| Literature DB >> 33720995 |
Michael H J Rhodin1, Nicole V McAllister1, Jonathan Castillo1, Sarah L Noton2, Rachel Fearns2, In Jong Kim1, Jianming Yu1, Thomas P Blaisdell1, Joseph Panarese1, Brian C Shook1, Yat Sun Or1, Bryan Goodwin1, Kai Lin1.
Abstract
EDP-938 is a novel non-fusion replication inhibitor of respiratory syncytial virus (RSV). It is highly active against all RSV-A and B laboratory strains and clinical isolates tested in vitro in various cell lines and assays, with half-maximal effective concentrations (EC50s) of 21, 23 and 64 nM against Long (A), M37 (A) and VR-955 (B) strains, respectively, in the primary human bronchial epithelial cells (HBECs). EDP-938 inhibits RSV at a post-entry replication step of the viral life cycle as confirmed by time-of-addition study, and the activity appears to be mediated by viral nucleoprotein (N). In vitro resistance studies suggest that EDP-938 presents a higher barrier to resistance compared to viral fusion or non-nucleoside L polymerase inhibitors with no cross-resistance observed. Combinations of EDP-938 with other classes of RSV inhibitors lead to synergistic antiviral activity in vitro. Finally, EDP-938 has also been shown to be efficacious in vivo in a non-human primate model of RSV infection.Entities:
Year: 2021 PMID: 33720995 PMCID: PMC7993833 DOI: 10.1371/journal.ppat.1009428
Source DB: PubMed Journal: PLoS Pathog ISSN: 1553-7366 Impact factor: 6.823