In VitroActivity of E1210, a Novel Antifungal, against Clinically Important Yeasts and Molds

Abstract

ABSTRACTE1210 is a new antifungal compound with a novel mechanism of action and broad spectrum of antifungal activity. We investigated thein vitroantifungal activities of E1210 compared to those of fluconazole, itraconazole, voriconazole, amphotericin B, and micafungin against clinical fungal isolates. E1210 showed potent activities against mostCandidaspp. (MIC90of ≤0.008 to 0.06 μg/ml), except forCandida krusei(MICs of 2 to >32 μg/ml). E1210 showed equally potent activities against fluconazole-resistant and fluconazole-susceptibleCandidastrains. E1210 also had potent activities against various filamentous fungi, includingAspergillus fumigatus(MIC90of 0.13 μg/ml). E1210 was also active againstFusarium solaniand some black molds. Of note, E1210 showed the greatest activities againstPseudallescheria boydii(MICs of 0.03 to 0.13 μg/ml),Scedosporium prolificans(MIC of 0.03 μg/ml), andPaecilomyces lilacinus(MICs of 0.06 μg/ml) among the compounds tested. The antifungal action of E1210 was fungistatic, but E1210 showed no trailing growth ofCandida albicans, which has often been observed with fluconazole. In a cytotoxicity assay using human HK-2 cells, E1210 showed toxicity as low as that of fluconazole. Based on these results, E1210 is likely to be a promising antifungal agent for the treatment of invasive fungal infections.