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1

Martynyuk, T. V., and A. M. Aleevskaya. "Dynamics of the clinical functional and hemodynamic profile of patients with pulmonary arterial hypertension with initial monotherapy with endothelin receptor antagonists: bosentan vs. macitentan." Kardiologiia 60, no. 7 (2020): 28–35. http://dx.doi.org/10.18087/cardio.2020.7.n1136.

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Aim To compare results of 24-h treatments with bosentan and macitentan by the clinical functional status and indexes of pulmonary hemodynamics in patients with pulmonary arterial hypertension (PAH).Materials and methods Based on the Russian National Registry (NCT03707561), 44 patients older than 18 years with PAH (34 patients with idiopathic pulmonary hypertension (IPH) and 10 patients with Eisenmenger syndrome) were retrospectively included into this study. Based on the statistical method of pairwise comparison, two groups were formed and matched by age, gender, WHO functional class (FC), and
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2

Rahaghi, Franck F., Hassan M. Alnuaimat, Rana L. A. Awdish, et al. "Recommendations for the clinical management of patients receiving macitentan for pulmonary arterial hypertension (PAH): A Delphi consensus document." Pulmonary Circulation 7, no. 3 (2017): 702–11. http://dx.doi.org/10.1177/2045893217721695.

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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. Consensus recommendations were developed by a
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3

Tynan, Timothy, Kathryn Hird, Tara Hannon, and Eli Gabbay. "Pulmonary arterial hypertension outcomes upon endothelin-1 receptor antagonist switch to macitentan." Journal of International Medical Research 47, no. 5 (2019): 2177–86. http://dx.doi.org/10.1177/0300060519840130.

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Objectives To assess whether switching patients with suboptimally controlled pulmonary arterial hypertension from bosentan or ambrisentan to macitentan would improve six-minute walk test (6MWT) distance and World Health Organization functional class. Methods This was a retrospective cohort analysis of 37 patients from a single center. Patients were separated into three heterogeneous treatment groups and followed for 18 months: switch group (n = 14): patients switched to macitentan from bosentan/ambrisentan; added group (n = 11): patients who began macitentan as de novo therapy (n = 5) or who a
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4

Martynuk, T. V., S. N. Nakonechnikov, and I. Ye Chazova. "MACITENTAN: THE EVOLUTION OF THE CLASS ENDOTHELIN RECEPTOR ANTAGONISTS TO IMPROVE EFFICACY AND SAFETY OF PAH TREATMENT." Eurasian heart journal, no. 2 (June 30, 2013): 15–26. http://dx.doi.org/10.38109/2225-1685-2013-2-15-26.

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Pulmonary arterial hypertension (PAH) is a severe progressive disease, characterized by advanced remodeling of small pulmonary arteries and arterioles, which ultimately leads to right heart failure and death. Due to discovery of PAH pathophysiological targets, new medications have been developed and implemented into clinical practice. These medications compensate the deficiencies of endogenous prostacyclin and nitric oxide and also block the effects of endothelin-1 (ET-1). The role of the latter in PAH pathophysiology is related to its strong vasoconstrictory properties, as well as to a number
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5

Hanibuchi, Masaki, Sun-Jin Kim, Kenji Otsuka, et al. "Eradication of experimental brain metastases of human non-small cell lung cancer by macitentan, a dual antagonist of the endothelin A and B receptor, combined with paclitaxel." Journal of Clinical Oncology 30, no. 30_suppl (2012): 92. http://dx.doi.org/10.1200/jco.2012.30.30_suppl.92.

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92 Background: Treatment of patients with lung cancer brain metastases remains a major challenge because of the limited availability of standard therapy. Thus, the development of successful treatment options for these patients is mandatory. Recently, the endothelin axis was reported to be involved in cancer progression through its pleiotropic biological effects on cell survival, proliferation, invasion, and metastasis. Methods: In this study, we evaluated both the in vitro and in vivoeffects of macitentan, an orally bioavailable, dual endothelin A receptor and endothelin B receptor antagonist,
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6

Shinohara, Tsutomu, Hirofumi Sawada, Shoichiro Otsuki, et al. "Macitentan reverses early obstructive pulmonary vasculopathy in rats: early intervention in overcoming the survivin-mediated resistance to apoptosis." American Journal of Physiology-Lung Cellular and Molecular Physiology 308, no. 6 (2015): L523—L538. http://dx.doi.org/10.1152/ajplung.00129.2014.

