KP-103, a Novel Triazole Derivative, Is Effective in Preventing Relapse and Successfully Treating Experimental Interdigital Tinea Pedis and Tinea Corporis in Guinea Pigs

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.