Abstract
Rilpivirine (RPV) is a second-generation non-nucleoside reverse transcriptase inhibitor (NNRTI). It remains active against HIV strains harbouring mutations that affect first-generation agents. RPV is dosed once daily with food and has been coformulated into a single tablet containing tenofovir and emtricitabine. Two Phase III studies of treatment-naive patients found RPV and efavirenz to have similar safety and efficacy. However, suboptimal virological suppression with RPV occurred more commonly in patients with higher baseline viral loads (>100,000 copies/ml). The most common mutation that emerged during RPV therapy was E138K, which often occurred in combination with M184I. E138K is likely to cause cross-resistance to other NNRTIs thereby limiting the further utilization of this class.
Publication types
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Research Support, Non-U.S. Gov't
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Review
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Systematic Review
MeSH terms
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Alkynes
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Anti-HIV Agents / adverse effects
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Anti-HIV Agents / pharmacology
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Anti-HIV Agents / therapeutic use*
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Benzoxazines / adverse effects
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Benzoxazines / therapeutic use
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Clinical Trials as Topic
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Cyclopropanes
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Drug Interactions
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Drug Resistance, Viral
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Drug Substitution
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HIV Infections / drug therapy*
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HIV-1*
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Humans
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Nitriles / adverse effects
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Nitriles / pharmacology
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Nitriles / therapeutic use*
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Pyrimidines / adverse effects
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Pyrimidines / pharmacology
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Pyrimidines / therapeutic use*
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Reverse Transcriptase Inhibitors / adverse effects
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Reverse Transcriptase Inhibitors / pharmacology
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Reverse Transcriptase Inhibitors / therapeutic use*
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Rilpivirine
Substances
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Alkynes
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Anti-HIV Agents
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Benzoxazines
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Cyclopropanes
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Nitriles
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Pyrimidines
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Reverse Transcriptase Inhibitors
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Rilpivirine
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efavirenz