Lorenzen Thore, Stoehr Albrecht, Walther Irene, Plettenberg Andreas
ifi-Institut, am AK St. Georg, Haus K, Lohmühlenstr. 5, 20099 Hamburg, Germany.
Eur J Med Res. 2007 Oct 15;12(9):419-25.
CCR5 antagonists are a newly developed class of antiretroviral drugs which inhibit viral entry into the host cell by binding to the predominant HIV coreceptor. Data on the use of these new drugs in treatment-experienced HIV patients are emerging. Clinical trials on maraviroc and vicriviroc in pretreated patients recruited more than 1300 individuals. Interim results of these studies indicate that pretreated patients infected with CCR5-tropic viruses benefit from their use in optimized combination regimens. Maraviroc reduces the HIV-1 viral load in patients with previous triple-class failure by 1.96 log10 copies/ml versus 0.99 log10 copies/ml in placebo; vicriviroc shows potency by dose depending viral decrease of 1.51-1.68 log10 copies/ml compared to 0.29 log10 in placebo. As expected, CCR5 antagonists do not reduce viral load in patients harbouring CXCR4-tropic or dual/mixed tropic viruses. Nevertheless, since a considerable percentage of late-stage HIV patients still bear CCR5-tropic viruses, the use of CCR5 antagonists appears promising in properly selected treatment-experienced patients.
CCR5拮抗剂是一类新开发的抗逆转录病毒药物,通过与主要的HIV共受体结合来抑制病毒进入宿主细胞。关于这些新药在有治疗经验的HIV患者中使用的数据正在不断涌现。马拉维罗和维立维罗在经治患者中的临床试验招募了1300多名个体。这些研究的中期结果表明,感染CCR5嗜性病毒的经治患者在优化联合治疗方案中使用这些药物会受益。马拉维罗可使先前三联疗法失败的患者的HIV-1病毒载量降低1.96 log10拷贝/毫升,而安慰剂组为0.99 log10拷贝/毫升;维立维罗根据剂量显示出效力,病毒载量降低1.51 - 1.68 log10拷贝/毫升,而安慰剂组为0.29 log10。正如预期的那样,CCR5拮抗剂不会降低携带CXCR4嗜性或双嗜性/混合嗜性病毒患者的病毒载量。然而,由于相当比例的晚期HIV患者仍携带CCR5嗜性病毒,在经过适当选择的有治疗经验的患者中使用CCR5拮抗剂似乎很有前景。