Journal article

Publication year: 2011

Pages: 567-576

Journal: Expert Opinion on Investigational Drugs

Volume number: 20

Issue number: 4

ISSN: 1354-3784

eISSN: 1744-7658

DOI Link: https://doi.org/10.1517/13543784.2011.565048

Publisher: Taylor and Francis Group

Abstract: 

Areas covered: This review will help readers understand the mechanism of action of the soluble guanylate cyclase (sGC) stimulator riociguat (BAY 63-2521) and will provide a comprehensive summary regarding efficacy and safety of this drug in the management of PH. The most relevant publications up to December 2010 were used as sources for this review.

Expert opinion: Cyclic guanosine monophosphate (cGMP) is an important mediator of the preferential perfusion of well-ventilated regions throughout the lung. Drugs that increase cGMP levels could promote pulmonary vasorelaxation while maintaining optimal gas exchange. cGMP is generated by sGC, which can be stimulated by nitric oxide (NO). Riociguat stimulates sGC independently of NO and increases the sensitivity of sGC to NO, resulting in increased cGMP levels. Results to date suggest rapid, potent and prolonged efficacy and good tolerability in different types of PH. Phase III clinical trials are evaluating the long-term safety and clinical effectiveness of riociguat in pulmonary arterial hypertension (PAH) and chronic thromboembolic PH. Riociguat has the potential to become an important drug for the treatment of patients with PH.

Harvard Citation style: Schermuly, R., Janssen, W., Weissmann, N., Stasch, J., Grimminger, F. and Ghofrani, H. (2011) Riociguat for the treatment of pulmonary hypertension, Expert Opinion on Investigational Drugs, 20(4), pp. 567-576. https://doi.org/10.1517/13543784.2011.565048

APA Citation style: Schermuly, R., Janssen, W., Weissmann, N., Stasch, J., Grimminger, F., & Ghofrani, H. (2011). Riociguat for the treatment of pulmonary hypertension. Expert Opinion on Investigational Drugs. 20(4), 567-576. https://doi.org/10.1517/13543784.2011.565048