melarsoprol

Melarsoprol is an organoarsenic small molecule antiprotozoal drug used for the treatment of late-stage African trypanosomiasis (sleeping sickness), specifically when the central nervous system is involved. It is effective against both *Trypanosoma brucei gambiense* and *Trypanosoma brucei rhodesiense*. Melarsoprol acts as a prodrug, metabolized in the body to melarsen oxide, which irreversibly binds to sulfhydryl groups on key enzymes such as pyruvate kinase and trypanothione reductase in the parasite, thereby disrupting energy metabolism and leading to parasite death. The inability of the drug to distinguish between host and parasite enzymes results in significant toxicity. Melarsoprol has been used since 1949 but has largely been replaced by less toxic alternatives due to its severe side effects, including potentially fatal encephalopathy.

Brand names

Arsobal

Other names

melaminophenyl arsenicalmelarsen oxide prodrug