期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 29, 期 16, 页码 2415-2427出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2019.04.027
关键词
HCV; Hepatitis C Virus; Non-structural protein 5A; NS5A; Sustained viral response; SVR; Direct-acting-antiviral; DAA; Rule-of-five; Single-tablet regimen; Velpatasvir; GS-5816; Epclusa (R); Sofosbuvir
Direct-acting antiviral inhibitors have revolutionized the treatment of hepatitis C virus (HCV) infected patients. Herein is described the discovery of velpatasvir (VEL, GS-5816), a potent pan-genotypic HCV NS5A inhibitor that is a component of the only approved pan-genotypic single-tablet regimens (STRs) for the cure of HCV infection. VEL combined with sofosbuvir (SOF) is Epclusa (R), an STR with 98% cure-rates for genotype 1-6 HCV infected patients. Addition of the pan-genotypic HCV NS3/4A protease inhibitor voxilaprevir to SOF/VEL is the STR Voseve (R), which affords 97% cure-rates for genotype 1-6 HCV patients who have previously failed another treatment regimen.
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