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首页> 外文期刊>Drugs of today: Medicamentos de actualidad >Rilpivirine: a new addition to the anti-HIV-1 armamentarium.
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Rilpivirine: a new addition to the anti-HIV-1 armamentarium.

机译：Rilpivirine：抗HIV-1武器库的新成员。

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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已从急性疾病转变为慢性疾病，可以通过联合抗逆转录病毒疗法长期成功治疗。 Rilpivirine（TMC-278）是第二代非核苷类逆转录酶抑制剂（NNRTI），已定位成为HIV-1感染患者，特别是对于那些天真的治疗患者的进口治疗选择。在III期研究中，与目前的标准治疗药物依非韦伦相比，该药物在病毒学和免疫学方面具有相似的功效，同时引起的不良事件更少。但是，接受rilpivirine治疗的患者中有较高比例确实发生了病毒学衰竭，因此提供者将需要通过rilpivirine改善的耐受性来权衡这种风险。体外研究表明，与第一代NNRTI药物相比，利匹韦林作为具有更大柔韧性的二芳基嘧啶NNRTI，具有更高的抗药性遗传壁垒。长期的临床数据对于更好地了解rilpivirine对患者的抵抗力和抗病毒活性具有必要。 Rilpivirine将以独立药物的形式提供，并且还将与Tenofovir和Emtricitabine共同配制，以创建安全有效的抗逆转录病毒疗法，可以作为每日单剂量的片剂给药。

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