McPhee Fiona, Hernandez Dennis, Zhou Nannan, Ueland Joseph, Yu Fei, Vellucci Vincent, Huang Xin, Wang Xuning, Ishikawa Hiroki, Karino Yoshiyasu, Kumada Hiromitsu
Bristol-Myers Squibb Research and Development, Wallingford, CT, USA.
Bristol-Myers Squibb Research and Development, Hopewell, NJ, USA.
Antivir Ther. 2018;23(1):53-66. doi: 10.3851/IMP3177.
Daclatasvir (DCV; non-structural [NS]5A inhibitor) plus asunaprevir (ASV; NS3 inhibitor) plus beclabuvir (BCV; non-nucleoside NS5B inhibitor) is an approved regimen for hepatitis C virus (HCV) genotype (GT)-1 treatment in Japan. A comprehensive analysis of pre-treatment and treatment-emergent HCV resistance to this regimen ± ribavirin (RBV) was performed.
Data were pooled from five Phase 2/3 studies of DCV+ASV+BCV±RBV given for 12 weeks to GT-1a- or GT-1b-infected patients. The prevalence and impact of pre-treatment resistance-associated substitutions (RAS) in NS5A, NS3, and NS5B on sustained virological response (SVR) was assessed, as were emergent RAS and their post-treatment persistence.
Baseline NS5A RAS (GT-1a: M28T, Q30H/L/R/S, L31M, Y93C/H; GT-1b: L31I/M, Y93C/H) were present in 5% (26/561) of GT-1a and 16% (85/537) of GT-1b sequences. SVR12 for GT-1b without RBV was 100% (82/82) with RAS and >99% (427/428) without RAS. For GT-1a, SVR12 without RAS was 97% (85/88) with RBV and 92% (410/447) without RBV; SVR12 with RAS was 100% (2/2) with RBV and 54% (13/24) without RBV. Baseline NS3 (at R155 or D168) and NS5B (at P495) RAS were rare (≤1%). Treatment-emergent NS5A RAS (mostly Q30E/H/K/R±Y93H/N) in GT-1a persisted 60 weeks post-treatment, while NS3 RAS (mostly R155K) and NS5B-P495L/S were no longer detected after 48 or 24 weeks, respectively.
DCV+ASV+BCV±RBV was highly efficacious in HCV GT-1 infection, including HCV GT-1b with NS5A RAS. The fitness of treatment-emergent RAS post-treatment was NS5A > NS3 > NS5B; NS3 and NS5B RAS were generally replaced by wild-type sequence within 48 weeks.
在日本,达卡他韦(DCV;非结构蛋白[NS]5A抑制剂)联合阿舒瑞韦(ASV;NS3抑制剂)联合贝可拉唑韦(BCV;非核苷类NS5B抑制剂)是一种已获批的用于治疗丙型肝炎病毒(HCV)基因1型(GT-1)的方案。对该方案±利巴韦林(RBV)治疗前及治疗中出现的HCV耐药情况进行了全面分析。
汇总了五项2/3期研究的数据,这些研究将DCV+ASV+BCV±RBV给予GT-1a或GT-1b感染患者,疗程为12周。评估了NS5A、NS3和NS5B中治疗前耐药相关替代位点(RAS)的发生率及其对持续病毒学应答(SVR)的影响,以及出现的RAS及其治疗后的持续情况。
基线NS5A RAS(GT-1a:M28T、Q30H/L/R/S、L31M、Y93C/H;GT-1b:L31I/M、Y93C/H)在GT-1a序列中占5%(26/561),在GT-1b序列中占16%(85/537)。GT-1b患者不使用RBV时,有RAS的患者SVR12为100%(82/82),无RAS的患者>99%(427/428)。对于GT-1a患者,不使用RBV时,无RAS的患者SVR12为92%(410/447),使用RBV时为97%(85/88);有RAS的患者,使用RBV时SVR12为100%(2/2),不使用RBV时为54%(13/24)。基线NS3(R155或D168位点)和NS5B(P495位点)RAS罕见(≤1%)。治疗中出现的GT-1a NS5A RAS(大多为Q30E/H/K/R±Y93H/N)在治疗后持续60周,而NS3 RAS(大多为R155K)和NS5B-P495L/S分别在48周和24周后未再检测到。
DCV+ASV+BCV±RBV对HCV GT-1感染高度有效,包括伴有NS5A RAS的HCV GT-1b感染。治疗中出现的RAS在治疗后的适应性为NS5A>NS3>NS5B;NS3和NS5B RAS通常在48周内被野生型序列取代。