Absence of an active metabolite for the triazole antifungal pramiconazole

Pramiconazole is an antifungal with high potential for the treatment of dermatophyte and yeast infections of the skin. It is currently not known whether pramiconazole is active alone as the parent agent or assisted by active metabo­ lites. The in vitro metabolism as well as the metabolic stability of pramiconazole was investigated in subcellu­ lar liver fractions and isolated hepatocytes of several spe­ cies. Results indicate that the metabolism of pramicona­ zole was slow, since the enzyme­mediated disappearance of pramiconazole was rather slow. To investigate whether pramiconazole was converted into an active metabolite in humans, serum samples from healthy volunteers receiving a daily dose of 100 or 200 mg pramiconazole for one week