Development of a New Topical Antifungal Agent

描述（由申请人提供）：已鉴定出一种新型抗真菌化学品，能够以高灵敏度杀死红色毛癣菌。抗真菌活性对皮肤真菌而非其他真菌具有特异性。确定其活性的抗真菌剂的结构特征已被确定。将进行人体试验，以确定抗真菌化学品作为皮肤真菌感染引起的趾甲真菌病的局部治疗的有效性。一项初步临床试验显示，培养阳性红色毛癣菌趾甲真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。将开发用于测定化学品的HPLC测定法，并用于确定生产期间的制剂稳定性和质量控制。将在局部使用后测定人体中药物的全身水平。将进行微生物测定，以确定生产后和临床使用期间的制剂无菌性。如果研究成功，指甲真菌感染的局部治疗可能会消除对全身性抗真菌药物及其副作用的需要，以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.