Delespaux Vincent, de Koning Harry P
Trypanosomosis Unit, Department of Animal Health, Institute of Tropical Medicine Antwerpen, Nationalestraat 155, B-2000 Antwerp, Belgium.
Drug Resist Updat. 2007 Feb-Apr;10(1-2):30-50. doi: 10.1016/j.drup.2007.02.004. Epub 2007 Apr 3.
Despite the many decades of use of most of the current trypanocides, we know little of their mode of action. This may in part be because most of these will act on multiple targets once inside the cell, and they derive their selective action on the parasite from selective accumulation by the pathogen. Loss of this capacity for drug uptake by the trypanosome would thus be a major cause for drug resistance. We here discuss the use of current drugs against human and veterinary African trypanosomiasis, the prevalence, causes and mechanisms of drug resistance and new developments in trypanosomiasis therapy such as the introduction of nifurtimox and DB289.
尽管目前大多数锥虫杀灭剂已使用了数十年,但我们对它们的作用方式却知之甚少。部分原因可能是这些药物一旦进入细胞就会作用于多个靶点,它们对寄生虫的选择性作用源于病原体的选择性蓄积。因此,锥虫失去这种摄取药物的能力将是耐药性的一个主要原因。我们在此讨论当前药物在治疗人类和兽医非洲锥虫病中的应用、耐药性的流行情况、原因和机制,以及锥虫病治疗的新进展,如硝呋莫司和DB289的引入。