Development of a New Topical Antifungal Agent

描述(由申请人提供)：一种新的抗真菌化学物质已被鉴定，能够高敏感性地杀死红色毛霉菌。抗真菌活性是针对皮肤真菌，而不是其他真菌。已经确定了决定其活性的抗真菌剂的结构特征。将进行人体试验，以确定这种抗真菌化学物质作为局部治疗皮肤霉菌感染所致的脚趾甲真菌病的有效性。一项试点临床试验显示，培养阳性红色毛霉菌病患者三个月后真菌学治愈率为73%。 将进行剂量反应、安慰剂对照和开放试验，以确定相对真菌学和临床治愈率。将建立一种测定该化学物质的高效液相色谱分析方法，并用于确定制剂的稳定性和生产过程中的质量控制。该药物在人体内的全身水平将在局部使用后确定。将进行微生物学测试，以确定配方在生产后和临床使用期间的无菌情况。如果研究成功，指甲真菌感染的局部治疗可能不再需要全身抗真菌药物及其副作用来治疗这种常见的临床疾病。

DESCRIPTION (provided by applicant): A novel antifungal chemical has been identified that is capable of killing Trichophyton rubrum with high sensitivity. The antifungal activity is specific for dermatophyte and not other fungi. Structural characteristics of the antifungal agent that determine its activity have been identified. Human testing will be conducted to determine the effectiveness of the antifungal chemical as a topical treatment for toenail onychomycosis due to dermatophyte infection. A pilot clinical trial has revealed a mycological cure rate of 73% after three months in patients with culture positive Trichophyton rubrum toenail onychomycosis. Dose-response, placebo-controlled, and open trials will be conducted to determine relative mycologicai and clinical cure rates. An HPLC assay to measure the chemical will be developed and used to determine formulation stability and quality control during manufacture. Systemic levels of the drug will be determined in humans after topical use. Microbiologic assays will be conducted to determine formulation sterility following manufacture and during clinical use. If the studies are successful, topical treatment of fungal infections of nail may eliminate the need for systemic antifungal agents and their side effects for treatment of this common clinical condition.