An orally available, small-molecule polymerase inhibitor shows efficacy against a lethal morbillivirus infection in a large animal model

Sci Transl Med. 2014 Apr 16;6(232):232ra52. doi: 10.1126/scitranslmed.3008517.

Abstract

Measles virus is a highly infectious morbillivirus responsible for major morbidity and mortality in unvaccinated humans. The related, zoonotic canine distemper virus (CDV) induces morbillivirus disease in ferrets with 100% lethality. We report an orally available, shelf-stable pan-morbillivirus inhibitor that targets the viral RNA polymerase. Prophylactic oral treatment of ferrets infected intranasally with a lethal CDV dose reduced viremia and prolonged survival. Ferrets infected with the same dose of virus that received post-infection treatment at the onset of viremia showed low-grade viral loads, remained asymptomatic, and recovered from infection, whereas control animals succumbed to the disease. Animals that recovered also mounted a robust immune response and were protected against rechallenge with a lethal CDV dose. Drug-resistant viral recombinants were generated and found to be attenuated and transmission-impaired compared to the genetic parent virus. These findings may pioneer a path toward an effective morbillivirus therapy that could aid measles eradication by synergizing with vaccination to close gaps in herd immunity due to vaccine refusal.

MeSH terms

  • Administration, Oral
  • Animals
  • Chlorocebus aethiops
  • DNA-Directed RNA Polymerases / antagonists & inhibitors*
  • DNA-Directed RNA Polymerases / metabolism
  • Disease Models, Animal
  • Distemper Virus, Canine / drug effects
  • Distemper Virus, Canine / enzymology
  • Drug Resistance, Viral / drug effects
  • Enzyme Inhibitors / administration & dosage*
  • Enzyme Inhibitors / chemistry
  • Enzyme Inhibitors / pharmacology
  • Enzyme Inhibitors / therapeutic use*
  • Female
  • Ferrets / virology
  • Male
  • Morbillivirus Infections / drug therapy*
  • Morbillivirus Infections / virology
  • Small Molecule Libraries / administration & dosage*
  • Small Molecule Libraries / chemistry
  • Small Molecule Libraries / pharmacology
  • Small Molecule Libraries / therapeutic use*
  • Treatment Outcome
  • Vero Cells

Substances

  • Enzyme Inhibitors
  • Small Molecule Libraries
  • DNA-Directed RNA Polymerases