Presatovir (GS-5806) is a novel, orally bioavailable RSV fusion inhibitor with the potential to treat RSV infection in infants and adults[1].
In vitro, Presatovir exhibited strong antiviral activity against virus-infected HEp-2 cells, with a mean EC50 value of 0.35±0.14nM[2]. Presatovir showed low cytotoxicity in uninfected HEp-2 cells, with a 50% inhibitory concentration (CC50) of 48900±5600nM[2]. Presatovir inhibited RSV A2 replication in the HAE cell model with a mean EC50 of 0.37±0.28nM[2]. Presatovir antiviral activities against the RSV A and B subtypes were comparable, with mean EC50 of 0.51±0.25nM and 0.35±0.15nM, respectively[2].
References:
[1] Mackman RL, Sangi M, Sperandio D, et al. Discovery of an oral respiratory syncytial virus (RSV) fusion inhibitor (GS-5806) and clinical proof of concept in a human RSV challenge study. J Med Chem. 2015;58(4):1630-1643.
[2] Perron M, Stray K, Kinkade A, et al. GS-5806 Inhibits a Broad Range of Respiratory Syncytial Virus Clinical Isolates by Blocking the Virus-Cell Fusion Process. Antimicrob Agents Chemother. 2015;60(3):1264-1273.
Presatovir (GS-5806)是一种新型的、口服生物利用度高的呼吸道合胞病毒（RSV）融合抑制剂，具有治疗婴幼儿和成人RSV感染的潜力[1]。
在体外，Presatovir对病毒感染的HEp-2细胞表现出较强的抗病毒活性，平均EC50值为0.35±0.14nM[2]。Presatovir对未感染HEp-2细胞具有较低的细胞毒性，半数细胞毒性浓度（CC50）为48900±5600nM[2]。Presatovir在HAE细胞模型中抑制RSV A2复制，平均EC50为0.37±0.28nM[2]。Presatovir对RSV A和B亚型的抗病毒活性的平均EC50分别为0.51±0.25nM和0.35±0.15nM[2]。