Glecaprevir

Glecaprevir is a novel HCV NS3/4A protease inhibitor, with IC₅₀ values ranging from 3.5 to 11.3 nM. Glecaprevir is also a SARS-CoV 3CL^pro inhibitor with an IC₅₀ of 4.09 μM^[2]. IC50 & Target: IC50: 3.5~11.3 nM (HCV NS3/4A protease)^[1] In Vitro: Glecaprevir inhibits the enzymatic activity of HCV genotype 1-6 NS3/4A proteases with half maximal inhibitory concentration (IC₅₀) values ranging from 3.5 to 11.3 nM in a biochemical assay. Glecaprevir inhibites HCV subgenomic stable replicons containing proteases from HCV genotypes 1a, 1b, 2a, 2b, 3a, 4a, 5a, 6a and 6e in Huh-7 cells with 50% effective concentration (EC₅₀) values ranging from 0.21 to 4.6 nM. Glecaprevir is active against a replicon containing protease from genotype 3, the most difficult-to-treat HCV genotype, with an EC₅₀ value of 1.9 nM, which is 10- and 44-fold lower than those for paritaprevir and grazoprevir, respectively. The median Glecaprevir EC₅₀ values against replicons containing these genotype 1a, 1b, 2a, 2b, 3a, 4a, 4d, and 5a clinical samples are 0.08, 0.29, 1.6, 2.2, 2.3, 0.41, 0.17, and 0.12 nM, respectively, with an overall median EC₅₀ value of 0.30 nM (range=0.05~3.8 nM)^[1].