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Drugs of the Future
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Drugs Fut 2009, 34(6): 468
ISSN 0377-8282
e-ISSN 2013-0368
Copyright 2009 Clarivate
CCC: 0377-8282
DOI: 10.1358/dof.2009.034.06.1384256
Mulligan, C.
Pulmonary hypertension (PH) is a debilitating, ultimately fatal disease in which elevated pulmonary arterial pressure causes vascular remodeling, right heart hypertrophy and heart failure. Therapies have only been approved for one subcategory of PH (pulmonary arterial hypertension, or PAH), and survival rates remain low. Riociguat (BAY 63-2521) is a first-in-class drug developed by Bayer Schering Pharma as an oral PH therapy. It stimulates soluble guanylate cyclase (sGC), the receptor of the endogenous vasodilator nitric oxide (NO), by a dual mode of action: increasing sGC sensitivity to NO and directly stimulating sGC when NO is absent or low. Preclinical studies demonstrated vasorelaxant and antiremodeling properties. Phase I and proof-of-concept clinical trials supported further development. An open-label, uncontrolled phase II trial of riociguat in chronic thromboembolic PH and PAH has been completed, and phase III trials have begun in these indications. Further studies will investigate riociguat in PH associated with lung diseases.

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