Literature DB >> 18763217

Pramiconazole, a triazole compound for the treatment of fungal infections.

Aanand N Geria1, Noah S Scheinfeld.   

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.

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Year:  2008        PMID: 18763217

Source DB:  PubMed          Journal:  IDrugs        ISSN: 1369-7056


  5 in total

1.  In vitro profiling of pramiconazole and in vivo evaluation in Microsporum canis dermatitis and Candida albicans vaginitis laboratory models.

Authors:  Kelly de Wit; Caroline Paulussen; An Matheeussen; Koen van Rossem; Paul Cos; Louis Maes
Journal:  Antimicrob Agents Chemother       Date:  2010-08-30       Impact factor: 5.191

Review 2.  Resistance to antifungals that target CYP51.

Authors:  Josie E Parker; Andrew G S Warrilow; Claire L Price; Jonathan G L Mullins; Diane E Kelly; Steven L Kelly
Journal:  J Chem Biol       Date:  2014-08-27

Review 3.  Conazoles.

Authors:  Jan Heeres; Lieven Meerpoel; Paul Lewi
Journal:  Molecules       Date:  2010-06-09       Impact factor: 4.411

4.  The CCAAT-binding complex mediates azole susceptibility of Aspergillus fumigatus by suppressing SrbA expression and cleavage.

Authors:  Chi Zhang; Lu Gao; Yiran Ren; Huiyu Gu; Yuanwei Zhang; Ling Lu
Journal:  Microbiologyopen       Date:  2021-11       Impact factor: 3.139

5.  Antifungal mode of action of macrocarpal C extracted from Eucalyptus globulus Labill (Lan An) towards the dermatophyte Trichophyton mentagrophytes.

Authors:  Jack Ho Wong; Kit-Man Lau; Yu-On Wu; Ling Cheng; Chun-Wai Wong; David Tai-Wai Yew; Ping-Chung Leung; Kwok-Pui Fung; Mamie Hui; Tzi-Bun Ng; Clara Bik-San Lau
Journal:  Chin Med       Date:  2015-11-21       Impact factor: 5.455

  5 in total

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