Synonyms: compound 19f [PMID: 7830278] | OPC-6535 | OPC6535
Compound class:
Synthetic organic
Comment: Tetomilast is a PDE4 inhibitor. Inhibition of PDE4 blocks the oxidative burst in human neutrophils, which is a major mediator of tissue injury in inflammatory diseases. Tetomilast (OPC-6535) was originally identified as an inhibitor of superoxide production by human neutrophils [1]. The clinical potential of PDE4 inhibition in inflammatory bowel disease was reviewed by Salari and Abdollahiin 2012 [2].
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. |
Summary of Clinical Use |
Tetomilast (OPC-6535) has completed clinical trials for several inflammatory indications: ulcerative colitis (Phase 3 NCT00064454), Crohn's disease (Phase 2/3 Phase 2 NCT00989573) and COPD (Phase 3 NCT00874497 was terminated by the study sponsor, Otsuka Pharmaceutical). Phase 2 results from a trial in ulcerative colitis patients were reported in 2007 [3]. Whilst primary end points were not met in this study, secondary end points did indicate potential clinical activity. |
Mechanism Of Action and Pharmacodynamic Effects |
Tetomilast-mediated inhibition of PDE4 blunts the proinflammatory functions of leukocytes such as superoxide production and cytokine release. |