keyword
MENU ▼
Read by QxMD icon Read
search

Macitentan

keyword
https://www.readbyqxmd.com/read/29660192/characterization-of-degradation-products-of-macitentan-under-various-stress-conditions-by-using-liquid-chromatography-mass-spectrometry
#1
Naga Veera Yerra, Pavankumar Pallerla, Sukanya Pandeti, Jean-Claude Tabet, Jagadeshwar Reddy Thota
RATIONALE: Stress testing of a drug candidate is an important step in drug discovery and development process. The presence of degradation products in a drug affects the quality as well as safety and efficacy of drug formulation. Hence, it is essential to develop an efficient analytical method which could be useful for the separation, identification and characterization of all possible degradation products of drug. Macitentan (MT) is an endothelin receptor antagonist (ERA) drug used to treat high blood pressure in the lungs...
April 16, 2018: Rapid Communications in Mass Spectrometry: RCM
https://www.readbyqxmd.com/read/29623530/novel-insights-and-treatment-strategies-for-right-heart-failure
#2
REVIEW
Weiqin Lin, Ai-Ling Poh, W H Wilson Tang
PURPOSE OF REVIEW: The function of the right ventricle (RV) is intimately linked to its preload (systemic volume status) and afterload (pulmonary vasculature). In this review, we explore current knowledge in RV physiology, RV function assessment, causes of right heart failure (RHF), and specific treatment strategies for RHF. RECENT FINDINGS: We examine the evidence behind new pharmacological therapies available, such as macitentan and riociguat in the treatment of specific etiologies of RHF...
April 6, 2018: Current Heart Failure Reports
https://www.readbyqxmd.com/read/29590122/association-between-six-minute-walk-distance-and-long-term-outcomes-in-patients-with-pulmonary-arterial-hypertension-data-from-the-randomized-seraphin-trial
#3
Rogério Souza, Richard N Channick, Marion Delcroix, Nazzareno Galiè, Hossein-Ardeschir Ghofrani, Pavel Jansa, Franck-Olivier Le Brun, Sanjay Mehta, Loïc Perchenet, Tomás Pulido, B K S Sastry, Olivier Sitbon, Adam Torbicki, Lewis J Rubin, Gérald Simonneau
BACKGROUND: Patients with pulmonary arterial hypertension who achieve a six-minute walk distance of 380-440 m may have improved prognosis. Using the randomized controlled trial of macitentan in pulmonary arterial hypertension (SERAPHIN), the association between six-minute walk distance and long-term outcomes was explored. METHODS: Patients with six-minute walk distance data at Month 6 were dichotomized as above or below the median six-minute walk distance (400 m) and assessed for future risk of pulmonary arterial hypertension-related death or hospitalization and all-cause death...
2018: PloS One
https://www.readbyqxmd.com/read/29501590/modeling-of-pharmacokinetics-efficacy-and-hemodynamic-effects-of-macitentan-in-patients-with-pulmonary-arterial-hypertension
#4
Andreas Krause, Jochen Zisowsky, Jasper Dingemanse
BACKGROUND: Macitentan is the first endothelin receptor antagonist with demonstrated efficacy on morbidity and mortality in pulmonary arterial hypertension (PAH) in the pivotal study SERAPHIN. METHODS: The pharmacokinetics (PK) of macitentan and its active metabolite, ACT-132577, were characterized in a population model. Efficacy and hemodynamics (pharmacodynamics, PD) were related to PK based on PK/PD modeling. RESULTS: Sex, age, and body weight influenced the PK to a statistically significant extent...
February 28, 2018: Pulmonary Pharmacology & Therapeutics
https://www.readbyqxmd.com/read/29447737/pulmonary-arterial-hypertension-related-morbidity-is-prognostic-for-mortality
#5
