Activity of the HIV-1 attachment inhibitor BMS-626529, the active component of the prodrug BMS-663068, against CD4-independent viruses and HIV-1 envelopes resistant to other entry inhibitors

Antimicrob Agents Chemother. 2013 Sep;57(9):4172-80. doi: 10.1128/AAC.00513-13. Epub 2013 Jun 17.

Abstract

BMS-626529 is a novel small-molecule HIV-1 attachment inhibitor active against both CCR5- and CXCR4-tropic viruses. BMS-626529 functions by preventing gp120 from binding to CD4. A prodrug of this compound, BMS-663068, is currently in clinical development. As a theoretical resistance pathway to BMS-663068 could be the development of a CD4-independent phenotype, we examined the activity of BMS-626529 against CD4-independent viruses and investigated whether resistance to BMS-626529 could be associated with a CD4-independent phenotype. Finally, we evaluated whether cross-resistance exists between BMS-626529 and other HIV-1 entry inhibitors. Two laboratory-derived envelopes with a CD4-independent phenotype (one CXCR4 tropic and one CCR5 tropic), five envelopes from clinical isolates with preexisting BMS-626529 resistance, and several site-specific mutant BMS-626529-resistant envelopes were examined for their dependence on CD4 for infectivity or susceptibility to BMS-626529. Viruses resistant to other entry inhibitors (enfuvirtide, maraviroc, and ibalizumab) were also examined for susceptibility to BMS-626529. Both CD4-independent laboratory isolates retained sensitivity to BMS-626529 in CD4(-) cells, while HIV-1 envelopes from viruses resistant to BMS-626529 exhibited no evidence of a CD4-independent phenotype. BMS-626529 also exhibited inhibitory activity against ibalizumab- and enfuvirtide-resistant envelopes. While there appeared to be some association between maraviroc resistance and reduced susceptibility to BMS-626529, an absolute correlation cannot be presumed, since some CCR5-tropic maraviroc-resistant envelopes remained sensitive to BMS-626529. Clinical use of the prodrug BMS-663068 is unlikely to promote resistance via generation of CD4-independent virus. No cross-resistance between BMS-626529 and other HIV entry inhibitors was observed, which could allow for sequential or concurrent use with different classes of entry inhibitors.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Anti-HIV Agents / pharmacology*
  • Antibodies, Monoclonal / pharmacology
  • CCR5 Receptor Antagonists*
  • CD4 Antigens / metabolism
  • Cyclohexanes / pharmacology
  • Drug Resistance, Viral / drug effects
  • Enfuvirtide
  • HEK293 Cells
  • HIV Envelope Protein gp120 / metabolism
  • HIV Envelope Protein gp41 / pharmacology
  • HIV-1 / drug effects*
  • HIV-1 / growth & development
  • HIV-1 / metabolism
  • Humans
  • Maraviroc
  • Organophosphates / metabolism
  • Organophosphates / pharmacology
  • Peptide Fragments / pharmacology
  • Piperazines / metabolism
  • Piperazines / pharmacology*
  • Prodrugs / metabolism
  • Prodrugs / pharmacology
  • Receptors, CCR5 / metabolism
  • Receptors, CXCR4 / antagonists & inhibitors*
  • Receptors, CXCR4 / metabolism
  • Receptors, Virus / antagonists & inhibitors*
  • Receptors, Virus / metabolism
  • Triazoles / pharmacology*
  • Virus Internalization / drug effects*

Substances

  • Anti-HIV Agents
  • Antibodies, Monoclonal
  • BMS-626529
  • CCR5 Receptor Antagonists
  • CCR5 protein, human
  • CD4 Antigens
  • CXCR4 protein, human
  • Cyclohexanes
  • HIV Envelope Protein gp120
  • HIV Envelope Protein gp41
  • Organophosphates
  • Peptide Fragments
  • Piperazines
  • Prodrugs
  • Receptors, CCR5
  • Receptors, CXCR4
  • Receptors, Virus
  • Triazoles
  • Enfuvirtide
  • fostemsavir
  • ibalizumab
  • Maraviroc