Marc Iglarz

Dual ETA‐ETB receptor antagonism improves metabolic syndrome‐induced heart failure with preserved ejection fraction

Francesca Lockwood, Marianne Lachaux, Najah Harouki, Matthieu Soulié et autres

BACKGROUND: Metabolic syndrome (MetS) is a multifaceted disease associated with heart failure (HF), which affects the vascular system. The endothelin (ET) system is a key player in MetS and HF; therefore, targets for ET receptors are of therapeutic interest. OBJECTIVES: This study …

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Discovery of Galactopyranose‐1‐carboxamides as a New Class of Small, Novel, Potent, Selective, and Orally Active Galectin‐3 Inhibitors

Cornelia Zumbrunn, L’uboš Remeň, Christoph P. Sager, Corinna Grisostomi et autres

Abstract Galectin‐3 (Gal‐3), a β‐galactoside‐binding lectin, is implicated in diverse cellular functions ranging from immune response modulation to tissue homeostasis. Notably, increased Gal‐3 expression has been linked to the progression of numerous diseases, including cancer, fibrosis, and cardiovascular disorders, underscoring its potential …

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The novel lysophosphatidic acid receptor 1-selective antagonist, ACT-1016-0707, has unique binding properties that translate into effective antifibrotic and anti-inflammatory activity in different models of pulmonary fibrosis

Magdalena Birker, Maxime Boucher, Sylvie Poirey, R. O. Studer et autres

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Abstract P437: Correlation between plasma CT-proET-1 and renal dysfunction in patients with resistant hypertension. A biomarker analysis of the PRECISION study.

Peter Blattmann, Marc Iglarz, Roland F. Dreier, Parisa Danaietash et autres

Hypothesis: Endothelin (ET)-1 is upregulated in hypertension and especially resistant forms of hypertension. As ET-1 is a paracrine hormone involved in renal organ damage, we investigated the correlation between eGFR and activity of the ET system in the resistant hypertensive population of …

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Abstract 19: Effect of the endothelin receptor antagonist aprocitentan on plasma endothelin, renin and aldosterone concentrations in patients with resistant hypertension. A biomarker analysis of the PRECISION study.

Marc Iglarz, Peter Blattmann, Roland F. Dreier, Parisa Danaietash et autres

Hypothesis: Dual endothelin (ET) ETA/ETB receptor antagonist aprocitentan significantly reduced blood pressure in patients with resistant hypertension, who were still hypertensive despite standard background anti-hypertensive drugs including a diuretic, an ARB and a CCB (PRECISION trial, NCT03541174). The effect of aprocitentan in …

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Dose Selection for Clinical Development in the Treatment of Hypertension: The Aprocitentan Case and Lessons from the Past

M Bellet, Glenn D. Braunstein, Paul E. Verweij, Parisa Danaietash et autres

Dose selection plays a critical role in the clinical development of a drug. This current review highlights the lessons learned from previous dose finding studies (DFSs) of antihypertensive drugs and from the recent example of aprocitentan, a novel endothelin receptor antagonist for …

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Endothelin Receptor Blockade Improves Cerebral Blood Flow-Mediated Dilation in a Mouse Model of Alzheimer’s Disease

Daniel Henrion, Philippe Bonnin, Emilie Vessières, Anne-Laure Guihlot et autres

INTRODUCTION: Cerebral blood flow (CBF) is reduced in patients with Alzheimer's disease (AD). Flow-mediated dilation (FMD), which plays a key role in the regulation of blood flow, is attenuated by endothelin-1. We hypothesized that endothelin receptor blockade may improve CBF in AD. …

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Effects of the Dual Endothelin Receptor Antagonist Aprocitentan on Body Weight and Fluid Homeostasis in Healthy Subjects on a High Sodium Diet

Pierre Gueneau De Mussy, Patricia N. Sidharta, Grégoire Wuerzner, Marc Maillard et autres

Aprocitentan is a novel, oral, dual endothelin receptor antagonist (ERA) in development in difficult-to-control hypertension. As fluid retention and edema are concerns with ERAs, we investigated whether aprocitentan causes weight gain in healthy subjects on a high sodium diet and explored potential …

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Effects of macitentan and tadalafil monotherapy or their combination on the right ventricle and plasma metabolites in pulmonary hypertensive rats

Argen Mamazhakypov, Astrid Weiß, Sven Zukunft, Akylbek Sydykov et autres

Pulmonary arterial hypertension is a severe respiratory disease characterized by pulmonary artery remodeling. RV dysfunction and dysregulated circulating metabolomics are associated with adverse outcomes in pulmonary arterial hypertension. We investigated effects of tadalafil and macitentan alone or in combination on the RV …

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Pharmacological Characterization of Aprocitentan, a Dual Endothelin Receptor Antagonist, Alone and in Combination with Blockers of the Renin Angiotensin System, in Two Models of Experimental Hypertension

F. Trensz, Céline Bortolamiol, Markus Kramberg, Daniel Wanner et autres

The endothelin (ET) system has emerged as a novel target for hypertension treatment where a medical need persists despite availability of several pharmacological classes, including renin angiotensin system (RAS) blockers. ET receptor antagonism has demonstrated efficacy in preclinical models of hypertension, especially …

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Macitentan reduces progression of TGF-β1-induced pulmonary fibrosis and pulmonary hypertension

Pierre‐Simon Bellaye, Toyoshi Yanagihara, Elise Granton, Seidai Sato et autres

Idiopathic pulmonary fibrosis (IPF) is a progressive disease with an unknown cause. Two drugs, nintedanib and pirfenidone, have been shown to slow, but not stop, disease progression. Pulmonary hypertension (PH) is a frequent complication in IPF patients and is associated with poor …

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Selective Prostacyclin Receptor Agonist Selexipag, in Contrast to Prostacyclin Analogs, Does Not Evoke Paradoxical Vasoconstriction of the Rat Femoral Artery

Keith Morrison, Franck Haag, Roland Ernst, Marc Iglarz et autres

Selexipag [2-{4-[(5,6-diphenylpyrazin-2-yl)(isopropyl)amino]butoxy}- N -(methylsulfonyl)acetamide] is a selective nonprostanoid prostacyclin (PGI 2 ) receptor (IP receptor) agonist that is approved for the treatment of pulmonary arterial hypertension (PAH). In contrast to selexipag, PGI 2 analogs used in the clinic are nonselective agonists at …

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