source | Used for |
|---|---|
| ClinicalTrials.gov | Trial enrolment, design, endpoints, results |
Competitive intelligence
For the full competitive landscape — auto-detected comparators, recent regulatory actions across the set, upcoming PDUFA, patent timeline, sponsor landscape:
- Riociguat Oral Product CI brief — competitive landscape report
- Riociguat Oral Product updates RSS · CI watch RSS
- University of Calgary portfolio CI