Effect of Mutations at Position E138 in HIV-1 Reverse Transcriptase on Phenotypic Susceptibility and Virologic Response to Etravirine

作者：Lotke Tambuyzer, Steven Nijs, Bjorn Daems, Gastón Picchio, Johan Vingerhoets · 发表于：JAIDS Journal of Acquired Immune Deficiency Syndromes · 年份：2011 · DOI：10.1097/qai.0b013e3182237f74 · 被引用次数：78 · 研究领域：HIV/AIDS drug development and treatment、HIV Research and Treatment、HIV/AIDS Research and Interventions

The contribution of E138 mutations to etravirine resistance was investigated. Amino acids at position E138 after failure with etravirine in DUET were A (n = 1), G (n = 5), K (n = 3), P (n = 1), Q (n = 5), and V (n = 2). At baseline, only E138A and Q were found at 3.0% and 2.5%, respectively. Virologic response (less than 50 copies/mL) was observed in six of 12 and eight of 10 patients with E138A and E138Q, respectively. Site-directed mutants harboring E138A/G/K/Q/R or S showed etravirine fold change values of 2.9, 2.4, 2.6, 3.0, 3.6, and 2.8, respectively. E138G, K, and Q were added to the existing etravirine-weighted genotypic score including 17 etravirine resistance-associated mutations.