Pramiconazole, a triazole compound for the treatment of fungal infections

IDrugs. 2008 Sep;11(9):661-70.

Abstract

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.

Publication types

  • Review

MeSH terms

  • Animals
  • Antifungal Agents / administration & dosage*
  • Antifungal Agents / adverse effects
  • Antifungal Agents / pharmacokinetics
  • Clinical Trials as Topic
  • Drug Design
  • Drug Evaluation, Preclinical
  • Humans
  • Imidazoles / administration & dosage*
  • Imidazoles / adverse effects
  • Imidazoles / pharmacokinetics
  • Mycoses / drug therapy*
  • Mycoses / microbiology
  • Patents as Topic
  • Triazoles / administration & dosage*
  • Triazoles / adverse effects
  • Triazoles / pharmacokinetics

Substances

  • Antifungal Agents
  • Imidazoles
  • Triazoles
  • pramiconazole