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https://www.readbyqxmd.com/read/28315689/in-silico-prediction-of-hpxr-activators-using-structure-based-pharmacophore-modeling
#1
Nao Torimoto-Katori, Ruili Huang, Harutoshi Kato, Rikiya Ohashi, Menghang Xia
The activation of pregnane X receptor (PXR), a member of the nuclear receptor superfamily, can mediate potential drug-drug interactions by regulating the expression of several drug- mediated enzymes and transporters, resulting in reduced therapeutic efficacy or increased toxicity by producing reactive metabolites. Therefore, in the early stage of drug development, it is important to predict these risks using an in silico approach. We constructed a human PXR (hPXR) pharmacophore model based on known structural information of compounds that activate PXR...
March 15, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28303689/non-healing-ischaemic-digital-ulcer-in-a-systemic-sclerosis-patient-a-challenging-clinical-case
#2
Sophie Blaise, Matthieu Roustit, Alexandra Forli, Bernard Imbert, Jean-Luc Cracowski
Ischaemic digital ulcers (DUs) are an indicator of the severity of the microangiopathy in patients with systemic sclerosis (SSc). DUs are a frequent complication, affecting about 50% of patients with SSc, and are often recurrent. In cross-sectional studies involving patients with SSc, the frequency of ischaemic DUs was 12-16% with a major impact on hand function and quality of life. Effective therapy for DUs remains elusive. Intravenous iloprost has been demonstrated to have a positive effect on healing of active DUs...
March 16, 2017: International Wound 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
#3
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...
March 11, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28298655/dual-nep-ece-inhibition-improves-endothelial-function-in-mesenteric-resistance-arteries-of-32-week-old-shr
#4
Pieter Lemkens, Leon Ja Spijkers, Merlijn J Meens, Jelly Nelissen, Ben Janssen, Stephan Lm Peters, Paul Mh Schiffers, Jo Gr De Mey
Endothelin 1 (ET-1), a potent vasoconstrictor, pro-mitogenic and pro-inflammatory peptide, may promote development of endothelial dysfunction and arterial remodeling. ET-1 can be formed through cleavage of big-ET-1 by endothelin-converting enzyme (ECE) or neutral endopeptidase (NEP). We investigated whether chronic treatment with the novel dual NEP/ECE inhibitor SOL1 improves functional and structural properties of resistance-sized arteries of 32-week-old male spontaneously hypertensive rats (SHR). SHR received a chronic 4-week treatment with SOL1, losartan or hydralazine...
March 16, 2017: Hypertension Research: Official Journal of the Japanese Society of Hypertension
https://www.readbyqxmd.com/read/28289495/treatment-of-chronic-thromboembolic-pulmonary-hypertension-the-role-of-medical-therapy-and-balloon-pulmonary-angioplasty
#5
Timothy M Fernandes, David S Poch, William R Auger
Chronic thromboembolic pulmonary hypertension (CTEPH) is a potentially curable disease when treated with pulmonary thromboendarterectomy (PTE). However, even at experienced surgical centers, nearly one-third of patients with CTEPH will be deemed inoperable for reasons including distal disease, comorbidities, or out-of-proportion pulmonary hypertension. It is in these patients with inoperable CTEPH that pulmonary hypertension (PH)-targeted medical therapy and balloon pulmonary angioplasty have potential therapeutic value...
October 2016: Methodist DeBakey Cardiovascular Journal
https://www.readbyqxmd.com/read/28283234/endothelin-inhibitors-lower-pulmonary-vascular-resistance-and-improve-functional-capacity-in-patients-with-fontan-circulation
#6
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/28274813/possible-role-of-endothelin-receptor-against-hyperhomocysteinemia-and-%C3%AE-amyloid-induced-ad-type-of-vascular-dementia-in-rats
#7
Major Singh, Atish Prakash
Vascular dementia (VaD) is considered as the second commonest form of dementia after Alzheimer's disease (AD). The study was designed to investigate the effect of endothelin receptor against β-amyloid induced AD type of vascular dementia. This disease was induced by combine administration of single ICV (intracerebroventricle) infusion of β-amyloid (Aβ) once and chronic oral administration of L-Methionine for 21 days. Bosentan (dual endothelin receptor antagonist) was administered for 21 days. Behavioral alterations were observed during different time interval of the study...
