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Biological Activity

Ledipasvir-d6 is intended for use as an internal standard for the quantification of ledipasvir by GC- or LC-MS. Ledipasvir is an inhibitor of hepatitis C virus (HCV) non-structural protein 5A (NS5A).1,2 It inhibits viral replication in genotype 1a and 1b HCV replicon cells (EC50s = 0.031 and 0.004 nM, respectively). It also inhibits viral replication in genotype 2a, 2b, 3a, 4a, 4d, 5a, 6a, and 6e HCV replicon cells (EC50s = 0.11-530 nM).2 Lepidasvir acts synergistically with IFN-α, ribavirin , or GS-9669 and additively with GS-9451, simeprevir , daclatasvir , or PSI-7977 to inhibit viral replication in genotype 1a HCV replicon cells. Formulations containing ledipasvir have been used in combination therapy for the treatment of chronic HCV infection.

References

1.Link, J.O., Taylor, J.G., Xu, L., et al.Discovery of ledipasvir (GS-5885): A potent, once-daily oral NS5A inhibitor for the treatment of hepatitis C virus infectionJ. Med. Chem.57(5)2033-2046(2014) 2.Cheng, G., Tian, Y., Doehle, B., et al.In vitro antiviral activity and resistance profile characterization of the hepatitis C virus NS5A inhibitor ledipasvirAntimicrob. Agents Chemother.60(3)1847-1853(2016)