Synonyms: Alvesco® | Omnaris® | RPR-251526
ciclesonide is an approved drug (FDA (2006))
Compound class:
Synthetic organic
Comment: Ciclesonide is a prodrug. The active metabolite is desisobutyrylciclesonide (PubChem CID 6918281). It is a clinically used inhalation corticosteroid/glucocorticoid drug.
![]() 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. ✖![]() View more information in the IUPHAR Pharmacology Education Project: ciclesonide |
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Bioactivity Comments |
The IC50 for ciclesonide at the human glucocorticoid receptor is 210 nM, compared to 1.75 nM for the active metabolite, desisobutyrylciclesonide. Ki values show the same pattern of higher affinity of desisobutyrylciclesonide (37 nM for ciclesonide vs 0.31 nM for desisobutyrylciclesonide) [1]. SARS-CoV-2: Ciclesonide is able to block SARS-CoV-2 replication in vitro, with an EC90 concentration of 6.3 μM [2] (note that this data is from a preprint article posted to bioRxiv, so has not been certified by peer review). This effect is predicted to occur through inhibition of the virus' nonstructural protein (NSP) 15. In the same assay mometasone, mifepristone and algestone also inhibited SARS-CoV-2 replication, whereas cortisone, prednisolone, dexamethasone and fluticasone did not. |
Selectivity at nuclear hormone receptors | ||||||||||||||||||||||||||||||||||
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