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Antivir Ther. 2012;17(8):1495-502. doi: 10.3851/IMP2254. Epub 2012 Aug 10.

Rilpivirine, a novel non-nucleoside reverse transcriptase inhibitor for the management of HIV-1 infection: a systematic review.

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Jefferson School of Pharmacy, Thomas Jefferson University, Philadelphia, PA, USA.


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.

[Indexed for MEDLINE]

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