Other substances

[SARSHRC-PEG4]2-chol

An anti-SARS-CoV-2 lipopeptide.

Phase of research

Potential treatment - pre-clinical evidence

How it helps

Antiviral

Drug status

Experimental

1
 Supporting references
0
 Contradictory references
0
 AI-suggested references
0
 Clinical trials

General information

[SARSHRC-PEG4]2-chol is a dimeric lipopeptide composed of two Heptad Repeat domains of SARS-CoV-2 Spike protein and a lipidic moiety. In animal models, it was shown to have a very good toxicity profile and distribution in respiratory tract upon intranasal administration. [SARSHRC-PEG4]2-chol is a potent agent in SARS-CoV-2 infection prevention in vitro and in a ferret model of respiratory virus transmission. The lipopeptide has also a long shelf life at room temperature (de Vries et al., 2021).

 

Structure image - [SARSHRC-PEG4]2-chol

Supporting references

Link Tested on Impact factor Notes Publication date
Intranasal fusion inhibitory lipopeptide prevents direct-contact SARS-CoV-2 transmission in ferrets
Spike protein Peptide Animal model In vitro 		in vitro binding assay; primary HAE cells (cytotoxicity); Vero E6 cells; TMPRSS-overexpressing Vero E6 cells; hACE2 mice (biodistribution); ferrets 41.85

The peptide disrupts conformational rearrangement of Spike protein that precedes membrane fusion and viral entry (also in B.1.1.7 and B.1.351 variants). The lipid moiety is proposed to anchor the lipopeptide to the host cells, thus contributing to its antiviral activity. The lipopeptide displays almost no cytotoxicity in vitro. [SARSHRC-PEG4]2-chol experimentally reached micromolar level concentration in murine lungs at 1 hour after intranasal administration. The lipopeptide inhibited virus entry in TMPRSS2-overexpressing Vero E6 cells with an EC50 of ca 5 nM (ca. 300 nM in standard Vero E6 cells). Ferrets which were intranasally administered [SARSHRC-PEG4]2-chol (in 2% DMSO) prior to co-housing with an infectious ferret were fully protected from SARS-CoV-2 infection, whereas 100% of mock-treated co-housed ferrets got infected. The lipopeptide was not as soluble in sucrose solution (with is more appropriate for the use in humans) as in DMSO, yet the lipopeptide formulation with sucrose still provided a significant protection.

 Feb/17/2021
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