Vita-Salute San Raffaele University, Laboratory of Virology and Microbiology, Milan, Italy.
J Infect Dis. 2011 Dec 1;204(11):1811-5. doi: 10.1093/infdis/jir636. Epub 2011 Oct 7.
Novel integrase inhibitors are in advanced clinical development, and cross-resistance data are needed to consider the possibility to plan a sequential usage within this class of antiretroviral drugs. Ex vivo phenotypic assays were conducted on 11 wild-type and 27 fully replicating recombinant viruses obtained from 11 patients failing previous raltegravir-containing regimens. Dolutegravir maintained its activity in vitro on viruses with mutations in position 143 and 155. However, viruses with mutation Q148R associated with secondary mutations and the combination Q148H+G140S were instead associated with a reduced level of susceptibility to dolutegravir in vitro.
新型整合酶抑制剂已进入临床开发的后期阶段，需要进行交叉耐药性数据研究，以考虑在这一类抗逆转录病毒药物中进行序贯使用的可能性。对 11 例先前接受拉替拉韦治疗方案失败的患者中获得的 11 株野生型和 27 株完全复制的重组病毒进行了体外表型测定。多替拉韦在体外对位置 143 和 155 发生突变的病毒仍保持活性。然而，与次要突变相关的 Q148R 突变病毒以及 Q148H+G140S 组合突变病毒的体外对多替拉韦的敏感性降低。