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It remains unknown whether current disease-targeting therapy can histologically reverse obstructive pulmonary vasculopathy and how the timing of the therapy influences the antiremodeling effects of the compound. We test the hypothesis that a novel endothelin receptor antagonist macitentan reverses the early and/or late stages of occlusive pulmonary vascular disease (PVD) in rats. Rats with pulmonary arterial hypertension (PAH), which were produced by combined exposure to a vascular endothelial growth factor receptor inhibitor Sugen 5416 and hypobaric hypoxia for 3 wk, were assigned to receive
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7

Martynyuk, T. V., S. N. Nakonechnikov, and I. Ye Chazova. "OPTIMIZATION OF SPECIFIC THERAPY FOR PULMONARY ARTERIAL HYPERTENSION: THE POSSIBILITIES OF USING ENDOTHELIN RECEPTOR ANTAGONISTS." Eurasian heart journal, no. 2 (June 30, 2017): 20–27. http://dx.doi.org/10.38109/2225-1685-2017-2-20-27.

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Modern concepts of pulmonary arterial hypertension (PAH) pathogenesis focus on the key role of endothelial dysfunction of pulmonary vessels. To control the activation of endothelin-1 system, endothelin receptor antagonists (ERA) are current ly used. Until recently, this class of drugs in our country and abroad was represented by two drugs: the sulfonamide derivative - a nonselective ERA bosentan and a non-sulfonamide derivative - ambrisentan, which blocks only ETA-receptors. Not the selectivity of ERAs, but their pharmacokinetic characteristics determine the differences in the profile of effic
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8

Trivedi, Jahanvee K., Chirag J. Patel, and M. M. Patel. "RP-HPLC METHOD DEVELOPMENT AND VALIDATION OF MACITENTAN WITH ITS KNOWN AND UNKNOWN DEGRADATION IMPURITIES IN ITS TABLET DOSAGE FORM." International Journal of Applied Pharmaceutics 10, no. 5 (2018): 81. http://dx.doi.org/10.22159/ijap.2018v10i5.26211.

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Objective: To develop and validate macitentan with its known and unknown degradation impurities in its tablet dosage form.Methods: The RP-HPLC method for macitentan and its impurities was developed and three potential degradation impurities MCA-02, MCA-01 and degradation impurity and N-propyl derivative and N-N dimethyl derivative process impurities were separated. Chromatographic separation was achieved within 70 min on Inertsil C8 (250*4.6 mm, 5 µm) column, Using mobile phase A [Ammonium acetate (ph 4.5 adjusted with glacial acetic acid)] and mobile phase B acetonitrile in gradient elution.
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9

Vachiéry, Jean-Luc, Marion Delcroix, Hikmet Al-Hiti, et al. "Macitentan in pulmonary hypertension due to left ventricular dysfunction." European Respiratory Journal 51, no. 2 (2018): 1701886. http://dx.doi.org/10.1183/13993003.01886-2017.

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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 treatmen
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10

Qin, Jinlv, Guizuo Wang, and Dong Han. "Benefits of Macitentan in Patients with Pulmonary Hypertension: A Systematic Review and Meta-Analysis of Randomized Controlled Trials." Global Heart 18, no. 1 (2023): 58. http://dx.doi.org/10.5334/gh.1274.

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Background: This systematic review and meta-analysis aimed to determine the efficacy of macitentan in patients with pulmonary hypertension (PH). Methods: A systematic search was made of PubMed, Embase, Cochrane Library, and clinicaltrials.gov, without language restrictions. Randomized controlled trials (RCTs) on treatment of PH with macitentan, compared with placebo or blank, were reviewed. Studies were pooled to weighted mean differences (WMDs) and risk ratios (RRs), with 95% confidence intervals (CIs). Results: Six RCTs (enrolling 1,003 participants) met the inclusion criteria. Macitentan sh
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11

Albayrak, Mevlut, and Alptug Atila. "Development and Validation of Novel UPLC-MS/MS Method for the Analysis of Macitentan in Pharmaceutical Formulations." Current Pharmaceutical Analysis 15, no. 5 (2019): 554–59. http://dx.doi.org/10.2174/1573412915666190314142531.