Vallerie V McLaughlin, Marius M Hoeper, Richard N Channick, Kelly M Chin, Marion Delcroix, Sean Gaine, Hossein-Ardeschir Ghofrani, Pavel Jansa, Irene M Lang, Sanjay Mehta, Tomás Pulido, B K S Sastry, Gérald Simonneau, Olivier Sitbon, Rogério Souza, Adam Torbicki, Victor F Tapson, Loïc Perchenet, Ralph Preiss, Pierre Verweij, Lewis J Rubin, Nazzareno Galiè
BACKGROUND: Registry data suggest that disease progression in pulmonary arterial hypertension (PAH) is indicative of poor prognosis. However, the prognostic relevance of PAH-related morbidity has not been formally evaluated in randomized controlled trials. OBJECTIVES: The purpose of these analyses was to assess the impact of morbidity events on the risk of subsequent mortality using the landmark method and data from the SERAPHIN and GRIPHON studies. METHODS: For each study, the risk of all-cause death up to the end of the study was assessed from the landmark time point (months 3, 6, and 12) according to whether a patient had experienced a primary endpoint morbidity event before the landmark...
February 20, 2018: Journal of the American College of Cardiology
https://www.readbyqxmd.com/read/29437943/macitentan-in-pulmonary-hypertension-due-to-left-ventricular-dysfunction
#6
Jean-Luc Vachiéry, Marion Delcroix, Hikmet Al-Hiti, Michela Efficace, Martin Hutyra, Gabriela Lack, Kelly Papadakis, Lewis J Rubin
The MELODY-1 study evaluated macitentan for pulmonary hypertension because of left heart disease (PH-LHD) in patients with combined post- and pre-capillary PH.63 patients with PH-LHD and diastolic pressure gradient ≥7 mmHg and pulmonary vascular resistance (PVR) >3WU were randomised to macitentan 10 mg (n=31) or placebo (n=32) for 12 weeks. The main end-point assessed a composite of significant fluid retention (weight gain ≥5% or ≥5 kg because of fluid overload or parenteral diuretic administration) or worsening in New York Heart Association functional class from baseline to end of treatment...
February 2018: European Respiratory Journal: Official Journal of the European Society for Clinical Respiratory Physiology
https://www.readbyqxmd.com/read/29421995/new-drugs-therapeutic-strategies-and-future-direction-for-the-treatment-of-pulmonary-arterial-hypertension
#7
Valentina Mercurio, Anna Bianco, Giacomo Campi, Alessandra Cuomo, Nermin Diab, Angela Mancini, Paolo Parrella, Mario Petretta, Paul Hassoun, Domenico Bonaduce
Despite recent advances in pulmonary arterial hypertension (PAH) treatment, this condition is still characterized by an extremely poor prognosis. In this review, we discuss the use of newly-approved drugs for PAH treatment with already known mechanisms of action (macitentan), innovative targets (riociguat and selexipag), and novel therapeutic approaches with initial up-front combination therapy. Secondly, we describe new potential signalling pathways and investigational drugs with promising role in the treatment of PAH...
January 31, 2018: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/29341047/german-guideline-for-idiopathic-pulmonary-fibrosis-update-on-pharmacological-therapies-2017
#8
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...
February 2018: Pneumologie
https://www.readbyqxmd.com/read/29286546/serious-liver-injury-associated-with-macitentan-a-case-report
#9
Thao T Tran, Allen D Brinker, Monica Muñoz
Several endothelin receptor antagonists (ERAs) that were developed for the treatment of pulmonary arterial hypertension (PAH), including bosentan and sitaxentan, have been linked to clinically significant hepatocellular injury, as well as liver failure. We describe the first case of fulminant hepatitis to be reported in association with the ERA macitentan. This case was recently identified within the U.S. Food and Drug Administration Adverse Event Reporting System (FAERS) and describes liver transplantation occurring 13 months after macitentan initiation in a young patient (23 years old) with idiopathic PAH New York Heart Association (NYHA) functional class III...
