Eva Becker‐Pelster

ATMOS, a Proof-of-Concept trial of inhaled mosliciguat in untreated PAH or CTEPH

Hossein Ardeschir Ghofrani, Hanno Leuchte, Hikmet Al‐Hiti, Michael Halank et autres

Background: Mosliciguat is a soluble guanylate cyclase (sGC) activator for dry powder inhalation. Unlike sGC stimulators, mosliciguat also targets nitric oxide (NO) insensitive apo-sGC important in conditions of oxidative stress to increase cyclic guanosine monophosphate (cGMP). Objectives: Assess peak percent change (PPC) …

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New Generation of sGC Stimulators: Discovery of Imidazo[1,2-a]pyridine Carboxamide BAY 1165747 (BAY-747), a Long-Acting Soluble Guanylate Cyclase Stimulator for the Treatment of Resistant Hypertension

Alexandros Vakalopoulos, Frank Wunder, Ingo V. Hartung, Gorden Redlich et autres

Herein, we describe the identification, chemical optimization, and preclinical characterization of novel soluble guanylate cyclase (sGC) stimulators. Given the very broad therapeutic opportunities for sGC stimulators, new tailored molecules for distinct indications with specific pharmacokinetics, tissue distribution, and physicochemical properties will be …

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Inhaled mosliciguat (BAY 1237592): targeting pulmonary vasculature via activating apo-sGC

Eva Becker‐Pelster, Michael G. Hahn, Martina Delbeck, Lisa Dietz et autres

BACKGROUND: Oxidative stress associated with severe cardiopulmonary diseases leads to impairment in the nitric oxide/soluble guanylate cyclase signaling pathway, shifting native soluble guanylate cyclase toward heme-free apo-soluble guanylate cyclase. Here we describe a new inhaled soluble guanylate cyclase activator to target apo-soluble …

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Soluble GC stimulators and activators: Past, present and future

Peter Sandner, Markus Follmann, Eva Becker‐Pelster, Michael G. Hahn et autres

The discovery of soluble GC (sGC) stimulators and sGC activators provided valuable tools to elucidate NO-sGC signalling and opened novel pharmacological opportunities for cardiovascular indications and beyond. The first-in-class sGC stimulator riociguat was approved for pulmonary hypertension in 2013 and vericiguat very …

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Direct soluble guanylate cyclase activation improves vascular function in a mouse model of sickle cell disease

Karin P. Potoka, Christina Mucci, Stephanie M. Mutchler, Marta Bueno et autres

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