{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,4,5]],"date-time":"2026-04-05T06:29:15Z","timestamp":1775370555074,"version":"3.50.1"},"reference-count":39,"publisher":"American Society for Microbiology","issue":"5","license":[{"start":{"date-parts":[[2001,5,1]],"date-time":"2001-05-01T00:00:00Z","timestamp":988675200000},"content-version":"tdm","delay-in-days":0,"URL":"https:\/\/journals.asm.org\/non-commercial-tdm-license"}],"content-domain":{"domain":["journals.asm.org"],"crossmark-restriction":true},"short-container-title":["Antimicrob Agents Chemother"],"published-print":{"date-parts":[[2001,5]]},"abstract":"<jats:title>ABSTRACT<\/jats:title>\n          <jats:p>\n            The in vitro activity of KP-103, a novel triazole derivative, against pathogenic fungi that cause dermatomycoses and its therapeutic efficacy against plantar tinea pedis and cutaneous candidiasis in guinea pigs were investigated. MICs were determined by a broth microdilution method with morpholinepropanesulfonic acid-buffered RPMI 1640 medium for\n            <jats:italic>Candida<\/jats:italic>\n            species and with Sabouraud dextrose broth for dermatophytes and by an agar dilution method with medium C for\n            <jats:italic>Malassezia furfur<\/jats:italic>\n            . KP-103 was the most active of all the drugs tested against\n            <jats:italic>Candida albicans<\/jats:italic>\n            (geometric mean [GM] MIC, 0.002 \u03bcg\/ml), other\n            <jats:italic>Candida<\/jats:italic>\n            species including\n            <jats:italic>Candida parapsilosis<\/jats:italic>\n            and\n            <jats:italic>Candida glabrata<\/jats:italic>\n            (GM MICs, 0.0039 to 0.0442 \u03bcg\/ml), and\n            <jats:italic>M. furfur<\/jats:italic>\n            (GM MIC, 0.025 \u03bcg\/ml). KP-103 (1% solution) was highly effective as a treatment for guinea pigs with cutaneous candidiasis and achieved mycological eradication in 8 of the 10 infected animals, whereas none of the imidazoles tested (1% solutions) was effective in even reducing the levels of the infecting fungi. KP-103 was as active as clotrimazole and neticonazole but was less active than lanoconazole and butenafine against\n            <jats:italic>Trichophyton rubrum<\/jats:italic>\n            (MIC at which 80% of isolates are inhibited [MIC\n            <jats:sub>80<\/jats:sub>\n            ], 0.125 \u03bcg\/ml) and\n            <jats:italic>Trichophyton mentagrophytes<\/jats:italic>\n            (MIC\n            <jats:sub>80<\/jats:sub>\n            , 0.25 \u03bcg\/ml). However, KP-103 (1% solution) exerted therapeutic efficacy superior to that of neticonazole and comparable to those of lanoconazole and butenafine, yielding negative cultures for all samples from guinea pigs with plantar tinea pedis tested. This suggests that KP-103 has better pharmacokinetic properties in skin tissue than the reference drugs. Because the in vitro activity of KP-103, unlike those of the reference drugs, against\n            <jats:italic>T. mentagrophytes<\/jats:italic>\n            was not affected by hair as a keratinic substance, its excellent therapeutic efficacy seems to be attributable to good retention of its antifungal activity in skin tissue, in addition to its potency.\n          <\/jats:p>","DOI":"10.1128\/aac.45.5.1493-1499.2001","type":"journal-article","created":{"date-parts":[[2002,7,27]],"date-time":"2002-07-27T10:06:42Z","timestamp":1027764402000},"page":"1493-1499","update-policy":"https:\/\/doi.org\/10.1128\/asmj-crossmark-policy-page","source":"Crossref","is-referenced-by-count":36,"title":["In Vitro Antifungal Activity of KP-103, a Novel Triazole Derivative, and Its Therapeutic Efficacy against Experimental Plantar Tinea Pedis and Cutaneous Candidiasis in Guinea Pigs"],"prefix":"10.1128","volume":"45","author":[{"given":"Yoshiyuki","family":"Tatsumi","sequence":"first","affiliation":[{"name":"<!--label omitted: 1-->Central Research Laboratories, Kaken Pharmaceutical Co., Ltd., 14 Minamikawara-cho, Shinomiya, Yamashina, Kyoto, Kyoto 607-8042,1 and"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Mamoru","family":"Yokoo","sequence":"additional","affiliation":[{"name":"<!--label omitted: 1-->Central Research Laboratories, Kaken Pharmaceutical Co., Ltd., 14 Minamikawara-cho, Shinomiya, Yamashina, Kyoto, Kyoto 607-8042,1 and"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Tadashi","family":"Arika","sequence":"additional","affiliation":[{"name":"<!--label omitted: 1-->Central Research Laboratories, Kaken Pharmaceutical Co., Ltd., 14 Minamikawara-cho, Shinomiya, Yamashina, Kyoto, Kyoto 607-8042,1 and"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Hideyo","family":"Yamaguchi","sequence":"additional","affiliation":[{"name":"<!--label omitted: 2-->Research Institute of Medical Mycology, Teikyo University, 359 Otsuka, Hachioji, Tokyo 192-0395,2 Japan"}],"role":[{"role":"author","vocabulary":"crossref"}]}],"member":"235","reference":[{"key":"e_1_3_1_2_2","doi-asserted-by":"crossref","first-page":"545","DOI":"10.2336\/nishinihonhifu.52.545","article-title":"Activity of topical antifungals on infected sites\u2014skin permeability and adsorption to horny materials.","volume":"52","author":"Arika T.","year":"1990","unstructured":"Arika T. 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