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Tolciclate against dermatophytes

I Carneri, G Monti, A Bianchi

    Arzneimittel-Forschung
    |January 1, 1976
    PubMed
    Summary
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    Toliciclate (KC 9147) is a colorless topical antimycotic effective against dermatophytes. It demonstrates superior efficacy and lipophilicity compared to tolnaftate in preclinical skin infection models.

    Area of Science:

    • Dermatology
    • Mycology
    • Pharmacology

    Background:

    • Dermatomycoses treatment historically relied on dyes, posing aesthetic challenges.
    • Existing topical antifungals like tolnaftate have limitations in efficacy and lipophilicity.

    Purpose of the Study:

    • To evaluate the antimycotic properties of 0-(1,2,3,4-Tetrahydro-1,4-methanonaphthalen-6-yl)-m-N-dimethylthiocarbanilate (toliciclate; KC 9147).
    • To compare the efficacy of toliciclate with tolnaftate in preclinical models.

    Main Methods:

    • In vitro susceptibility testing against dermatophytes.
    • Fungicidal activity assessment after prolonged contact.
    • Liposolubility comparison with tolnaftate.
    • In vivo efficacy evaluation in guinea pig skin infections.

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    Main Results:

    • Toliciclate exhibits potent in vitro activity against dermatophytes (0.01–0.1 µg/ml).
    • It is fungicidal upon extended topical application.
    • Toliciclate is colorless and soluble in well-tolerated excipients, unlike traditional dyes.
    • Demonstrates significantly higher liposolubility than tolnaftate.
    • In vivo, toliciclate is 3-10 times more active than tolnaftate against experimental dermatophyte infections.

    Conclusions:

    • Toliciclate represents a promising new topical agent for dermatomycoses.
    • Its favorable properties, including efficacy, safety profile, and cosmetic acceptability, warrant further investigation.