Read by QxMD icon Read


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...
October 19, 2016: Expert Opinion on Drug Metabolism & Toxicology
Raktim K Ghosh, Somedeb Ball, Avash Das, Dhrubajyoti Bandyopadhyay, Samhati Mondal, Debjit Saha, Anjan Gupta
Pulmonary arterial hypertension (PAH) is a relatively rare disease which due to its chronic nature has always been difficult to treat effectively. Selexipag is an oral prostacyclin (PGI2) agonist, which 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...
September 27, 2016: Journal of Clinical Pharmacology
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
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 pharmacological interventions for pulmonary arterial hypertension (PAH). METHODS: MEDLINE, Cochrane register, EMBASE, CINAHL and were searched (January 1, 1990 - March 3, 2016). Randomized controlled trials (RCTs) of approved pharmacological agents - endothelin receptor antagonists (ERA), phosphodiesterase inhibitors (PDE5i), oral/inhaled and intravenous/subcutaneous prostanoids, riociguat, and selexipag, alone or in combination for pulmonary arterial hypertension (PAH) reporting at least one efficacy outcome were selected...
September 8, 2016: Chest
Karim El-Kersh, J Shaun Smith
No abstract text is available yet for this article.
August 17, 2016: American Journal of Therapeutics
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
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
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
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
Shirin Bruderer, Kaori Okubo, Hideya Mukai, Tim Mant, Jasper Dingemanse
PURPOSE: Selexipag is a new orally available nonprostanoid prostacyclin receptor agonist for the treatment of pulmonary arterial hypertension. Warfarin is commonly used in patients with pulmonary arterial hypertension. Possible pharmacodynamic and pharmacokinetic interactions between selexipag and warfarin in healthy individuals were investigated. METHODS: This was a double-blind, 2-way, 2-treatment crossover, Phase I study. Nineteen healthy men received a single dose of selexipag 400 μg or placebo on day 1, followed by selexipag 400 μg or placebo BID on days 2 to 12...
May 2016: Clinical Therapeutics
Priska Kaufmann, Hans G Cruz, Andreas Krause, Ivan Ulč, Atef Halabi, Jasper Dingemanse
AIM: The aim of the present study was to explore the effect of hepatic or renal dysfunction on the pharmacokinetics (PK), tolerability and safety of selexipag, an orally active prostacyclin receptor agonist. METHODS: Two prospective, open-label studies evaluated the PK of selexipag and its active metabolite ACT-333679 in healthy subjects and in subjects with mild, moderate and severe hepatic impairment or severe renal function impairment (SRFI). A single dose of 200 μg or 400 μg was administered...
August 2016: British Journal of Clinical Pharmacology
Chris Fellner
Lesinurad (Zurampic) for gout-related hyperuricemia; selexipag (Uptravi) for pulmonary arterial hypertension; sugammadex (Bridion) to reverse neuromuscular blockade after surgery; and alectinib (Alecensa) for lung cancer.
February 2016: P & T: a Peer-reviewed Journal for Formulary Management
Sri N Batchu, Syamantak Majumder, Bridgit B Bowskill, Kathryn E White, Suzanne L Advani, Angela S Brijmohan, Youan Liu, Kerri Thai, Paymon M Azizi, Warren L Lee, Andrew Advani
Discovery of common pathways that mediate both pancreatic β-cell function and end-organ function offers the opportunity to develop therapies that modulate glucose homeostasis and separately slow the development of diabetes complications. Here, we investigated the in vitro and in vivo effects of pharmacological agonism of the prostaglandin I2 (IP) receptor in pancreatic β-cells and in glomerular podocytes. The IP receptor agonist MRE-269 increased intracellular 3',5'-cyclic adenosine monophosphate (cAMP), augmented glucose-stimulated insulin secretion (GSIS), and increased viability in MIN6 β-cells...
May 2016: Diabetes
(no author information available yet)
No abstract text is available yet for this article.
