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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 on 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. |
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