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Macitentan

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https://www.readbyqxmd.com/read/29039837/-a-patient-with-severe-idiopathic-pulmonary-arterial-hypertension-is-there-a-way-out
#1
N A Tsareva, S N Avdeev, G V Neklyudova
The paper considers a clinical example of current therapy for idiopathic pulmonary arterial hypertension in a female patient with its clinical deterioration. It shows the tactics of switching from one drug (bosentan) to others (macitentan) within in the same pathogenetic therapy group (endothelin receptor antagonists). The latest pulmonary hypertension classification (Nice, 2013) is presented. The current strategies of pathogenetic therapy for pulmonary hypertension are discussed.
2017: Terapevticheskiĭ Arkhiv
https://www.readbyqxmd.com/read/28919201/macitentan-for-the-treatment-of-inoperable-chronic-thromboembolic-pulmonary-hypertension-merit-1-results-from-the-multicentre-phase-2-randomised-double-blind-placebo-controlled-study
#2
Hossein-Ardeschir Ghofrani, Gérald Simonneau, Andrea M D'Armini, Peter Fedullo, Luke S Howard, Xavier Jaïs, David P Jenkins, Zhi-Cheng Jing, Michael M Madani, Nicolas Martin, Eckhard Mayer, Kelly Papadakis, Dominik Richard, Nick H Kim
BACKGROUND: Macitentan is beneficial for long-term treatment of pulmonary arterial hypertension. The microvasculopathy of chronic thromboembolic pulmonary hypertension (CTEPH) and pulmonary arterial hypertension are similar. METHODS: The phase 2, double-blind, randomised, placebo-controlled MERIT-1 trial assessed macitentan in 80 patients with CTEPH adjudicated as inoperable. Patients identified as WHO functional class II-IV with a pulmonary vascular resistance (PVR) of at least 400 dyn·s/cm(5) and a walk distance of 150-450 m in 6 min were randomly assigned (1:1), via an interactive voice/web response system, to receive oral macitentan (10 mg once a day) or placebo...
September 8, 2017: Lancet Respiratory Medicine
https://www.readbyqxmd.com/read/28919198/macitentan-for-treatment-of-cteph-why-merit-merits-attention
#3
Adam Torbicki
No abstract text is available yet for this article.
September 8, 2017: Lancet Respiratory Medicine
https://www.readbyqxmd.com/read/28867027/macitentan-in-pulmonary-arterial-hypertension-associated-with-congenital-heart-defects
#4
EDITORIAL
Julie Wacker, Robert G Weintraub
No abstract text is available yet for this article.
October 2017: Heart, Lung & Circulation
https://www.readbyqxmd.com/read/28779766/the-discovery-of-macitentan-a-standard-medicinal-chemistry-program
#5
Martin H Bolli
A plethora of properties are typically studied during a medicinal chemistry program and many of these parameters may shape the cascade of compound selection. Given the task to discover a molecule with a profile superior to that of the dual endothelin receptor antagonist bosentan, we tailored our compound profiling cascade to the specific properties that were not optimal in bosentan, namely in vivo efficacy and safety. Contrary to conventional thinking, we therefore focused on corresponding in vivo experiments...
August 9, 2017: Chimia
https://www.readbyqxmd.com/read/28708138/blocking-endothelin-1-receptor-%C3%AE-catenin-circuit-sensitizes-to-chemotherapy-in-colorectal-cancer
#6
Roberta Cianfrocca, Laura Rosanò, Piera Tocci, Rosanna Sestito, Valentina Caprara, Valeriana Di Castro, Ruggero De Maria, Anna Bagnato
The limited clinical response to conventional chemotherapeutics observed in colorectal cancer (CRC) may be related to the connections between the hyperactivated β-catenin signaling and other pathways in CRC stem-like cells (CRC-SC). Here, we show the mechanistic link between the endothelin-1 (ET-1)/ET-1 receptor (ET-1R) signaling and β-catenin pathway through the specific interaction with the signal transducer β-arrestin1 (β-arr1), which initiates signaling cascades as part of the signaling complex. Using a panel of patient-derived CRC-SC, we show that these cells secrete ET-1 and express ETAR and β-arr1, and that the activation of ETAR/β-arr1 axis promotes the cross-talk with β-catenin signaling to sustain stemness, epithelial-to-mesenchymal transition (EMT) phenotype and response to chemotherapy...
