The in vitro activity of R 51,211 (itraconazole, accepted generic name; Janssen Pharmaceutica, Beerse, Belgium), a new orally active triazole, was compared with those of two existing orally active azoles, ketoconazole and BAY n 7133, and a topical agent, Ro 14-4767/002. An agar dilution procedure (Kimmig agar) was performed with 148 isolates of pathogenic fungi. Incubation was at 30 degrees C from 48 h to 7 days. R 51,211 was dissolved in 0.2 N HCl in absolute ethanol, ketoconazole was dissolved in 0.2 N HCl alone, BAY n 7133 was dissolved in absolute ethanol, and Ro 14-4767/002 was dissolved in dimethyl sulfoxide. R 51,211 and Ro 14-4767/002 were the most active drugs against isolates of Histoplasma capsulatum, and R 51,211 showed the greatest activity in vitro against isolates of Blastomyces dermatitidis and Cryptococcus neoformans. Ro 14-4767/002 was the most active drug against 30 isolates of dermatophytes, followed by R 51,211, ketoconazole, and BAY n 7133. R 51,211 showed the best activity in vitro against 19 isolates of Aspergillus fumigatus and Aspergillus flavus, as well as 19 isolates of dematiaceous fungi. All four drugs had 90% MICs of greater than or equal to 16 micrograms/ml when tested with isolates of zygomycetous fungi.

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Oxiconazole (Ro 13–8996) is a recently described imidazole derivative intended for topical use. 128 isolates of pathogenic fungi were tested in vitro against oxiconazole, miconazole, and ketoconazole using an agar dilution method. Results indicated that miconazole was markedly more active than either oxiconazole or ketoconazole against Candida albicans while ketoconazole was the more active compound against Candida parapsilosis. A species specific difference in the susceptibilities of isolates of Aspergillus fumigatus and Aspergillus flavus to all three imidazoles with A. flavus being more susceptible was noted. Both Mucor and Rhizopus were more susceptible to oxiconazole than to either miconazole or ketoconazole. There were no noticeable differences among the dermatophytes in tests with the three drugs with all geometric mean minimum inhibition concentrations (MIC) being less than 1.0 μgml^-1. The dematiaceous fungi also demonstrated no major differences in susceptibility to the three drugs. One isolate of Pseudallescheria boydii was relatively resistant to all three drugs (MIC ≥16 μgml^-1).

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