Open AccessIn Vitro and In Vivo Activities of CS-758 (R-120758), a New Triazole Antifungal Agent
Author(s) -
Yasuki Kamai,
Tamako Harasaki,
Takashi Fukuoka,
Satoshi Ohya,
Katsuhisa Uchida,
Hideyo Yamaguchi,
Shōgo Kuwahara
Publication year - 2002
Publication title -
antimicrobial agents and chemotherapy
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.07
H-Index - 259
eISSN - 1070-6283
pISSN - 0066-4804
DOI - 10.1128/aac.46.2.367-370.2002
Subject(s) - fluconazole , itraconazole , aspergillus fumigatus , candida albicans , cryptococcus neoformans , in vivo , amphotericin b , cryptococcosis , microbiology and biotechnology , aspergillosis , triazole , aspergillus flavus , pharmacology , in vitro , biology , aspergillus , chemistry , antifungal , immunology , biochemistry , organic chemistry
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.