Etravirine

一种NNRTI；对野生型HIV-1菌株LAI、SF2和Ba-L有效（EC50s=1.4-4.8nM），但对HIV-2菌株ROD无效（EC50=3,479nM）；对携带NNRTI耐药性相关突变的18种HIV-1菌株有效（所有EC50s=<5nM）；在用编码NL4.3HIV-1感染性分子克隆的质粒转染的HEK293T细胞中，增加病毒多聚蛋白Gag和Gag-Pol的细胞内加工，并减少病毒颗粒的产生，浓度为5μM。An NNRTI; active against the wild-type HIV-1 strains LAI, SF2, and Ba-L (EC50s = 1.4-4.8 nM) but not the HIV-2 strain ROD (EC50 = 3,479 nM); active against 18 HIV-1 strains carrying NNRTI resistance-associated mutations (EC50s = <5 nM for all); increases intracellular processing of the viral polyproteins Gag and Gag-Pol and decreases viral particle production in HEK293T cells transfected with a plasmid encoding the NL4.3 infectious molecular clone of HIV-1 at 5 μM.