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Selexipag

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https://www.readbyqxmd.com/read/29745254/treatment-of-rat-congenital-diaphragmatic-hernia-with-sildenafil-and-ns-304-selexipag-s-active-compound-at-the-pseudoglandular-stage-improves-lung-vasculature
#1
Daphne S Mous, Heleen M Kool, Petra E Burgisser, Marjon J Buscop-van Kempen, Koji Nagata, Anne Boerema-de Munck, Joost van Rosmalen, Oleh Dzyubachyk, Rene Mh Wijnen, Dick Tibboel, Robbert J Rottier
Patients with congenital diaphragmatic hernia (CDH) often suffer from severe pulmonary hypertension and the choice of current vasodilator therapy is mostly based on trial and error. Since pulmonary vascular abnormalities are already present early during development, we performed a study to modulate these pulmonary vascular changes at an early stage during gestation. Pregnant Sprague-Dawley rats were treated with nitrofen at day 9.5 of gestation (E9.5) to induce CDH in the offspring and subsequently the phosphodiesterase-5 inhibitor sildenafil and/or the novel prostaglandin-I receptor agonist selexipag (NS-304) were administered from E17...
May 10, 2018: American Journal of Physiology. Lung Cellular and Molecular Physiology
https://www.readbyqxmd.com/read/29720235/effects-of-selexipag-and-its-active-metabolite-in-contrasting-the-profibrotic-myofibroblast-activity-in-cultured-scleroderma-skin-fibroblasts
#2
Maurizio Cutolo, Barbara Ruaro, Paola Montagna, Renata Brizzolara, Emanuela Stratta, Amelia Chiara Trombetta, Stefano Scabini, Pier Paolo Tavilla, Aurora Parodi, Claudio Corallo, Nicola Giordano, Sabrina Paolino, Carmen Pizzorni, Alberto Sulli, Vanessa Smith, Stefano Soldano
BACKGROUND: Myofibroblasts contribute to fibrosis through the overproduction of extracellular matrix (ECM) proteins, primarily type I collagen (COL-1) and fibronectin (FN), a process which is mediated in systemic sclerosis (SSc) by the activation of fibrogenic intracellular signaling transduction molecules, including extracellular signal-regulated kinases 1 and 2 (Erk1/2) and protein kinase B (Akt). Selexipag is a prostacyclin receptor agonist synthesized for the treatment of pulmonary arterial hypertension...
May 2, 2018: Arthritis Research & Therapy
https://www.readbyqxmd.com/read/29607828/t-cell-large-granular-lymphocytic-leukemia-with-pulmonary-hypertension
#3
Sidra Khalid, Hamed Daw, Miriam Jacob, Megan Nakashima
T cell large granular lymphocytic leukemia is a hematological disorder which is characterized by the proliferation of CD 3+ cytotoxic T cells. We present a case about a patient who was diagnosed with T cell large granular lymphocytic leukemia and then developed pulmonary hypertension. He was treated for his leukemia with methotrexate and simultaneously treated for his pulmonary hypertension with selexipag and ambrisentan. As his leukemia improved, we also noticed an improvement in his pulmonary hypertension from a NYHA class IV to class I...
January 2018: Gulf Journal of Oncology
https://www.readbyqxmd.com/read/29588339/selective-prostacyclin-receptor-agonist-selexipag-in-contrast-to-prostacyclin-analogs-does-not-evoke-paradoxical-vasoconstriction-of-the-rat-femoral-artery
#4
Keith Morrison, Franck Haag, Roland Ernst, Marc Iglarz, Martine Clozel
Selexipag [2-{4-[(5,6-diphenylpyrazin-2-yl)(isopropyl)amino]butoxy}- N -(methylsulfonyl)acetamide] is a selective nonprostanoid prostacyclin (PGI2 ) receptor (IP receptor) agonist that is approved for the treatment of pulmonary arterial hypertension (PAH). In contrast to selexipag, PGI2 analogs used in the clinic are nonselective agonists at prostanoid receptors and can also activate contractile prostaglandin E receptor 3 (EP3 ) receptors. Leg pain is a common side effect in patients receiving treatment with PGI2 analogs and peripheral vasoconstriction can be responsible for side effects related to muscular ischemia...
