Tioconazole, a New Broad-Spectrum Antifungal Agent: Preclinical Studies Related to Vaginal Candidiasis

Abstract

Tioconazole is a new broad-spectrum imidazole antifungal agent with in vitro activity against common yeast pathogens approximately fourfold greater than miconazole. Experimental cream formulations are effective for topical therapy in murine vaginal candidiasis. Systemic exposure to tioconazole following vaginal application is less than that following oral administration. Chronic toxicity studies revealed effects only after oral dosing.

Inhibition and killing of Candida albicans in vitro by five imidazoles in clinical use

“…These modifications have resulted in several active compounds which have proceeded to clinical use in topical or systemic administration or both. Some in vitro comparisons of activity have been made with various organisms (2,6,14,15,21,23). Conclusions about mechanisms of action have sometimes been related to the results (21), although it is unclear whether the differences seen would apply to different fungal species.…”

Development of new multicomponent crystals of the antifungal drug tioconazole and the assessment of their biopharmaceutical attributes

“…A PANalytical X'pert 3 powder X-ray diffractometer was used for the PXRD data collection. The data collection was done at room temperature using monochromated Cu Kα 1 radiation ( λ = 1.54060 Å) generated at 45 kV and 40 mA in the reflection geometry.…”

“…2 Besides the slight hepatomegaly and delayed parturition observed at higher oral doses (at 100 and 150 mg kg −1 ), no mutagenic, cytogenetic, or teratogenic issues were noted in animals for TCZ. 3 However, the poor water solubility and toxicity of TCZ remain the major challenge and have limited its use only as a topical agent. 4,5 Recently, several organometallic complexes of TCZ with Co( ii ), Cu( ii ), Zn( ii ), and Cd( ii ) metals have been reported with promising cytotoxicity activities against colon and cervical cancer cell lines.…”

Tioconazole in the Treatment of Vaginal Candidiasis

“…Pfizer), a new member of the imidazole class of antifungal agents, exhibits marked activity in vitro against a broad spectrum of pathogenic yeasts and other fungi and to a lesser degree against certain bacteria and protozoa. It is also effective in a variety of in vivo experimental models of fungal infections [1].…”