March 5, 2017: Brain Research Bulletin
https://www.readbyqxmd.com/read/28273180/synthesis-in-vitro-and-in-vivo-evaluation-of-3%C3%AE-18f-fluorocholic-acid-for-the-detection-of-drug-induced-cholestasis-in-mice
#8
Stef De Lombaerde, Sara Neyt, Ken Kersemans, Jeroen Verhoeven, Lindsey Devisscher, Hans Van Vlierberghe, Christian Vanhove, Filip De Vos
INTRODUCTION: Drug-induced cholestasis is a liver disorder that might be caused by interference of drugs with the hepatobiliary bile acid transporters. It is important to identify this interference early on in drug development. In this work, Positron Emission Tomography (PET)-imaging with a 18F labeled bile acid analogue was introduced to detect disturbed hepatobiliary transport of bile acids. METHODS: 3β-[18F]fluorocholic acid ([18F]FCA) was prepared by nucleophilic substitution of a mesylated precursor with [18F]fluoride, followed by deprotection with sodium hydroxide...
2017: PloS One
https://www.readbyqxmd.com/read/28257550/tolerability-of-switch-to-macitentan-from-bosentan-in-pulmonary-arterial-hypertension
#9
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
https://www.readbyqxmd.com/read/28237536/early-experience-of-macitentan-for-pulmonary-arterial-hypertension-in-adult-congenital-heart-disease
#10
S Herbert, W Gin-Sing, L Howard, R M R Tulloh
BACKGROUND: Endothelin receptor antagonists (ERA) have been recognised as effective therapy for pulmonary arterial hypertension in congenital heart disease (CHD-PH), and Eisenmenger syndrome (ES) since the Breathe 5 study. A new dual receptor antagonist - Macitentan - is currently undergoing trials to determine its efficacy in simple ES. To date there is little information on this therapy in CHD and we report our first experience, some with more complex diseases. METHODS: Data was collected prospectively from September 2014...
February 6, 2017: Heart, Lung & Circulation
https://www.readbyqxmd.com/read/28223322/eta-receptors-blockade-by-activating-etb-receptors-increases-vascular-permeability-and-induces-exaggerated-fluid-retention
#11
Magali Vercauteren, Frederic Trensz, Anne Pasquali, Christophe Cattaneo, Daniel S Strasser, Patrick Hess, Marc Iglarz, Martine Clozel
Endothelin receptor antagonists have been associated with fluid retention. It has been suggested that, of the two endothelin receptor subtypes, ETB receptors should not be blocked, because of their involvement in natriuresis and diuresis. Surprisingly, clinical data suggest that ETA-selective antagonists pose a greater risk of fluid overload than dual antagonists. The purpose of this study was to evaluate the contribution of each endothelin receptor to fluid retention and vascular permeability in rats. Sitaxentan and ambrisentan as ETA-selective antagonists, bosentan and macitentan as dual antagonists were used as representatives of each class, respectively...
February 21, 2017: Journal of Pharmacology and Experimental Therapeutics
https://www.readbyqxmd.com/read/28214014/controlling-the-digital-ulcerative-disease-in-systemic-sclerosis-is-associated-with-improved-hand-function
#12
Luc Mouthon, Patrick H Carpentier, Catherine Lok, Pierre Clerson, Virginie Gressin, Eric Hachulla, Alice Bérezné, Elisabeth Diot, Aurélie Khau Van Kien, Patrick Jego, Christian Agard, Anne-Bénédicte Duval-Modeste, Agnès Sparsa, Eve Puzenat, Marie-Aleth Richard
OBJECTIVES: Ischemic digital ulcers (DU) represent a major complication of systemic sclerosis (SSc). We investigated the impact of controlling the ulcerative disease on disability, pain, and quality of life in SSc patients receiving bosentan. METHODS: ECLIPSE (Study AC-052-517) is a 2-year prospective, multicenter, and observational study. Patients with SSc who experienced at least 1 DU in the previous year and received bosentan were included between October 2009 and March 2011...