June 2018: Journal of Pharmacology and Experimental Therapeutics
https://www.readbyqxmd.com/read/29521655/selexipag-in-congenital-heart-disease-associated-pulmonary-arterial-hypertension-and-eisenmenger-syndrome-first-report
#5
Karim El-Kersh, Sally Suliman, J Shaun Smith
No abstract text is available yet for this article.
January 23, 2018: American Journal of Therapeutics
https://www.readbyqxmd.com/read/29513930/reply
#6
LETTER
Christopher P Denton, Ariane L Herrick
No abstract text is available yet for this article.
March 7, 2018: Arthritis & Rheumatology
https://www.readbyqxmd.com/read/29468921/cross-species-comparison-of-the-metabolism-and-excretion-of-selexipag
#7
Tomohiko Ichikawa, Tetsuhiro Yamada, Alexander Treiber, Carmela Gnerre, Jérôme Segrestaa, Swen Seeland, Kiyoko Nonaka
1. The metabolism of the prostacyclin receptor agonist selexipag (NS-304; ACT-293987) and its active metabolite MRE-269 (ACT-333679) has been investigated in liver microsomes and hepatocytes of rats, dogs, and monkeys. MRE-269 formation is the main pathway of selexipag metabolism, irrespective of species. Some interspecies differences were evident for both compounds in terms of both metabolic turnover and metabolic profiles. The metabolism of MRE-269 was slower than that of selexipag in all three species. 2...
March 21, 2018: Xenobiotica; the Fate of Foreign Compounds in Biological Systems
https://www.readbyqxmd.com/read/29447737/pulmonary-arterial-hypertension-related-morbidity-is-prognostic-for-mortality
#8
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/29421995/new-drugs-therapeutic-strategies-and-future-direction-for-the-treatment-of-pulmonary-arterial-hypertension
#9
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/29307087/targeting-the-prostacyclin-pathway-with-selexipag-in-patients-with-pulmonary-arterial-hypertension-receiving-double-combination-therapy-insights-from-the-randomized-controlled-griphon-study
#10
J Gerry Coghlan, Richard Channick, Kelly Chin, Lilla Di Scala, Nazzareno Galiè, Hossein-Ardeschir Ghofrani, Marius M Hoeper, Irene M Lang, Vallerie McLaughlin, Ralph Preiss, Lewis J Rubin, Gérald Simonneau, Olivier Sitbon, Victor F Tapson, Sean Gaine
BACKGROUND: In pulmonary arterial hypertension (PAH), combination therapy is an important treatment strategy. Although randomized controlled trial data are available to support the combination of two therapies, data regarding triple combination therapy are few. OBJECTIVE: The phase III GRIPHON trial enrolled 1156 patients with PAH, including 376 receiving background double combination therapy. We evaluated the efficacy and safety of selexipag as a third agent in these patients and further analyzed this subgroup according to symptom burden at baseline as indicated by World Health Organization (WHO) functional class (FC)...
February 2018: American Journal of Cardiovascular Drugs: Drugs, Devices, and Other Interventions
https://www.readbyqxmd.com/read/29193819/efficacy-and-safety-of-selexipag-in-adults-with-raynaud-s-phenomenon-secondary-to-systemic-sclerosis-a-randomized-placebo-controlled-phase-ii-study
#11
RANDOMIZED CONTROLLED TRIAL
Christopher P Denton, Éric Hachulla, Gabriela Riemekasten, Andreas Schwarting, Jean-Marie Frenoux, Aline Frey, Franck-Olivier Le Brun, Ariane L Herrick
OBJECTIVE: To determine the effect of selexipag, an oral, selective IP prostacyclin receptor agonist, on the frequency of attacks of Raynaud's phenomenon (RP) in patients with systemic sclerosis (SSc). METHODS: Patients with SSc-related RP were randomized 1:1 to placebo (n = 38) or selexipag (n = 36) in individualized doses (maximum of 1,600 μg twice daily) during a 3-week titration period. The primary end point was the weekly average number of RP attacks during the study maintenance period, analyzed using a Bayesian approach with a negative binomial model adjusted for baseline number of RP attacks...
