【摘 要】
：
Oral triazoles such as itraconazole and fluconazole are used for the treatment of fungal infections of the skin caused by dermatophytes and yeasts.They inhibit the fungal 14a-demethylase (CYP51) preve
【机 构】
：
Barrier Therapeutics,subsidiary of Stiefel,a GSK company Belgium
【出 处】
：
中国上海第七届国际新药发明科技年会
论文部分内容阅读
Oral triazoles such as itraconazole and fluconazole are used for the treatment of fungal infections of the skin caused by dermatophytes and yeasts.They inhibit the fungal 14a-demethylase (CYP51) preventing the formation of ergosterol,a vital compound of the fungal cell membrane.Areas for improvement in triazole drug development include specificity for CYP51,PK profile,dosing schedule,efficacy,safety profile,drug interactions,and development of resistant strains of fungi.New triazoles with potential advantages in these areas are currently in development.Pramiconazole is presented as an example.Pramiconazole has an in vitro antifungal activity similar or superior to itraconazole against various dermatophytes and Candida species.It has remarkable activity against Malassesia spp (10-fold versus ketoconazole).
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