October 2017: Cell Death and Differentiation
https://www.readbyqxmd.com/read/28671484/recommendations-for-the-clinical-management-of-patients-receiving-macitentan-for-pulmonary-arterial-hypertension-pah-a-delphi-consensus-document
#7
Franck F Rahaghi, Hassan M Alnuaimat, Rana L A Awdish, Vijay P Balasubramanian, Robert C Bourge, Charles D Burger, John Butler, C Gregory Cauthen, Murali M Chakinala, Bennett P deBoisblanc, Michael S Eggert, Peter Engel, Jeremy Feldman, J Wesley McConnell, Myung Park, Jeffrey S Sager, Namita Sood, Harold I Palevsky
In patients treated with macitentan (Opsumit®, Actelion Pharmaceuticals Ltd., Basel, Switzerland) for pulmonary arterial hypertension (PAH), prevention and/or effective management of treatment-related adverse events may improve adherence. However, management of these adverse events can be challenging and the base of evidence and clinical experience for macitentan is limited. In the absence of evidence, consensus recommendations from physicians experienced in using macitentan to treat PAH may benefit patients and physicians who are using macitentan...
July 2017: Pulmonary Circulation
https://www.readbyqxmd.com/read/28628863/simultaneous-quantification-of-endothelin-receptor-antagonists-and-phosphodiesterase-5-inhibitors-currently-used-in-pulmonary-arterial-hypertension
#8
Yeliz Enderle, Lukas Witt, Heinrike Wilkens, Ekkehard Grünig, Walter E Haefeli, Jürgen Burhenne
Combination treatment with endothelin receptor antagonists (ERA) and phosphodiesterase 5 inhibitors (PDE5I) improved efficacy of pulmonary arterial hypertension (PAH) therapy. However, drug-drug interactions, variable exposure, non-adherence can influence plasma levels. For these reasons, drug quantification may be advantageous particularly in patients with poor treatment responses. We developed, validated, and applied an assay for the simultaneous quantification of ambrisentan, bosentan, macitentan, sildenafil, and tadalafil as well as their main (and partly active) metabolites in human plasma...
September 5, 2017: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/28558396/-german-guideline-for-idiopathic-pulmonary-fibrosis-update-on-pharmacological-therapies-2017
#9
Jürgen Behr, Andreas Günther, Francesco Bonella, Klaus Geißler, Dirk Koschel, Michael Kreuter, Antje Prasse, Nicolas Schönfeld, Helmut Sitter, Joachim Müller-Quernheim, Ulrich Costabel
Idiopathic pulmonary fibrosis (IPF) is a severe and often fatal disease with a median survival of 2 - 4 years after diagnosis. Since the publication of the German IPF guideline in 2013 new treatment trials have been published, necessitating an update of the pharmacological therapy of IPF. Different from the previous guideline, the GRADE system was discarded and replaced by the Oxford evidence classification system which allows a more differentiated judgement. The following pharmacological therapies were rated not suitable for the treatment of IPF patients (recommendation A; evidence 1-b): triple therapy with prednisolone, azathioprine and acetyl-cysteine; imatinib; ambrisentan; bosentan; macitentan...
July 2017: Pneumologie
https://www.readbyqxmd.com/read/28550241/acute-effects-of-moderate-altitude-on-biomarkers-of-cardiovascular-inflammation-and-endothelial-function-and-their-differential-modulation-by-dual-endothelin-receptor-blockade
#10
Michael Lichtenauer, Bjoern Goebel, Vera Paar, Bernhard Wernly, Thomas Gecks, Ilonka Rohm, Martin Förster, Stefan Betge, Hans R Figulla, Uta C Hoppe, Malte Kelm, Marcus Franz, Christian Jung
BACKGROUND: Endothelial dysfunction is accompanied by the release of microparticles (MP). OBJECTIVE: We sought to investigate the effect of moderate hypoxia on circulatory levels of microparticles, biomarkers of cardiovascular function and inflammation and on echocardiographic parameters in healthy volunteers staying at an altitude of 2978 m. METHODS: Eighteen healthy volunteers were subjected to moderate hypoxia by staying at 2978 m above sea level for three days...