February 2018: Pharmacotherapy
https://www.readbyqxmd.com/read/29280064/macitentan-in-pulmonary-arterial-hypertension-a-focus-on-combination-therapy-in-the-seraphin-trial
#10
REVIEW
Pavel Jansa, Tomás Pulido
SERAPHIN was a double-blind, placebo-controlled, event-driven phase III trial that evaluated the effects of long-term treatment with macitentan, an oral endothelin receptor antagonist, in patients with pulmonary arterial hypertension (PAH). The majority of patients were receiving PAH therapy at enrollment, providing the opportunity to evaluate the efficacy and safety of macitentan in combination with other PAH therapies (predominantly phosphodiesterase type 5 inhibitors [PDE-5i]). In patients receiving background therapy, macitentan reduced the risk of morbidity/mortality by 38% compared with placebo (hazard ratio [HR] 0...
February 2018: American Journal of Cardiovascular Drugs: Drugs, Devices, and Other Interventions
https://www.readbyqxmd.com/read/29233198/clinical-efficacy-and-safety-of-switch-from-bosentan-to-macitentan-in-children-and-young-adults-with-pulmonary-arterial-hypertension
#11
Ebru Aypar, Dursun Alehan, Tevfik Karagöz, Hayrettin Hakan Aykan, İlker Ertugrul
BACKGROUND: Macitentan is an orally active, potent, dual endothelin receptor antagonist and is the only registered treatment for pulmonary arterial hypertension that significantly reduced morbidity and mortality in a long-term event-driven study. Aim Few studies compared the clinical efficacy and safety of switch from bosentan to macitentan only in adult patients with pulmonary arterial hypertension. We aimed to evaluate the clinical efficacy and safety of switch from bosentan to macitentan in children and young adults...
April 2018: Cardiology in the Young
https://www.readbyqxmd.com/read/29174582/macitentan-in-daily-clinical-practice-a-single-centre-1-year-experience
#12
S Cadenas-Menéndez, P Álvarez-Vega, J Martín-Moreiras, M Barreiro-Pérez, M Á Gómez-Sánchez, P L Sánchez-Fernández
The effectiveness and safety of macitentan, a dual endothelin-receptor antagonist (ERA) approved for the treatment of pulmonary arterial hypertension (PAH), were shown in an extensive clinical trial oriented towards morbidity and mortality events. Our aim was to describe a single centre's experience of the utilization of macitentan in patients with PAH in clinical practice settings. Thirteen patients with different aetiologies and previous PAH treatments were studied. After 12 months of macitentan treatment, 11 patients improved their functional class (FC), all patients improved their 6-minute walk distance (6MWD) test, and 10 patients lowered their NT-proBNP plasma levels...
November 22, 2017: Revista Portuguesa de Pneumologia
https://www.readbyqxmd.com/read/29163807/macitentan-a-double-antagonist-of-endothelin-receptors-efficiently-impairs-migration-and-microenvironmental-survival-signals-in-chronic-lymphocytic-leukemia
#13
Rossana Maffei, Stefania Fiorcari, Tiziana Vaisitti, Silvia Martinelli, Stefania Benatti, Giulia Debbia, Davide Rossi, Patrizia Zucchini, Leonardo Potenza, Mario Luppi, Gianluca Gaidano, Silvia Deaglio, Roberto Marasca
The crosstalk between chronic lymphocytic leukemia (CLL) cells and tumor microenvironment is essential for leukemic clone maintenance, supporting CLL cells survival, proliferation and protection from drug-induced apoptosis. Over the past years, the role of several soluble factors involved in these processes has been studied. CLL cells express higher levels of endothelin 1 (ET-1) and ETA receptor as compared to normal B cells. Upon ET-1 stimulation, CLL cells improve their survival and proliferation and reduce their sensitivity to the phosphoinositide-3-kinase δ inhibitor idelalisib and to fludarabine...
