体外研究(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, respe
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参考文献 |
[1]. Ng TI, et al. In Vitro Antiviral Activity and Resistance Profile of the Next-Generation Hepatitis C Virus NS3/4A Protease Inhibitor Glecaprevir. Antimicrob Agents Chemother. 2017 Oct 30. pii: AAC.01620-17.[2]. Qi Sun, et al. Bardoxolone and bardoxolone methyl, two Nrf2 activators in clinical trials, inhibit SARS-CoV-2 replication and its 3C-like protease. Signal Transduct Target Ther. 2021 May 29;6(1):212.
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