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Selexipag

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https://www.readbyqxmd.com/read/28420826/efficacy-and-safety-of-an-orally-administered-selective-prostacyclin-receptor-agonist-selexipag-in-japanese-patients-with-pulmonary-arterial-hypertension
#1
Nobuhiro Tanabe, Satoshi Ikeda, Nobuhiro Tahara, Keiichi Fukuda, Masaru Hatano, Hiroshi Ito, Tomotaka Nakayama, Toshihisa Anzai, Akiyoshi Hashimoto, Teruo Inoue, Kouji Kajinami, Yasuki Kihara, Hideyuki Kinoshita, Koichiro Kuwahara, Toyoaki Murohara, Osamu Okazaki, Satoshi Sakai, Toru Satoh, Yutaka Takeda, Yasuchika Takeishi, Mitsugu Taniguchi, Hiroshi Watanabe, Takeshi Yamamoto, Keiko Yamauchi-Takihara, Koichiro Yoshioka, Shigetake Sasayama
BACKGROUND: Selexipag is an orally available prostacyclin receptor (IP receptor) agonist with a non-prostanoid structure. In this open-label Phase II trial, the efficacy and safety of selexipag in Japanese patients with pulmonary arterial hypertension (PAH) is examined.Methods and Results:Selexipag was administered at 200 μg twice daily and titrated up to 1,600 μg by increments of 200 μg in 37 subjects to reach the individual maximum tolerated dose. At 16 weeks, in 33 patients comprising the per-protocol set, the pulmonary vascular resistance (PVR; primary endpoint) decreased from 683...
April 18, 2017: Circulation Journal: Official Journal of the Japanese Circulation Society
https://www.readbyqxmd.com/read/28399721/the-prostacyclin-pathway-in-pulmonary-arterial-hypertension-a-clinical-review
#2
R Del Pozo, I Hernandez Gonzalez, P Escribano-Subias
Prostacyclin is produced in vascular endothelial cells and acts via the IP prostacyclin receptor to cause vasodilation and inhibit smooth muscle cell proliferation and platelet aggregation. Prostacyclin production is reduced in pulmonary arterial hypertension (PAH), and drugs targeting the prostacyclin pathway are one of the pharmacotherapeutic options for PAH. Areas covered: The prostacyclin pathway and drugs that target it are discussed, including synthetic prostacyclin (epoprostenol), prostacyclin analogs (iloprost, treprostinil, beraprost) and selective prostacyclin IP receptor agonists (selexipag)...
April 24, 2017: Expert Review of Respiratory Medicine
https://www.readbyqxmd.com/read/28277164/pharmacokinetics-of-the-selective-prostacyclin-receptor-agonist-selexipag-in-rats-dogs-and-monkeys
#3
Tomohiko Ichikawa, Tetsuhiro Yamada, Alexander Treiber, Carmela Gnerre, Kiyoko Nonaka
1. This study examined the pharmacokinetics, distribution, metabolism and excretion of the selective prostacyclin receptor agonist selexipag (NS-304; ACT-293987) and its active metabolite MRE-269 (ACT-33679). The compounds were investigated following oral and/or intravenous administration to intact rats, dogs and monkeys, and bile-duct-cannulated rats and dogs. 2. After oral administration of [(14)C]selexipag, selexipag was well absorbed in rats and dogs with total recoveries of over 90% of the dose, mainly in the faeces...
March 2, 2017: Xenobiotica; the Fate of Foreign Compounds in Biological Systems
https://www.readbyqxmd.com/read/27990270/recent-advances-in-the-management-of-pulmonary-arterial-hypertension
#4
REVIEW
Halley Tsai, Yon K Sung, Vinicio de Jesus Perez
Over the past 20 years, there has been an explosion in the development of therapeutics to treat pulmonary arterial hypertension (PAH), a rare but life-threatening disorder associated with progressive elevation of pulmonary pressures and severe right heart failure. Recently, the field has seen the introduction of riociguat, a soluble guanylate cyclase stimulator, a new endothelin receptor antagonist (macitentan), and oral prostanoids (treprostinil and selexipag). Besides new drugs, there have been significant advances in defining the role of upfront combination therapy in treatment-naïve patients as well as proposed methods to deliver systemic prostanoids by use of implantable pumps...
