Comparable In Vitro Activities of Second-Generation HIV-1 Integrase Strand Transfer Inhibitors (INSTIs) on HIV-1 Clinical Isolates with INSTI Resistance Mutations

  • Antimicrob Agents Chemother. 2019 Dec 20;64(1):e01717-19. doi: 10.1128/AAC.01717-19.
Francesco Saladini  1 ,  Alessia Giannini  2 ,  Adele Boccuto  2 ,  Filippo Dragoni  2 ,  Alice Appendino  2 ,  Edoardo Albanesi  2 ,  Ilaria Vicenti  2 ,  Maurizio Zazzi  2
Affiliations
  • 1. Department of Medical Biotechnologies, University of Siena, Siena, Italy [email protected].
  • 2. Department of Medical Biotechnologies, University of Siena, Siena, Italy.
PMID: 31611362 DOI: 10.1128/AAC.01717-19
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.

Keywords
HIV-1 resistance; bictegravir; cabotegravir; dolutegravir; integrase inhibitors; phenotypic assay.
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