Ledipasvir D-tartrate with EC50 values of 34 pM against GT1a and 4 pM against GT1b replicon. is an inhibitor of the hepatitis C virus NS5A.

GT1b: 4 pM , GT1a:（EC50）34 pM

Ledipasvir is highly protein-bound both in human serum and in the cell-culture medium (containing 10% BSA) of the replicon assay[1]. Ledipasvir exhibits an EC50 value of 141 nM against the JFH/3a-NS5A replicon[2].?Ledipasvir has GT1a and 1b EC50 values of 31 and 4 pM, respectively, and protein-adjusted EC50 values of 210 pM (GT1a) and 27 pM (GT1b) and the intrinsic EC50 of 39 is 310 fM for GT1a and 40 fM for GT1b.

Ledipasvir exhibits favorable pharmacokinetics, including prolonged half-lives in plasma (rat 1.83 ± 0.22 hr, dog 2.63 ± 0.18 hr), low systemic clearance (CL), and moderate distribution volumes (Vss) surpassing total body water volume[1]. Its effectiveness is underscored by its high replicon potency, low clearance, commendable bioavailability, and extended half-lives across rat, dog, and monkey models, with a low predicted clearance in humans. The pharmacokinetic properties of Ledipasvir have been assessed in both rats and dogs.