Long-acting CR-NNRTIs to Treat HIV

• Marked synergy with current FDA-approved NRTIs (e.g. tenofovir (TDF), INSTIs, and pharma clinical compounds (A)
  • Excellent candidate for combination therapy regimens
  • Pre-Exposure Prophylaxis (PrEP)
• Highly soluble with 2-21 nM potency vs. drug-resistant strains, including K101P (e.g., rilpivirine ineffective against K101P) in MT-2 T- cell/HIV-1 assay
• Excellent ADME-Tox and physiological properties (B)
  • No off targets including HERG and CYP3A
  • Excellent in vivo oral bioavailability in mice
• Efficacy in humanized mouse AIDS model (C)
  • CD4+ ; viral load undetectable
  • Single dose, long-acting (4 week) sustained release nanoparticle formulation
• Issued US Patent 9,382,245 and related pending IP & Publications