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https://www.readbyqxmd.com/read/27917591/the-pde4-inhibitor-roflumilast-reduces-weight-gain-by-increasing-energy-expenditure-and-leads-to-improved-glucose-metabolism
#1
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
#2
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
#3
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
#4
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
#5
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...
November 2, 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
#6
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
#7
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
#8
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
#9
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
#10
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
#11
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
#12
Kevin R Kelly, Alex Mejia, Avvaru Suhasini, An-Ping Lin, John G Kuhn, Anand Karnad, Steven Weitman, Ricardo C T Aguiar
PURPOSE: In this study, we aimed to validate our extensive pre-clinical 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 anti-tumor activity of the FDA-approved PDE4 inhibitor roflumilast in combination with prednisone in patients with advanced B cell malignancies. EXPERIMENTAL DESIGN: Single center, exploratory phase Ib open-label, non-randomized study...
August 19, 2016: Clinical Cancer Research: An Official Journal of the American Association for Cancer Research
https://www.readbyqxmd.com/read/27453494/molecularly-targeted-therapies-for-asthma-current-development-challenges-and-potential-clinical-translation
#13
REVIEW
Ibrahim Sulaiman, Jonathan Chee Woei Lim, Hon Liong Soo, Johnson Stanslas
Extensive research into the therapeutics of asthma has yielded numerous effective interventions over the past few decades. However, adverse effects and ineffectiveness of most of these medications especially in the management of steroid resistant severe asthma necessitate the development of better medications. Numerous drug targets with inherent airway smooth muscle tone modulatory role have been identified for asthma therapy. This article reviews the latest understanding of underlying molecular aetiology of asthma towards design and development of better antiasthma drugs...
October 2016: Pulmonary Pharmacology & Therapeutics
https://www.readbyqxmd.com/read/27423044/simultaneous-determination-of-roflumilast-and-its-metabolite-in-human-plasma-by-lc-ms-ms-application-for-a-pharmacokinetic-study
#14
Xinge Cui, Jie Huang, Xin Zheng, Ji Jiang, Yun Kuang, Pei Hu
Roflumilast had shown good efficacy and safety in Caucasian COPD patients after oral administration of 0.5mg. The main active metabolite of it is roflumilast N-oxide. A reliable liquid chromatography-tandem mass spectrometry (LC-MS/MS) quantitation method was developed for the simultaneous determination of them in human plasma with rather low limits of quantitation for roflumilast (0.02ng/mL) and roflumilast N-oxide (0.04ng/mL). Human plasma samples were prepared by solid phase extraction (SPE), which ensured high recovery and slight matrix effect for the both analytes...
September 1, 2016: Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences
https://www.readbyqxmd.com/read/27418821/potential-treatment-benefits-and-safety-of-roflumilast-in-copd-a-systematic-review-and-meta-analysis
#15
REVIEW
Lianfang Yuan, Xuan Dai, Meng Yang, Qiling Cai, Na Shao
BACKGROUND: Current evidence suggests that roflumilast is efficacious in treating COPD, especially in preventing the acute exacerbation of COPD. OBJECTIVES: This study was designed to evaluate the clinical effects and safety of roflumilast in the treatment of stable COPD using randomized clinical trial (RCT) data. METHODS: A MEDLINE, EMBASE, and Cochrane Controlled Trials Register search was carried out. RCTs reporting the treatment effects of roflumilast in COPD were identified...
2016: International Journal of Chronic Obstructive Pulmonary Disease
https://www.readbyqxmd.com/read/27401583/virtual-screening-of-drugbank-reveals-two-drugs-as-new-bcrp-inhibitors
#16
Floriane Montanari, Anna Cseke, Katrin Wlcek, Gerhard F Ecker
The breast cancer resistance protein (BCRP) is an ABC transporter playing a crucial role in the pharmacokinetics of drugs. The early identification of substrates and inhibitors of this efflux transporter can help to prevent or foresee drug-drug interactions. In this work, we built a ligand-based in silico classification model to predict the inhibitory potential of drugs toward BCRP. The model was applied as a virtual screening technique to identify potential inhibitors among the small-molecules subset of DrugBank...
