Mutations that confer resistance to Ledipasvir in Hepatitis C Virus replicon cells, which are found in NS5A, infer that NS5A is the direct target of Ledipasvir.
Ledipasvir is a novel Hepatitis C Virus NS5A inhibitor that is best administered adjunctively with other antiviral drugs, leading to very successful results. A cure rate of up to 100 percent is possible when Ledipasvir is used in the correct combinations of drug cocktails. By effectively inhibiting the viral phosphoprotein NS5A Ledipasvir aids in controlling viral assembly, replication and secretion.
Ledipasvir is primarily eliminated in the feces, with a renal excretion being considered as a minor elimination pathway. Whole blood and plasma levels of Ledipasvir are undetectable at both 36 and 48 hours post dosage.
Reports that Ledipasvir, when used in combination with Sofosbuvir and Tenofovir may increase Tenofovir levels in the body. While severe toxicity has not been documented a concern regarding co-administration of Tenofovir with Ledipasvir may lead to renal toxicity. The majority of adverse effects reported are not severe and include fatigue, nausea, dizziness and diarrhea.