Hepatitis C virus (HCV) is an enveloped, single-stranded, positive-sense RNA virus in the Flaviviridae family. Ombitasvir is a HCV NS5A inhibitor with pan-genotypic activity. Ombitasvir had EC50s of 14.1 and 5.0 pM against genotype 1a-H77 and 1b-Con1 sub-genomic replicons, respectively. It demonstrated broad genotypic activity, with EC50s of 0.82 to 19.3 pM against genotype 2a, 2b, 3a, 4a, and 5a replicons and 366 pM against a genotype 6a replicon. Among a panel of HCV genotype 1 to 6 isolates, the EC50 of ombitasvir ranged from 0.1 to15.1 pM against NS5A from 66 genotype 1 to 5 isolates. In addition, ombitasvir was active against the genotype 2a JFH-1 replicon, with an EC50 of 0.82 pM. In a 3-day monotherapy study (5, 25, 50, or 200 mg; once daily) in 12 HCV genotype 1-infected patients, decreases in HCV RNA up to 3.1 log10 IU/ml were observed. And wild-type virus was largely suppressed by ombitasvir during 3-day monotherapy, and at doses higher than 5 mg, resistant variant M28V was also suppressed[3].
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