Efficacy of PLD-118, a novel inhibitor of Candida isoleucyl-tRNA synthetase, against experimental oropharyngeal and esophageal candidiasis caused by fluconazole-resistant C. albicans Academic Article uri icon


MeSH Major

  • Antifungal Agents
  • Candida albicans
  • Candidiasis
  • Cycloleucine
  • Enzyme Inhibitors
  • Fluconazole
  • Isoleucine-tRNA Ligase


  • PLD-118, formerly BAY 10-8888, is a synthetic antifungal derivative of the naturally occurring beta-amino acid cispentacin. We studied the activity of PLD-118 in escalating dosages against experimental oropharyngeal and esophageal candidiasis (OPEC) caused by fluconazole (FLC)-resistant Candida albicans in immunocompromised rabbits. Infection was established by fluconazole-resistant (MIC > 64 microg/ml) clinical isolates from patients with refractory esophageal candidiasis. Antifungal therapy was administered for 7 days. Study groups consisted of untreated controls; animals receiving PLD-118 at 4, 10, 25, or 50 mg/kg of body weight/day via intravenous (i.v.) twice daily (BID) injections; animals receiving FLC at 2 mg/kg/day via i.v. BID injections; and animals receiving desoxycholate amphotericin B (DAMB) i.v. at 0.5 mg/kg/day. PLD-118- and DAMB-treated animals showed a significant dosage-dependent clearance of C. albicans from the tongue, oropharynx, and esophagus in comparison to untreated controls (P

publication date

  • October 2004



  • Academic Article



  • eng

PubMed Central ID

  • PMC521932

Digital Object Identifier (DOI)

  • 10.1128/AAC.48.10.3959-3967.2004

PubMed ID

  • 15388459

Additional Document Info

start page

  • 3959

end page

  • 67


  • 48


  • 10