In vitro and in vivo efficacies of the new triazole albaconazole against Cryptococcus neoformans

Antimicrob Agents Chemother. 2004 Feb;48(2):384-7. doi: 10.1128/AAC.48.2.384-387.2004.


The activity of albaconazole (UR-9825; J. Uriach & Cía. S.A., Barcelona, Spain) was compared to that of fluconazole against 12 isolates of Cryptococcus neoformans in vitro and against 1 isolate in vivo in a rabbit model of cryptococcal meningitis. Albaconazole was 100-fold more potent in vitro than fluconazole on a per-weight basis and was fungicidal at potentially relevant concentrations for two isolates. MICs ranged from </=0.0012 to 1.25 micro g/ml, with the MICs for most isolates being between 0.039 and 0.156 micro g/ml. Isolates were from human immunodeficiency virus (HIV)-infected and non-HIV-infected patients and were of serotypes A, B, and C; and the fluconazole MICs for some of the isolates were elevated. Infected rabbits were treated with either fluconazole or albaconazole at dosages ranging from 5 to 80 mg/kg of body weight/day. The peak concentrations of albaconazole in serum and cerebrospinal fluid (CSF) averaged 4.14 and 0.62 micro g/ml, respectively, in animals receiving 80 mg/kg/day. Comparison of the concentrations in serum and CSF suggested a level of CSF penetration of approximately 15%. Despite limited penetration into the subarachnoid space, at all three doses tested albaconazole was as effective as fluconazole for the treatment of cryptococcal meningitis in rabbits.

Publication types

  • Comparative Study
  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Animals
  • Antifungal Agents / pharmacology*
  • Antifungal Agents / therapeutic use*
  • Colony Count, Microbial
  • Cryptococcus neoformans / drug effects*
  • Fluconazole / therapeutic use
  • Meningitis, Cryptococcal / drug therapy*
  • Meningitis, Cryptococcal / microbiology
  • Microbial Sensitivity Tests
  • Quinazolines / pharmacology*
  • Quinazolines / therapeutic use*
  • Rabbits
  • Survival Analysis
  • Triazoles / pharmacology*
  • Triazoles / therapeutic use*


  • Antifungal Agents
  • Quinazolines
  • Triazoles
  • Fluconazole
  • albaconazole