Introduction: A key objective with highly active antiretroviral therapy for the treatment of HIV infection has been the optimization of antiretroviral drug combinations for individual patients.
Areas covered: Overall, non-nucleoside reverse transcriptase inhibitor (NNRTI)-based regimens (in combination with two nucleoside reverse transcriptase inhibitors (NRTIs)) have become mainstays for initial ARV regimens. Early NNRTIs, efavirenz and nevirapine, are similarly efficacious, but differ according to their toxicity profiles. Newer NNRTIs, rilpivirine and etravirine are also efficacious. Etravirine was designed to overcome common first-line NNRTI resistance mutations, and serves as a second line agent.
Expert opinion: As a class, NNRTIs are key components of ARV regimens. Currently, there are 3 NNRTIs that may be used in first-line regimens, and one in second-line regimens. ARV regimen optimization depends on matching individual drug efficacy, safety, resistance, and toxicity profiles to particular patients. Once-daily dosing options are essential to treatment simplification strategies, which have been shown to enhance regimen compliance and durabiltiy. These are especially important due to the low genetic barrier to resistance generally associated with NNRTIs. As newer drugs are introduced, especially as part of once-daily, single-tablet regimens, this will expand the number of convenient and efficacious treatment options available.