2017: Clinical Hemorheology and Microcirculation
https://www.readbyqxmd.com/read/28532389/the-use-of-macitentan-in-fontan-circulation-a-case-report
#11
Polyvios Demetriades, Amir Aziz, Robin Condliffe, Sarah E Bowater, Paul F Clift
BACKGROUND: The Fontan circulation, a result of a palliative procedure in patients with single systemic ventricles, is defined by chronically elevated pulmonary vascular resistance. When traditional heart failure therapies fail, pharmacological agents that reduce pulmonary artery pressures may be used. These include endothelial-receptor antagonists, prostanoids and phosphodiesterase type 5 inhibitors. We report the first use of macitentan, an endothelin-receptor antagonist, in a patient with a Fontan circulation...
May 22, 2017: BMC Cardiovascular Disorders
https://www.readbyqxmd.com/read/28494463/plasma-drug-concentrations-in-patients-with-pulmonary-arterial-hypertension-on-combination-treatment
#12
Ekkehard Grünig, Johanna Ohnesorge, Nicola Benjamin, Jürgen Burhenne, Yeliz Enderle, Benjamin Egenlauf, Christine Fischer, Satenik Harutyunova, Andrea Huppertz, Hans Klose, Walter E Haefeli
BACKGROUND: Combination therapy with the phosphodiesterase type 5 inhibitors (PDE-5i) sildenafil or tadalafil and the endothelin receptor antagonists (ERA) bosentan, ambrisentan, or macitentan may cause mutual pharmacokinetic interactions in patients with pulmonary arterial hypertension (PAH). OBJECTIVE: The objective of this study was to analyze plasma drug concentrations in PAH patients receiving different combination treatments. METHODS: PAH patients receiving a stable combination treatment with ERA and PDE-5i with targeted dosage for at least 1 month were routinely assessed, including clinical parameters and plasma drug concentrations...
2017: Respiration; International Review of Thoracic Diseases
https://www.readbyqxmd.com/read/28462837/design-synthesis-and-evaluation-of-1-3-6-trisubstituted-4-oxo-1-4-dihydroquinoline-2-carboxylic-acid-derivatives-as-eta-receptor-selective-antagonists-using-fret-assay
#13
Nikhil Khadtare, Ralph Stephani, Vijaya Korlipara
The endothelin axis and in particular the two receptor subtypes, ETA and ETB, are under investigation for the treatment of various diseases such as pulmonary arterial hypertension, fibrosis, renal failure and cancer. Previous work in our lab has shown that 1,3,6-trisubstituted-4-oxo-1,4-dihydroquinoline-2-carboxylic acid derivatives exhibit noteworthy endothelin receptor antagonist activity. A series of analogues with modifications centered around position 6 of the heterocyclic quinolone core and replacement of the aryl carboxylic acid group with an isosteric tetrazole ring was designed and synthesized to further optimize the structure activity relationship...
June 1, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28378883/pharmacokinetics-of-macitentan-in-patients-with-pulmonary-arterial-hypertension-and-comparison-with-healthy-subjects
#14
Milena Issac, Jasper Dingemanse, Patricia N Sidharta
Macitentan is a worldwide approved dual endothelin receptor antagonist that has demonstrated efficacy in the treatment of pulmonary arterial hypertension (PAH) in a phase 3 clinical trial, SERAPHIN, at a dose of 10 mg once daily. During this trial, trough plasma concentrations (Ctrough ) of macitentan and its active metabolite,  ACT-132577,  were obtained at steady state in 242 patients, indicating that mean Ctrough of both analytes was about 2-fold higher in PAH patients than in healthy subjects. To further investigate the pharmacokinetics (PK) of macitentan and its active metabolite, ACT-132577,  a 24-hour PK profile was recorded at steady state in 20 PAH patients in the open-label extension of SERAPHIN...
August 2017: Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/28378734/-pharmacoeconomic-aspects-of-macitentan-in-the-therapy-of-pulmonary-arterial-hypertension
#15
O M Moiseeva, A V Rudakova
AIM: To provide a pharmacoeconomic estimate of macitentan versus bosentan in therapy for pulmonary arterial hypertension (PAH). SUBJECT AND METHODS: An analysis was carried out on the basis of a social perspective for patients, whose mean age was 50 years. A budget impact analysis was performed without discounting; with the time horizon of the study being 5 years. Assessing the cost- effectiveness of endothelin receptor antagonists used a Markov model based on the meta-analysis of clinical trials...
