In vitro and in vivo efficacy of the triazole TAK-187 against Cryptococcus neoformans

Antimicrob Agents Chemother. 1998 Oct;42(10):2630-2. doi: 10.1128/AAC.42.10.2630.

Abstract

Multiple isolates of Cryptococcus neoformans, including those with fluconazole resistance, were tested to assess the in vitro activity of the new triazole TAK-187. MICs of TAK-187 were at least eightfold lower than those of fluconazole, and fungicidal concentrations for most isolates were 4 microg/ml or less. TAK-187 also was evaluated as intermittent therapy using two dosages in a rabbit model of experimental cryptococcal meningitis. Compared to daily treatment with fluconazole, as little as two doses of TAK-187 given 7 days apart were found to be effective. Plasma and cerebrospinal fluid TAK-187 concentrations were many times higher than MICs and fungicidal concentrations. Based upon its therapeutic efficacy and long half-life in the rabbit model, TAK-187 should be investigated for intermittent dosing in treatment or suppression of cryptococcal infections in humans.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antifungal Agents / pharmacology*
  • Cryptococcosis / drug therapy
  • Cryptococcus neoformans / drug effects*
  • Microbial Sensitivity Tests
  • Rabbits
  • Triazoles / pharmacology*

Substances

  • Antifungal Agents
  • Triazoles
  • TAK 187