Enanta Pharmaceuticals Inc., Watertown, Massachusetts, United States of America.
Department of Microbiology, Boston University School of Medicine, Boston, Massachusetts, United States of America.
PLoS Pathog. 2021 Mar 15;17(3):e1009428. doi: 10.1371/journal.ppat.1009428. eCollection 2021 Mar.
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.
EDP-938 是一种新型的非融合 RSV 复制抑制剂。它在体外的各种细胞系和检测中对所有 RSV-A 和 B 实验室株和临床分离株均具有高度活性,对 Long(A)、M37(A)和 VR-955(B)株的半数最大有效浓度(EC50)分别为 21、23 和 64 nM,在原代人支气管上皮细胞(HBECs)中。EDP-938 通过添加时间研究证实,在 RSV 生命周期的进入后复制步骤中抑制 RSV,并且该活性似乎由病毒核蛋白(N)介导。体外耐药性研究表明,与病毒融合或非核苷 L 聚合酶抑制剂相比,EDP-938 具有更高的耐药屏障,且未观察到交叉耐药性。EDP-938 与其他 RSV 抑制剂类别联合使用可在体外产生协同抗病毒活性。最后,EDP-938 还在 RSV 感染的非人类灵长类动物模型中显示出体内疗效。