2017: Terapevticheskiĭ Arkhiv
https://www.readbyqxmd.com/read/28369585/from-the-cover-mechanisticinsights-in-cytotoxic-and-cholestatic-potential-of-the-endothelial-receptor-antagonists-using-heparg-cells
#16
Matthew Gibson Burbank, Ahmad Sharanek, Audrey Burban, Hervé Mialanne, Hélène Aerts, Christiane Guguen-Guillouzo, Richard John Weaver, André Guillouzo
Several endothelin receptor antagonists (ERAs) have been developed for the treatment of pulmonary arterial hypertension (PAH). Some of them have been related to clinical cases of hepatocellular injury (sitaxentan [SIT]) and/or cholestasis (bosentan [BOS]). We aimed to determine if ambrisentan (AMB) and macitentan (MAC), in addition to BOS and SIT, could potentially cause liver damage in man by use of human HepaRG cells. Our results showed that like BOS, MAC-induced cytotoxicity and cholestatic disorders characterized by bile canaliculi dilatation and impairment of myosin light chain kinase signaling...
June 1, 2017: Toxicological Sciences: An Official Journal of the Society of Toxicology
https://www.readbyqxmd.com/read/28329315/seraphin-haemodynamic-substudy-the-effect-of-the-dual-endothelin-receptor-antagonist-macitentan-on-haemodynamic-parameters-and-nt-probnp-levels-and-their-association-with-disease-progression-in-patients-with-pulmonary-arterial-hypertension
#17
Nazzareno Galiè, Pavel Jansa, Tomás Pulido, Richard N Channick, Marion Delcroix, Hossein-Ardeschir Ghofrani, Franck-Olivier Le Brun, Sanjay Mehta, Loïc Perchenet, Lewis J Rubin, B K S Sastry, Gérald Simonneau, Olivier Sitbon, Rogério Souza, Adam Torbicki
Aims: The effect of macitentan on haemodynamic parameters and NT-proBNP levels was evaluated in pulmonary arterial hypertension (PAH) patients in the SERAPHIN study. Association between these parameters and disease progression, assessed by the primary endpoint (time to first morbidity/mortality event), was explored. Methods and results: Of the 742 randomized patients, 187 with right heart catheterization at baseline and month 6 participated in a haemodynamic sub-study...
April 14, 2017: European Heart Journal
https://www.readbyqxmd.com/read/28300593/functional-estimation-of-endothelin-1-receptor-antagonism-by-bosentan-macitentan-and-ambrisentan-in-human-pulmonary-and-radial-arteries-in-vitro
#18
James A Angus, Paul F Soeding, Richard J A Hughes, Christine E Wright
BACKGROUND: Endothelin receptor antagonists are approved for pulmonary arterial hypertension. Development of selective ETA-receptor antagonists over mixed or dual receptor antagonists has depended on a range of receptor binding assays, second messenger assays and functional blood vessel assays. This study compared the 3 clinically-approved endothelin receptor antagonists in assays of human isolated pulmonary and radial arteries in vitro. METHODS: Human isolated pulmonary (i...
June 5, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28283234/endothelin-inhibitors-lower-pulmonary-vascular-resistance-and-improve-functional-capacity-in-patients-with-fontan-circulation
#19
Gabriella Agnoletti, Simona Gala, Francesca Ferroni, Roberto Bordese, Lorenzo Appendini, Carlo Pace Napoleone, Laura Bergamasco
OBJECTIVES: To evaluate the effects of endothelin inhibitors (ERAs) on hemodynamic and functional parameters in patients post-Fontan procedure with high pulmonary vascular resistance (PVR). METHODS: Among our cohort of patients with Fontan circulation, 8 children, 8 adolescents, and 8 adults had PVR ≥2 WU*m(2). These patients were treated with ERAs (minors with bosentan, adults with macitentan) and reevaluated after 6 months. Pre- and posttreatment hemodynamic variables were assessed by cardiac catheterization...
February 10, 2017: Journal of Thoracic and Cardiovascular Surgery
https://www.readbyqxmd.com/read/28257550/tolerability-of-switch-to-macitentan-from-bosentan-in-pulmonary-arterial-hypertension
#20
Zeenat Safdar, Aishwarya Thakur, Adaani Frost
OBJECTIVES: Pulmonary arterial hypertension (PAH) is a progressive disease that can be treated with several medications. Macitentan, an endothelin receptor antagonist (ERA), has received approval as a PAH therapy. We report our data regarding the tolerability in patients with PAH who were switched from bosentan to macitentan. METHODS: At the Baylor Pulmonary Hypertension Program, 24 patients with PAH who had been taking bosentan and were switched to macitentan were identified in this retrospective study...
March 2017: Southern Medical Journal
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