What is "melarsoprol"

n. A drug used to treat sleeping sickness.

Melarsoprol ( INN) is a prodrug used in the treatment of East African (rhodesiense) human African trypanosomiasis. It is produced by Sanofi-Aventis and is on the World Health Organization's List of Essential Medicines.

Freidheim demonstrated in 1949 the effects of melarsoprol against late-state trypanosomiasis. Melarsoprol is the dimercaptopropanol derivative of melarsen oxide (Mel Ox), whose structure is shown below:

The main drug prescribed is Mel B, however, an alarming number of side effects occur from treatment. The active metabolite of Mel B is Mel Ox, which is taken up by the TbAT1 adenosine transporter in T. brucei brucei. Due to side effects similar to arsenic poisoning, other pharmacological agents have become first-line treatments for stage one of the disease and for certain trypanosomes.