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Introduction: Macitentan is an endothelin receptor antagonist drug used in the treatment of pulmonary arterial hypertension. Materials and Methods: A new, sensitive, simple, accurate and rapid ultra-performance liquid chromatography in combination with tandem triple quadruple mass spectrometry (UPLC-MS/MS) method has been developed and validated for the determination of macitentan in pharmaceutical formulations. Macitentan and bosentan which are used as internal standard (IS) were detected using atmospheric pressure chemical ionization (APCI) in positive ion, multiple reaction monitoring (MRM)
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12

Morales-Loredo, Humberto, David Jones, Adelaeda Barrera, et al. "A dual blocker of endothelin A/B receptors mitigates hypertension but not renal dysfunction in a rat model of chronic kidney disease and sleep apnea." American Journal of Physiology-Renal Physiology 316, no. 5 (2019): F1041—F1052. http://dx.doi.org/10.1152/ajprenal.00018.2019.

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Obstructive sleep apnea is characterized by recurrent episodes of pharyngeal collapse during sleep, resulting in intermittent hypoxia (IH), and is associated with a high incidence of hypertension and accelerated renal failure. In rodents, endothelin (ET)-1 contributes to IH-induced hypertension, and ET-1 levels inversely correlate with glomerular filtration rate in patients with end-stage chronic kidney disease (CKD). Therefore, we hypothesized that a dual ET receptor antagonist, macitentan (Actelion Pharmaceuticals), will attenuate and reverse hypertension and renal dysfunction in a rat model
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13

Simonneau, Gérald, Richard N. Channick, Marion Delcroix, et al. "Incident and prevalent cohorts with pulmonary arterial hypertension: insight from SERAPHIN." European Respiratory Journal 46, no. 6 (2015): 1711–20. http://dx.doi.org/10.1183/13993003.00364-2015.

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In SERAPHIN, a long-term, randomised, controlled trial (NCT00660179) in pulmonary arterial hypertension (PAH), macitentan significantly reduced the risk of morbidity/mortality and PAH-related death/hospitalisation. We evaluated disease progression and the effect of macitentan in treatment-naïve incident and prevalent cohorts.Patients allocated to placebo, or macitentan 3 mg or 10 mg were classified by time from diagnosis to enrolment as incident (≤6 months; n=110) or prevalent (>6 months; n=157). The risk of morbidity/mortality and PAH-related death/hospitalisation was determined using Cox
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14

Moisseeva, O. M., and A. V. Rudakova. "Pharmacoeconomic aspects of macitentan in the therapy of pulmonary arterial hypertension." Terapevticheskii arkhiv 89, no. 3 (2017): 72–77. http://dx.doi.org/10.17116/terarkh201789372-77.

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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. The cost of bosentan was calculated from the 2016 registered prices with VAT. That of macitentan
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15

Mamazhakypov, Argen, Astrid Weiß, Sven Zukunft, et al. "Effects of macitentan and tadalafil monotherapy or their combination on the right ventricle and plasma metabolites in pulmonary hypertensive rats." Pulmonary Circulation 10, no. 4 (2020): 204589402094728. http://dx.doi.org/10.1177/2045894020947283.

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Pulmonary arterial hypertension is a severe respiratory disease characterized by pulmonary artery remodeling. RV dysfunction and dysregulated circulating metabolomics are associated with adverse outcomes in pulmonary arterial hypertension. We investigated effects of tadalafil and macitentan alone or in combination on the RV and plasma metabolomics in SuHx and PAB models. For SuHx model, rats were injected with SU5416 and exposed to hypoxia for three weeks and then were returned to normoxia and treated with either tadalafil (10 mg/kg in chow) or macitentan (10 mg/kg in chow) or their combinatio
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16

Belge, Catharina, and Marion Delcroix. "Treatment of pulmonary arterial hypertension with the dual endothelin receptor antagonist macitentan: clinical evidence and experience." Therapeutic Advances in Respiratory Disease 13 (January 2019): 175346661882344. http://dx.doi.org/10.1177/1753466618823440.

