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Flubendazole as a macrofilaricide: History and background

机译:氟苯达唑作为大杀螨剂:历史和背景

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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.
机译:苯并咪唑驱虫药长期以来一直被用于控制土壤传播的蠕虫感染。氟苯达唑(FBZ)于1980年被批准用于兽医和人用药物治疗胃肠道线虫感染。长期以来,众所周知,在各种临床前模型和人类中,肠胃外注射FBZ均可导致较高的大杀丝效力。作为刺激发现和开发新的大型杀线虫剂(特别是针对盘尾丝虫病)的努力的一部分,最近的研究致力于开发新的制剂,这些制剂可提供较高的FBZ口服生物利用度,从而为该重新用途药物的潜在临床开发铺平了道路用于治疗人类丝虫病。这篇综述总结了导致该计划的背景信息,并总结了从中汲取的一些教训。

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