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Roflumilast

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https://www.readbyqxmd.com/read/28201975/selective-inhibition-of-phosphodiesterases-4a-b-c-and-d-isoforms-in-chronic-respiratory-diseases-current-and-future-evidences
#1
Sonia Contreras, Javier Milara, Esteban Morcillo, Julio Cortijo
Chronic respiratory diseases affect millions of people every day. According to World Health Organization estimates, ~235 million people suffer from asthma, ~64 million suffer from chronic obstructive pulmonary disease (COPD), and millions more suffer from allergic rhinitis around the world. In recent last years, the first phosphodiesterase 4 (PDE4) inhibitor, roflumilast, was approved as a treatment to reduce the risk of exacerbations in stable and severe COPD associated with chronic bronchitis and a history of exacerbations...
February 13, 2017: Current Pharmaceutical Design
https://www.readbyqxmd.com/read/28196344/identification-characterization-and-in-silico-admet-prediction-of-roflumilast-degradation-products
#2
Mariana S Pinheiro, Gil M Viana, Bárbara de A Abrahim Vieira, Alessandra Mendonça Teles de Souza, Carlos Rangel Rodrigues, Rita de Cássia E E Marins, Lúcio M Cabral, Valéria P de Sousa
The present study reports the degradation behavior of roflumilast (RFL), a new drug developed for the treatment of chronic obstructive pulmonary disease. The degradation of RFL was tested under various stress conditions as per the guidelines of the International Conference on Harmonization. The degradation products (DPs) of RFL were identified, characterized and in silico predictions were made of their pharmacokinetic properties, absorption, distribution, metabolism, excretion and toxicity (ADMET). RFL was subjected to various stress conditions including photodegradation, alkaline and acidic hydrolysis, oxidative and metallic degradation...
February 6, 2017: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/28146642/randomized-double-blind-controlled-trial-of-roflumilast-at-acute-exacerbations-of-copd
#3
Alex J Mackay, Anant Rc Patel, Richa Singh, Raymond J Sapsford, Gavin C Donaldson, Niyati Prasad, Udo-Michael Goehring, Tsz Keung Nip, Jadwiga A Wedzicha
No abstract text is available yet for this article.
February 1, 2017: American Journal of Respiratory and Critical Care Medicine
https://www.readbyqxmd.com/read/28108651/roflumilast-and-aquaporin-2-regulation-in-rat-renal-inner-medullary-collecting-duct
#4
Ezigbobiara N Umejiego, Yanhua Wang, Mark A Knepper, Chung-Lin Chou
Roflumilast is a cyclic nucleotide phosphodiesterase inhibitor that is FDA-approved for treatment of chronic obstructive pulmonary disease. With a view toward possible use for treatment of patients with X-linked nephrogenic diabetes insipidus (NDI) due to hemizygous mutations in the V2 vasopressin receptor, this study sought to determine the effect of roflumilast on aquaporin-2 (AQP2) phosphorylation, AQP2 trafficking, and water permeability in the rat inner medullary collecting duct (IMCD). In the presence of the vasopressin analog dDAVP (0...
January 2017: Physiological Reports
https://www.readbyqxmd.com/read/28088839/pharmacokinetic-pharmacodynamic-modeling-of-the-pde4-inhibitor-tak-648-in-type-2-diabetes-early-translational-approaches-for-human-dose-prediction
#5
N Plock, S Vollert, M Mayer, G Hanauer, G Lahu
TAK-648 is a PDE4 inhibitor with demonstrated preclinical antidiabetic properties. Our objective was to develop a translational pharmacokinetic/pharmacodynamic (PK/PD) model for human type 2 diabetes (T2D) dose prediction using HbA1c results from a db/db mouse study. Estimated parameters in combination with tPDE4i values calculated for the clinical roflumilast dose of 500 μg were used to translate preclinical effects of TAK-648 to required exposure in humans. A first-in-human study with single TAK-648 doses of 0...
January 15, 2017: Clinical and Translational Science
https://www.readbyqxmd.com/read/28056550/co-inhalation-of-roflumilast-rather-than-formoterol-with-fluticasone-more-effectively-improves-asthma-in-asthmatic-mice
#6
Hussam A Murad, Hamed S Habib, Misbahuddin M Rafeeq, Mansour I Sulaiman, Amer S Abdulrahman, Mohamad Nidal Khabaz
Roflumilast is approved as an add-on therapy for chronic obstructive pulmonary disease. The inflammation in chronic obstructive pulmonary disease is mainly neutrophilic, while in asthma it is mainly eosinophilic, studies addressing role of roflumilast in eosinophilic inflammation are recommended. Also in severe asthma, the dominant inflammatory cells are neutrophils. Thus, roflumilast has a potential off-label use in the treatment of asthma. This study was designed to evaluate the effects of co-inhalation of roflumilast and fluticasone compared to that of formoterol and fluticasone in ovalbumin-sensitized and-challenged BALB/c mice...
