LATE-BREAKING ABSTRACT: Safety, pharmacokinetic and pharmacodynamic profile of RV1162, a narrow spectrum kinase inhibitor, in healthy subjects and COPD patients

Russell, Paul; Stevenson, Chris; Charron, Catherine E.; Brindley, Charlie; Singh, Dave

doi:10.1183/13993003.congress-2015.pa4361

Cited by 4 publications

(4 citation statements)

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“…RV-568 is a potent inhaled p38 inhibitor that inhibits all four isoforms of p38 and also the Src family kinase Hck and is referred to as a narrow spectrum kinase inhibitor, which significantly increased FEV 1 and reduced sputum malondealdehyde after 2 weeks of administration (Russell et al, 2013). No clinical studies of p38 inhibitors in asthma have been reported, and most of the drugs in development for COPD have now been discontinued.…”

Section: B P38 Inhibitorsmentioning

confidence: 99%

Kinases as Novel Therapeutic Targets in Asthma and Chronic Obstructive Pulmonary Disease

Barnes

2016

Pharmacological Reviews

103

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Section: B P38 Inhibitorsmentioning

confidence: 99%

Kinases as Novel Therapeutic Targets in Asthma and Chronic Obstructive Pulmonary Disease

Barnes

2016

Pharmacological Reviews

103

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“…Various preclinical studies have reported its efficacy in inhibiting proinflammatory cytokine gene expression, histamine-induced hyperresponsiveness and human rhinovirus (HRV) 16 inflammation and replication [47][48][49][50][51][52]. In 28 GOLD II/III COPD subjects it was reported that RV568 was superior to placebo in FEV1 measurements, serum and sputum inflammatory markers and was safe [53]. With these safety, pharmacokinetic and pharmacodynamic profiles, inhaled RV568 has been advanced into further Phase II clinical studies in COPD subjects (NCT01867762).…”

Section: Novel Anti-inflammatory Agents (mentioning

confidence: 98%

Emerging therapeutic strategies in COPD

Babu

Morjaria

2015

Drug Discovery Today

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“…The administration of 100 μg/day RV-568 was well tolerated in COPD patients for seven days [169]. Studies have shown that inhaled RV-568 significantly improves the FEV1 index after 14 days and reduces sputum malondialdehyde and myeloperoxidase levels [170]. Furthermore, another study indicated that RV-568 inhibits the expression of IL-1β and CXCL-8 cytokines by 90% and 73%, respectively, at the highest administered doses [171].…”

Section: Insights From Clinical Trialsmentioning

confidence: 99%

p38 MAPK signaling in chronic obstructive pulmonary disease pathogenesis and inhibitor therapeutics

Ahmadi,

Ahrari,

Salimian

et al. 2023

Cell Commun Signal

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Background Chronic obstructive pulmonary disease (COPD) is characterized by persistent respiratory symptoms and airflow limitation due to airway and/or alveolar remodeling. Although the abnormalities are primarily prompted by chronic exposure to inhaled irritants, maladjusted and self-reinforcing immune responses are significant contributors to the development and progression of the disease. The p38 isoforms are regarded as pivotal hub proteins that regulate immune and inflammatory responses in both healthy and disease states. As a result, their inhibition has been the subject of numerous recent studies exploring their therapeutic potential in COPD. Main body We performed a systematic search based on the PRISMA guidelines to find relevant studies about P38 signaling in COPD patients. We searched the PubMed and Google Scholar databases and used “P38” AND “COPD” Mesh Terms. We applied the following inclusion criteria: (1) human, animal, ex vivo and in vitro studies; (2) original research articles; (3) published in English; and (4) focused on P38 signaling in COPD pathogenesis, progression, or treatment. We screened the titles and abstracts of the retrieved studies and assessed the full texts of the eligible studies for quality and relevance. We extracted the following data from each study: authors, year, country, sample size, study design, cell type, intervention, outcome, and main findings. We classified the studies according to the role of different cells and treatments in P38 signaling in COPD. Conclusion While targeting p38 MAPK has demonstrated some therapeutic potential in COPD, its efficacy is limited. Nevertheless, combining p38 MAPK inhibitors with other anti-inflammatory steroids appears to be a promising treatment choice. Clinical trials testing various p38 MAPK inhibitors have produced mixed results, with some showing improvement in lung function and reduction in exacerbations in COPD patients. Despite these mixed results, research on p38 MAPK inhibitors is still a major area of study to develop new and more effective therapies for COPD. As our understanding of COPD evolves, we may gain a better understanding of how to utilize p38 MAPK inhibitors to treat this disease.

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LATE-BREAKING ABSTRACT: Safety, pharmacokinetic and pharmacodynamic profile of RV1162, a narrow spectrum kinase inhibitor, in healthy subjects and COPD patients

Cited by 4 publications

References 0 publications

Kinases as Novel Therapeutic Targets in Asthma and Chronic Obstructive Pulmonary Disease

Kinases as Novel Therapeutic Targets in Asthma and Chronic Obstructive Pulmonary Disease

Emerging therapeutic strategies in COPD

p38 MAPK signaling in chronic obstructive pulmonary disease pathogenesis and inhibitor therapeutics

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