Rilpivirine in the light of the genotypic drug resistance data

Rilpivirine, a second generation non-nucleoside reverse transcriptase inhibitor has been recently approved for the treatment-naive HIV-1 infected subjects. One of the characteristic features of this agent is activity in the setting of the K103N mutation and higher genetic barrier to resistance in comparison to the first generation agents. Key rilpivirine associated mutations include K101E/P, E138A/G/K/Q/R, V179L, Y181C/I/V, H221Y, F227C, M230I/L and Y188L, while additional variants with possible influence on drug susceptibility are V90I, L100I, K101T, 106I, E138S, V179D/I, Y188L, V189I, G190A/E/S, and M230V. Primary key rilpivirine associated mutations are transmitted infrequently - from 0.4% to 4.6% which warrants widespread use of the agent, while development of secondary drug mutations among patients with viral load below 100,000 copies/ml is comparable to efavirenz. This allows for a durable long-term treatment with rilpivirine.