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Macitentan (10 mg once daily orally), a dual endothelin receptor antagonist (ERA) developed by modifying the structure of bosentan to increase the efficacity and safety, is approved for the treatment of pulmonary arterial hypertension (PAH). The pivotal SERAPHIN trial, (a landmark trial in the history of PAH trials because of the large number of included patients, the long-term follow up and the first trial with morbidity/mortality as the primary endpoint) showed a reduction of the risk of a morbidity or mortality event by 45% over the treatment time compared with placebo. The positive effect
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17

Sheffer, Joe. "Macitentan: Endothelin receptor antagonist." Pharmacy Today 19, no. 12 (2013): 50. http://dx.doi.org/10.1016/s1042-0991(15)31059-8.

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18

Patel, Trina, and Kate McKeage. "Macitentan: First Global Approval." Drugs 74, no. 1 (2013): 127–33. http://dx.doi.org/10.1007/s40265-013-0156-6.

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19

Zebadúa, Rodrigo, Andrea Priscila Hernández-Pérez, Antonio García, et al. "Macitentan in the treatment of pulmonary arterial hypertension." Future Cardiology 17, no. 1 (2021): 49–58. http://dx.doi.org/10.2217/fca-2020-0012.

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Pulmonary arterial hypertension (PAH) is an uncommon but lethal and progressive disease in which prostacyclin, nitric oxide and endothelin-1 pathways are disturbed and contribute to the pathophysiology of this disease. Endothelin receptor antagonists are a class of drugs that have been approved as PAH therapy. Macitentan is a lipophilic, tissue specific, dual receptor antagonist with a higher potency than bosentan and a reduced risk of hepatic injury. Macitentan has shown a reduction in morbidity and mortality due to PAH at long-term follow-up and improvements in hemodynamics, exercise capacit
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20

Arkhipova, O. A., T. V. Martynyuk, and I. E. Chazova. "A clinical case of long-term macitentan therapy in a female patient with idiopathic pulmonary hypertension." Terapevticheskii arkhiv 88, no. 12 (2016): 88–93. http://dx.doi.org/10.17116/terarkh2016881288-93.

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In late 2015, the Russian Federation registered the new non-selective endothelin receptor antagonist macitentan for the pathogenetic therapy of pulmonary arterial hypertension. The given clinical case demonstrates the possibility of using macitentan in a female patient with idiopathic pulmonary hypertension and its ability to affect the clinical, hemodynamic, and functional status of patients and to slow down the progression of the disease.
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21

Benza, Raymond L., Cassandra A. Lickert, Lin Xie, et al. "Comparative effectiveness of endothelin receptor antagonists on mortality in patients with pulmonary arterial hypertension in a US Medicare population: a retrospective database analysis." Pulmonary Circulation 10, no. 4 (2020): 204589402095415. http://dx.doi.org/10.1177/2045894020954158.

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Limited evidence is available on outcomes associated with currently available medications from the endothelin receptor antagonist drug class (bosentan, ambrisentan, and macitentan) in elderly patients with pulmonary arterial hypertension. We evaluated mortality in predominantly elderly patients with pulmonary arterial hypertension in the US taking endothelin receptor antagonists. A retrospective administrative claims study was conducted using the Centers for Medicare and Medicaid Services national Medicare database. Patients with pulmonary arterial hypertension were identified using diagnostic
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22

Steven, Sebastian, Matthias Oelze, Michael Hausding, et al. "The Endothelin Receptor Antagonist Macitentan Improves Isosorbide-5-Mononitrate (ISMN) and Isosorbide Dinitrate (ISDN) Induced Endothelial Dysfunction, Oxidative Stress, and Vascular Inflammation." Oxidative Medicine and Cellular Longevity 2018 (December 27, 2018): 1–17. http://dx.doi.org/10.1155/2018/7845629.

