Dalbavancin
A lipoglycopeptide antibiotic.
General information
Dalbavancin is a semi-synthetic lipoglycopeptide antibiotic which impedes Gram-positive bacterial cell wall biosynthesis (NCIt). The drug was computationally modelled and in vitro observed to bind the host’s ACE2 receptor and thus inhibit its interaction with SARS-CoV-2 Spike protein. It is mainly active at post-entry stages of infection. It potently inhibits SARS-CoV-2 infection in Vero E6 cells. The moderate capability of dalbavancin to inhibit cathepsin L might add to its anti-coronaviral properties. Dalbavancin inhibits viral replication and tissue damage in mouse and rhesus macaque models and has a long serum half-life (Wang et al., 2020).
Dalbavancin on DrugBank
Dalbavancin on PubChem
Dalbavancin on Wikipedia
Marketed as
DALVANCE; XYDALBA; ZEVEN
KGPGQDLTDHGEGT-SZUNQUCBSA-N (InChI Key)
Supporting references
| Link | Tested on | Impact factor | Notes | Publication date |
|---|---|---|---|---|
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Dalbavancin binds ACE2 to block its interaction with SARS-CoV-2 spike protein and is effective in inhibiting SARS-CoV-2 infection in animal models
Biophysical assay Cathepsin L Small molecule Peptide Animal model In vitro In silico |
in silico; in vitro binding assay; in vitro biophysical assay; Vero E6 cells; Caco-2 cells; HEK293/hACE2 cells; hACE mice; rhesus macaques | 20.51 | The drug was computationally modelled to bind the host’s ACE2 receptor and thus inhibit its interaction with SARS-CoV-2 Spike protein. It binds human ACE2 receptor and potently (EC50 of ca. 12 nM) inhibits SARS-CoV-2 replication in Vero E6 cells (less potently in TMPRSS2-expressing Caco-2 cells). It also blocks the virus’ replication and pathogenicity in mouse and rhesus macaque models. Dalbavancin appears safe and also has favourable pharmacokinetic properties. |
Dec/01/2020 |
