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https://www.readbyqxmd.com/read/28500979/ultra-sensitive-and-selective-quantification-of-endothelin-1-in-human-plasma-using-ultra-performance-liquid-chromatography-coupled-to-tandem-mass-spectrometry
#1
Yosuke Suzuki, Lukas Witt, Walter Mier, Gerd Mikus, Christoph Markert, Walter E Haefeli, Jürgen Burhenne
Endothelin-1 (ET-1) is a potent endogenous vasoconstrictor peptide and the plasma concentrations are commonly quantified by immunoassays such as enzyme-linked immuno-sorbent assays (ELISA) with the disadvantage of possible cross-reactivity with closely related endothelin derivatives. The aim of this study was to develop and validate an ultra-sensitive and selective assay for the quantification of ET-1 in human plasma, using ultra-performance liquid chromatography with tandem mass spectrometry (UPLC-MS/MS) after solid phase extraction...
April 29, 2017: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/28495568/quantitative-analyses-of-the-influence-of-parameters-governing-rate-determining-process-of-hepatic-elimination-of-drugs-on-the-magnitudes-of-drug-drug-interactions-via-hepatic-oatps-and-cyp3a-using-physiologically-based-pharmacokinetic-models
#2
Takashi Yoshikado, Maeda Kazuya, Hiroyuki Kusuhara, Ken-Ichi Furihata, Yuichi Sugiyama
Physiologically-based pharmacokinetic (PBPK) models were constructed for hepatic organic anion transporting polypeptides (OATPs) and cytochrome P450 3A (CYP3A) substrates (bosentan, repaglinide, clarithromycin, and simeprevir), a CYP3A probe substrate (midazolam), and selective inhibitors for OATPs (rifampicin) and CYP3A (itraconazole), though the role of OATPs in the hepatic uptake of clarithromycin is unclear. The pharmacokinetic data were obtained from our previous clinical drug-drug interaction (DDI) study...
May 8, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28494463/plasma-drug-concentrations-in-patients-with-pulmonary-arterial-hypertension-on-combination-treatment
#3
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...
May 12, 2017: Respiration; International Review of Thoracic Diseases
https://www.readbyqxmd.com/read/28486684/superior-vasodilation-of-human-pulmonary-vessels-by-vardenafil-compared-with-tadalafil-and-sildenafil-additive-effects-of-bosentan%C3%A2
#4
Michael Ried, Reiner Neu, Karla Lehle, Christian Großer, Tamas Szöke, Gunter Lang, Hans-Stefan Hofmann, Markus Hoenicka
OBJECTIVES: Pulmonary arterial hypertension is characterized by pulmonary vascular proliferation and remodelling, leading to a progressive increase in pulmonary arterial resistance. Vasodilator properties of 3 different phosphodiesterase (PDE)-5 inhibitors alone and in combination with an endothelin (ET) receptor antagonist were compared in an ex vivo model. METHODS: Segments of human pulmonary arteries (PAs) and pulmonary veins (PVs) were harvested from lobectomy specimens...
May 9, 2017: Interactive Cardiovascular and Thoracic Surgery
https://www.readbyqxmd.com/read/28484975/a-clinical-cassette-dosing-study-for-evaluating-the-contribution-of-hepatic-oatps-and-cyp3a-to-drug-drug-interactions
#5
Takashi Yoshikado, Kazuya Maeda, Sawako Furihata, Hanano Terashima, Takeshi Nakayama, Keiko Ishigame, Kazunobu Tsunemoto, Hiroyuki Kusuhara, Ken-Ichi Furihata, Yuichi Sugiyama
PURPOSE: To demonstrate the relative importance of organic anion-transporting polypeptides (OATPs) and cytochrome P450 3A (CYP3A) in the hepatic elimination of substrate drugs. METHODS: A cocktail of subtherapeutic doses of bosentan, repaglinide, clarithromycin, darunavir, simeprevir, and midazolam (CYP3A probe) was administered orally to eight healthy volunteers. Rifampicin (OATP inhibitor; 600 mg, p.o.) and itraconazole (CYP3A inhibitor; 200 mg, i.v.) were coadministered with the cocktail in the second and third phases, respectively...
May 8, 2017: Pharmaceutical Research
https://www.readbyqxmd.com/read/28468519/atrasentan-for-the-treatment-of-diabetic-nephropathy
#6
Jesus Egido, Jorge Rojas-Rivera, Sebastian Mas, Marta Ruiz-Ortega, Ana Belen Sanz, Emilio Gonzalez Parra, Carmen Gomez-Guerrero
Endothelin-1 (ET-1) is the most potent vasoconstrictor, and is involved in the renal regulation of salt and water homeostasis. When produced in excess in the kidney, ET-1 promotes proteinuria and tubulointerstitial injury. There is great interest in the clinical use of endothelin receptor antagonists (ERAs) in chronic kidney disease (CKD), mainly in diabetic nephropathy (DN). Areas covered: Physiopathological actions of ET-1 on the kidney. Both dual ETAR/ETBR (bosentan) or ETAR specific endothelin antagonists (avosentan and atrasentan, among others), which have progressed to early clinical development, with particular emphasis on atrasentan...