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Objective. Organic nitrates such as isosorbide-5-mononitrate (ISMN) and isosorbide dinitrate (ISDN) are used for the treatment of patients with chronic symptomatic stable coronary artery disease and chronic congestive heart failure. Limiting side effects of these nitrovasodilators include nitrate tolerance and/or endothelial dysfunction mediated by oxidative stress. Here, we tested the therapeutic effects of the dual endothelin (ET) receptor antagonist macitentan in ISMN- and ISDN-treated animals. Methods and Results. Organic nitrates (ISMN, ISDN, and nitroglycerin (GTN)) augmented the oxidati
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23

Cutolo, Maurizio, Paola Montagna, Renata Brizzolara, et al. "Effects of Macitentan and Its Active Metabolite on Cultured Human Systemic Sclerosis and Control Skin Fibroblasts." Journal of Rheumatology 42, no. 3 (2015): 456–63. http://dx.doi.org/10.3899/jrheum.141070.

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Objective.To investigate the effects of the endothelin 1 (ET-1) receptor antagonists (ETRA) macitentan, its active metabolite ACT-132577, and bosentan on myofibroblast activation and extracellular matrix production induced by ET-1 in cultured systemic sclerosis (SSc) and control skin fibroblasts.Methods.Fibroblasts were obtained from skin biopsies of 6 patients with SSc and 5 healthy subjects. Some cultured cells were untreated or treated with macitentan, ACT-132577, or bosentan alone (10 μM). Other cultured cells were treated with ET-1 alone (100 nM) or with ETRA, and after 1 h, also with ET-
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24

Retuerto-Guerrero, M., C. Moriano, I. Castellví, B. Atienza-Mateo, and E. Diez Álvarez. "AB0921 EFFICACY AND SAFETY OF MACITENTAN IN REFRACTORY DIGITAL ULCERS." Annals of the Rheumatic Diseases 82, Suppl 1 (2023): 1677.2–1678. http://dx.doi.org/10.1136/annrheumdis-2023-eular.6359.

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BackgroundRaynaud’s phenomenon (Rp) is used to describe a symptom complex caused by digital vascular involvement. The presence of digital ulcerations (DU) should prompt further evaluation for secondary causes of Rp. Among the conditions that may be associated with Rp are Systemic Autoimmune Rheumatic Diseases (SARDs), especially Systemic Sclerosis (SSc). DU are a major cause of morbidity and have a high recurrence rate in most patients and may be refractory to multiple treatments.Macitentan is a dual endothelin receptor antagonist authorized to treat pulmonary hypertension. Its efficacy in the
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Liu, Zhong-Yu, Man-Ting Au, Tian-Wei He, et al. "Less Vertebral Bone Mass after Treatment with Macitentan in Mice: A Pilot Study." BioMed Research International 2019 (February 19, 2019): 1–6. http://dx.doi.org/10.1155/2019/2075968.

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Purpose. Blood vessels and skeleton interact together. Endothelin-1 is a potent vasoconstrictor and also has an effect on bone metabolism. The dual antagonist to both endothelin-1 type A and B receptors, Macitentan, has been approved for clinical management of pulmonary arterial hypertension while little is known about the secondary effect of the drug on spine. We aimed to answer how vertebral bone mass responded to Macitentan treatment in mice. Methods. Sixteen male balb/c mice at 6 months were randomly assigned into 2 groups. Vehicle and Macitentan were administrated via intraperitoneal inje
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"Macitentan." Reactions Weekly 1840, no. 1 (2021): 247. http://dx.doi.org/10.1007/s40278-021-90390-x.

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"Macitentan." Reactions Weekly 1914, no. 1 (2022): 279. http://dx.doi.org/10.1007/s40278-022-18865-6.

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"Macitentan." Reactions Weekly 2017, no. 1 (2024): 272. http://dx.doi.org/10.1007/s40278-024-63248-5.