January 1, 2017: Experimental Biology and Medicine
https://www.readbyqxmd.com/read/27997807/roflumilast-n-oxide-in-combination-with-formoterol-enhances-the-anti-inflammatory-effect-of-dexamethasone-in-asm-cells
#7
Brijeshkumar S Patel, Md Mostafizur Rahman, Gina Baehring, Dikaia Xenaki, Francesca Su-May Tang, Brian G Oliver, Alaina J Ammit
Roflumilast is an orally active phosphodiesterase 4 (PDE4) inhibitor approved for use in chronic obstructive pulmonary disease. Roflumilast N-oxide (RNO) is the active metabolite of roflumilast and has demonstrated anti-inflammatory impact in vivo and in vitro. To date, the effect of RNO on the synthetic function of airway smooth muscle (ASM) cells is unknown. We address this herein and investigate the effect of RNO on β2-adrenoceptor-mediated, cAMP-dependent responses in ASM cells in vitro, and whether RNO enhances steroid-induced repression of inflammation...
December 20, 2016: American Journal of Respiratory Cell and Molecular Biology
https://www.readbyqxmd.com/read/27971548/cost-effectiveness-of-roflumilast-as-add-on-to-triple-inhaled-therapy-vs-triple-inhaled-therapy-in-patients-with-severe-and-very-severe-copd-associated-with-chronic-bronchitis-in-sweden
#8
A Engström, N Varol
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/27917591/the-pde4-inhibitor-roflumilast-reduces-weight-gain-by-increasing-energy-expenditure-and-leads-to-improved-glucose-metabolism
#9
Julia Möllmann, Florian Kahles, Corinna Lebherz, Ben Kappel, Christer Baeck, Frank Tacke, Christian Werner, Massimo Federici, Nikolaus Marx, Michael Lehrke
AIMS: The PDE4 inhibitor roflumilast is a clinically approved anti-inflammatory drug used for the treatment of chronic obstructive pulmonary disease. In addition, roflumilast was found to reduce body weight and improve glucose metabolism by a yet unknown mechanism. MATERIALS AND METHODS: Metabolic effects of roflumilast were investigated in C57BL/6J mice on high fat western-type diet treated with or without roflumilast for a period of 12 weeks. RESULTS: Roflumilast led to a marked reduction of body weight gain, which became apparent in the second week following treatment initiation and was attributable to a pronounced increase of energy expenditure...
December 5, 2016: Diabetes, Obesity & Metabolism
https://www.readbyqxmd.com/read/27853934/evaluation-of-in-vitro-cytochrome-p450-inhibition-and-in-vitro-fate-of-structurally-diverse-n-oxide-metabolites-case-studies-with-clozapine-levofloxacin-roflumilast-voriconazole-and-zopiclone
#10
Poonam Giri, Sneha Naidu, Nirmal Patel, Harilal Patel, Nuggehally R Srinivas
BACKGROUND AND OBJECTIVES: The role of metabolite(s) to elicit potential clinical drug-drug interaction (DDI) via cytochrome P450 enzymes (CYP) is gaining momentum. In this context, the role of N-oxides for in vitro CYP inhibition has not been evaluated. The objectives of this study were: (a) to examine in vitro CYP inhibition of N-oxides of clozapine, levofloxacin, roflumilast, voriconazole and zopiclone in a tiered approach and (b) evaluate in vitro fate of aforementioned N-oxides examined in recombinant CYPs, human microsomes and hepatocytes...
November 16, 2016: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/27844172/xanthines-and-phosphodiesterase-inhibitors
#11
D Spina, C P Page
Theophylline is an orally acting xanthine that has been used since 1937 for the treatment of respiratory diseases including asthma and chronic obstructive pulmonary disease (COPD). However, in most treatment guidelines, xanthines have now been consigned to third-line therapy because of their narrow therapeutic window and propensity for drug-drug interactions. However, lower than conventional doses of theophylline considered to be bronchodilator are now known to have anti-inflammatory actions of relevance to the treatment of respiratory disease...
