Rilpivirine

Rilpivirine is an orally administered, non-nucleoside reverse transcriptase inhibitor that is a component drug in combination therapy for antiretroviral-naive patients with HIV-1 infection. The randomized, double-blind, double-dummy, multinational ECHO and THRIVE trials in antiretroviral-naive adult patients with HIV-1 infection compared rilpivirine with efavirenz, administered with background nucleoside/nucleotide antiretroviral regimens. Rilpivirine 25 mg once daily recipients had a treatment response (confirmed plasma HIV-1 RNA level of <50 copies/mL at 48 weeks; primary endpoint) that was noninferior to that of efavirenz 600 mg once daily recipients. The response rates in the rilpivirine and efavirenz groups were 83% and 84% (ECHO) and 87% and 83% (THRIVE). Virological failure rates in rilpivirine and efavirenz groups in the intent-to-treat analysis were 11% and 4% in the ECHO trial and 7% and 5% in the THRIVE trial. In a pooled analysis of both trials, in rilpivirine recipients with an HIV-1 RNA level of >100,000 copies/mL at baseline, the virological failure rate at 48 weeks was 15% (vs 6% with efavirenz), whereas in those with a level of ≤100,000 copies/mL, the virological failure rate was 4% (vs 3% with efavirenz). In general, rilpivirine was better tolerated than efavirenz throughout treatment. Rilpivirine recipients had significantly fewer treatment-related adverse events, discontinuations because of adverse events, psychiatric-neurological adverse events and a significantly lower rate of blood lipid abnormalities.