Synonyms: RPL554
Compound class:
Synthetic organic
Comment: Ensifentrine (RPL-554) is an inhibitor of phosphodiesterases 3 and 4 (PDE3 and PDE4) [2]. It has bronchodilatory action [4,6] that is associated with short-term improvement in lung function [3], and has been investigated for therapeutic potential in asthma and chronic obstructive pulmonary disease (COPD). Ensifentrine also has anti-inflammatory effects in vitro (e.g. reducing TNFα release from human monocytes) and in vivo. Anti-inflammatory action in bronchial epithelial cells from cystic fibrosis patients is likely mediated via inhibition of PDE4 isozymes [5]. Ensifentrine is active when delivered orally or by inhalation [1].
COVID-19: A pilot study of ensifentrine in hospitalised COVID-19 patients was initiated in mid-late 2020. Ligand Activity Visualisation ChartsThese are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts. ✖ |
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No information available. |
Clinical Trials | |||||
Clinical Trial ID | Title | Type | Source | Comment | References |
NCT04527471 | Study of Ensifentrine or Placebo Delivered Via pMDI in Hospitalized Patients With COVID-19 | Phase 2 Interventional | Verona Pharma plc | ||
NCT04542057 | A Phase 3 Trial to Evaluate the Safety and Efficacy of Ensifentrine in Patients With COPD | Phase 3 Interventional | Verona Pharma plc | ||
NCT00001693 | Phase I-II Multiple-Dose Safety and Efficacy Study of a Selective Inhibitor of Cyclooxygenase - 2 (SC-58635) in Hereditary Non-Polyposis Colorectal Cancer (HNPCC) Patients and Carriers | Phase 1 Interventional | National Institutes of Health Clinical Center (CC) | 7 |