Discovery of a Novel Class of Orally Bioavailable HIV1 Fusion Inhibitors

1
Discovery of a Novel Class of Orally Bioavailable
HIV-1 Fusion Inhibitors

• gt400,000 compounds screened in a proprietary,
  cell-based gp41 6HB inhibition assay

Compounds prevent exposure of gp41 extended
intermediate.
Compounds bind Env before
and after CD4 engagement.
2
Unique Features of New Class of Fusion Inhibitors

• Novel target site and mechanism of action
• Block downstream of attachment inhibitors and
  upstream of enfuvirtide
• Active against most BMS-806-resistant and
  enfuvirtide-resistant mutants
• Active against both X4 R5 viruses, unlike
  coreceptor antagonists
• Potential for oral delivery, unlike enfuvirtide