Other substances

Clofazimine

An anti-mycobacterial drug.

Phase of research

Potential treatment - pre-clinical evidence

How it helps

Antiviral

Drug status

Used to treat other disease

Supporting references

Contradictory references

AI-suggested references

Clinical trials

General information

Clofazimine is a red fat-soluble phenazine dye with anti-mycobacterial properties. It is used for the treatment of leprosy (NCIt, LiverTox).

Clofazimine on DrugBank
Clofazimine on PubChem
Clofazimine on Wikipedia

Marketed as

CLOFOZINE; HANSEPRAN; LAMCOIN; LAMPREN; LAMPRÈNE

CC(C)N=C1C=C2C(=NC3=CC=CC=C3N2C4=CC=C(C=C4)Cl)C=C1NC5=CC=C(C=C5)Cl

Supporting references

Link	Tested on	Impact factor	Notes	Publication date
Morphological Cell Profiling of SARS-CoV-2 Infection Identifies Drug Repurposing Candidates for COVID-19 Preprint	Huh7 cells			May/27/2020
Identification of Potent and Safe Antiviral Therapeutic Candidates Against SARS-CoV-2 Small molecule In vitro Screening	Vero cells	5.09		Nov/25/2020
Discovery of SARS-CoV-2 antiviral drugs through large-scale compound repurposing Small molecule In vitro Screening	Vero E6 cells	42.78		Jul/24/2020
Clofazimine broadly inhibits coronaviruses including SARS-CoV-2 Spike protein nsp13 Small molecule Animal model In vitro	Vero E6 cells; Caco-2 cells; human embryonic stem cell-derived cardiomyocytes; human primary small airway epithelial cells; golden Syrian hamsters; (VSV) SARS-CoV-2 Spike pseudovirus; SARS-CoV-2 isolate USA-WA1/2020	42.78	The drug inhibited SARS-CoV-2 Spike mediated cell entry in a dose-dependent manner in vitro. It displayed efficacy even when added to cell culture post viral exposure. This might be in part explained by its observed inhibitory activity against SARS-CoV-2 helicase nsp13. Clofazimine inhibited SARS-CoV-2 infection in Vero E6 cell with an EC50 of 0.31 μM (which is a concentration achievable in plasma after a single 200 mg dose) and it showed efficacy in SARS-Cov-2 inhibition in Caco-2 cells, human embryonic stem cell-derived cardiomyocytes, human primary small airway epithelial cells and human lung tissue (ex vivo). In a hamster model, the drug reduced viral replication in lungs and viral shedding in faeces. It also prevented virus-induced lung pathology. Clofazimine acted synergistically with remdesivir in vitro.	Mar/16/2021
Drugs that inhibit TMEM16 proteins block SARS-CoV-2 Spike-induced syncytia. Small molecule In vitro Mechanism	in vitro fluorescence assay; Vero cells; HEK293 cells; Calu-3 cells; SARS-CoV-2 strain IC19/2020	42.78	The drug was identified based on its ability to prevent SARS-CoV-2-induced syncytia formation. Clofazimine inhibited SARS-CoV-2 replication in Vero cells with an IC50 of 2.56 μM It displayed antiviral activity also in Calu-3 cells.	Apr/07/2021

AI-suggested references

Link	Publication date
Artificial intelligence approach fighting COVID-19 with repurposing drugs	May/15/2020
High-Throughput Screening of an FDA-Approved Drug Library Identifies Inhibitors against Arenaviruses and SARS-CoV-2	Sep/30/2021
4,4'-Diaminodiphenyl Sulfone (DDS) as an Inflammasome Competitor.	Aug/19/2020
Drug repurposing against SARS-CoV-1, SARS-CoV-2 and MERS-CoV	Apr/30/2021
Clofazimine derivatives as potent broad-spectrum antiviral agents with dual-target mechanism	Sep/23/2020
Virtual high throughput screening: Potential Inhibitors for SARS-CoV-2 PLPRO and 3CLPRO Proteases	May/05/2021
Repurposing Based Identification of Novel Inhibitors against MmpS5-MmpL5 Efflux Pump of Mycobacterium smegmatis: A Combined In Silico and In Vitro Study	Sep/20/2021

Clinical trials

ID	Title	Status	Phase	Start date	Completion date
NCT04465695	Dual Therapy With Interferon Beta-1b and Clofazimine for COVID-19	Recruiting	Phase 2	Jul/14/2020	Sep/30/2021
Alternative id - UW 20-463 Interventions - Drug: Interferon beta-1b\|Drug: Clofazimine Study type - Interventional Study results - No Results Available Locations - The University of Hong Kong, Queen Mary Hospital, Hong Kong, Hong Kong, China Study designs - Allocation: Randomized\|Intervention Model: Parallel Assignment\|Masking: None (Open Label)\|Primary Purpose: Treatment Enrollment - 81 Age - 18 Years and older (Adult, Older Adult) Outcome measures - Clinical alleviation of symptoms\|Hospitalisation\|Time to negative viral load\|Inflammatory changes\|Mortality\|Adverse events

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