July 8, 2016: Journal of Biomolecular Screening
https://www.readbyqxmd.com/read/27390702/the-safety-and-effectiveness-of-the-current-treatment-regimen-with-or-without-roflumilast-in-advanced-copd-patients-a-systematic-review-and-meta-analysis-of-randomized-controlled-trials
#17
Saeideh Jafari Andarian, Alireza Olyaeemanesh, Seyed Alireza Hosseini, Ali Akbari Sari, Shahram Firoozbakhsh, Mojtaba Nouhi Jadesi, Mohammadreza Mobinizadeh
BACKGROUND: Chronic obstructive pulmonary disease (COPD) is a chronic respiratory disease, which reduces the lung function and causes respiratory symptoms over time, and it is primarily associated with shortness of breath, cough and sputum production. Roflumilast, which is a long-acting selective inhibitor, reduces the anti-inflammatory effect of the main symptoms of COPD. The aim of this study was to compare the clinical effectiveness of adding roflumilast to the current treatment regimen of patients with severe COPD...
2016: Medical Journal of the Islamic Republic of Iran
https://www.readbyqxmd.com/read/27388992/pde4-inhibition-as-potential-treatment-of%C3%A2-epidermolysis-bullosa-acquisita
#18
Hiroshi Koga, Andreas Recke, Gestur Vidarsson, Hendri H Pas, Marcel F Jonkman, Takashi Hashimoto, Anika Kasprick, Saeedeh Ghorbanalipoor, Hermann Tenor, Detlef Zillikens, Ralf J Ludwig
Pemphigoid diseases such as epidermolysis bullosa acquisita (EBA) may be difficult to treat. In pemphigoid diseases, mucocutaneous blistering is caused by autoantibodies to hemidesmosomal antigens; in EBA the autoantigen is type VII collagen. Despite growing insights into pemphigoid disease pathogenesis, corticosteroids are still a mainstay of treatment. In experimental EBA, myeloid cell activation is a key event leading to blistering. Activation of these cells depends on phosphodiesterase (PDE) 4. We therefore evaluated the potential for PDE4 inhibition in EBA: PDE4 was highly expressed in inflammatory cells and in the epidermis of patients compared with healthy skin samples...
July 5, 2016: Journal of Investigative Dermatology
https://www.readbyqxmd.com/read/27306372/pharmacokinetics-of-roflumilast-and-its-active-metabolite-roflumilast-n-oxide-in-healthy-chinese-subjects-after-single-and-multiple-oral-doses
#19
Qian Li, Yiya Wang, Lingye Liu, Pengcheng Ma, Li Ding
BACKGROUND AND OBJECTIVES: Roflumilast is a selective, oral phosphodiesterase 4 inhibitor approved for the treatment of severe chronic obstructive pulmonary disease. The aim of this study was to evaluate the pharmacokinetics of roflumilast and roflumilast N-oxide in healthy Chinese subjects, and the effects of gender and food on their respective pharmacokinetic profiles. METHODS: 36 healthy Chinese subjects were recruited in a randomized, single-center, open-label, parallel group study and assigned to 0...
June 15, 2016: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/27279341/drug-safety-evaluation-of-roflumilast-for-the-treatment-of-copd-a-meta-analysis
#20
Paola Rogliani, Luigino Calzetta, Mario Cazzola, Maria Gabriella Matera
INTRODUCTION: Roflumilast is the only phosphodiesterase 4 inhibitor approved for the treatment of COPD patients with chronic cough and sputum, and a history of exacerbations, but the compliance to treatment is reduced by poorly tolerated adverse events (AEs). AREAS COVERED: The synthesis of clinical evidences indicates that roflumilast 500μg once-daily increased the risk of AEs, with no impact on the risk of serious AEs (SAEs), compared with placebo. Gastrointestinal AEs were common in patients treated with roflumilast, that may also induce headache, backpain and insomnia...
August 2016: Expert Opinion on Drug Safety
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