December 2017: Arthritis & Rheumatology
https://www.readbyqxmd.com/read/29096938/temporary-treatment-interruptions-with-oral-selexipag-in-pulmonary-arterial-hypertension-insights-from-the-prostacyclin-pgi-2-receptor-agonist-in-pulmonary-arterial-hypertension-griphon-study
#12
Ioana R Preston, Richard N Channick, Kelly Chin, Lilla Di Scala, Harrison W Farber, Sean Gaine, Nazzareno Galiè, Hossein-Ardeschir Ghofrani, Marius M Hoeper, Irene M Lang, Vallerie V McLaughlin, Ralph Preiss, Gérald Simonneau, Olivier Sitbon, Victor F Tapson, Lewis J Rubin
BACKGROUND: Parenteral prostacyclin analogs that target the prostacyclin pathway have been used to treat pulmonary arterial hypertension (PAH) since the 1990s. Abrupt discontinuation of parenteral prostacyclin analogs can be associated with acute deterioration of PAH. Less is known about temporary interruption of oral therapies that target the prostacyclin pathway, such as selexipag. METHODS: We evaluated the frequency, duration, reasons, and consequences of temporary selexipag interruptions among PAH patients enrolled in the Prostacyclin (PGI2 ) Receptor Agonist in Pulmonary Arterial Hypertension (GRIPHON) study...
March 2018: Journal of Heart and Lung Transplantation
https://www.readbyqxmd.com/read/29073911/successful-transition-from-treprostinil-to-selexipag-in-patient-with-severe-pulmonary-arterial-hypertension
#13
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/29071454/what-is-the-role-of-oral-prostacyclin-pathway-medications-in-pulmonary-arterial-hypertension-management
#14
REVIEW
Rama El Yafawi, Joel A Wirth
PURPOSE OF REVIEW: Prostacyclin pathway medications have been shown to be highly efficacious in the treatment of pulmonary arterial hypertension (PAH) through multiple prospective clinical trials and more than two decades of clinical experience. The strongest support for prostacyclin use in PAH management is with parenteral administration. Numerous risks and limitations of parenteral delivery systems as well as significant patient burdens restrict widespread parenteral use. Highly effective and tolerable oral prostacyclin preparations to manage PAH have long been sought...
October 25, 2017: Current Hypertension Reports
https://www.readbyqxmd.com/read/28922964/oral-treprostinil-in-the-treatment-of-pulmonary-arterial-hypertension
#15
REVIEW
Jeremy Feldman, Naomi Habib, John Radosevich, Mohan Dutt
Pulmonary arterial hypertension (PAH) is a rare disease resulting in progressive remodeling of the pulmonary vasculature and eventual right ventricular failure. Despite the development of 13 therapies for PAH since 2000, the use of continuously infused prostanoids retains a special role. Infused medications present unique challenges, and the search for an efficacious oral prostanoid culminated in the FDA approval of oral treprostinil - a first in class oral prostanoid medication approved to treat pulmonary arterial hypertension (PAH)...
October 2017: Expert Opinion on Pharmacotherapy
https://www.readbyqxmd.com/read/28891448/a-special-focus-on-selexipag-treatment-of-pulmonary-arterial-hypertension
#16
Louise M Sorensen, Markus Wehland, Marcus Kruger, Ulf Simonsen, Mohamed Z Nassef, Manfred Infanger, Daniela Grimm
BACKGROUND: This review focuses on the treatment of pulmonary arterial hypertension (PAH) with selexipag and compares its drug-related therapeutic effects with those of prostacyclin analogues. METHODS: We searched the relevant literature and summarized the current clinical trials concerning selexipag and PAH. RESULTS: With only few cases per million, PAH is a rare disease, but when untreated it can be life-threatening. PAH is linked to elevated levels of endothelin (ET-1) and decreased levels of nitric oxide (NO) and prostacyclin (PGI2)...
