氟苯达唑作为一种杀微丝蚴药物：历史与背景。
Flubendazole as a macrofilaricide: History and background.
机构信息
Institute of Parasitology, McGill University, Ste-Anne-de-Bellevue, Québec, Canada.
NTDSC/MDP, Task Force for Global Health, Decatur, Georgia, United States of America.
出版信息
PLoS Negl Trop Dis. 2019 Jan 16;13(1):e0006436. doi: 10.1371/journal.pntd.0006436. eCollection 2019 Jan.
Abstract
Benzimidazole anthelmintics have long been employed for the control of soil-transmitted helminth infections. Flubendazole (FBZ) was approved in 1980 for the treatment of gastrointestinal nematode infections in both veterinary and human medicine. It has also long been known that parenteral administration of FBZ can lead to high macrofilaricidal efficacy in a variety of preclinical models and in humans. As part of an effort to stimulate the discovery and development of new macrofilaricides, particularly for onchocerciasis, research has recently been devoted to the development of new formulations that would afford high oral bioavailability of FBZ, paving the way for potential clinical development of this repurposed drug for the treatment of human filariases. This review summarizes the background information that led to this program and summarizes some of the lessons learned from it.
摘要
苯并咪唑类驱虫药长期以来一直被用于控制土壤传播性蠕虫感染。氟苯达唑（FBZ）于 1980 年被批准用于兽医和人类医学中治疗胃肠道线虫感染。长期以来，人们还知道，静脉内给予 FBZ 可导致多种临床前模型和人类中出现高的大丝虫杀灭效果。作为努力刺激新的大丝虫杀剂的发现和开发的一部分，特别是用于盘尾丝虫病，最近的研究致力于开发新的制剂，以提供 FBZ 的高口服生物利用度，为重新利用这种药物治疗人类丝虫病的潜在临床开发铺平道路。本综述总结了导致该计划的背景信息，并总结了从中获得的一些经验教训。
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