title: KP-103, a novel triazole derivative, is effective in preventing relapse and successfully treating experimental interdigital tinea pedis and tinea corporis in guinea pigs.
abstract: The therapeutic efficacy of KP-103, a triazole derivative, for 10 guinea pigs with interdigital tinea pedis or tinea corporis was investigated. Topical KP-103 solution (0.25 to 1%) was dose-dependently effective in treating both dermatophytoses. A 1% KP-103-treatment rendered all infected skins culture-negative on day-2 posttreatment. A high negative-culture rate was obtained with 1% solutions of butenafine and lanoconazole but not with 1% neticonazole solution. The follow up study performed on day-30 and day-9 posttreatment demonstrated that the relapse rates for 1% KP-103-treated animals with tinea pedis and for those with tinea corporis were 20 and 30%, respectively, and that these values were the same as those for 1% butenafine-treated animals, but lower than those for 1% lanoconazole-treated animals (55 and 80%, respectively). When a single dose of 1% KP-103 was applied to the back skin 48 hr before fungal inoculation, 9 of the 10 animals were protected from the dermatophytosis, suggesting that active KP-103 is retained in skin tissue for at least 48 hr after dosing. Moreover, it was suggested that KP-103 retains a high activity in the horny layer because of its lower keratin-affinity. The effectiveness of KP-103 against dermatophytoses may be due to the favorable pharmacokinetic properties in the skin tissues, together with its potent antifungal activity.
authors.affiliation: Central Research Laboratories, Kaken Pharmaceutical Co., Ltd., Kyoto, Japan. tatsumi_yoshiyuki@kaken.co.jp
authors.forename: Yoshiyuki
authors.initials: Y
authors.lastname: Tatsum
authors.forename: Mamoru
authors.initials: M
authors.lastname: Yokoo
authors.forename: Tadashi
authors.initials: T
authors.lastname: Arika
authors.forename: Hideyo
authors.initials: H
authors.lastname: Yamaguchi
mesh_terms: D000818:Animals; D019072:Antibiotic Prophylaxis / Q000639:trends; D000935:Antifungal Agents / Q000494:pharmacology / Q000627:therapeutic use*; D001231:Aspergillus flavus / Q000254:growth & development / Q000472:pathogenicity; D004195:Disease Models, Animal; D004353:Drug Evaluation, Preclinical; D006168:Guinea Pigs; D007633:Keratins / Q000819:agonists / Q000378:metabolism; D008297:Male; D008826:Microbial Sensitivity Tests; D055502:Secondary Prevention; D014005:Tinea / Q000145:classification / Q000188:drug therapy* / Q000517:prevention & control; D014008:Tinea Pedis / Q000188:drug therapy* / Q000517:prevention & control; D014034:Toes; D016896:Treatment Outcome; D014230:Triazoles / Q000493:pharmacokinetics / Q000627:therapeutic use*; D014249:Trichophyton / Q000187:drug effects / Q000254:growth & development / Q000472:pathogenicity
chemical_list: D000935:Antifungal Agents; D014230:Triazoles; D007633:Keratins; C431707:efinaconazole