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The search for antivirals remains a priority in the fight against COVID-19. In this article published in the journal PLoS Pathogens, scientists screened drug actives to identify previously undetected antiviral activity. Since these have already received marketing authorization for other pathologies, they can quickly be offered for the treatment of COVID-19. The researchers thus identified clofoctol, a antibiotic (An antibiotic (from the Greek anti: « againstΒ Β», and bios: « the…) used in respiratory infections. In model animal (An animal (from the Latin animus, spirit, or vital principle) is, according to the classical classification, a…)this compound reduces the pathology (Pathology, a term from ancient Greek, is literally the speech, the…) induced by SARS-CoV-2.

Hospitalizations related to COVID-19 fell rapidly after the implementation of a vaccination (Vaccination is a process of introducing an external agent (the…) to large scale (The large ladder, also called aerial ladder or auto ladder, is a…). This preventive approach does not, however, prevent viral transmission. In addition, the protection induced by vaccines against new variants turns out to be less good and it is also less effective in immunodeficient people. A complementary approach to fight against SARS-CoV2 consists in using antiviral molecules which make it possible to control the infection at the beginning of the sickness (Disease is an alteration of the functions or health of a living organism, animal…)but the development of this type of medication (A drug is a substance or composition presented as possessing…) is relatively long. To accelerate the identification of antivirals in the context (The context of an event includes the circumstances and conditions surrounding it; the…) of the health crisis (Health crises are major pandemics, which affect between ten…), research quickly focused on the repositioning of clinically tested drugs. The first attempts at targeted repositioning were disappointing in the context of COVID-19, however.

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An alternative way, in this type of approach, consists in screening on a large scale banks of active principles of drugs in order to highlight a activity (The term activity can refer to a profession.) previously unidentified antiviral, to then be able to quickly offer a clinical evaluation of the drug in the context of COVID-19. Indeed, the authorized compounds have well-documented safety and pharmacokinetic characteristics in patients and could therefore be rapidly available for the treatment of COVID-19.

In this context, the scientists screened a library of 1942 compounds that had already received marketing authorization or had already beenobject (In general, the word object (from the Latin objectum, 1361) designates an entity defined in…) of clinical trials. For this, they tested the ability of these compounds to inhibit the multiplication (Multiplication is one of the four operations of elementary arithmetic…) of SARS-CoV2 in culture (The UNESCO definition of culture is as follows [1] πŸ™‚ cellular. Antiviral activity has been identified for a few dozen molecules and, among these, a compound that has not been identified by other research teams research (Scientific research designates in the first place all the actions undertaken with a view to…) caught their attention. This molecule (A molecule is an electrically neutral chemical assembly of at least two atoms, which…), called clofoctol, showed very good antiviral activity against SARS-CoV-2 at inhibitory concentrations far below those seen clinically in human lungs. This drug had also been developed as an antibiotic to treat respiratory bacterial infections. Until 2005, it was sold in France under the name OctofΓ¨ne and is still used in Italy under the name Gram+. The researchers confirmed the antiviral activity of clofoctol in human lung cells as well as in a mouse model and also demonstrated an effect anti-inflammatory (An anti-inflammatory is a medicine to fight inflammation.) of this compound. The preclinical validation of this molecule could make it possible to propose a repositioning of clofoctol in the treatment of COVID-19.


The antiviral activity of clofoctol was identified following the phenotypic screening of 1942 active ingredients of medicinal products which have been or are still used clinically against other pathologies. The anti-SARS-CoV-2 activity of clofoctol has been validated in cell culture and confirmed in a mouse model of SARS-CoV-2 infection. Additionally, anti-inflammatory activity was observed for clofoctol in this animal model.
Β© Sandrine Belouzard

To know more:

Clofoctol inhibits SARS-CoV-2 replication and reduces lung pathology in mice
Belouzard S, Machelart A, Sencio V, Vausselin T, Hoffmann E, Deboosere N, Rouille Y, Desmarets L, SΓ©ron K, Danneels A, Robil C, Belloy L, Moreau C, Piveteau C, Biela A, Vandeputte D, Heumel S , Deruyter L, Dumont L, Leroux F, Engelmann I, Alidjinou EK, Hober D, Brodin P, Beghyn T, Trottein F, DΓ©prez B, Dubuisson J.
PLoS Pathogens May 19, 2022. https://doi.org/10.1371/journal.ppat.1010498

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