2016: F1000Research
https://www.readbyqxmd.com/read/27988834/selexipag-a-review-in-pulmonary-arterial-hypertension
#5
REVIEW
Sean T Duggan, Susan J Keam, Celeste B Burness
Selexipag (Uptravi(®)) is an orally active, first-in-class, selective prostacyclin IP receptor agonist. Selexipag was approved recently in the EU for the long-term treatment of pulmonary arterial hypertension (PAH) in adult patients with WHO functional class (FC) II or III as combination therapy in patients insufficiently controlled with an endothelin receptor antagonist and/or a phosphodiesterase type 5 inhibitor or as monotherapy in patients who are not candidates for these therapies, and in the USA for the treatment of PAH (WHO Group I) to delay disease progression and reduce the risk of hospitalization for PAH...
February 2017: American Journal of Cardiovascular Drugs: Drugs, Devices, and Other Interventions
https://www.readbyqxmd.com/read/27971557/cost-effectiveness-analysis-of-selexipag-versus-inhaled-iloprost-in-the-treatment-of-pulmonary-arterial-hypertension-pah-in-sweden
#6
J Wlodarczyk, E Hunsche, B Silberberg, D Kemp, B Anell, K Corcoran, R Minacori, M Stevenson, A Beaudet
No abstract text is available yet for this article.
November 2016: Value in Health: the Journal of the International Society for Pharmacoeconomics and Outcomes Research
https://www.readbyqxmd.com/read/27919660/a-comparison-of-vasodilation-mode-among-selexipag-ns-304-2-4-5-6-diphenylpyrazin-2-yl-isopropyl-amino-butoxy-n-methylsulfonyl-acetamide-its-active-metabolite-mre-269-and-various-prostacyclin-receptor-agonists-in-rat-porcine-and-human-pulmonary-arteries
#7
Chiaki Fuchikami, Kohji Murakami, Koyuki Tajima, Junko Homan, Keiji Kosugi, Kazuya Kuramoto, Michiko Oka, Keiichi Kuwano
Selexipag (NS-304; [2-{4-[(5,6-diphenylpyrazin-2-yl)(isopropyl)amino]butoxy}-N- (methylsulfonyl)acetamide]) is a novel, orally available non-prostanoid prostacyclin receptor (IP receptor) agonist that has recently been approved for the treatment of pulmonary arterial hypertension (PAH). We examined the effect of the active metabolite of selexipag, MRE-269, and IP receptor agonists that are currently available as PAH therapeutic drugs on the relaxation of rat, porcine and human pulmonary artery. cAMP formation in human pulmonary artery smooth muscle cells was induced by all test compounds (MRE-269, epoprostenol, iloprost, treprostinil and beraprost sodium) and suppressed by IP receptor antagonists (CAY10441 and 2-[4-(1H-indol-4-yloxymethyl)-benzyloxycarbonylamino]-3-phenyl-propionic acid)...
December 3, 2016: European Journal of Pharmacology
https://www.readbyqxmd.com/read/27910296/the-year-since-the-guidelines-a-concise-update-on-recent-advances-in-pulmonary-hypertension
#8
Abhishek Mishra, Maninder Singh, Edo Kaluski
Since the updated pulmonary hypertension (PH) guidelines published in 2015, two major landmark trials have provided additional insight regarding therapeutic algorithms of PH. In this review, we concisely summarized the key findings of peer‑reviewed studies published in the last one year in the field of PH. These studies have enhanced our therapeutic abilities by introducing a new potent agent, selexipag, and by demonstrating the advantage of upfront combination therapy (endothelin receptor antagonist and phosphodiesterase‑5 inhibitor) versus single agent therapy in group 1 PH...
2017: Minerva Cardioangiologica
https://www.readbyqxmd.com/read/27899043/use-of-biologics-and-other-novel-therapies-for-the-treatment-of-systemic-sclerosis
#9
Cosimo Bruni, Emanuela Praino, Yannick Allanore, Oliver Distler, Armando Gabrielli, Florenzo Iannone, Marco Matucci-Cerinic
Systemic sclerosis (SSc) is a systemic autoimmune disease characterized by vasculopathy, inflammation and fibrosis. These three main disease-determining pathways are the target of the currently available treatments used to possibly modify the progression of disease-related manifestations, although this synergy has not been fully applied on SSc joint, skin or lung involvement yet. Areas covered: we describe the current status of SSc treatment/therapy performing a literature search in MEDLINE/Pubmed and Thomson Reuter's Web of Science for articles published until March 2016...
