Maeda Jun, Nanjoh Yasuko, Koga Hiroyasu, Toga Tetsuo, Makimura Koichi, Tsuboi Ryoji
Nihon Nohyaku Co., Ltd.
Med Mycol J. 2016;57(1):J1-6. doi: 10.3314/mmj.57.J1.
The minimum inhibitory concentration (MIC) and the minimum fungicidal concentration (MFC) of luliconazole against Trichophyton rubrum (14 strains) and Trichophyton mentagrophytes (14 strains), which are the most common cause of tinea, were compared with those of 6 topical antifungal drugs of lanoconazole, bifonazole, efinaconazole, liranaftate, naftifine and terbinafine. Luliconazole showed the most potent antifungal activity (MIC90 =0.00098 μg/ml and MFC90 =0.0078 μg/ml) among the compounds tested against the two species. Efinaconazole and bifonazole, the drug of azole-class, showed a large MFC/MIC ratio. On the other hand, these ratios of luliconazole and lanoconazole were as small as those of liranaftate, naftifine and terbinafine which are thought to possess fungicidal mechanism. These results suggest that luliconazole possesses fungicidal activity against both species of Trichophyton. In this study, we found that luliconazole had the most potent antifungal activity among the major topical antimycotics used in Japan and the US. Luliconazole would be the best-in-class drug for dermatophytosis in clinics.
将卢立康唑对红色毛癣菌(14株)和须癣毛癣菌(14株)(这两种是癣最常见的病因)的最低抑菌浓度(MIC)和最低杀菌浓度(MFC),与6种外用抗真菌药物(即氯康唑、联苯苄唑、艾氟康唑、利拉萘酯、萘替芬和特比萘芬)的MIC和MFC进行了比较。在针对这两种菌测试的化合物中,卢立康唑显示出最强的抗真菌活性(MIC90 =0.00098μg/ml,MFC90 =0.0078μg/ml)。唑类药物艾氟康唑和联苯苄唑显示出较大的MFC/MIC比值。另一方面,卢立康唑和氯康唑的这些比值与被认为具有杀菌机制的利拉萘酯、萘替芬和特比萘芬的比值一样小。这些结果表明,卢立康唑对两种毛癣菌均具有杀菌活性。在本研究中,我们发现卢立康唑在日本和美国使用的主要外用抗真菌药物中具有最强的抗真菌活性。卢立康唑将成为临床上治疗皮肤癣菌病的同类最佳药物。