Riociguat is a stimulator of soluble guanylate cyclase indicated for the management of persistent or recurrent chronic thromboembolic pulmonary hypertension and pulmonary arterial hypertension. Riociguat is marketed under the brand Adempas® by Bayer HealthCare Pharmaceuticals.
- Mechanism
- Curator reviewed
Riociguat is a stimulator of soluble guanylate cyclase (sGC), an enzyme in the cardiopulmonary system and the receptor for nitric oxide (NO). When NO binds to sGC, the enzyme catalyzes synthesis of the signaling molecule cyclic guanosine monophosphate (cGMP). Intracellular cGMP plays an important role in regulating processes that influence vascular tone, proliferation, fibrosis and inflammation. Pulmonary hypertension is associated with endothelial dysfunction, impaired synthesis of nitric oxide and insufficient stimulation of the NO-sGC-cGMP pathway.
Riociguat has a dual mode of action. It sensitizes sGC to endogenous NO by stabilizing the NO-sGC binding. Riociguat also directly stimulates sGC via a different binding site, independently of NO. Riociguat stimulates the NO-sGC-cGMP pathway and leads to increased generation of cGMP with subsequent vasodilation.
- Primary indication
- Riociguat is indicated for the treatment of adults with persistent/recurrent chronic thromboembolic pulmonary hypertension (CTEPH), (WHO Group 4) after surgical treatment, or inoperable CTEPH, to improve exercise capacity and WHO functional class.Curator reviewed · 2 structured indications
- Formula / weight
- C20H19FN8O2 · 422.4157 g/mol (avg)
- First approval
- Canada, 2013 · United States, 2013 · European Union, 2016
- Code names
- BAY 41-2272 · BAY 63-2521 · MK-4836
- Brand names
Resolves to
WXXSNCNJFUAIDG-UHFFFAOYSA-NSMILESCOC(=O)N(C)C1=C(N)N=C(N=C1N)C1=NN(CC2=C(F)C=CC=C2)C2=C1C=CC=N2What you can answer from here — as of May 26, 2026
Which drugs share a target with Riociguat, and which of those have an active Phase 3 trial?
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