November 15, 2016: Handbook of Experimental Pharmacology
https://www.readbyqxmd.com/read/27821246/erratum-to-effect-of-roflumilast-novel-phosphodiesterase-4-inhibitor-on-lung-chronic-graft-versus-host-disease-in-mice
#12
Sei Won Kim, Ji Young Lim, Chin Kook Rhee, Ji Hye Kim, Chan Kwon Park, Tae Jung Kim, Chul Soo Cho, Chang Ki Min, Hyoung Kyu Yoon
No abstract text is available yet for this article.
November 4, 2016: Experimental Hematology
https://www.readbyqxmd.com/read/27804148/efficacy-of-phosphodiesterase-4-inhibitors-in-juvenile-batten-disease-cln3
#13
Amy Aldrich, Megan E Bosch, Rachel Fallet, Jessica Odvody, Maria Burkovetskaya, Kakulavarapu V Rama Rao, Jonathan D Cooper, Arlene V Drack, Tammy Kielian
OBJECTIVE: Juvenile neuronal ceroid lipofuscinosis (JNCL), or juvenile Batten disease, is a pediatric lysosomal storage disease caused by autosomal recessive mutations in CLN3, typified by blindness, seizures, progressive cognitive and motor decline, and premature death. Currently, there is no treatment for JNCL that slows disease progression, which highlights the need to explore novel strategies to extend the survival and quality of life of afflicted children. Cyclic adenosine monophosphate (cAMP) is a second messenger with pleiotropic effects, including regulating neuroinflammation and neuronal survival...
December 2016: Annals of Neurology
https://www.readbyqxmd.com/read/27747018/efficiency-and-safety-of-roflumilast-combined-with-long-acting-bronchodilators-on-moderate-to-severe-stable-chronic-obstructive-pulmonary-disease-patients-a-meta-analysis
#14
Peng Luo, Shuo Li, Yitai Chen, Yuwen Luo, Yun Li, Kai Wang, Yuxia Huang, Xin Chen
BACKGROUND: Roflumilast, a phosphodiesterase-4 inhibitor recommended by clinical guideline, is always being used in combination with at least one long-acting bronchodilator in patients with stable chronic obstructive pulmonary disease (COPD). However, there are few evidences about whether the combination of roflumilast and long-acting bronchodilators is safer and more effective in patients with moderate-to-very severe stable COPD. In our study, we investigate the effect and safety of roflumilast combined with long-acting bronchodilators on moderate-to-severe stable COPD patients...
September 2016: Journal of Thoracic Disease
https://www.readbyqxmd.com/read/27625465/body-mass-index-airflow-obstruction-dyspnea-and-exercise-index-is-not-modified-after-6-months-therapy-with-roflumilast-in-a-cohort-of-patients-with-chronic-obstructive-pulmonary-disease
#15
Silvano Dragonieri, Vitaliano N Quaranta, Pierluigi Carratu, Donato Lacedonia, Giovanna Elisiana Carpagnano, Annamaria Milano, Giuseppina D'Alba, Teresa Ranieri, Maria Pia Foschino Barbaro, Onofrio Resta
No abstract text is available yet for this article.
September 2016: Lung India: Official Organ of Indian Chest Society
https://www.readbyqxmd.com/read/27613392/pharmacological-strategies-to-reduce-exacerbation-risk-in-copd-a-narrative-review
#16
REVIEW
Marc Miravitlles, Anthony D'Urzo, Dave Singh, Vladimir Koblizek
Identifying patients at risk of exacerbations and managing them appropriately to reduce this risk represents an important clinical challenge. Numerous treatments have been assessed for the prevention of exacerbations and their efficacy may differ by patient phenotype. Given their centrality in the treatment of COPD, there is strong rationale for maximizing bronchodilation as an initial strategy to reduce exacerbation risk irrespective of patient phenotype. Therefore, in patients assessed as frequent exacerbators (>1 exacerbation/year) we propose initial bronchodilator treatment with a long-acting muscarinic antagonist (LAMA)/ long-acting β2-agonist (LABA)...
