Rilpivirine-Tenofovir disoproxil fumarate-Emtricitabine (Complera)

Rilpivirine-tenofovir disoproxil fumarate (DF)-emtricitabine is a single-tablet regimen option for certain treatment-naïve individuals. This single-tablet regimen is generally well tolerated, but several important factors limit its use. Notably, rilpivirine-tenofovir DF-emtricitabine should not be offered to individuals with HIV RNA level above 100,000 copies/mL or CD4 count below 200 cells/mm³ due to inferior virologic response rates. In addition, it must be taken with a meal and it is contraindicated for individuals who are taking a proton pump inhibitor. A similar option with a different tenofovir component (rilpivirine-tenofovir alafenamide-emtricitabine) is also available and may be preferable because of potential for reduced risk of renal adverse events and bone toxicity.

Rilpivirine-tenofovir DF-emtricitabine was compared with efavirenz-tenofovir DF-emtricitabine and demonstrated similar virologic efficacy overall, except that more virologic failures occurred in the rilpivirine arm in the subset of participants with baseline HIV RNA greater than 100,000 copies/mL or baseline CD4 count less than 200 cells/mm³ or less than 95% adherence [ECHO (C209)]. A subsequent study showed similar virologic efficacy with these two regimens, even in patients with baseline HIV RNA greater than 100,000 copies/mL, but more treatment-emergent resistance occurred in the rilpivirine arm, particularly in subjects with a baseline HIV RNA above 100,000 copies/mL [STaR (GS-264-0110)]. Participants in both studies tolerated rilpivirine better than efavirenz. Among individuals who developed virologic failure, rates of NNRTI resistance, NNRTI cross-resistance, and accompanying NRTI resistance were higher with rilpivirine-based therapy than efavirenz-based therapy. Several studies of switching to the fixed dose regimen of rilpivirine-tenofovir DF-emtricitabine from other antiretroviral regimens in patients with well-controlled HIV and no resistance to components of the study drugs have shown excellent safety and virologic control, including switches from efavirenz-tenofovir DF-emtricitabine [GS-264-0111] and from two NRTIs plus ritonavir-boosted protease inhibitor [SPIRIT (GS-264-0106)].

Rilpivirine-tenofovir DF-emtricitabine is generally well tolerated. Side effects can include headache, insomnia, depression, rash, or elevation of hepatic transaminases. Supratherapeutic doses of rilpivirine can cause QT prolongation; therefore, caution should be used when prescribing rilpivirine-containing therapy with other QT prolonging agents or medications that may significantly increase levels of rilpivirine; if rilpivirine must be used in either these situations, QT should be monitored.

For a listing of the most common clinically significant mutations associated with rilpivirine (RPV) resistance, see the NNRTI Resistance Notes on the Stanford University HIV Drug Resistance Database.

For a listing of the most common clinically significant mutations associated with tenofovir DF (TDF) and/or emtricitabine (FTC) resistance, see the NRTI Resistance Notes on the Stanford University HIV Drug Resistance Database.