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Bosentan Is a Substrate of Human OATP1B1 and OATP1B3: Inhibition of Hepatic Uptake as the Common Mechanism of Its Interactions with Cyclosporin A, Rifampicin, and Sildenafil
The elimination process of the endothelin receptor antagonist bosentan (Tracleer) in humans is entirely dependent on metabolism mediated by two cytochrome P450 (P450) enzymes, i.e., CYP3A4 andExpand
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Pharmacology of Macitentan, an Orally Active Tissue-Targeting Dual Endothelin Receptor Antagonist
Macitentan, also called Actelion-1 or ACT-064992 [N-[5-(4-bromophenyl)-6-(2-(5-bromopyrimidin-2-yloxy)ethoxy)-pyrimidin-4-yl]-N′-propylaminosulfonamide], is a new dual ETA/ETB endothelin (ET)Expand
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Absorption, distribution, metabolism, and excretion of macitentan, a dual endothelin receptor antagonist, in humans
Macitentan is a tissue-targeting, dual endothelin receptor antagonist, currently under phase 3 investigation in pulmonary arterial hypertension. In this study the disposition and metabolism ofExpand
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The discovery of N-[5-(4-bromophenyl)-6-[2-[(5-bromo-2-pyrimidinyl)oxy]ethoxy]-4-pyrimidinyl]-N'-propylsulfamide (Macitentan), an orally active, potent dual endothelin receptor antagonist.
Starting from the structure of bosentan (1), we embarked on a medicinal chemistry program aiming at the identification of novel potent dual endothelin receptor antagonists with high oral efficacy.Expand
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Developmental biology of the common marmoset: proposal for a "postnatal staging".
The published knowledge on neurobiological, psychological, and ethological aspects of development in Callithrix jacchus is still limited. We have collected published and unpublished data from severalExpand
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Inhibitory and Inductive Effects of Rifampin on the Pharmacokinetics of Bosentan in Healthy Subjects
This study was conducted to investigate the effect of rifampin on the pharmacokinetics of bosentan. Healthy male subjects received bosentan 125 mg b.i.d. for 6.5 days in the presence or absence ofExpand
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2-imino-thiazolidin-4-one derivatives as potent, orally active S1P1 receptor agonists.
Sphingosine-1-phosphate (S1P) is a widespread lysophospholipid which displays a wealth of biological effects. Extracellular S1P conveys its activity through five specific G-protein coupled receptorsExpand
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Discovery and Characterization of ACT‐335827, an Orally Available, Brain Penetrant Orexin Receptor Type 1 Selective Antagonist
Stress relief: Orexin neuropeptides regulate arousal and stress processing through orexin receptor type 1 (OXR-1) and 2 (OXR-2) signaling. A selective OXR-1 antagonist, represented by aExpand
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In vivo and in vitro studies exploring the pharmacokinetic interaction between bosentan, a dual endothelin receptor antagonist, and glyburide
In a clinical trial with patients with chronic heart failure, a higher incidence ofelevated levels of liver transaminases was observed during concomitant treatment with bosentan, a dual endothelinExpand
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Novel benzo[1,4]diazepin-2-one derivatives as endothelin receptor antagonists.
Since its discovery in 1988 by Yanagisawa et al., endothelin (ET), a potent vasoconstrictor, has been widely implicated in the pathophysiology of cardiovascular, cerebrovascular, and renal diseases.Expand
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