2017: Current Pharmaceutical Design
https://www.readbyqxmd.com/read/28818881/selexipag-for-the-treatment-of-connective-tissue-disease-associated-pulmonary-arterial-hypertension
#17
Sean Gaine, Kelly Chin, Gerry Coghlan, Richard Channick, Lilla Di Scala, Nazzareno Galiè, Hossein-Ardeschir Ghofrani, Irene M Lang, Vallerie McLaughlin, Ralph Preiss, Lewis J Rubin, Gérald Simonneau, Olivier Sitbon, Victor F Tapson, Marius M Hoeper
Patients with connective tissue disease-associated pulmonary arterial hypertension (PAH-CTD) have a poor prognosis compared with other aetiologies. The underlying CTD can influence treatment response and outcomes. We characterised the GRIPHON study PAH-CTD subgroup and evaluated response to selexipag.Of 334 patients with PAH-CTD, PAH was associated with systemic sclerosis (PAH-SSc) in 170, systemic lupus erythematosus (PAH-SLE) in 82 and mixed CTD/CTD-other in 82. For the primary composite endpoint of morbidity/mortality, hazard ratios (HR) and 95% CI were calculated using Cox proportional hazard models...
August 2017: European Respiratory Journal: Official Journal of the European Society for Clinical Respiratory Physiology
https://www.readbyqxmd.com/read/28737453/the-metabolism-and-drug-drug-interaction-potential-of-the-selective-prostacyclin-receptor-agonist-selexipag
#18
Carmela Gnerre, Jérôme Segrestaa, Swen Seeland, Päivi Äänismaa, Thomas Pfeifer, Stephane Delahaye, Ruben de Kanter, Tomohiko Ichikawa, Tetsuhiro Yamada, Alexander Treiber
- The metabolism of selexipag has been studied in vivo in man and the main excreted metabolites were identified. Also, metabolites circulating in human plasma have been structurally identified and quantified. - The main metabolic pathway of selexipag in man is the formation of the active metabolite ACT-333679. Other metabolic pathways include oxidation and dealkylation reactions. All primary metabolites undergo subsequent hydrolysis of the sulphonamide moiety to their corresponding acids. ACT-333679 undergoes conjugation with glucuronic acid and aromatic hydroxylation to P10, the main metabolite detected in human faeces...
July 24, 2017: Xenobiotica; the Fate of Foreign Compounds in Biological Systems
https://www.readbyqxmd.com/read/28715853/effect-of-gemfibrozil-and-rifampicin-on-the-pharmacokinetics-of-selexipag-and-its-active-metabolite-in-healthy-subjects
#19
RANDOMIZED CONTROLLED TRIAL
Shirin Bruderer, Marc Petersen-Sylla, Margaux Boehler, Tatiana Remeňová, Atef Halabi, Jasper Dingemanse
AIMS: Based on in vitro data, there is evidence to suggest that cytochrome P450 (CYP) 2C8 is involved in the metabolism of selexipag and its active metabolite, ACT-333679. The present study evaluated the possible pharmacokinetic interactions of selexipag with gemfibrozil, a strong CYP2C8 inhibitor, and rifampicin, an inducer of CYP2C8. METHODS: The study consisted of two independent parts, each conducted according to an open-label, randomized, crossover design. The pharmacokinetics and safety of selexipag and ACT-333679 were studied following single-dose administration either alone or in the presence of multiple-dose gemfibrozil (part I) or rifampicin (part II) in healthy male subjects...
December 2017: British Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/28702718/single-center-experience-using-selexipag-in-a-pediatric-population
#20
Roberto Gallotti, Diana E Drogalis-Kim, Gary Satou, Juan Alejos
Pulmonary arterial hypertension (PAH) is a rare and progressive disorder. Current treatment in the pediatric population includes phosphodiesterase 5 inhibitors (PDE-5i), endothelin receptor antagonists (ERA), and both inhaled and intravenous prostacyclin pathway agonists. As of December 22, 2015 the first oral prostacyclin pathway agonist, selexipag (Uptravi® ), was FDA approved in the US. In this case series, we discuss our single-center experience using selexipag in a pediatric population, composed of both patients with idiopathic PAH, and patients with congenital heart disease and PAH...
October 2017: Pediatric Cardiology
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