Swiss Tropical and Public Health Institute, 4003 Basel, Switzerland.
Curr Opin Pharmacol. 2012 Oct;12(5):562-6. doi: 10.1016/j.coph.2012.05.001. Epub 2012 May 29.
The need for new drugs against tropical parasites such as Plasmodium falciparum and Trypanosoma brucei is persistent since problems with resistance and toxicity are jeopardizing the currently available medicines. Public-private partnerships aiming to develop new medicines for malaria and sleeping sickness have, over the past 12 years, brought forward several drug candidates that have entered clinical trials. These are the synthetic peroxide OZ439 and the spiroindolone NITD609 against P. falciparum, fexinidazole and the oxaborole SCYX-7158 against T. brucei. A further class of high chemotherapeutic potential are the diamidines, novel members of which may serve as back-up compounds against trypanosomes and other parasites. Thus, finally, new therapeutic agents against malaria and sleeping sickness are within reach.
由于耐药性和毒性问题危及现有药物,因此对抗疟原虫和布氏锥虫等热带寄生虫的新药的需求仍然存在。过去 12 年来,旨在开发疟疾和昏睡病新药的公私合作伙伴关系提出了几种已进入临床试验的候选药物。这些候选药物包括针对疟原虫的合成过氧化物 OZ439 和螺环吲哚酮 NITD609、针对布氏锥虫的 fexinidazole 和 oxaborole SCYX-7158。另一种具有高化疗潜力的药物是二脒类化合物,其中一些新成员可能作为对抗锥虫和其他寄生虫的备用化合物。因此,针对疟疾和昏睡病的新治疗药物终于触手可及。