Clinical implications of riociguat pharmacokinetics and pharmacodynamics: introduction to the riociguat clinical pharmacology supplement

Riociguat (BAY 63-2521) is a novel oral soluble guanylate cyclase (sGC) stimulator developed for the treatment of pulmonary arterial hypertension (PAH) and chronic thromboembolic pulmonary hypertension (CTEPH).1 It targets the nitric oxide (NO)–sGC–cyclic guanosine monophosphate (cGMP) pathway and, via a dual mode of action, both stimulates sGC directly, independently of NO, and sensitizes sGC to endogenous NO by stabilizing NO-sGC binding. As a result, riociguat restores the NO-sGC-cGMP pathway, increasing intracellular levels of cGMP,13 thereby addressing the imbalance of vasoconstriction over vasodilation that is present in the lung vasculature of patients with pulmonary hypertension (PH).4

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Pharmacology: Pharmacokinetics and Pharmacodynamics
Pulmonary Arterial Hypertension
Pulmonary Hypertension


Reiner Frey, Wolfgang Mück

Published in:

Pulmonary Circulation Vol 6: No S1 cover image

March 2016

Pulmonary Circulation Vol 6: No S1

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