May 4, 2017: Expert Opinion on Investigational Drugs
https://www.readbyqxmd.com/read/28449795/long-term-effect-of-endothelin-receptor-antagonism-with-bosentan-on-the-morbidity-and-mortality-of-patients-with-severe-chronic-heart-failure-primary-results-of-the-enable-trials
#7
Milton Packer, John J V McMurray, Henry Krum, Wolfgang Kiowski, Barry M Massie, Avi Caspi, Craig M Pratt, Mark C Petrie, David DeMets, Isaac Kobrin, Sebastien Roux, Karl Swedberg
OBJECTIVES: The objective of this clinical trial was to evaluate the long-term effect of endothelin receptor antagonism with bosentan on the morbidity and mortality of patients with severe chronic heart failure. BACKGROUND: Endothelin may play a role in heart failure, but short-term clinical trials with endothelin receptor antagonists have reported disappointing results. Long-term trials are lacking. METHODS: In 2 identical double-blind trials, we randomly assigned 1,613 patients with New York Heart Association functional class IIIb to IV heart failure and an ejection fraction <35% to receive placebo or bosentan (target dose 125 mg twice daily) for a median of 1...
May 2017: JACC. Heart Failure
https://www.readbyqxmd.com/read/28435843/mmp-7-is-a-predictive-biomarker-of-disease-progression-in-patients-with-idiopathic-pulmonary-fibrosis
#8
Yasmina Bauer, Eric S White, Simon de Bernard, Peter Cornelisse, Isabelle Leconte, Adele Morganti, Sebastien Roux, Oliver Nayler
Idiopathic pulmonary fibrosis (IPF) is a progressive interstitial lung disease with poor prognosis, which is characterised by destruction of normal lung architecture and excessive deposition of lung extracellular matrix. The heterogeneity of disease progression in patients with IPF poses significant obstacles to patient care and prevents efficient development of novel therapeutic interventions. Blood biomarkers, reflecting pathobiological processes in the lung, could provide objective evidence of the underlying disease...
January 2017: ERJ Open Research
https://www.readbyqxmd.com/read/28429342/assessment-of-serum-endothelin-1-levels-in-rat-appendicitis-model-and-the-effects-of-bosentan
#9
S B Sarsu, K Sahin, H Kilincaslan, S L Mirapoglu, N Buyukpınarbasili, M E Duz, I Aydogdu
OBJECTIVE: In this study, the diagnostic value of serum endothelin-1 (ET-1) levels and the therapeutic effects of bosentan have been investigated in an experimental appendicitis rat model. MATERIALS AND METHODS: Twenty-one male Sprague-Dawley rats were chosen for the study. The rats were allocated into three groups as follows: Group 1 (control, n = 7), Group 2 (appendicitis, n = 7), and Group 3 (bosentan treatment, n = 7). At the 6th hour of the experiment, Groups 1 and 2 received 2 ml saline, and group 3 received 30 mg/kg bosentan intraperitoneally...
April 2017: European Review for Medical and Pharmacological Sciences
https://www.readbyqxmd.com/read/28424444/a-successful-cesarean-delivery-without-fetal-or-maternal-morbidity-in-an-eisenmenger-patient-with-cor-triatriatum-sinistrum-double-orifice-mitral-valve-large-ventricular-septal-defect-and-single-ventricle-who-was-under-long-term-bosentan-treatment
#10
Hacer Ceren Tokgöz, Cihangir Kaymaz, Nertila Poci, Özgür Yaşar Akbal, Selçuk Öztürk
Presently described is successful cesarean delivery in a pregnancy superimposed on long-term bosentan treatment in an Eisenmenger syndrome patient with cor triatriatum sinistrum, double-orifice mitral valve, and large ventricular septal defect resulting in single functioning ventricle with double outlets. Cesarean delivery was performed at 27th week of gestation without maternal or fetal morbidity. The infant had no congenital cardiovascular abnormality or any probable teratogenic effect of bosentan treatment during pregnancy...
March 2017: Türk Kardiyoloji Derneği Arşivi: Türk Kardiyoloji Derneğinin Yayın Organıdır
https://www.readbyqxmd.com/read/28401480/target-mediated-drug-disposition-pharmacokinetic-pharmacodynamic-model-of-bosentan-and-endothelin-1
#11
Anke-Katrin Volz, Andreas Krause, Walter Emil Haefeli, Jasper Dingemanse, Thorsten Lehr
BACKGROUND AND OBJECTIVES: Bosentan is a competitive antagonist on endothelin receptor A and B (ETA and ETB), displacing the endogenous binding partner endothelin-1 (ET-1) from its binding sites. After administration of escalating single doses of 10-750 mg as an intravenous (i.v.) infusion, bosentan showed dose-dependent pharmacokinetics (PK). The aim of this analysis was to develop a PK model of bosentan after i.v. administration including competitive antagonism with ET-1 and to analyze its influence on blood pressure and heart rate with a combined pharmacokinetic/pharmacodynamic (PK/PD) model...
