Non-structural protein 5A (NS5A) is important for RNA synthesis and virus assembly making it as an attractive target for intervention in chronic Hepatitis C virus (HCV) infection[3]. Elbasvir is a small molecule inhibitor of NS5A of HCV being developed as a component of treatment regimens for chronic HCV infection. In the 3-day replicon assay, the EC90 of elbasvir was 0.006 nM for both the wild-type 1a_H77 and 1b_con1 replicons. The EC90 of elbasvir ranged from 0.01 to 0.02 nM for genotype 1a and 0.01 to 0.03 nM for genotype 1b. In a phase 1 study, elbasvir once daily for 5 days resulted in mean reductions in HCV RNA levels of 3.7-5.1 log10 IU/mL in patients with genotype 1a or 1b infections when given 5-50 mg/day and of ~3 log10 IU/mL in patients with genotype 3 when given 50 or 100 mg/day. In later phase 2 trials, treatment with elbasvir combined with grazoprevir (an investigational once-daily NS3/4A-protease inhibitor) ± ribavirin for 12 weeks produced SVR12 (sustained virologic response) rates of 87-98% for patients with genotype-1 infections[4].
Elbasvir 细胞实验
Cell Line
Concentration
Treated Time
Description
References
GT1a(H77) replicon cells
0.006 nM (EC90)
72 hours
Evaluate the inhibitory effect of Elbasvir on HCV RNA replication, results showed Elbasvir has high potency in GT1a(H77) replicon cells.
搜索
