Bepridil is potent against SARS-CoV-2 in vitro | Academic Article individual record
abstract

Guided by a computational docking analysis, about 30 Food and Drug Administration/European Medicines Agency (FDA/EMA)-approved small-molecule medicines were characterized on their inhibition of the severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) main protease (Mp ro). Of these small molecules tested, six displayed a concentration that inhibits response by 50% (IC50) value below 100 μM in inhibiting Mp ro, and, importantly, three, that is, pimozide, ebastine, and bepridil, are basic molecules that potentiate dual functions by both raising endosomal pH to interfere with SARS-CoV-2 entry into the human cell host and inhibiting Mp ro in infected cells. A live virus-based modified microneutralization assay revealed that bepridil possesses significant anti-SARS-CoV-2 activity in both Vero E6 and A459/ACE2 cells in a dose-dependent manner with low micromolar effective concentration, 50% (EC50) values. Therefore, the current study urges serious considerations of using bepridil in COVID-19 clinical tests.

authors
author list (cited authors)
Vatansever, E. C., Yang, K. S., Drelich, A. K., Kratch, K. C., Cho, C., Kempaiah, K. R., ... Liu, W. R.
publication date
2021
keywords
  • Lung
  • Pneumonia
  • Biodefense
  • Vaccine Related
  • Emerging Infectious Diseases
  • Infectious Diseases
  • Prevention
altmetric score

150.75

citation count

29

PubMed ID
33597253
identifier
519628SE
Digital Object Identifier (DOI)
start page
e2012201118
end page
e2012201118
volume
118
issue
10