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Bepridil is potent against SARS-CoV-2 In Vitro
Erol C Vatansever1, Kai Yang1, Kaci C Kratch1
1The Texas A&M Drug Discovery Laboratory, Department of Chemistry, Texas A&M University, College Station, TX 77843, USA.
Biorxiv : the Preprint Server for Biology
|June 9, 2020
Summary
Bepridil and other small molecules inhibit SARS-CoV-2 MPro, a key viral enzyme. Bepridil shows promise for COVID-19 treatment by blocking viral entry and replication.
Area of Science:
- Pharmacology
- Virology
- Drug Discovery
Background:
- The SARS-CoV-2 main protease (MPro) is a critical target for antiviral therapies.
- Identifying existing FDA/EMA-approved small molecules for repurposing can accelerate COVID-19 treatment development.
Approach:
- Computational docking analysis was used to screen approximately 30 approved small molecule medicines for MPro inhibition.
- Six compounds demonstrated MPro inhibition with IC50 values under 100 μM.
- Bepridil, pimozide, and ebastine were identified as basic small molecules with potential dual antiviral functions.
Key Points:
- Bepridil exhibited potent inhibition of SARS-CoV-2 cytopathogenic effects in cell-based assays.
- In Vero E6 cells, bepridil achieved complete inhibition below 5 μM.
- In A549 cells, bepridil achieved complete inhibition below 6.25 μM.
- The dual action of raising endosomal pH and inhibiting MPro offers a unique therapeutic strategy.
Conclusions:
- Bepridil demonstrates significant antiviral activity against SARS-CoV-2 in vitro.
- The findings support the clinical investigation of bepridil as a potential COVID-19 therapeutic.
- Repurposing approved small molecules offers a viable strategy for rapid COVID-19 drug development.
