ABSTRACT
Melarsoprol is a melaminophenyl-based trivalent organic arsenical introduced as an antitrypanosomal drug for the treatment of human African trypanosomiasis (HAT) in 1949 (Barrett and Gilbert, 2006). Experimental work commenced with arsenical agents for treatment of HAT as early as 1904, with the agent tryparsamide introduced in 1919 (Wery, 1994; Maser et al., 2003). Although this was the first antitrypanosomal agent that crossed the blood–brain barrier, it was only effective against Trypanosoma brucei gambiense, not T. brucei rhodesiense. Unfortunately, widespread resistance reduced the utility of this drug. In 1940, the synthesis of the arsenic compound melarsen oxide led to the successful development of melarsoprol in 1949 (Friedheim, 1949).
