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

Investigation of mutual pharmacokinetic interactions between macitentan, a novel endothelin receptor antagonist, and sildenafil in healthy subjects

(2014) Patricia N. Sidharta et al.   BRITISH JOURNAL OF CLINICAL PHARMACOLOGY

Investigation of the Effect of Macitentan on the Pharmacokinetics and Pharmacodynamics of Warfarin in Healthy Male Subjects

(2014) Patricia N. Sidharta et al.   CLINICAL DRUG INVESTIGATION

CYP2C9, SLCO1B1, SLCO1B3, and ABCB11 Polymorphisms in Patients With Bosentan-Induced Liver Toxicity

(2014) M Roustit et al.   CLINICAL PHARMACOLOGY & THERAPEUTICS

Effectiveness of Spironolactone Plus Ambrisentan for Treatment of Pulmonary Arterial Hypertension (from the [ARIES] Study 1 and 2 Trials)

(2013) Bradley A. Maron et al.   AMERICAN JOURNAL OF CARDIOLOGY

Investigation of the Effects of Ketoconazole on the Pharmacokinetics of Macitentan, a Novel Dual Endothelin Receptor Antagonist, in Healthy Subjects

(2013) Jacob Atsmon et al.   CLINICAL PHARMACOKINETICS

Association of CYP2C9*2 With Bosentan-Induced Liver Injury

(2013) S M Markova et al.   CLINICAL PHARMACOLOGY & THERAPEUTICS

Interaction profile of macitentan, a new non-selective endothelin-1 receptor antagonist, in vitro

(2013) Johanna Weiss et al.   EUROPEAN JOURNAL OF PHARMACOLOGY

Relative bioavailability of a newly developed pediatric formulation of bosentan vs. the adult formulation

(2013) Marcelo M. Gutierrez et al.   INTERNATIONAL JOURNAL OF CLINICAL PHARMACOLOGY AND THERAPEUTICS

An exploratory panel of biomarkers for risk prediction in pulmonary hypertension: Emerging role of CT-proET-1

(2013) João Silva Marques et al.   JOURNAL OF HEART AND LUNG TRANSPLANTATION

Macitentan and Morbidity and Mortality in Pulmonary Arterial Hypertension

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

Dysregulated Renin–Angiotensin–Aldosterone System Contributes to Pulmonary Arterial Hypertension

(2012) Frances S. de Man et al.   AMERICAN JOURNAL OF RESPIRATORY AND CRITICAL CARE MEDICINE

Neurohormonal Axis in Patients with Pulmonary Arterial Hypertension

(2012) Frances S. de Man et al.   AMERICAN JOURNAL OF RESPIRATORY AND CRITICAL CARE MEDICINE

Endothelin Axis Is Upregulated in Human and Rat Right Ventricular Hypertrophy

(2012) Jayan Nagendran et al.   CIRCULATION RESEARCH

Relation of Bosentan, Iloprost, and Sildenafil with Growth Factor Levels in Monocrotaline-Induced Pulmonary Hypertension

(2012) Semra Yigitaslan et al.   CLINICAL AND EXPERIMENTAL HYPERTENSION

Leptin and regulatory T-lymphocytes in idiopathic pulmonary arterial hypertension

(2012) Alice Huertas et al.   EUROPEAN RESPIRATORY JOURNAL

Efficacy, safety and pharmacokinetics of bosentan in portopulmonary hypertension

(2012) L. Savale et al.   EUROPEAN RESPIRATORY JOURNAL

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

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

(2012) John Gatfield et al.   PLoS One

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

(2012) Shirin Bruderer et al.   XENOBIOTICA

An update on the use of ambrisentan in pulmonary arterial hypertension

(2012) Michele D’Alto   Therapeutic Advances in Respiratory Disease

Effect of Cyclosporine and Rifampin on the Pharmacokinetics of Macitentan, a Tissue-Targeting Dual Endothelin Receptor Antagonist

(2011) Shirin Bruderer et al.   AAPS Journal

Long-Term Pulmonary Hemodynamic Effects of Ambrisentan in Pulmonary Arterial Hypertension

(2011) James R. Klinger et al.   AMERICAN JOURNAL OF CARDIOLOGY

Ambrisentan

(2011) James E. Frampton   American Journal of Cardiovascular Drugs

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

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

Sitaxentan-related acute liver failure in a patient with pulmonary arterial hypertension