April 11, 2017: Clinical Pharmacokinetics
https://www.readbyqxmd.com/read/28393009/a-case-of-anti-aminoacyl-trna-synthetase-ars-antibody-positive-polymyositis-pm-dermatomyositis-dm-associated-interstitial-pneumonia-ip-successfully-controlled-with-bosentan-therapy
#12
Tomoyuki Naito, Yosuke Tanaka, Mitsunori Hino, Akihiko Gemma
A 72-year-old woman was admitted to our hospital and was diagnosed with interstitial pneumonia (IP) associated with amyopathic dermatomyositis (ADM). The patient experienced three acute IP exacerbations in the 7 years that followed, which were each treated and resolved with steroid pulse therapy. The patient was closely examined for respiratory failure with right heart catheterization (RHC), which demonstrated that she had a mean pulmonary artery pressure (mPAP) of 34 mmHg. The patient was thus diagnosed as having pulmonary hypertension (PH) associated with anti-synthetase syndrome (ASS) and was started on bosentan therapy, which led to improvements in mPAP as well as in subjective symptoms over time...
2017: Respiratory Medicine Case Reports
https://www.readbyqxmd.com/read/28378734/-pharmacoeconomic-aspects-of-macitentan-in-the-therapy-of-pulmonary-arterial-hypertension
#13
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/mechanistic-insights-in-cytotoxic-and-cholestatic-potential-of-the-endothelial-receptor-antagonists-using-heparg-cells
#14
Matthew Gibson Burbank, Ahmad Sharanek, Audrey Burban, Hervé Mialanne, Hélène Aerts, Christiane Guguen-Guillouzo, Richard John Weaver, André Guillouzo
Several endothelin receptor antagonists have been developed for the treatment of pulmonary arterial hypertension. Some of them have been related to clinical cases of hepatocellular injury (sitaxentan) and/or cholestasis (bosentan). We aimed to determine if ambrisentan and macitentan, in addition to bosentan and sitaxentan, could potentially cause liver damage in man by use of human HepaRG cells. Our results showed that like bosentan, macitentan induced cytotoxicity and cholestatic disorders characterized by bile canaliculi dilatation and impairment of myosin light chain kinase signaling...
March 24, 2017: Toxicological Sciences: An Official Journal of the Society of Toxicology
https://www.readbyqxmd.com/read/28357073/effect-of-bosentan-is-correlated-with-mmp-9-timp-1-ratio-in-bleomycin-induced-pulmonary-fibrosis
#15
Wan-Li Zuo, Jie-Min Zhao, Ji-Xiong Huang, Wei Zhou, Ze-Hong Lei, Yan-Ming Huang, Yan-Fen Huang, Hai-Gang Li
Pulmonary fibrosis (PF) is a life-threatening non-tumorous disease characterized by progressive fibrosis and worsening lung function. Various drugs, such as bleomycin, can contribute to lung injury and PF, with lung injury potentially occurring in 10% of bleomycin users. Bleomycin is the most commonly used drug in the establishment of an animal model of PF in rats. Matrix metalloproteinases (MMPs) and tissue inhibitors of metalloproteinases (TIMPs) serve an important role in controlling tissue organization and fibrosis following injury...
February 2017: Biomedical Reports
https://www.readbyqxmd.com/read/28338297/atrial-flutter-regression-in-hiv-associated-pulmonary-arterial-hypertension-after-treatment-with-bosentan
#16
Mario Francesco Damiani, Cristina Scoditti, Elioda Bega, Silvano Dragonieri, Pierluigi Carratù, Alfredo Scoditti, Onofrio Resta
Pulmonary arterial hypertension (PAH) is a rare condition characterized by an increase in pulmonary arterial resistance leading to right heart failure and death. Arrhythmias are a growing problem in PAH; therefore, maintenance of sinus rhythm is considered to be an important treatment aim in these patients. We described the case of a 46-year-old woman with HIV-associated pulmonary arterial hypertension  who developed atrial flutter. After treatment with bosentan, it was observed a significant improvement in clinical and haemodynamic parameters...
November 29, 2016: Monaldi Archives for Chest Disease, Archivio Monaldi Per le Malattie del Torace
https://www.readbyqxmd.com/read/28315689/in-silico-prediction-of-hpxr-activators-using-structure-based-pharmacophore-modeling
#17
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
#18
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
#19
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/28298655/dual-nep-ece-inhibition-improves-endothelial-function-in-mesenteric-resistance-arteries-of-32-week-old-shr
#20
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
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