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1st-in-Class Agents:

  • Proline-rich antimicrobial peptides (AMPs)
  • Protein translation inhibitors via a novel mechanism of action
  • Two series (apidaecins and oncocins) in development

LPA Advantages:

  • Activity through binding to 70S ribosome & other related mechanisms
  • No membrane disruption, unlike most other classes of AMPs
  • No mammalian cytotoxicity or hemolysis (caused past AMP failures)
  • Efficacious in variety of mouse infection models

Apidaecin Highlights:

  • Activity vs. Gram-negative MDR, efflux-defective, and colistin-resistant strains
  • No cross-resistance with strains resistant to ribosome-targeting antibiotics
  • Efficacious in sepsis, thigh infection, and urinary tract infection in vivo models
  • First known inhibitors of translation termination