Peltenburg N Chantal, Bierau Jörgen, Bakker Jaap A, Schippers Jolanda A, Lowe Selwyn H, Paulussen Aimée D C, van den Bosch Bianca J C, Leers Mathie P G, Hansen Bettina E, Verbon Annelies
Department of Internal medicine, Division Infectious Diseases, Erasmus Medical Center, Rotterdam, The Netherlands.
Department of Medical Microbiology and Infectious Diseases, Erasmus Medical Center, Rotterdam, The Netherlands.
PLoS One. 2018 Jan 12;13(1):e0191069. doi: 10.1371/journal.pone.0191069. eCollection 2018.
The purine analogues tenofovir and abacavir are precursors of potential substrates for the enzyme Inosine 5'-triphosphate pyrophosphohydrolase (ITPase). Here, we investigated the association of ITPase activity and ITPA genotype with the occurrence of adverse events (AEs) during combination antiretroviral therapy (cART) for human immunodeficiency virus (HIV) infection. In 393 adult HIV-seropositive patients, AEs were defined as events that led to stop of cART regimen. ITPase activity ≥4 mmol IMP/mmol Hb/hour was considered as normal. ITPA genotype was determined by testing two ITPA polymorphisms: c.94C>A (p.Pro32Thr, rs1127354) and c.124+21A>C (rs7270101). Logistic regression analysis determined odds ratios for developing AEs. In tenofovir-containing regimens decreased ITPase activity was associated with less AEs (p = 0.01) and longer regimen duration (p = 0.001). In contrast, in abacavir-containing regimens decreased ITPase activity was associated with more AEs (crude p = 0.02) and increased switching of medication due to AEs (p = 0.03). ITPA genotype wt/wt was significantly associated with an increase in the occurrence of AEs in tenofovir-containing regimens. Decreased ITPase activity seems to be protective against occurrence of AEs in tenofovir-containing cART, while it is associated with an increase in AEs in abacavir-containing regimens.
嘌呤类似物替诺福韦和阿巴卡韦是肌苷5'-三磷酸焦磷酸水解酶(ITPase)潜在底物的前体。在此,我们研究了ITPase活性和ITPA基因型与人类免疫缺陷病毒(HIV)感染的联合抗逆转录病毒疗法(cART)期间不良事件(AE)发生情况的关联。在393名成年HIV血清阳性患者中,AE被定义为导致cART方案停用的事件。ITPase活性≥4 mmol IMP/mmol Hb/小时被视为正常。通过检测两种ITPA多态性来确定ITPA基因型:c.94C>A(p.Pro32Thr,rs1127354)和c.124 + 21A>C(rs7270101)。逻辑回归分析确定了发生AE的比值比。在含替诺福韦的方案中,ITPase活性降低与较少的AE(p = 0.01)和更长的方案持续时间(p = 0.001)相关。相比之下,在含阿巴卡韦的方案中,ITPase活性降低与更多的AE(粗p = 0.02)和因AE导致的药物更换增加(p = 0.03)相关。ITPA基因型wt/wt与含替诺福韦方案中AE发生率增加显著相关。ITPase活性降低似乎对含替诺福韦的cART中AE的发生具有保护作用,而在含阿巴卡韦的方案中则与AE增加相关。