Department of Infectious Diseases, Hospital Carlos III, Madrid, Spain.
AIDS Rev. 2013 Oct-Dec;15(4):238-9.
Raltegravir is a highly potent antiretroviral agent, with arguably one of the most favorable adverse event profiles in the HIV armamentarium. However, its standard twice-daily (BID) dosing schedule makes it less convenient than once-daily (QD) options. Although pharmacokinetic data suggest that QD raltegravir may provide adequate drug levels, the randomized phase III QDMRK trial (Eron, et al. Lancet Infect Dis. 2011;11:907-15) showed that 800 mg QD raltegravir failed to meet the criteria for non-inferiority when compared with 400 mg BID RAL in antiretroviral-naive HIV-infected individuals. 83% of patients in the QD arm achieved undetectable HIV viremia, in comparison with 89% in the BID arm. This was largely due to poorer efficacy among people with high baseline viral load (74 vs. 84%, respectively).
拉替拉韦是一种高效的抗逆转录病毒药物，其不良反应谱在 HIV 治疗药物中可说是最有利的之一。但是，其标准的每日两次（BID）给药方案使其不如每日一次（QD）方案方便。虽然药代动力学数据表明 QD 拉替拉韦可能提供足够的药物水平，但随机 III 期 QDMRK 试验（Eron 等人，柳叶刀感染病。2011;11:907-15）显示，与每日两次 400 毫克 RAL 相比，800 毫克 QD 拉替拉韦在初治 HIV 感染患者中未能达到非劣效性标准。QD 组中 83%的患者达到了无法检测到的 HIV 病毒血症，而 BID 组中为 89%。这主要是由于基线病毒载量较高的患者疗效较差（分别为 74%和 84%）。
