Ketoconazole — a new broad spectrum orally active antimycotic

Thienpont, D; Cutsem, J. Van; Gerven, F. Van; Heeres, Jan; Janßen, Paul

doi:10.1007/bf01960348

Cited by 91 publications

(33 citation statements)

References 4 publications

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“…Ketoconazole shows better efficacy in a rat vaginal candidiasis model (8,9,14) than in the mouse model, and published data do suggest that azoles are less efficacious in the mouse model (3,8,14). However, both models have some predictive value for human efficacy.…”

Section: Discussionmentioning

confidence: 99%

Activity of UK-49,858, a bis-triazole derivative, against experimental infections with Candida albicans and Trichophyton mentagrophytes

Richardson¹,

Brammer²,

Marriott³

et al. 1985

Antimicrob Agents Chemother

151

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The therapeutic potential of UK-49,858, a difluorophenyl bis-triazole derivative, has been assessed by evaluating its activity against systemic infections with Candida albicans in normal mice and rats and in mice with impaired defence mechanisms, against vaginal infections with C. albicans in mice, and against dermal infections with Trichophyton mentagrophytes in guinea pigs. Orally administered ketoconazole was used as a comparative agent throughout, and parenterally administered amphotericin B was included in the study of C. albicans systemic infection in normal mice. The activity of UK-49,858 given orally to mice or rats infected systemically with C. albicans was far superior to that of ketoconazole. In addition, UK-49,858 showed activity comparable to that of amphotericin B when given parenterally, although the latter gave more prolonged protection. UK-49,858 was also effective orally in curing experimental candidal vaginitis in mice and trichophytosis in guinea pigs, against which it was approximately 10 times more active than ketoconazole. These data suggest that UK-49,858 may be of value in the treatment of both C. albicans and dermatophyte fungal infections in man.

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Section: Discussionmentioning

confidence: 99%

Activity of UK-49,858, a bis-triazole derivative, against experimental infections with Candida albicans and Trichophyton mentagrophytes

Richardson¹,

Brammer²,

Marriott³

et al. 1985

Antimicrob Agents Chemother

151

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“…Ketoconazole is an orally active, antifungal imidazole derivative synthesized and developed by Janssen Pharmaceutica in 1977 (127,302). It is considered to be the "gold standard" among the azole derivative antifungal drugs.…”

Section: Ketoconazolementioning

confidence: 99%

Overview of medically important antifungal azole derivatives

1988

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Fungal infections are a major burden to the health and welfare of modern humans. They range from simply cosmetic, non-life-threatening skin infections to severe, systemic infections that may lead to significant debilitation or death. The selection of chemotherapeutic agents useful for the treatment of fungal infections is small. In this overview, a major chemical group with antifungal activity, the azole derivatives, is examined. Included are historical and state of the art information on the in vitro activity, experimental in vivo activity, mode of action, pharmacokinetics, clinical studies, and uses and adverse reactions of imidazoles currently marketed (clotrimazole, miconazole, econazole, ketoconazole, bifonazole, butoconazole, croconazole, fenticonazole, isoconazole, oxiconazole, sulconazole, and tioconazole) and under development (aliconazole and omoconazole), as well as triazoles currently marketed (terconazole) and under development (fluconazole, itraconazole, vibunazole, alteconazole, and ICI 195,739).

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“…Unfortunately, 5-FC has several well-known disadvantages that restrict its use clinically (2). Originally designated as compound R 41400, KCZ is a highly promising, new imidazole-containing drug that was synthesized and initially evaluated in the laboratories of Janssen Pharmaceutica, Beerse, Belgium (8,11). In this report, we have assessed the in vitro activity of KCZ-5-FC combinations against various potentially pathogenic or opportunistic species of yeasts.…”

mentioning

confidence: 99%