News
SARS-CoV-2 programme open for partnering
We’re pleased to announce the completion of one of the SARS-CoV-2 programmes, selected for screening in 2020. The programme is now open for partnering opportunities.
The aim of the programme was to identify novel inhibitors of viral entry into host cells as a small-molecule therapeutic option to protect against SARS-CoV2 infections and minimise disease severity in SARS-CoV2 patients.
The importance of identifying small-molecule inhibitors of COVID-19
It’s likely that highly contagious and lethal coronaviruses will emerge again in the future. To be prepared for these future pandemics, novel therapies that neutralise multiple strains are needed.
As has been witnessed with the current pandemic, protection by vaccines or antibodies is decreasing with SARS-CoV-2 mutants, and repurposed antiviral drugs like hydroxychloroquine have little or no effect on hospitalised COVID-19 patients.
First-in-class small-molecule medications with a novel mode-of-action can limit further spread of the disease in unvaccinated populations, but also minimise the risk of poor vaccine efficacy against new variants of SARS-CoV2.
Results of the ELF programme
The ELF partnership performed a comprehensive screening assay cascade for hit triaging and characterization, resulting in high-quality hits comprised of various compound clusters and singletons. A total of 12 compounds were successfully resynthesized, of which the inhibitory activity of 11 was reconfirmed. The results were presented to the Programme Owner, Pivot Park Screening Centre, who is now looking for partners to progress the most promising molecules.
Next steps
With the ELF work complete, this SARS-CoV-2 programme is now open for partnering for:
- Profiling hit series in cellular viral entry assays and efficacy determination for other spike variants
- Mode-of-action determination
- Structure-enabled computational chemistry
- Hit-to-lead chemistry and Structure-Activity Relationship (SAR) studies
- In-vitro ADME-Tox studies
- In-vivo Proof of Concept
More information on the screening programme is available here. If you are interested in collaborating on this programme, please get in touch with the European Lead Factory Programme Office at programme@europeanleadfactory.eu.