February 15, 2016: Medical Letter on Drugs and Therapeutics
Lesley J Scott
Selexipag (Uptravi(®)) is a highly selective, long-acting, nonprostanoid, prostacyclin receptor agonist that is being developed by Actelion Pharmaceuticals Ltd and Nippon Shinyaku. Oral selexipag is approved in the USA for the treatment of pulmonary arterial hypertension (PAH; WHO Group I) to delay disease progression and reduce the risk of hospitalization for PAH. It has subsequently been approved in Canada for the long-term treatment of PAH, and received a positive opinion in the EU for the treatment of PAH in adult patients with WHO functional class II-III...
March 2016: Drugs
Olivier Sitbon, Richard Channick, Kelly M Chin, Aline Frey, Sean Gaine, Nazzareno Galiè, Hossein-Ardeschir Ghofrani, Marius M Hoeper, Irene M Lang, Ralph Preiss, Lewis J Rubin, Lilla Di Scala, Victor Tapson, Igor Adzerikho, Jinming Liu, Olga Moiseeva, Xiaofeng Zeng, Gérald Simonneau, Vallerie V McLaughlin
BACKGROUND: In a phase 2 trial, selexipag, an oral selective IP prostacyclin-receptor agonist, was shown to be beneficial in the treatment of pulmonary arterial hypertension. METHODS: In this event-driven, phase 3, randomized, double-blind, placebo-controlled trial, we randomly assigned 1156 patients with pulmonary arterial hypertension to receive placebo or selexipag in individualized doses (maximum dose, 1600 μg twice daily). Patients were eligible for enrollment if they were not receiving treatment for pulmonary arterial hypertension or if they were receiving a stable dose of an endothelin-receptor antagonist, a phosphodiesterase type 5 inhibitor, or both...
December 24, 2015: New England Journal of Medicine
Kamal Sharma
The endothelin (ET), nitric oxide (NO) and prostacyclin (PGI2) pathways are involved in pulmonary arterial hypertension (PAH) pathogenesis. While ET and NO are targeted early in the disease process, limitations of current pharmacotherapies that target the PGI2 pathway (PGI2 or PGI2 analogues) result in them not being used or delayed. Selexipag is a novel oral, selective agonist of the PGI2 (IP) receptor. Activation of the IP receptor induces vasodilation in the pulmonary circulation and inhibits the proliferation of vascular smooth muscle cells, key factors in PAH pathogenesis...
2016: Expert Review of Respiratory Medicine
Priska Kaufmann, Jasper Dingemanse
No abstract text is available yet for this article.
October 2015: American Journal of Cardiovascular Drugs: Drugs, Devices, and Other Interventions
Nuggehally R Srinivas
No abstract text is available yet for this article.
October 2015: American Journal of Cardiovascular Drugs: Drugs, Devices, and Other Interventions
Tetsuo Asaki, Keiichi Kuwano, Keith Morrison, John Gatfield, Taisuke Hamamoto, Martine Clozel
Prostacyclin controls cardiovascular function via activation of the prostacyclin receptor. Decreased prostacyclin production occurs in several cardiovascular diseases. However, the clinical use of prostacyclin and its analogues is complicated by their chemical and metabolic instability. A medicinal chemistry program searched for novel nonprostanoid prostacyclin receptor agonists not subject to these limitations. A compound with a diphenylpyrazine structural core was synthesized. Metabolic stability and agonist potency were optimized through modification of the linear side chain...
September 24, 2015: Journal of Medicinal Chemistry
Fetch more papers »
Fetching more papers... Fetching...
Read by QxMD. Sign in or create an account to discover new knowledge that matter to you.
Remove bar
Read by QxMD icon Read

Search Tips

Use Boolean operators: AND/OR

diabetic AND foot
diabetes OR diabetic

Exclude a word using the 'minus' sign

Virchow -triad

Use Parentheses

water AND (cup OR glass)

Add an asterisk (*) at end of a word to include word stems

Neuro* will search for Neurology, Neuroscientist, Neurological, and so on

Use quotes to search for an exact phrase

"primary prevention of cancer"
(heart or cardiac or cardio*) AND arrest -"American Heart Association"