(2011) W.-T. N. Lee et al.   EUROPEAN RESPIRATORY JOURNAL

Endothelin receptor expression in idiopathic pulmonary arterial hypertension: effect of bosentan and epoprostenol treatment

(2011) S. M. Hall et al.   EUROPEAN RESPIRATORY JOURNAL

Clinical Pharmacokinetics and Drug-Drug Interactions of Endothelin Receptor Antagonists in Pulmonary Arterial Hypertension

(2011) Jürgen Venitz et al.   JOURNAL OF CLINICAL PHARMACOLOGY

Bosentan attenuates right ventricular hypertrophy and fibrosis in normobaric hypoxia model of pulmonary hypertension

(2011) Gaurav Choudhary et al.   JOURNAL OF HEART AND LUNG TRANSPLANTATION

Treatment of pulmonary arterial hypertension with targeted therapies

(2011) Dermot S. O'Callaghan et al.   Nature Reviews Cardiology

Autocrine Fibroblast Growth Factor-2 Signaling Contributes to Altered Endothelial Phenotype in Pulmonary Hypertension

(2010) Ly Tu et al.   AMERICAN JOURNAL OF RESPIRATORY CELL AND MOLECULAR BIOLOGY

Mutual pharmacokinetic interactions between bosentan and lopinavir/ritonavir in healthy participants

(2010) Jasper Dingemanse et al.   ANTIVIRAL THERAPY

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

Effect of Steady-State Ambrisentan on the Pharmacokinetics of a Single Dose of the Oral Contraceptive Norethindrone (Norethisterone) 1 mg/Ethinylestradiol 35 μg in Healthy Subjects

(2010) Rebecca Spence et al.   CLINICAL DRUG INVESTIGATION

Long-term efficacy of bosentan in treatment of pulmonary arterial hypertension in children

(2010) A. A. Hislop et al.   EUROPEAN RESPIRATORY JOURNAL

Short and long term anti-inflammatory effects of bosentan therapy in patients with pulmonary arterial hypertension: relation to clinical and hemodynamic responses

(2010) George K Karavolias et al.   EXPERT OPINION ON THERAPEUTIC TARGETS

Bosentan

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

Pharmacokinetic and clinical profile of a novel formulation of bosentan in children with pulmonary arterial hypertension: the FUTURE-1 study

(2009) Maurice Beghetti 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

Liver toxicity: the Achilles' heel of endothelin receptor antagonist therapy?

(2009) M. M. Hoeper   EUROPEAN RESPIRATORY JOURNAL

Long-Term Ambrisentan Therapy for the Treatment of Pulmonary Arterial Hypertension

(2009) Ronald J. Oudiz et al.   JOURNAL OF THE AMERICAN COLLEGE OF CARDIOLOGY

Cellular and Molecular Basis of Pulmonary Arterial Hypertension

(2009) Nicholas W. Morrell et al.   JOURNAL OF THE AMERICAN COLLEGE OF CARDIOLOGY

Endothelin receptor blockade in the management of pulmonary arterial hypertension: Selective and dual antagonism

(2009) Terence K. Trow et al.   RESPIRATORY MEDICINE

Ambrisentan Therapy in Patients With Pulmonary Arterial Hypertension Who Discontinued Bosentan or Sitaxsentan Due to Liver Function Test Abnormalities

(2008) Michael D. McGoon et al.   CHEST

Ambrisentan for the Treatment of Pulmonary Arterial Hypertension

(2008) Nazzareno Galiè et al.   CIRCULATION

Endothelin receptor antagonists in pulmonary arterial hypertension

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

An antiproliferative BMP-2/PPARγ/apoE axis in human and murine SMCs and its role in pulmonary hypertension

(2008) Georg Hansmann et al.   JOURNAL OF CLINICAL INVESTIGATION

Pharmacology of Macitentan, an Orally Active Tissue-Targeting Dual Endothelin Receptor Antagonist

(2008) M. Iglarz et al.   JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS

Treatment of patients with mildly symptomatic pulmonary arterial hypertension with bosentan (EARLY study): a double-blind, randomised controlled trial

(2008) N Galiè et al.   LANCET