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Rilpivirine: a new addition to the anti-HIV-1 armamentarium.

机译：Rilpivirine：抗HIV-1 armamentium的新添加。

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摘要

HIV has shifted from an acute illness to a chronic condition that can be successfully managed long-term with combination antiretroviral therapy. Rilpivirine (TMC-278) is a second-generation non-nucleoside reverse transcriptase inhibitor (NNRTI) that is positioned to become an importation therapy option for HIV-1-infected patients, particularly for those that are naive to therapy. In phase III studies this agent demonstrated similar virologic and immunologic efficacy compared to a current standard of care, efavirenz, while causing less adverse events. A higher proportion of rilpivirine-treated patients did experience virologic failure, however, and providers will need to weigh this risk with the improved tolerability of rilpivirine. In vitro studies have demonstrated that rilpivirine, as a diarylpyrimidine NNRTI with greater flexibility, has a higher genetic barrier to resistance when compared to first-generation NNRTI agents. Longer-term clinical data will be necessary to better understand rilpivirine's durability and activity against viral resistance in patients. Rilpivirine will be available as a stand-alone agent and will also be coformulated with tenofovir and emtricitabine to create a safe and effective antiretroviral regimen that can be administered as a single daily-dosed tablet.
机译：HIV从急性疾病转向慢性病症，可以通过组合抗逆转录病毒治疗来成功管理长期。瑞哌啶（TMC-278）是第二代非核苷逆转录酶抑制剂（NNRTI），其定位为成为HIV-1感染患者的进口治疗选择，特别是对于幼稚对治疗的患者。在III期研究中，与目前的护理标准，EFAVIRENZ相比，该试剂表现出类似的病毒学和免疫疗效，同时导致较少的不良事件。然而，瑞培治疗的患者的较高比例患者体验了病毒学失败，并且提供者需要对瑞哌啶的改善的耐受性来称量这种风险。体外研究表明，与第一代NNRTI试剂相比，瑞培作为一种具有更高柔韧性的二芳基嘧啶NnRTI的遗传阻隔，其具有更高的遗传阻隔。需要长期临床数据，以更好地了解瑞培耐久性和免受患者病毒抗性的耐久性和活性。 Rilpivirine将作为独立剂可用，也将用替诺福韦和Emtricistabine成种，以产生安全有效的抗逆转录病毒方案，可以作为单一的每日剂量给药。

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