Anti-candidal activity of GBR-14206, a new imidazole derivative: Intravenous administration in lipid emulsion form.

GBR-14206, a new imidazole derivative, has been evaluated against systemic infection with Candida albicans in normal and immunocompromised mice. The therapeutic effect of GBR-14206 (as a lipid emulsion) given intravenously to mice infected systemically with C. albicans was superior to that of miconazole. GBR-14206 also showed a candicidal effect in the blood stream at the therapeutic dose. In addition, GBR-14206 inhibited the hyphal growth (yeast to hyphal transformation) in Eagle's minimum essential medium and methionine synthetic medium at the respective concentrations of 0.20 and 0.05μg/ml, which were approximately 3 to 7 times more active than miconazole.These properties suggested that GBR-14206 may be useful for the therapy of systemic candidiasis in human.