New Study Suggests Ceftaroline Fosamil May Be Effective in Treating COVID-19

Researchers from the Federal University of Santa Maria have conducted a study that investigates the potential of ceftaroline fosamil as an inhibitor of SARS-CoV-2 replication. The study highlights the importance of targeting SARS-CoV-2 proteases M^pro and PL^pro in the development of antiviral drugs for COVID-19 treatment. Ceftaroline fosamil, a fifth-generation cephalosporin antibiotic, exhibits inhibitory effects on viral replication in vitro at submicromolar concentrations.

Key Takeaways:

• The study suggests that ceftaroline fosamil and its metabolites are potential inhibitors of PL^pro and M^pro, critical targets for antiviral drug development.
• In silico analyses demonstrate that ceftaroline fosamil and its metabolites are more stable with M^pro than PL^pro, while in vitro biochemical analysis indicates PL^pro as the preferred target.
• The study found that ceftaroline fosamil inhibited viral replication in the human Calu-3 cell model at submicromolar concentrations when added to cell culture medium at 12 h.
• The reactivity of sulfur in the 1,2,4-thiadiazole moiety warrants further exploration for the development of viral protease inhibitors.
• The study suggests that ceftaroline fosamil should be evaluated as a potential repurposing agent for COVID-19, considering not only viral proteases but also other viral targets and relevant cellular pathways.

Statistics:

• The study investigated the effects of ceftaroline fosamil and its metabolites on SARS-CoV-2 proteases M^pro and PL^pro.
• In silico analyses demonstrated that ceftaroline fosamil and its metabolites are more stable with M^pro than PL^pro (dock scores: 71.112 and 60.716, respectively).
• Ceftaroline fosamil inhibited viral replication in the human Calu-3 cell model at submicromolar concentrations (EC50: 0.23 μM).
• The study found that ceftaroline fosamil exhibits a preferential inhibitory effect on PL^pro (IC50: 0.44 μM) compared to M^pro (IC50: 1.31 μM).

Sources:

• In Silico and In Vitro Studies of the Approved Antibiotic Ceftaroline Fosamil and Its Metabolites as Inhibitors of SARS-CoV-2 Replication. Viruses, 2025, 17(4), 491.
• MDPI AG. (Publisher)
• Federal University Santa Maria. (Research Institution)
• Cassia Delgado. (Corresponding Author)
• Pablo Andrei Nogara, Milene Dias Miranda, Alice Santos Rosa, Vivian Neuza Santos Ferreira, Luisa Tozatto Batista, Thamara Kelcya Fonseca Oliveira, Folorunsho Bright Omage, Flavia Motta, Izabela Marques Bastos, Laura Orian, Joao Batista Teixeira Rocha. (Authors)