In vitro and in vivo activities of CS-758 (R-120758), a new triazole antifungal agent.

Abstract

The activity of CS-758 (R-120758), a new triazole antifungal agent, was evaluated and compared with those of fluconazole, itraconazole, and amphotericin B in vitro and with those of fluconazole and itraconazole in vivo. CS-758 exhibited potent in vitro activity against clinically important fungi. The activity of CS-758 against Candida spp. was superior to that of fluconazole and comparable or superior to those of itraconazole and amphotericin B. CS-758 retained potent activity against Candida albicans strains with low levels of susceptibility to fluconazole (fluconazole MIC, 4 to 32 microg/ml). Against Aspergillus spp. and Cryptococcus neoformans, the activity of CS-758 was at least fourfold superior to those of the other drugs tested. CS-758 also exhibited potent in vivo activity against murine systemic infections caused by C. albicans, C. neoformans, Aspergillus fumigatus, and Aspergillus flavus. The 50% effective doses against these infections were 0.41 to 5.0 mg/kg of body weight. These results suggest that CS-758 may be useful in the treatment of candidiasis, cryptococcosis, and aspergillosis.

• Authors: Yasuki Kamai, Tamako Harasaki, Takashi Fukuoka, Satoshi Ohya, Katsuhisa Uchida, Hideyo Yamaguchi, Shogo Kuwahara
• Journal: Antimicrobial agents and chemotherapy (Antimicrob Agents Chemother) Vol. 46 Issue 2 Pg. 367-70 (Feb 2002) ISSN: 0066-4804 [Print] United States
• PMID: 11796343 (Publication Type: Journal Article)

Chemical References

• Antifungal Agents
• Triazoles
• R-120758

Topics

• Animals
• Antifungal Agents (pharmacology, therapeutic use)
• Aspergillus (drug effects)
• Candida (drug effects)
• Cryptococcus neoformans (drug effects)
• Disease Models, Animal
• Mice
• Microbial Sensitivity Tests
• Mycoses (drug therapy)
• Treatment Outcome
• Triazoles (pharmacology, therapeutic use)