An alternative form of melarsoprol in sleeping sickness

作者：Kennedy Peter G E^*

来源：Trends in Parasitology, 2012, 28(8): 307-310.

DOI：10.1016/j.pt.2012.05.003

• sleeping sickness
• human African trypanosomiasis (HAT)
• central nervous system (CNS)
• complexed melarsoprol.

Human African trypanosomiasis (HAT), or sleeping sickness, is a major threat to human health throughout sub-Saharan Africa. Almost always fatal if untreated or inadequately treated, a commonly used drug for treating late-stage HAT, and the only drug for late-stage Trypanosome brucei rhodesiense, is intravenous melarsoprol, which kills 5% of patients receiving it. Melarsoprol cyclodextrin inclusion complexes have been tested in a highly reliable mouse model of HAT. These complexes increase the oral bioavailability of melarsoprol making them effective orally and both curative and nontoxic in doses that are equivalent to those of intravenous melarsoprol. It is argued that a small clinical trial of this drug in HAT is justified to potentially improve the outcome of patients with late-stage rhodesiense disease.

• 出版日期2012-8