December 12, 2016: Expert Review of Clinical Immunology
https://www.readbyqxmd.com/read/27895464/selexipag-in-the-treatment-of-pulmonary-arterial-hypertension-design-development-and-therapy
#10
REVIEW
Elizabeth Ashley Hardin, Kelly M Chin
Pulmonary arterial hypertension is characterized by abnormalities in the small pulmonary arteries including increased vasoconstriction, vascular remodeling, proliferation of smooth muscle cells, and in situ thrombosis. Selexipag, a novel, oral prostacyclin receptor agonist, has been shown to improve hemodynamics in a phase II clinical trial and reduce clinical worsening in a large phase III clinical trial involving patients with pulmonary arterial hypertension. In this paper, we describe the prostacyclin signaling pathway, currently available oral prostanoid medications, and the development and clinical use of selexipag...
2016: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/27885399/absolute-oral-bioavailability-of-selexipag-a-novel-oral-prostacyclin-ip-receptor-agonist
#11
RANDOMIZED CONTROLLED TRIAL
Priska Kaufmann, Noémie Hurst, Béatrice Astruc, Jasper Dingemanse
PURPOSE: The aim of this single-center, open-label study was to assess the absolute bioavailability of an oral (tablet) versus intravenous (i.v.) formulation of selexipag in healthy subjects. METHODS: A pilot phase in three healthy male subjects, which preceded the main study, consisted of a single 20-minute i.v. infusion of 50 μg selexipag. Its objectives were to ensure the safety of the i.v. formulation and to select the i.v. dose for the main study. The main study had a randomized, two-way crossover design in 16 healthy male subjects...
February 2017: European Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/27756196/pharmacokinetic-drug-evaluation-of-selexipag-for-the-treatment-of-pulmonary-arterial-hypertension
#12
REVIEW
Mayank Sardana, Matthew Moll, Harrison W Farber
Management of pulmonary arterial hypertension (PAH) remains challenging even in the contemporary era. Intravenous prostacyclin therapy, while associated with decreased mortality, has practical limitations and requires significant lifestyle modifications. The recently approved long-acting oral IP prostacyclin receptor agonist for treatment of PAH, selexipag, is a non-prostanoid agent that vasodilates, impacts remodeling (anti-proliferative), reduces endothelial cell dysfunction, inhibits platelet aggregation (anti-thrombotic), and increases right heart inotropy...
December 2016: Expert Opinion on Drug Metabolism & Toxicology
https://www.readbyqxmd.com/read/27670133/selexipag-in-pulmonary-arterial-hypertension-most-updated-evidence-from-recent-preclinical-and-clinical-studies
#13
REVIEW
Raktim K Ghosh, Somedeb Ball, Avash Das, Dhrubajyoti Bandyopadhyay, Samhati Mondal, Debjit Saha, Anjan Gupta
Pulmonary arterial hypertension (PAH) is a relatively rare disease that, due to its chronic nature, has always been difficult to treat effectively. Selexipag is an oral prostacyclin (PGI2 ) agonist that was approved by US Food and Drug Administration (US FDA) in December 2015 for the treatment of PAH. After its success in phase 1 and phase 2 clinical trials regarding the convenient oral twice-daily dosing and low side-effect profile, selexipag raised the hope of controlling the disease progression in PAH patients...
May 2017: Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/27627939/update-on-pharmacotherapy-for-pulmonary-hypertension
#14
REVIEW
David L Prior, Heath Adams, Trevor J Williams
Pulmonary arterial hypertension (PAH) is a rare disease with a poor prognosis if not treated. Pharmacological treatment options for PAH have increased significantly over the past 10 years, with availability of intravenous, oral and inhaled drugs targeting the nitric oxide, endothelin and prostacyclin pathways. Treatment with these therapies in specialised pulmonary hypertension centres has resulted in reductions in patient symptoms, disease progression and mortality, and improved exercise capacity. Recognition of chronic thromboembolic pulmonary hypertension is important, as this cause of pulmonary hypertension may be amenable to surgical treatment...
