MOPDX06: The Antiretroviral Efficacy of a Novel Compound BIT225: Inhibition of HIV1 Release from Hum

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MOPDX06 The Antiretroviral Efficacy of a Novel
Compound BIT225 Inhibition of HIV-1 Release
from Human Macrophage Reservoirs

• Aim To measure and understand BIT225 anti-HIV-1
  activity
• Method Used acutely or chronically infected MDM
  at various stages of cellular differentiation to
  look at BIT225 effects. We visualised BIT225
  effects using EM and employed the indicator cell
  line TZM-bls to investigate where BIT225 may be
  acting in the virus life cycle
• Results

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• Results continued..
• Conclusions BIT225 inhibits HIV-1 release
  (gt90) from chronically infected d14 MDMs
• BIT225 affects Vpu ion channels (CROI 2007).
  EM suggests defects in virion
  packaging/budding
• BIT225 acts post-integration
• WEPEA089 BIT225 inhibits HIV-1 transmission to
  CD4 T cells
• BIT225 has completed pre-clinical studies and is
  currently in Phase I studies in healthy volunteers

Comparison of BIT225 to other antiretroviral drugs
140
120
100
80
viral integration of solvent control
(Luminescence)
60
40
20
0
225
AZT
EFV
LPV
SQV
(10uM)
(100nM)
(10nM)
(100nM)
(10nM)
Drug (concentration)