September 10, 2016: Respiratory Research
https://www.readbyqxmd.com/read/27606039/benefits-of-early-roflumilast-treatment-after-hospital-or-emergency-department-discharge-for-a-copd-exacerbation
#17
Qing Lee, Michelle Mocarski, Shawn X Sun
BACKGROUND: Chronic lower respiratory disease, which includes chronic obstructive pulmonary disease (COPD), is the third leading cause of death in the United States. Roflumilast is an oral, once-daily, selective phosphodiesterase-4 inhibitor approved for reducing the risk for COPD exacerbations in patients with severe COPD associated with chronic bronchitis and a history of exacerbations. OBJECTIVES: To evaluate the effects of roflumilast treatment timing on COPD exacerbation rates (primary objective) and on resource utilization and healthcare costs (secondary objective) after hospital or emergency department discharge associated with a COPD exacerbation...
May 2016: American Health & Drug Benefits
https://www.readbyqxmd.com/read/27585384/effect-of-roflumilast-and-inhaled-corticosteroid-long-acting-%C3%AE-2-agonist-on-chronic-obstructive-pulmonary-disease-exacerbations-re-2-spond-a-randomized-clinical-trial
#18
Fernando J Martinez, Klaus F Rabe, Sanjay Sethi, Emilio Pizzichini, Andrew McIvor, Antonio Anzueto, Vijay K T Alagappan, Shahid Siddiqui, Ludmyla Rekeda, Christopher J Miller, Sofia Zetterstrand, Colin Reisner, Stephen I Rennard
RATIONALE: Moderate and severe exacerbations are incompletely prevented by maximal inhalation therapy in patients with severe chronic obstructive pulmonary disease. OBJECTIVES: To determine whether roflumilast reduces moderate and/or severe chronic obstructive pulmonary disease exacerbations in patients at risk for exacerbations despite treatment with inhaled corticosteroid/long-acting β2-agonist with or without a long-acting muscarinic antagonist (LAMA). METHODS: In this 52-week, phase 4, double-blind, placebo-controlled RE(2)SPOND (Roflumilast Effect on Exacerbations in Patients on Dual [LABA/ICS] Therapy) trial (NCT01443845), participants aged 40 years or older with severe/very severe chronic obstructive pulmonary disease, chronic bronchitis, two or more exacerbations and/or hospitalizations in the previous year, and receiving inhaled corticosteroid/long-acting β2-agonist with or without LAMA daily for 3 or more months were equally randomized to once-daily roflumilast, 500 μg (n = 1,178), or placebo (n = 1,176)...
September 1, 2016: American Journal of Respiratory and Critical Care Medicine
https://www.readbyqxmd.com/read/27574416/effects-of-roflumilast-in-copd-patients-receiving-inhaled-corticosteroid-long-acting-%C3%AE-2-agonist-fixed-dose-combination-re-2-spond-rationale-and-study-design
#19
Stephen I Rennard, Fernando J Martinez, Klaus F Rabe, Sanjay Sethi, Emilio Pizzichini, Andrew McIvor, Shahid Siddiqui, Antonio Anzueto, Haiyuan Zhu
BACKGROUND: Roflumilast, a once-daily, selective phosphodiesterase-4 inhibitor, reduces the risk of COPD exacerbations in patients with severe COPD associated with chronic bronchitis and a history of exacerbations. The RE(2)SPOND study is examining whether roflumilast, when added to an inhaled corticosteroid/long-acting β2-agonist (ICS/LABA) fixed-dose combination (FDC), further reduces exacerbations. The methodology is described herein. METHODS: In this Phase IV, multicenter, double-blind, placebo-controlled, parallel-group trial, participants were randomized 1:1 (stratified by long-acting muscarinic antagonist use) to receive roflumilast or placebo, plus ICS/LABA FDC, for 52 weeks...
2016: International Journal of Chronic Obstructive Pulmonary Disease
https://www.readbyqxmd.com/read/27542768/safety-and-pharmacodynamics-of-the-pde4-inhibitor-roflumilast-in-advanced-b-cell-malignancies
#20
Kevin Kelly, Alex Mejia, Avvaru N Suhasini, An-Ping Lin, John Kuhn, Anand B Karnad, Steven Weitman, Ricardo C T Aguiar
PURPOSE: In this study, we aimed to validate our extensive preclinical data on phosphodiesterase 4 (PDE4) as actionable target in B-cell malignancies. Our specific objectives were to determine the safety, pharmacokinetics, and pharmacodynamics (PI3K/AKT activity), as well as to capture any potential antitumor activity of the PDE4 inhibitor roflumilast in combination with prednisone in patients with advanced B-cell malignancies. EXPERIMENTAL DESIGN: Single-center, exploratory phase Ib open-label, nonrandomized study...
August 19, 2016: Clinical Cancer Research: An Official Journal of the American Association for Cancer Research
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