Second-generation HIV-1 integrase strand transfer inhibitors (INSTIs) dolutegravir (DTG), bictegravir (BIC), and cabotegravir (CAB) showed a high genetic barrier to resistance and limited cross-resistance with first-generation INSTIs raltegravir (RAL) and elvitegravir (EVG). In this study, DTG, BIC, and CAB demonstrated a comparable activity on a panel of INSTI-resistant strains isolated from patients exposed to RAL, EVG, and/or DTG, with a significantly reduced susceptibility only with the pathway Q148H/K/R plus one to two additional INSTI mutations.
Saladini, F., Giannini, A., Boccuto, A., Dragoni, F., Appendino, A., Albanesi, E., et al. (2020). Comparable in vitro activity of second-generation HIV-1 integrase strand transfer inhibitors (INSTIs) on HIV-1 clinical isolates with INSTI resistance mutations. ANTIMICROBIAL AGENTS AND CHEMOTHERAPY, 64(1) [10.1128/AAC.01717-19].
Comparable in vitro activity of second-generation HIV-1 integrase strand transfer inhibitors (INSTIs) on HIV-1 clinical isolates with INSTI resistance mutations
Saladini, Francesco
;Giannini, Alessia;Boccuto, Adele;Dragoni, Filippo;Appendino, Alice;Albanesi, Edoardo;Vicenti, Ilaria;Zazzi, Maurizio
2020-01-01
Abstract
Second-generation HIV-1 integrase strand transfer inhibitors (INSTIs) dolutegravir (DTG), bictegravir (BIC), and cabotegravir (CAB) showed a high genetic barrier to resistance and limited cross-resistance with first-generation INSTIs raltegravir (RAL) and elvitegravir (EVG). In this study, DTG, BIC, and CAB demonstrated a comparable activity on a panel of INSTI-resistant strains isolated from patients exposed to RAL, EVG, and/or DTG, with a significantly reduced susceptibility only with the pathway Q148H/K/R plus one to two additional INSTI mutations.
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https://hdl.handle.net/11365/1083062