Clofoctol

Clofoctol

Clinical data
AHFS/Drugs.com	International Drug Names
Routes of administration	Rectal (suppository) [1]
ATC code	J01XX03 ( WHO )
Pharmacokinetic data
Bioavailability	98% [1]
Metabolism	Hepatic glucuronidation [1]
Excretion	Biliary [1]
Identifiers
IUPAC name 2-[(2,4-dichlorophenyl)methyl]- 4-(2,4,4-trimethylpentan-2-yl)phenol
CAS Number	37693-01-9  Y
PubChem CID	2799
ChemSpider	2697  Y
UNII	704083NI0R
KEGG	D07244  Y
ChEMBL	ChEMBL1476605
CompTox Dashboard (EPA)	DTXSID5045889
ECHA InfoCard	100.048.739
Chemical and physical data
Formula	C21H26Cl2O
Molar mass	365.34 g·mol−1
3D model (JSmol)	Interactive image
SMILES Clc1cc(Cl)ccc1Cc2cc(ccc2O)C(C)(C)CC(C)(C)C
InChI InChI=1S/C21H26Cl2O/c1-20(2,3)13-21(4,5)16-7-9-19(24)15(11-16)10-14-6-8-17(22)12-18(14)23/h6-9,11-12,24H,10,13H2,1-5H3 Y Key:HQVZOORKDNCGCK-UHFFFAOYSA-N Y
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Clofoctol is a bacteriostatic antibiotic. It is used in the treatment of respiratory tract and ear, nose and throat infections caused by Gram-positive bacteria. ^[1] It has been marketed in France till 2005 under the trade name Octofene and in Italy as Gramplus.^{[ citation needed ]}

It is only functional against Gram-positive bacteria. ^[2]

It penetrates into human lung tissue. ^[3]

A French company, Apteeus had been developing clofoctol as a potential therapy against SARS-CoV-2 in 2020-2021, but eventually the repurposing of the drug was abandoned, due to a lack of volunteers. ^{[4] [5] [6] [7] [8] [9]} A mouse study showed repurposed drug clofoctol blocks SARS-CoV-2 replication. ^{[10] [11]}

References

1. "Gramplus" (in Italian). Studio Medico Torrino. July 25, 2007. Archived from the original on March 8, 2016. Retrieved 2007-08-10.
2. Combe J, Simonnet F, Yablonsky F, Simonnet G (1980). "[Clofoctol binding by the bacteria (author's transl)]". Journal de Pharmacologie (in French). 11 (4): 411–425. PMID   6782374.
3. Danesi R, Gasperini M, Senesi S, Freer G, Angeletti CA, Del Tacca M (1988). "A pharmacokinetic study of clofoctol in human plasma and lung tissue by using a microbiological assay". Drugs Under Experimental and Clinical Research. 14 (1): 39–43. PMID   3391105.
4. Marcelli S (2020-10-13). "Pasteur Lille obtient 5 M€ de LVMH pour repositionner un ancien médicament, l'Octofene, sur le traitement du Covid" [Pasteur Lille obtains €5 million from LVMH to reposition an old drug, Octofene, for the treatment of Covid] (in French). AEF info. Archived from the original on 2020-10-17. Retrieved 2020-10-13.
5. Haroche F (2021-09-13). "La piste clofoctol. Interview du Pr Xavier Nassif". Jim.fr. Archived from the original on 2021-09-13.
6. "Hope for an Anti-COVID Drug". arte.tv. ARTE Reportage. ARTE G.E.I.E. 2021-05-21. Archived from the original on 2022-05-27. Retrieved 2024-06-03.
7. Blanquart J, Tonolli F (2022-07-04). "La molécule miracle !" [The miracle molecule!]. Wéo (in French). Archived from the original on 2022-07-16. Retrieved 2024-06-03.
8. Mounier JL (2020-10-01). "French institute aims to start human trials of 'promising' Covid-19 drug this winter". France 24. Archived from the original on 2020-10-01. Retrieved 2024-06-02.
9. Demollien N (2020-06-20). "Covid-19 : un reportage sur les chercheurs de l'institut Pasteur de Lille ce samedi sur Arte" [Covid-19: a report on researchers from the Pasteur Institute in Lille this Saturday on Arte]. actu.fr (in French). Archived from the original on 2020-06-21. Retrieved 2024-06-02.
10. Thomas L (2022-05-23). "Repurposed drug clofoctol blocks SARS-CoV-2 replication in mouse study". News-Medical. Archived from the original on 2022-05-23. Retrieved 2024-06-02.
11. Belouzard S, Machelart A, Sencio V, Vausselin T, Hoffmann E, Deboosere N, et al. (May 2022). Menachery VD (ed.). "Clofoctol inhibits SARS-CoV-2 replication and reduces lung pathology in mice". PLOS Pathogens. 18 (5): e1010498. doi: 10.1371/journal.ppat.1010498 . PMC   9119441 . PMID   35587469.