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"MACITENTAN." Drug Data Report 31, no. 2 (2009): 143. http://dx.doi.org/10.1358/ddr.2009.031.02.1287227.

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"Macitentan." Reactions Weekly 1693, no. 1 (2018): 313. http://dx.doi.org/10.1007/s40278-018-43203-3.

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"Macitentan." Reactions Weekly 1641, no. 1 (2017): 160. http://dx.doi.org/10.1007/s40278-017-27074-1.

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"Macitentan." Reactions Weekly 1653, no. 1 (2017): 200. http://dx.doi.org/10.1007/s40278-017-30628-y.

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"Macitentan." Reactions Weekly 1699, no. 1 (2018): 186. http://dx.doi.org/10.1007/s40278-018-45454-1.

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"Macitentan." Reactions Weekly 1600, no. 1 (2016): 135. http://dx.doi.org/10.1007/s40278-016-17220-y.

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"Macitentan." Reactions Weekly 1668, no. 1 (2017): 256. http://dx.doi.org/10.1007/s40278-017-35728-7.

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"Macitentan." Reactions Weekly 1675, no. 1 (2017): 154. http://dx.doi.org/10.1007/s40278-017-37922-x.

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"Macitentan." Reactions Weekly 1761, no. 1 (2019): 237. http://dx.doi.org/10.1007/s40278-019-64609-5.

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"Macitentan." Reactions Weekly 1966, no. 1 (2023): 202. http://dx.doi.org/10.1007/s40278-023-43655-9.

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"Macitentan." Reactions Weekly 2069, no. 1 (2025): 215. https://doi.org/10.1007/s40278-025-86873-7.

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Weathers, Shiao-Pei, Julie Rood-Breithaupt, John de Groot, et al. "Results of a phase I trial to assess the safety of macitentan in combination with temozolomide for the treatment of recurrent glioblastoma." Neuro-Oncology Advances 3, no. 1 (2021). http://dx.doi.org/10.1093/noajnl/vdab141.

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Abstract Background There is an urgent need for additional therapies to treat recurrent glioblastoma (GBM). Preclinical studies suggest that high dose macitentan, an oral dual endothelin receptor antagonist, enhances the cytotoxic effects of temozolomide (TMZ) in GBM, improving survival. This phase I trial investigated the maximum tolerated dose of macitentan combined with TMZ in patients with recurrent GBM and assessed the safety and tolerability of high dose macitentan in these patients (NCT01499251). Methods Adults with recurrent GBM received ascending doses of macitentan from 30 mg once da
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"Macitentan/sildenafil." Reactions Weekly 1844, no. 1 (2021): 268. http://dx.doi.org/10.1007/s40278-021-91715-7.

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"Macitentan/selexipag." Reactions Weekly 1864, no. 1 (2021): 220. http://dx.doi.org/10.1007/s40278-021-99150-4.

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"Macitentan/sildenafil." Reactions Weekly 1929, no. 1 (2022): 385. http://dx.doi.org/10.1007/s40278-022-26009-4.

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"Epoprostenol/Macitentan." Reactions Weekly 2029, no. 1 (2024): 264. http://dx.doi.org/10.1007/s40278-024-68442-z.

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"Macitentan/Sildenafil." Reactions Weekly 2016, no. 1 (2024): 268. http://dx.doi.org/10.1007/s40278-024-62761-9.

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"Macitentan/selexipag." Reactions Weekly 1933, no. 1 (2022): 270. http://dx.doi.org/10.1007/s40278-022-28221-5.

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"Macitentan/treprostinil." Reactions Weekly 1787, no. 1 (2020): 332. http://dx.doi.org/10.1007/s40278-020-73970-4.

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"Macitentan/riociguat." Reactions Weekly 1745, no. 1 (2019): 173. http://dx.doi.org/10.1007/s40278-019-59336-x.

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"Macitentan/sildenafil." Reactions Weekly 1932, no. 1 (2022): 369. http://dx.doi.org/10.1007/s40278-022-27734-x.

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"Macitentan/tadalafil." Reactions Weekly 1932, no. 1 (2022): 370. http://dx.doi.org/10.1007/s40278-022-27735-x.

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