Drug intelligence / Profile preview

riociguat

Development stage
Approved
Lead developer
Bayer
Modality
Small Molecules
Administration
Oral
01

Overview

Riociguat is a small molecule stimulator of soluble guanylate cyclase (sGC), developed and marketed by Bayer, indicated for the treatment of pulmonary arterial hypertension (PAH, WHO Group 1) and chronic thromboembolic pulmonary hypertension (CTEPH) in adults. It works by sensitizing sGC to endogenous nitric oxide (NO) and directly stimulating sGC independently of NO, leading to increased production of cyclic guanosine monophosphate (cGMP). This results in vasodilation, antiproliferative, and antifibrotic effects that help lower pulmonary blood pressure and improve exercise capacity. Riociguat is the first approved drug from the class of sGC stimulators for both PAH and CTEPH[1][2][3][4][6][8].

Brand names
Adempas
Other names
Riociguatummethyl N-[4,6-diamino-2-[1-[(2-fluorophenyl)methyl]-1H-pyrazolo[3,4-b]pyridin-3-yl]-5-pyrimidinyl]-N-methyl-carbaminate
02

Targets

sGC (Soluble Guanylyl Cyclase)

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