Pramiconazole from Barrier
Therapeutics Inc is a new addition to the family of
triazole antifungal agents that act by inhibiting fungal cell membrane
ergosterol synthesis, thereby leading to increased cell permeability and destruction. Barrier
Therapeutics was developing an oral formulation of
pramiconazole for the potential treatment of
seborrheic dermatitis (erythematosquamous
skin disease),
onychomycosis and
dermatomycosis (including
tinea versicolor,
tinea pedis and
tinea cruris/corporis). In preclinical studies,
pramiconazole exhibited similar or superior antifungal activity to
ketoconazole and
itraconazole, and selectively inhibited
ergosterol synthesis with a broad spectrum activity.
Pramiconazole was absorbed rapidly and had a long half-life, allowing for once-daily dosing. In phase I and II clinical trials,
pramiconazole reduced the growth of Candida albicans, Malassezia globosa, Microsporum canis, Trichophyton mentagrophytes and Trichophyton rubrum, and was generally well tolerated. At the time of publication, Barrier
Therapeutics had suspended the development of
pramiconazole as part of a series of cost-cutting initiatives; the company had also been acquired by Stiefel Laboratories Inc. No formal announcement had been made regarding the further development of
pramiconazole. The results of studies performed to date suggest that
pramiconazole may be useful in the treatment of
dermatomycoses when oral treatment is mandated. Promising preclinical and early phase II clinical data warrant the further development of the
drug in larger clinical trials.