1 Hanover Medical School , Hanover, Germany .
AIDS Patient Care STDS. 2014 Apr;28(4):168-75. doi: 10.1089/apc.2013.0310. Epub 2014 Mar 24.
The once daily, single-tablet regimen (STR) combining rilpivirine (RPV), emtricitabine (FTC), and tenofovir disoproxil fumarate (TDF) provides a simplified treatment option for antiretroviral therapy (ART)-naïve patients with baseline HIV-1 RNA (BLVL) of ≤100,000 copies/mL. The aim of this analysis is to compare long-term efficacy, safety, and tolerability of RPV+FTC/TDF vs. efavirenz (EFV)+FTC/TDF as individual components in subjects with BLVL ≤100,000 copies/mL. Week 96 efficacy and safety data from subjects with BLVL ≤100,000 copies/mL, who received daily RPV 25 mg or EFV 600 mg with FTC/TDF in the phase 3, randomized, double-blind, double-dummy, active-controlled, registrational trials ECHO and THRIVE, were analyzed. Virologic response was evaluated by intent-to-treat, time to loss of virological response (ITT-TLOVR), and Snapshot algorithms. Through Week 96, RPV+FTC/TDF demonstrated non-inferior efficacy to EFV+FTC/TDF (84% vs. 81%, respectively; ITT-TLOVR) in 543 subjects with BLVL ≤100,000 copies/mL, and overall rates of virologic failure (VF) were 5.9% vs. 2.4%, respectively. Resistance development was lower in Year 2 than Year 1. Subjects in both arms with suboptimal adherence (≤95%) had lower virologic responses (63% vs. 62%, respectively). Treatment with RPV+FTC/TDF was associated with significantly fewer treatment-related adverse events (AEs), grade 2-4 AEs, neurological and psychiatric AEs (including dizziness and abnormal dreams/nightmares), and rash. Additionally, grade 2-4 treatment-emergent laboratory abnormalities and grade 1-3 lipid abnormalities were significantly less common with RPV+FTC/TDF than EFV+FTC/TDF. RPV+FTC/TDF demonstrated non-inferior efficacy to EFV+FTC/TDF in ART-naïve subjects with BLVL ≤100,000 copies/mL and was associated with a higher rate of VF but a more favorable safety and tolerability profile through Week 96.
每日一次、单片方案（STR）联合利匹韦林（RPV）、恩曲他滨（FTC）和富马酸替诺福韦二吡呋酯（TDF）为基线 HIV-1 RNA（BLVL）≤100,000 拷贝/mL 的初治抗逆转录病毒治疗（ART）患者提供了简化的治疗选择。本分析旨在比较 BLVL≤100,000 拷贝/mL 的患者中 RPV+FTC/TDF 与 EFV+FTC/TDF 作为个体成分的长期疗效、安全性和耐受性。接受每日 RPV 25mg 或 EFV 600mg 联合 FTC/TDF 的 BLVL≤100,000 拷贝/mL 的患者在 ECHO 和 THRIVE 3 期、随机、双盲、双模拟、活性对照、注册试验中达到了第 96 周的疗效和安全性数据。通过第 96 周，在 BLVL≤100,000 拷贝/mL 的 543 例患者中，RPV+FTC/TDF 与 EFV+FTC/TDF 相比显示出非劣效性疗效（分别为 84%和 81%；ITT-TLOVR），总的病毒学失败（VF）率分别为 5.9%和 2.4%。第二年的耐药率低于第一年。在依从性≤95%（包括依从性≤95%）的两个治疗组中，病毒学应答率较低（分别为 63%和 62%）。RPV+FTC/TDF 治疗与较少的治疗相关不良事件（AE）、2-4 级 AE、神经和精神科 AE（包括头晕和异常梦境/噩梦）以及皮疹相关。此外，与 EFV+FTC/TDF 相比，RPV+FTC/TDF 治疗的 2-4 级治疗时出现的实验室异常和 1-3 级血脂异常的发生率显著较低。在 BLVL≤100,000 拷贝/mL 的初治患者中，RPV+FTC/TDF 与 EFV+FTC/TDF 相比显示出非劣效性疗效，并且在第 96 周时，VF 发生率较高，但安全性和耐受性较好。