January 13, 2017: Seminars in Arthritis and Rheumatism
https://www.readbyqxmd.com/read/28213957/a-bosentan-pharmacokinetic-study-to-investigate-dosing-regimens-in-paediatric-patients-with-pulmonary-arterial-hypertension-future-3
#13
R M F Berger, M Gehin, M Beghetti, D Ivy, A Kusic-Pajic, P Cornelisse, S Grill, D Bonnet
AIM: To investigate whether increasing bosentan dosing frequency from 2 mg/kg twice daily (b.i.d.) to 2 mg/kg three times daily (t.i.d.) in children with pulmonary arterial hypertension (PAH) (from ≥3 months to <12 years of age) would increase exposure. METHODS: An open-label, prospective, randomised, multicentre, multiple-dose, Phase 3 study was conducted. Patients (n = 64) were randomised 1:1 to receive oral doses of bosentan of 2 mg/kg b.i...
February 18, 2017: British Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/28173639/bosentan-and-rifampin-interactions-modulate-influx-transporter-and-cytochrome-p450-expression-and-activities-in-primary-human-hepatocytes
#14
Kyoung-Moon Han, Sun-Young Ahn, Hyewon Seo, Jaesuk Yun, Hye Jin Cha, Ji-Soon Shin, Young-Hoon Kim, Hyungsoo Kim, Hye-Kyung Park, Yong-Moon Lee
The incidence of polypharmacy-which can result in drug-drug interactions-has increased in recent years. Drug-metabolizing enzymes and drug transporters are important polypharmacy modulators. In this study, the effects of bosentan and rifampin on the expression and activities of organic anion-transporting peptide (OATP) and cytochrome P450 (CYP450) 2C9 and CYP3A4 were investigated in vitro. HEK293 cells and primary human hepatocytes overexpressing the target genes were treated with bosentan and various concentrations of rifampin, which decreased the uptake activities of OATP transporters in a dose-dependent manner...
February 6, 2017: Biomolecules & Therapeutics
https://www.readbyqxmd.com/read/28156176/respirable-controlled-release-polymeric-colloid-rcrpc-of-bosentan-for-the-management-of-pulmonary-hypertension-in-vitro-aerosolization-histological-examination-and-in-vivo-pulmonary-absorption
#15
COMPARATIVE STUDY
Lydia A Hanna, Emad B Basalious, Omaima N ELGazayerly
Bosentan is an endothelin receptor antagonist (ERA) prescribed for patients with pulmonary arterial hypertension (PAH). The oral delivery of bosentan possesses several drawbacks such as low bioavailability (about 50%), short duration of action, frequent administration, hepatotoxicity and systemic hypotension. The pulmonary administration would circumvent the pre-systemic metabolism thus improving the bioavailability and avoids the systemic adverse effects of oral bosentan. However, the short duration of action and the frequent administration are the major drawbacks of inhalation therapy...
November 2016: Drug Delivery
https://www.readbyqxmd.com/read/28138822/drug-reaction-with-eosinophilia-and-systemic-symptoms-dress-syndrome-and-the-rheumatologist
#16
REVIEW
Marwan H Adwan
PURPOSE OF THE REVIEW: The purpose of the review is to summarise the various drugs used in rheumatology practice implicated in the causation of DRESS syndrome. RECENT FINDINGS: The most commonly reported drugs are allopurinol, sulfasalazine and minocycline, which pose a very high risk for DRESS syndrome development, followed by strontium ranelate and dapsone. Other, less commonly reported, drugs include leflunomide, hydroxychloroquine, non-steroidal anti-inflammatory drugs, febuxostat, bosentan and solcitinib...
