Laboratory of Clinical Pharmacology and Pharmacogenetics, Department of Medical Sciences, University of Turin, Turin.
Laboratory of Clinical Pharmacology and Pharmacogenetics, Department of Medical Sciences, University of Turin, Turin.
Int J Antimicrob Agents. 2024 Aug;64(2):107200. doi: 10.1016/j.ijantimicag.2024.107200. Epub 2024 May 18.
Despite its effectiveness, combination antiretroviral treatment (cART) has a limited effect on HIV DNA reservoir, which establishes early during primary HIV infection (PHI) and is maintained by latency, homeostatic T-cells proliferation, and residual replication. This limited effect can be associated with low drug exposure in lymphoid tissues and/or suboptimal adherence to antiretroviral drugs (ARVs). The aim of this study was to assess ARV concentrations in plasma, peripheral blood mononuclear cells (PBMCs) and lymph nodes (LNs), and their association to HIV RNA and HIV DNA decay during PHI. Participants were randomised to receive standard doses of darunavir/cobicistat (Arm I), dolutegravir (Arm II) or both (Arm III), with a backbone of tenofovir alafenamide and emtricitabine. Total HIV DNA was measured using digital-droplet PCR in PBMCs at baseline, 12 and 48 weeks. Drug concentrations in plasma and PBMCs were determined at 2, 12 and 48 weeks (LNs at 12 weeks) by UHPLC-MS/MS. Seventy-two participants were enrolled, mostly male (n=68), with a median age of 34 years and variable Fiebig stages (V-VI 57.7%, I-II 23.9%, and III-IV 18.3%). Twenty-six patients were assigned to Arm I, 27 to Arm II and 19 to Arm III. After 48 weeks, most patients had undetectable viremia, with minor differences in HIV RNA decay between arms. Patients with Fiebig I-II showed faster HIV RNA and HIV DNA decay. Intracellular tissue penetration was high for nucleoside analogues and low-moderate for darunavir and dolutegravir. Only tenofovir diphosphate concentrations in PBMCs showed correlation with HIV DNA decay. Overall, these results indicate that the timing of treatment initiation and intracellular tenofovir penetration are primary and secondary factors, respectively, affecting HIV reservoir.
尽管联合抗逆转录病毒治疗(cART)有效,但对 HIV 病毒 DNA 储存库的作用有限,该储存库在原发性 HIV 感染(PHI)早期建立,并通过潜伏、稳态 T 细胞增殖和残余复制来维持。这种有限的作用可能与淋巴组织中药物暴露不足和/或抗逆转录病毒药物(ARV)依从性不理想有关。本研究旨在评估 PHI 期间血浆、外周血单核细胞(PBMC)和淋巴结(LNs)中的 ARV 浓度及其与 HIV RNA 和 HIV DNA 衰减的关系。参与者被随机分配接受达芦那韦/考比司他(Arm I)、多替拉韦(Arm II)或两者(Arm III)的标准剂量治疗,均以替诺福韦艾拉酚胺和恩曲他滨为骨干。在基线、12 周和 48 周时,使用数字液滴 PCR 在 PBMC 中测量总 HIV DNA。通过 UHPLC-MS/MS 在 2、12 和 48 周时(在 12 周时测量 LNs)测定血浆和 PBMC 中的药物浓度。72 名参与者入组,大多数为男性(n=68),中位年龄为 34 岁,Fiebig 分期不同(V-VI 57.7%,I-II 23.9%,III-IV 18.3%)。26 名患者被分配到 Arm I,27 名患者被分配到 Arm II,19 名患者被分配到 Arm III。48 周后,大多数患者的病毒血症无法检测到,各臂之间 HIV RNA 衰减的差异较小。Fiebig I-II 期患者的 HIV RNA 和 HIV DNA 衰减较快。核苷类似物的细胞内组织穿透率较高,达芦那韦和多替拉韦的穿透率较低至中等。只有 PBMC 中的替诺福韦二磷酸浓度与 HIV DNA 衰减相关。总体而言,这些结果表明治疗开始的时机和细胞内替诺福韦穿透是影响 HIV 储存库的主要和次要因素。