VCH-916 是一种新型非核苷 HCV NS5B 聚合酶抑制剂。
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VCH-916 is a novel nonnucleoside HCV NS5B polymerase inhibitor.IC50 Value: Target: HCVVCH-916 is a novel allosteric inhibitor of HCV NS5B polymerase. The RNA-dependent RNA polymerase (NS5B) of HCV is one of the attractive validated targets for development of new drugs to block HCV infection. VCH-916 is currently being evaluated for safety/tolerability, pharmacokinetics and anti-viral efficacy in chronically infected HCV patient.
参考文献:
[1]. Ludmila Gerber, Tania M. Welzel, Stefan Zeuzem. New therapeutic strategies in HCV: polymerase inhibitors. Liver International. 2013,33(s1): 85-92
[2]. Abdelrahman S. Mayhoub. Hepatitis C RNA-dependent RNA polymerase inhibitors: A review of structure-activity and resistance relationships; different scaffolds and mutations. Bioorganic & Medicinal Chemistry. 2012, 20 (10): 3150-3161.
[3]. Debasis Dasa, Jian Honga, Shu-Hui Chena, et al. Recent advances in drug discovery of benzothiadiazine and related analogs as HCV NS5B polymerase inhibitors. Bioorganic & Medicinal Chemistry. 2011, 19(16): 4690-4703
[4]. Pierre L Beaulieu. Recent advances in the development of NS5B polymerase inhibitors for the treatment of hepatitis C virus infection. Informahealthcare. 2009, 19(2): 145-164
[5]. Safety,Tolerability and Pharmacokinetics of Multiple Ascending Doses of VCH 916 in Subjects With Chronic Hep C Infection
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