January 2017: Current Rheumatology Reports
https://www.readbyqxmd.com/read/28134077/dual-endothelin-receptor-antagonists-contrast-the-effects-induced-by-endothelin-1-on-cultured-human-microvascular-endothelial-cells
#17
Stefano Soldano, Sabrina Paolino, Carmen Pizzorni, Amelia Chiara Trombetta, Paola Montagna, Renata Brizzolara, Claudio Corallo, Nicola Giordano, Alberto Sulli, Maurizio Cutolo
OBJECTIVES: To evaluate the ability of dual endothelin (ET) receptor antagonists (ETA/ETB -ETA/BRAs) to contrast the ET-1-induced effects on cultured human microvascular endothelial cells (HMVECs). METHODS: Some cultured HMVECs were untreated, or treated with ET-1 (100nM) or transforming growth factor β1 (TGFβ1, 10ng/mL) alone for 6 days, in order to induce the endothelial-to-mesenchymal transition (EndoMT). Other cultured HMVECs were pre-treated for 1hr with ETA/BRAs bosentan (10μM) or macitentan (1μM, 10μM) before the stimulation with ET-1 for 6 days...
January 27, 2017: Clinical and Experimental Rheumatology
https://www.readbyqxmd.com/read/28121194/in-vitro-characterization-studies-of-self-microemulsified-bosentan-systems
#18
Harini Chowdary Vadlamudi, Prasanna Raju Yalavarthi, M V Basaveswara Rao, Arun Rasheed, Tejeswari N
CONTEXT: Bosentan is a poorly soluble drug and pose challenges in design delivery systems. OBJECTIVE: To enhance the solubility, dissolution and shelf-life of bosentan by formulating it as S-SMEDDS capsules. MATERIALS AND METHODS: Solubility of bosentan was tested in various liquid vehicles such as oils (rice bran and sunflower), surfactants (span 20 and tween 80) and co-surfactants (PEG 400 and propylene glycol) and microemulsions were developed...
January 25, 2017: Drug Development and Industrial Pharmacy
https://www.readbyqxmd.com/read/28119496/treatment-of-pulmonary-arterial-hypertension-using-initial-combination-therapy-of-bosentan-and-iloprost
#19
Xinpeng Han, Yuhai Zhang, Liang Dong, Liying Fang, Yaqin Chai, Mengjie Niu, Yongping Yu, Lingli Liu, Xuemin Yang, Shuoyao Qu, Shengqing Li
BACKGROUND: Monotherapy and sequential combination therapy have been widely used in the treatment of pulmonary arterial hypertension (PAH). There is limited evidence for initial combination therapy in patients with PAH, particularly those with World Health Organization (WHO) functional class III or IV. METHODS: Twenty-seven consecutive treatment-naive PAH subjects with WHO functional class III or IV PAH were randomized into 3 groups with a 1:1:1 ratio: a combination therapy group with 125 mg of bosentan twice daily plus 10 μg of iloprost 4-6 times/d; a bosentan monotherapy group with 125 mg of bosentan twice daily; and a iloprost monotherapy group with 10 μg of iloprost 4-6 times/d...
January 24, 2017: Respiratory Care
https://www.readbyqxmd.com/read/28078552/pediatric-development-of-bosentan-facilitated-by-modeling-and-simulation
#20
Jochen Zisowsky, Martine Géhin, Andjela Kusic-Pajic, Andreas Krause, Maurice Beghetti, Jasper Dingemanse
BACKGROUND: Bosentan is approved for use in adult patients with pulmonary arterial hypertension. The primary aim of the pharmacokinetic modeling was the provision of a systematic guidance for study design and enhanced understanding of pharmacokinetics across the entire pediatric age range. METHODS: A physiologically based pharmacokinetic model was developed for the pediatric population; starting from an adult model, the effects of body weight, age, and maturation of relevant metabolizing enzymes were incorporated to extrapolate the pharmacokinetics to children...
April 2017: Paediatric Drugs
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