From the Cover: MechanisticInsights in Cytotoxic and Cholestatic Potential of the Endothelial Receptor Antagonists Using HepaRG Cells

Disruption of BSEP Function in HepaRG Cells Alters Bile Acid Disposition and Is a Susceptive Factor to Drug-Induced Cholestatic Injury

(2016) Xi Qiu et al.   MOLECULAR PHARMACEUTICS

Update on pulmonary arterial hypertension pharmacotherapy

(2016) Arash Velayati et al.   POSTGRADUATE MEDICINE

Rho-kinase/myosin light chain kinase pathway plays a key role in the impairment of bile canaliculi dynamics induced by cholestatic drugs

(2016) Ahmad Sharanek et al.   Scientific Reports

Pharmacokinetic and pharmacodynamic evaluation of macitentan, a novel endothelin receptor antagonist for the treatment of pulmonary arterial hypertension

(2015) Patricia N Sidharta et al.   Expert Opinion on Drug Metabolism & Toxicology

Comparative Localization and Functional Activity of the Main Hepatobiliary Transporters in HepaRG Cells and Primary Human Hepatocytes

(2015) Pamela Bachour-El Azzi et al.   TOXICOLOGICAL SCIENCES

Cellular Accumulation and Toxic Effects of Bile Acids in Cyclosporine A-Treated HepaRG Hepatocytes

(2015) Ahmad Sharanek et al.   TOXICOLOGICAL SCIENCES

Pharmacokinetic–Pharmacodynamic Relationships of Macitentan, a New Endothelin Receptor Antagonist, After Multiple Dosing in Healthy Korean Subjects

(2014) Li Young Ahn et al.   American Journal of Cardiovascular Drugs

Clinical Pharmacology of Endothelin Receptor Antagonists Used in the Treatment of Pulmonary Arterial Hypertension

(2014) Marie-Camille Chaumais et al.   American Journal of Cardiovascular Drugs

Macitentan for the treatment of pulmonary arterial hypertension

(2014) Namita Sood   EXPERT OPINION ON PHARMACOTHERAPY

Long-term results from the EARLY study of bosentan in WHO functional class II pulmonary arterial hypertension patients

(2014) Gérald Simonneau et al.   INTERNATIONAL JOURNAL OF CARDIOLOGY

Evaluation of the Endothelin Receptor Antagonists Ambrisentan, Bosentan, Macitentan, and Sitaxsentan as Hepatobiliary Transporter Inhibitors and Substrates in Sandwich-Cultured Human Hepatocytes

(2014) Eve-Irene Lepist et al.   PLoS One

Different Dose-Dependent Mechanisms Are Involved in Early Cyclosporine A-Induced Cholestatic Effects in HepaRG Cells

(2014) Ahmad Sharanek et al.   TOXICOLOGICAL SCIENCES

Bioactivation of Sitaxentan in Liver Microsomes, Hepatocytes, and Expressed Human P450s with Characterization of the Glutathione Conjugate by Liquid Chromatography Tandem Mass Spectrometry

(2013) John C. L. Erve et al.   CHEMICAL RESEARCH IN TOXICOLOGY

Double-Blind, Placebo-Controlled Clinical Trial With a Rho-Kinase Inhibitor in Pulmonary Arterial Hypertension

(2013) Yoshihiro Fukumoto et al.   CIRCULATION JOURNAL

Macitentan and Morbidity and Mortality in Pulmonary Arterial Hypertension

(2013) Tomás Pulido et al.   NEW ENGLAND JOURNAL OF MEDICINE

A Multifactorial Approach to Hepatobiliary Transporter Assessment Enables Improved Therapeutic Compound Development

(2013) Ryan E. Morgan et al.   TOXICOLOGICAL SCIENCES

Early Identification of Clinically Relevant Drug Interactions With the Human Bile Salt Export Pump (BSEP/ABCB11)

(2013) Jenny M. Pedersen et al.   TOXICOLOGICAL SCIENCES

Influence of sildenafil and tadalafil on the enzyme- and transporter-inducing effects of bosentan and ambrisentan in LS180 cells

(2012) Johanna Weiss et al.   BIOCHEMICAL PHARMACOLOGY

Oxidative stress plays a major role in chlorpromazine-induced cholestasis in human HepaRG cells

(2012) Sébastien Anthérieu et al.   HEPATOLOGY

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

(2012) Martin H. Bolli et al.   JOURNAL OF MEDICINAL CHEMISTRY

Long-Term Hepatic Safety of Ambrisentan in Patients With Pulmonary Arterial Hypertension

(2012) Ori Ben-Yehuda et al.   JOURNAL OF THE AMERICAN COLLEGE OF CARDIOLOGY

Clinical safety, pharmacokinetics, and efficacy of ambrisentan therapy in children with pulmonary arterial hypertension

(2012) Shinichi Takatsuki et al.   PEDIATRIC PULMONOLOGY

Slow Receptor Dissociation Kinetics Differentiate Macitentan from Other Endothelin Receptor Antagonists in Pulmonary Arterial Smooth Muscle Cells

(2012) John Gatfield et al.   PLoS One

An overview of the preclinical toxicity and potential carcinogenicity of sitaxentan (Thelin®), a potent endothelin receptor antagonist developed for pulmonary arterial hypertension

(2012) Keith Owen et al.   REGULATORY TOXICOLOGY AND PHARMACOLOGY

Absorption, distribution, metabolism, and excretion of macitentan, a dual endothelin receptor antagonist, in humans

(2012) Shirin Bruderer et al.   XENOBIOTICA

Pulmonary Arterial Hypertension

(2011) Vallerie V. McLaughlin et al.   CURRENT PROBLEMS IN CARDIOLOGY

Macitentan: entry-into-humans study with a new endothelin receptor antagonist

(2011) Patricia N. Sidharta et al.   EUROPEAN JOURNAL OF CLINICAL PHARMACOLOGY

Liver toxicity of sitaxentan in pulmonary arterial hypertension

(2011) N. Galie et al.   EUROPEAN RESPIRATORY JOURNAL

Automated detection of hepatotoxic compounds in human hepatocytes using HepaRG cells and image-based analysis of mitochondrial dysfunction with JC-1 dye

(2011) K. Pernelle et al.   TOXICOLOGY AND APPLIED PHARMACOLOGY

Evaluation of the endothelin receptor antagonists ambrisentan, darusentan, bosentan, and sitaxsentan as substrates and inhibitors of hepatobiliary transporters in sandwich-cultured human hepatocytesThis article is one of a selection of papers published in the two-part special issue entitled 20 Years of Endothelin Research.

(2010) J. Craig Hartman et al.   CANADIAN JOURNAL OF PHYSIOLOGY AND PHARMACOLOGY

Bosentan

(2009) Sohita Dhillon et al.   American Journal of Cardiovascular Drugs

The effects of sitaxentan on sildenafil pharmacokinetics and pharmacodynamics in healthy subjects

(2009) Fiona Stavros et al.   BRITISH JOURNAL OF CLINICAL PHARMACOLOGY

Sitaxentan-induced hepatic failure in two patients with pulmonary arterial hypertension

(2009) A. Lavelle et al.   EUROPEAN RESPIRATORY JOURNAL

Ambrisentan

(2008) Jamie D Croxtall et al.   DRUGS

Endothelin receptor antagonists in pulmonary arterial hypertension

(2008) J. Dupuis et al.   EUROPEAN RESPIRATORY JOURNAL