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clofazimine is an approved drug (FDA (1986))
Compound class: Synthetic organic
Comment: Clofazimine is a phenazine dye with anti-mycobacterial action (possibly via DNA binding) but is no longer perscribed in the US. It also has anti-inflammatory activities. State-dependent block of Kv1.3 channels by clofazimine offers therapeutic potential for selective immunosuppression in the context of autoimmune diseases in which Kv1.3-expressing T cells play a significant role .
SARS-CoV-2: A report in Nature has identified that clofazimine has anti-coronavirus activity, and that this is synergistic with the antiviral activity of remdesivir . The drug was found to inhibit viral spike-mediated cell fusion and viral helicase activity in vitro, which translated to reduced pulmonary viral load, gut viral shedding and inflammation in an in vivo infection model. The authors suggest that their data supports the use of clofazimine in an outpatient setting for those infected with SARS-CoV-2, or for hospitalised COVID-19 patients if combined with remdesivir. Based on this evidence it is planned to progress clofazimine + remdesivir directly into Phase 2 clinical trial. A trial of clofazimine + interferon-1β is already underway.
Ligand Activity Visualisation Charts
These 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.✖
|Compound class||Synthetic organic|
|Approved drug?||Yes (FDA (1986))|
|WHO Essential Medicine||WHO Essential Medicines List (EML) (22nd List, 2021). Access PDF version.
Click to view more information about the WHO Model Lists of Essential Medicines.
|International Nonproprietary Names|
|GtoPdb PubChem SID||315661264|
|Search Google for chemical match using the InChIKey||WDQPAMHFFCXSNU-UHFFFAOYSA-N|
|Search Google for chemicals with the same backbone||WDQPAMHFFCXSNU|
|Search PubMed clinical trials||clofazimine|
|Search PubMed titles||clofazimine|
|Search PubMed titles/abstracts||clofazimine|
|UniChem Compound Search for chemical match using the InChIKey||WDQPAMHFFCXSNU-UHFFFAOYSA-N|
|UniChem Connectivity Search for chemical match using the InChIKey||WDQPAMHFFCXSNU-UHFFFAOYSA-N|