Author: Vatansever, Erol C.; Yang, Kai S.; Drelich, Aleksandra K.; Kratch, Kaci C.; Cho, Chia-Chuan; Kempaiah, Kempaiah Rayavara; Hsu, Jason C.; Mellott, Drake M.; Xu, Shiqing; Tseng, Chien-Te K.; Liu, Wenshe Ray
Title: Bepridil is potent against SARS-CoV-2 in vitro Cord-id: 7p5kpmac Document date: 2021_3_9
ID: 7p5kpmac
Snippet: 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 (M(p)(ro)). Of these small molecules tested, six displayed a concentration that inhibits response by 50% (IC(50)) value below 100 μM in inhibiting M(p)(ro), and, importantly, three, that is, pimozide, ebastine, and bepridil, a
Document: 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 (M(p)(ro)). Of these small molecules tested, six displayed a concentration that inhibits response by 50% (IC(50)) value below 100 μM in inhibiting M(p)(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 M(p)(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% (EC(50)) values. Therefore, the current study urges serious considerations of using bepridil in COVID-19 clinical tests.
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