Out of six clinically approved drugs for the treatment of HAT, five (suramin, pentamidine, melarsoprol, eflornithine and nifurtimox) have had been discovered more than 30 years ago. Because suramin and pentamidine are ionized at physiological pH, they are unable to cross the blood brain barrier in therapeutic concentrations and are thus used for the treatment of hemolymphatic early stage HAT, caused by T. b. rhodesiense and T. b. gambiense infections, respectively. The treatment of the second or neurological stage, when the parasites invade the central nervous system (CNS), relies on the organoarsenical drug melarsoprol and the more recently registered eflornithine. The latter is ineffective against T. b. rhodesiense sleeping sickness and is used primarily to control CNS-involved HAT caused by T. b. gambiense. All the existing anti-trypanosomal therapies suffer from unacceptable toxicity, poor efficacy, difficulties of administration, and increasing treatment failures due to the development of parasite resistance [4] [5] [6] [7] [8] [9] . In the last couple of decades, no new drug has been developed for treatment of early-stage HAT, and only one drug has been developed for late-stage HAT [1, 3, 5] . The need is great for new orally active drugs for the control and eradication of this disease.