Synonyms: Lamprene®
clofazimine is an approved drug (FDA (1986))
Compound class:
Synthetic organic
Comment: Clofazimine is a phenazine dye with antimycobacterial properties [3]. It has both antibacterial and 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 [4].
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 [7]. 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 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 |
Clofazimine is used in combination with the antibacterials, rifampicin and dapsone, as multidrug therapy (MDT) for the treatment of leprosy [2]. Clofazimine is on the World Health Organisation's List of Essential Medicines. It is not commercially available in the US, but can been obtained from the National Hansen's Disease (Leprosy) Program (NHDP) of the US Department of Health and Human Services when required [5]. |
Mechanism Of Action and Pharmacodynamic Effects |
Clofazimine inhibits bacterial DNA replication and proliferation [2]. |
Clinical Trials | |||||
Clinical Trial ID | Title | Type | Source | Comment | References |
NCT04465695 | Dual Therapy With Interferon Beta-1b and Clofazimine for COVID-19 | Phase 2 Interventional | The University of Hong Kong | ||
NCT03009396 | Open Label Efficacy and Safety of Anti-MAP (Mycobacterium Avium Ssp. Paratuberculosis) Therapy in Adult Crohn's Disease | Phase 3 Interventional | RedHill Biopharma Limited | RHB-104 is a fixed-dose combination of clofazimine, |
1,6 |
External links |
For extended ADME data see the following: Drugs.com |