Department of Gastroenterology and Metabolism, Applied Life Science, Institute of Biomedical & Health Science, Hiroshima University, Hiroshima, Japan; Liver Research Project Center, Hiroshima University, Hiroshima, Japan.
Liver Research Project Center, Hiroshima University, Hiroshima, Japan; PhoenixBio Co., Ltd., Higashihiroshima, Japan.
Virus Res. 2016 Feb 2;213:62-68. doi: 10.1016/j.virusres.2015.11.010. Epub 2015 Nov 10.
We previously reported that interferon (IFN)-free direct-acting antiviral combination treatment succeeded in eradicating genotype 1b hepatitis C virus (HCV) in human hepatocyte chimeric mice. In this study, we examined the effect of vaniprevir (MK7009, NS3/4A protease inhibitor) and BMS-788329 (NS5A inhibitor) combination treatment on HCV genotype 1b and the expression of IFN-stimulated genes (ISGs) using a subgenomic replicon system and the same animal model. Combination treatment with vaniprevir and BMS-788329 significantly reduced HCV replication compared to vaniprevir monotherapy in HCV replicon cells (Huh7/Rep-Feo cells). HCV genotype 1b-infected human hepatocyte chimeric mice were treated with vaniprevir alone or in combination with BMS-788329 for four weeks. Vaniprevir monotherapy reduced serum HCV RNA titers in mice, but viral breakthrough was observed in mice with high HCV titers. Ultra-deep sequence analysis revealed a predominant replacement by drug-resistant substitutions at 168 in HCV NS3 region in these mice. Conversely, in mice with low HCV titers, HCV was eradicated by vaniprevir monotherapy without viral breakthrough. In contrast to monotherapy, combination treatment with vaniprevir and BMS-788329 succeeded in completely eradicating HCV regardless of serum viral titer. IFN-alpha treatment significantly increased ISG expression; however, vaniprevir and BMS-788329 combination treatment caused no increase in ISG expression both in cultured cells and in mouse livers. Therefore, combination treatment with vaniprevir and BMS-788329 eliminated HCV via a non-ISG-mediated mechanism. This oral treatment might offer an alternative DAA combination therapy for patients with chronic hepatitis C.
我们之前报道过无干扰素直接作用抗病毒药物联合治疗在人源肝嵌合小鼠模型中成功根除了基因 1b 型丙型肝炎病毒(HCV)。在这项研究中,我们使用亚基因组复制子系统和相同的动物模型,研究了 NS3/4A 蛋白酶抑制剂凡尼普韦(MK7009)和 NS5A 抑制剂 BMS-788329 联合治疗对 HCV 基因 1b 型和干扰素刺激基因(ISGs)表达的影响。与凡尼普韦单药治疗相比,凡尼普韦和 BMS-788329 联合治疗可显著降低 HCV 复制子细胞(Huh7/Rep-Feo 细胞)中的 HCV 复制。用凡尼普韦单药或联合 BMS-788329 对 HCV 基因 1b 感染的人源肝嵌合小鼠进行为期四周的治疗。凡尼普韦单药治疗可降低小鼠血清 HCV RNA 滴度,但在 HCV 滴度较高的小鼠中观察到病毒突破。超深度测序分析显示,这些小鼠 HCV NS3 区 168 位主要由耐药替换取代。相反,在 HCV 滴度较低的小鼠中,凡尼普韦单药治疗可根除 HCV,而无病毒突破。与单药治疗相比,凡尼普韦和 BMS-788329 联合治疗可成功根除 HCV,而与血清病毒滴度无关。IFN-α治疗可显著增加 ISG 表达;然而,凡尼普韦和 BMS-788329 联合治疗在培养细胞和小鼠肝脏中均未引起 ISG 表达增加。因此,凡尼普韦和 BMS-788329 联合治疗通过非 ISG 介导的机制消除了 HCV。这种口服治疗可能为慢性丙型肝炎患者提供一种替代的直接作用抗病毒药物联合治疗方案。