October 27, 2017: Oncotarget
https://www.readbyqxmd.com/read/29073911/successful-transition-from-treprostinil-to-selexipag-in-patient-with-severe-pulmonary-arterial-hypertension
#14
Asuka Furukawa, Yuichi Tamura, Hiroya Iwahori, Masato Goto, Narutaka Ohashi, Teruo Okabe, Akio Kawamura
BACKGROUND: In this report, we describe the first successful case of transition from subcutaneous administration of treprostinil to selexipag in a patient with severe pulmonary arterial hypertension (PAH), by evaluating hemodynamic changes and exercise tolerance. CASE PRESENTATION: A 38-year-old female with idiopathic PAH (IPAH) had received initial triple combination therapy (macitentan PO, tadalafil PO, and treprostinil SC) and achieved excellent improvement in hemodynamics...
October 26, 2017: BMC Pulmonary Medicine
https://www.readbyqxmd.com/read/29064353/dual-et-a-et-b-blockade-with-macitentan-improves-both-vascular-remodeling-and-angiogenesis-in-pulmonary-arterial-hypertension
#15
Valerie Nadeau, Francois Potus, Olivier Boucherat, Renee Paradis, Eve Tremblay, Marc Iglarz, Roxane Paulin, Sebastien Bonnet, Steeve Provencher
Dysregulated metabolism and rarefaction of the capillary network play a critical role in pulmonary arterial hypertension (PAH) etiology. They are associated with a decrease in perfusion of the lungs, skeletal muscles, and right ventricle (RV). Previous studies suggested that endothelin-1 (ET-1) modulates both metabolism and angiogenesis. We hypothesized that dual ETA /ETB receptors blockade improves PAH by improving cell metabolism and promoting angiogenesis. Five weeks after disease induction, Sugen/hypoxic rats presented severe PAH with pulmonary artery (PA) remodeling, RV hypertrophy and capillary rarefaction in the lungs, RV, and skeletal muscles (microCT angiogram, lectin perfusion, CD31 staining)...
January 2018: Pulmonary Circulation
https://www.readbyqxmd.com/read/29059078/macitentan-use-in-a-neurofibromatosis-type-1-patient-with-pulmonary-hypertension-and-external-jugular-phlebectasia
#16
Michele Correale, Nicola Tarantino, Giuseppe Paradiso, Ilenia Monaco, Matteo Di Biase, Natale Daniele Brunetti
No abstract text is available yet for this article.
October 20, 2017: American Journal of Therapeutics
https://www.readbyqxmd.com/read/29039837/-a-patient-with-severe-idiopathic-pulmonary-arterial-hypertension-is-there-a-way-out
#17
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
#18
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/cm5 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...
October 2017: Lancet Respiratory Medicine
https://www.readbyqxmd.com/read/28919198/macitentan-for-treatment-of-cteph-why-merit-merits-attention
#19
Adam Torbicki
No abstract text is available yet for this article.
October 2017: Lancet Respiratory Medicine
https://www.readbyqxmd.com/read/28867027/macitentan-in-pulmonary-arterial-hypertension-associated-with-congenital-heart-defects
#20
EDITORIAL
Julie Wacker, Robert G Weintraub
No abstract text is available yet for this article.
October 2017: Heart, Lung & Circulation
keyword
keyword
24272
1
2
Fetch more papers »
Fetching more papers... Fetching...
Read by QxMD. Sign in or create an account to discover new knowledge that matter to you.
Remove bar
Read by QxMD icon Read
×

Search Tips

Use Boolean operators: AND/OR

diabetic AND foot
diabetes OR diabetic

Exclude a word using the 'minus' sign

Virchow -triad

Use Parentheses

water AND (cup OR glass)

Add an asterisk (*) at end of a word to include word stems

Neuro* will search for Neurology, Neuroscientist, Neurological, and so on

Use quotes to search for an exact phrase

"primary prevention of cancer"
(heart or cardiac or cardio*) AND arrest -"American Heart Association"