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Pharmacokinetics, safety, and efficacy of bosentan in pediatric patients with pulmonary arterial hypertension
Bosentan, a dual endothelin‐receptor antagonist, is registered for the treatment of pulmonary arterial hypertension. Little is known about the effects of bosentan in children. This study wasExpand
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Clinical Pharmacology of Bosentan, a Dual Endothelin Receptor Antagonist
Bosentan, a dual endothelin receptor antagonist, is indicated for the treatment of patients with pulmonary arterial hypertension (PAH).Following oral administration, bosentan attains peak plasmaExpand
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Pharmacokinetic-pharmacodynamic interaction between the COMT inhibitor tolcapone and single-dose levodopa.
1. Single oral doses of the catechol-O-methyltransferase (COMT) inhibitor tolcapone (10-800 mg) or placebo were administered simultaneously with a dose of levodopa/benserazide 100/25 mg to sevenExpand
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Safety, tolerability, pharmacokinetics, and pharmacodynamics of macitentan, an endothelin receptor antagonist, in an ascending multiple‐dose study in healthy subjects
This multiple‐ascending‐dose study investigated safety, tolerability, pharmacokinetics, and pharmacodynamics, of macitentan, a new endothelin receptor antagonist (ERA) with sustained receptor bindingExpand
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Efficacy, safety and clinical pharmacology of macitentan in comparison to other endothelin receptor antagonists in the treatment of pulmonary arterial hypertension
Introduction: Macitentan is a novel dual endothelin receptor antagonist (ERA) showing sustained receptor occupancy. In vitro and in vivo animal studies have demonstrated its potency in antagonizingExpand
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Macitentan: entry-into-humans study with a new endothelin receptor antagonist
PurposeTo study the pharmacokinetics, pharmacodynamics, and tolerability of rising single doses of macitentan, an endothelin receptor antagonist, in healthy male subjects.MethodsThis double-blind,Expand
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Single- and multiple-dose pharmacokinetics of bosentan and its interaction with ketoconazole.
AIMS The present study was conducted to characterize the single- and multiple-dose pharmacokinetics of bosentan, a dual endothelin receptor antagonist, and to investigate a possible pharmacokineticExpand
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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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Pharmacokinetic Interaction Between Tadalafil and Bosentan in Healthy Male Subjects
Tadalafil, an oral phosphodiesterase 5 (PDE5) inhibitor, is being investigated as a treatment for pulmonary arterial hypertension. Bosentan is an oral endothelin receptor antagonist widely used inExpand
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Multiple-dose clinical pharmacology of the catechol-O-methyl-transferase inhibitor tolcapone in elderly subjects
Abstract.Objective: The purpose of this study was to assess the multiple-dose clinical pharmacology of tolcapone, a novel catechol-O-methyltransferase (COMT) inhibitor, in elderly subjects.Expand
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