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首页> 外文期刊>Antimicrobial agents and chemotherapy. >Cross-resistance profile determination of two second-generation HIV-1 integrase inhibitors using a panel of recombinant viruses derived from raltegravir-treated clinical isolates.
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Cross-resistance profile determination of two second-generation HIV-1 integrase inhibitors using a panel of recombinant viruses derived from raltegravir-treated clinical isolates.

机译：使用一组从raltegravir处理过的临床分离株中衍生的重组病毒，对两种第二代HIV-1整合酶抑制剂进行交叉耐药性测定。

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摘要

The integrase inhibitor raltegravir (RAL) is currently used for the treatment of both treatment-naive and treatment-experienced HIV-1-infected patients. Elvitegravir (EVG) is in late phases of clinical development. Since significant cross-resistance between RAL and EVG is observed, there is a need for second-generation integrase inhibitors (INIs) with a higher genetic barrier and limited cross-resistance to RAL/EVG. A panel of HIV-1 integrase recombinants, derived from plasma samples from raltegravir-treated patients (baseline and follow-up samples), were used to study the cross-resistance profile of two second-generation integrase inhibitors, MK-2048 and compound G. Samples with Q148H/R mutations had elevated fold change values with all compounds tested. Although samples with the Y143R/C mutation had reduced susceptibility to RAL, they remained susceptible to MK-2048 and compound G. Samples with the N155H mutation had no reduced susceptibility to compound G. In conclusion, our results allowed ranking of the INIs on the basis of the antiviral activities using recombinant virus stocks from RAL-treated patient viruses. The order according to decreasing susceptibility is compound G, MK-2048, and EVG.
机译：整合酶抑制剂raltegravir（RAL）目前用于治疗未接受过治疗和经历过HIV-1感染的患者。 Elvitegravir（EVG）处于临床开发的后期阶段。由于观察到RAL与EVG之间存在明显的交叉耐药性，因此需要具有更高遗传屏障和对RAL / EVG交叉耐药性有限的第二代整合酶抑制剂（INIs）。一组HIV-1整合酶重组体衍生自raltegravir治疗的患者的血浆样品（基线和随访样品），用于研究两种第二代整合酶抑制剂MK-2048和化合物G的交叉耐药性对于所有测试的化合物，具有Q148H / R突变的样品的倍数变化值均升高。尽管具有Y143R / C突变的样品对RAL的敏感性降低，但它们仍易受MK-2048和化合物G的影响。具有N155H突变的样品对化合物G的敏感性不降低。总之，我们的结果允许在INI上对INI进行排序。使用来自RAL治疗的患者病毒的重组病毒原液的抗病毒活性基础。根据敏感性降低的顺序是化合物G，MK-2048和EVG。

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