Literature DB >> 24461903

Efficacy and safety of the p38 MAPK inhibitor losmapimod for patients with chronic obstructive pulmonary disease: a randomised, double-blind, placebo-controlled trial.

Henrik Watz1, Helen Barnacle2, Benjamin F Hartley3, Robert Chan2.   

Abstract

BACKGROUND: The p38 MAPK pathway seems to be involved in pathogenesis of chronic obstructive pulmonary disease (COPD). Losmapimod is a potent and selective inhibitor of p38 MAPK. We assessed the effect of losmapimod on exercise tolerance in patients with COPD.
METHODS: We did this randomised, parallel-group, placebo-controlled trial at 46 secondary care centres in Argentina, Czech Republic, Estonia, Germany, Norway, South Korea, Ukraine, and USA between Nov 4, 2010, and Dec 22, 2011. We enrolled patients aged 40 years or older with moderate-to-severe COPD (6 min walking distance <350 m) who were current or previous smokers. Patients were randomly assigned (1:1:1:1) by a computer generated sequence to one of losmapimod 2·5 mg, 7·5 mg, or 15 mg, or placebo, twice daily for 24 weeks. Randomisation was stratified by country and exacerbation history (block size eight). Patients and investigators were masked to treatment assignment. The primary outcome was change in 6 min walking distance between baseline and week 24, assessed in the intention-to-treat population. This study is registered with ClinicalTrial.gov, number NCT01218126.
FINDINGS: We screened 886 patients, of whom 602 were enrolled and received treatment. The difference between the placebo group and the losmapimod groups for mean change of 6 min walk distance was not significant: -6·7 m (95% CI -18·2 to 4·9) for losmapimod 2·5 mg, -4·7 m (-16·1 to 6·8) for losmapimod 7·5 mg, and -3·4 m (-15·1 to 8·2) for losmapimod 15 mg. The safety profile was much the same in each group, although drug-related adverse events were more common with losmapimod 7·5 mg (n=19, 13%) and losmapimod 15 mg (n=20, 13%) than with placebo (n=11, 7%) and losmapimod 2·5 mg (n=13, 9%). The most common serious adverse events were COPD exacerbation resulting in admission to hospital (eight patients [5%] taking placebo, six [4%] taking losmapimod 2·5 mg, two [1%] taking losmapimod 7·5 mg, and three [2%] taking losmapimod 15 mg) and pneumonia (four [3%] vs 0 [0%] vs 1 [1%] vs 4 [3%]).
INTERPRETATION: Losmapimod did not cause an improvement in exercise tolerance or lung function, despite being well-tolerated in this COPD population. FUNDING: GlaxoSmithKline.
Copyright © 2014 Elsevier Ltd. All rights reserved.

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Year:  2013        PMID: 24461903     DOI: 10.1016/S2213-2600(13)70200-5

Source DB:  PubMed          Journal:  Lancet Respir Med        ISSN: 2213-2600            Impact factor:   30.700


  32 in total

1.  Blocking elevated p38 MAPK restores efferocytosis and inflammatory resolution in the elderly.

Authors:  Roel P H De Maeyer; Rachel C van de Merwe; Rikah Louie; Olivia V Bracken; Oliver P Devine; Daniel R Goldstein; Mohib Uddin; Arne N Akbar; Derek W Gilroy
Journal:  Nat Immunol       Date:  2020-04-06       Impact factor: 25.606

2.  The COPD Pipeline XXXIII.

Authors:  Nicholas Gross
Journal:  Chronic Obstr Pulm Dis       Date:  2017-01-09

3.  The COPD Pipeline, XXVI.

Authors:  Nicholas Gross
Journal:  Chronic Obstr Pulm Dis       Date:  2015-01-16

4.  Novel Noncatalytic Substrate-Selective p38α-Specific MAPK Inhibitors with Endothelial-Stabilizing and Anti-Inflammatory Activity.

Authors:  Nirav G Shah; Mohan E Tulapurkar; Aparna Ramarathnam; Amanda Brophy; Ramon Martinez; Kellie Hom; Theresa Hodges; Ramin Samadani; Ishwar S Singh; Alexander D MacKerell; Paul Shapiro; Jeffrey D Hasday
Journal:  J Immunol       Date:  2017-03-15       Impact factor: 5.422

5.  p38 Inhibition Ameliorates Inspiratory Resistive Breathing-Induced Pulmonary Inflammation.

Authors:  Dimitrios Toumpanakis; Vyronia Vassilakopoulou; Eleftheria Mizi; Athanasia Chatzianastasiou; Konstantinos Loverdos; Ioanna Vraila; Fotis Perlikos; Dionysios Tsoukalas; Charoula-Eleni Giannakopoulou; Adamantia Sotiriou; Maria Dettoraki; Vassiliki Karavana; Theodoros Vassilakopoulos
Journal:  Inflammation       Date:  2018-10       Impact factor: 4.092

Review 6.  Bringing Stability to the Chronic Obstructive Pulmonary Disease Patient: Clinical and Pharmacological Considerations for Frequent Exacerbators.

Authors:  Swati Gulati; J Michael Wells
Journal:  Drugs       Date:  2017-04       Impact factor: 9.546

Review 7.  Animal Models Reflecting Chronic Obstructive Pulmonary Disease and Related Respiratory Disorders: Translating Pre-Clinical Data into Clinical Relevance.

Authors:  Lloyd Tanner; Andrew Bruce Single
Journal:  J Innate Immun       Date:  2019-09-17       Impact factor: 7.349

Review 8.  Positioning new pharmacotherapies for COPD.

Authors:  Igor Z Barjaktarevic; Anthony F Arredondo; Christopher B Cooper
Journal:  Int J Chron Obstruct Pulmon Dis       Date:  2015-07-24

Review 9.  p38 MAPKs - roles in skeletal muscle physiology, disease mechanisms, and as potential therapeutic targets.

Authors:  Christopher M Brennan; Charles P Emerson; Jane Owens; Nicolas Christoforou
Journal:  JCI Insight       Date:  2021-06-22

10.  Oral and inhaled p38 MAPK inhibitors: effects on inhaled LPS challenge in healthy subjects.

Authors:  Dave Singh; Leonard Siew; Jared Christensen; Jonathan Plumb; Graham W Clarke; Steve Greenaway; Christelle Perros-Huguet; Nick Clarke; Iain Kilty; Lisa Tan
Journal:  Eur J Clin Pharmacol       Date:  2015-08-13       Impact factor: 3.064

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