AbstractThis chapter deals with the currently used therapeutic drugs for human African trypanosomiasis. The physicochemical properties, clinical application, therapy schedules, adverse reactions, pharmacokinetics, mode of action, efficacy, availability and costs of registered drugs for the treatment of first-stage disease (pentamidine and suramin), registered drugs for the treatment of second-stage disease (melarsoprol and eflornithine) and non-registered alternative drugs (nifurtimox and diminazene aceturate) are discussed.