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他瓦泊罗,一种用于局部治疗甲癣的新型含硼小分子,在两年致癌性研究中无致癌性。

Tavaborole, a novel boron-containing small molecule for the topical treatment of onychomycosis, is noncarcinogenic in 2-year carcinogenicity studies.

作者信息

Ciaravino Vic, Coronado Dina, Lanphear Cheryl, Shaikh Imran, Ruddock William, Chanda Sanjay

机构信息

Anacor Pharmaceuticals Inc, Palo Alto, CA, USA

Anacor Pharmaceuticals Inc, Palo Alto, CA, USA.

出版信息

Int J Toxicol. 2014 Sep-Oct;33(5):419-27. doi: 10.1177/1091581814545245. Epub 2014 Sep 7.

Abstract

Tavaborole, a cyclized boronic acid, has been approved by the Food and Drug Administration for the topical treatment of toenail onychomycosis. This novel, low-molecular-weight pharmaceutical compound has broad-spectrum antifungal activity against dermatophytes, yeasts, and molds responsible for the disease. Tavaborole was tested in 2-year carcinogenicity studies in mice (once daily dermal administration) and rats (once daily by oral gavage) as part of the extensive nonclinical safety program. There was no evidence of tavaborole-related neoplasms observed in either study. Based on the data gathered from these 2 carcinogenicity studies, tavaborole is considered noncarcinogenic.

摘要

环硼氮烷(tavaborole)是一种环化硼酸,已获美国食品药品监督管理局批准用于局部治疗趾甲甲癣。这种新型低分子量药物化合物对引起该疾病的皮肤癣菌、酵母菌和霉菌具有广谱抗真菌活性。作为广泛的非临床安全性计划的一部分,环硼氮烷在小鼠(每日一次经皮给药)和大鼠(每日一次经口灌胃)的两年致癌性研究中进行了测试。两项研究均未观察到与环硼氮烷相关的肿瘤证据。根据这两项致癌性研究收集的数据,环硼氮烷被认为无致癌性。

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