September 19, 2016: Medical Journal of Australia
https://www.readbyqxmd.com/read/27615023/comparative-effectiveness-of-pharmacologic-interventions-for-pulmonary-arterial-hypertension-a-systematic-review-and-network-meta-analysis
#15
Snigdha Jain, Rohan Khera, Saket Girotra, David Badesch, Zhen Wang, Mohammad Hassan Murad, Amy Blevins, Gregory A Schmidt, Siddharth Singh, Alicia K Gerke
BACKGROUND: We conducted a systematic review and network meta-analysis to examine comparative efficacy and tolerability of pharmacologic interventions for pulmonary arterial hypertension (PAH). METHODS: MEDLINE, the Cochrane Register, EMBASE, CINAHL, and clinicaltrials.gov were searched (January 1, 1990 to March 3, 2016). Randomized controlled trials (RCTs) studying the approved pharmacologic agents endothelin receptor antagonists (ERA), phosphodiesterase inhibitors (PDE5i), the oral/inhaled (PO/INH) and IV/subcutaneous (SC) prostanoids, and riociguat and selexipag, alone or in combination, for pulmonary arterial hypertension (PAH) and reporting at least one efficacy outcome were selected...
January 2017: Chest
https://www.readbyqxmd.com/read/27574945/transition-from-inhaled-treprostinil-to-selexipag-in-pulmonary-arterial-hypertension
#16
Karim El-Kersh, J Shaun Smith
No abstract text is available yet for this article.
August 17, 2016: American Journal of Therapeutics
https://www.readbyqxmd.com/read/27491673/a-contemporary-approach-to-pulmonary-arterial-hypertension
#17
REVIEW
Udhay Krishnan, Evelyn M Horn
In recent years, there have been major changes in the landscape of pulmonary arterial hypertension therapy with the introduction of novel agents and innovative treatment strategies for this progressive disease. The aim of this review is to discuss the evolution in trial design in this field and highlight the salient features of recently published studies. We also summarize our approach to therapy selection in this chronic disease and identify areas for future exploration. The therapeutic armamentarium now includes 13 approved therapies...
September 2016: Current Atherosclerosis Reports
https://www.readbyqxmd.com/read/27467883/selexipag-for-the-treatment-of-pulmonary-arterial-hypertension
#18
REVIEW
Manuel Jonas Richter, Henning Gall, Jan Grimminger, Friedrich Grimminger, Hossein-Ardeschir Ghofrani
INTRODUCTION: Targeted pulmonary vasoactive substances are the cornerstone of treatment in pulmonary arterial hypertension (PAH). Approved drugs act on various receptors and molecules within the pulmonary arteries, mainly causing pulmonary vasodilation and potentially reversing remodeling with consequent improvement of right ventricular function. A key role is attributed to the prostacyclin pathway and especially the prostacyclin receptor (IP). Selexipag is a recently developed, non-prostanoid, oral IP receptor agonist for the treatment of PAH which has been approved in countries/regions including the USA and Europe...
September 2016: Expert Opinion on Pharmacotherapy
https://www.readbyqxmd.com/read/27434819/new-paradigm-for-pulmonary-arterial-hypertension-treatment
#19
Yuichi Tamura, Richard N Channick
PURPOSE OF REVIEW: Pulmonary arterial hypertension (PAH) was previously considered a uniformly fatal disease, with patients succumbing to right heart failure and death at an average of 3 years after diagnosis. The past 20 years, however, have seen the development of numerous targeted therapies that have changed the natural history of PAH. As more pharmacologic agents have been approved and utilized, further advances in the design of and endpoints for clinical trials. This study will review some of these notable developments...
September 2016: Current Opinion in Pulmonary Medicine
https://www.readbyqxmd.com/read/27303095/mepolizumab
#20
Dennis J Cada, Ross J Bindler, Danial E Baker
Each month, subscribers to The Formulary Monograph Service receive 5 to 6 well-documented monographs on drugs that are newly released or are in late phase 3 trials. The monographs are targeted to Pharmacy & Therapeutics Committees. Subscribers also receive monthly 1-page summary monographs on agents that are useful for agendas and pharmacy/nursing in-services. A comprehensive target drug utilization evaluation/medication use evaluation (DUE/MUE) is also provided each month. With a subscription, the monographs are sent in print and are also available on-line...
May 2016: Hospital Pharmacy
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