Determination of the optimal single dose treatment for acoziborole, a novel drug for the treatment of human African trypanosomiasis: First-in-human study

by Tarral A, Hovsepian L, Duvauchelle T, Donazzolo Y, Latreille M, Felices M, Gualano V, Delhomme S, Valverde Mordt O, Blesson S, Voiriot P, Strub-Wourgaft N. Clinical Pharmacokinetics 2023. doi: https://doi.org/10.1007/s40262-023-01216-8

Summary: Acoziborole is a novel boron-containing candidate developed as an oral drug for the treatment of human African trypanosomiasis. In this Phase I trial, the best dose regimen for all stages of human African trypanosomiasis in 128 healthy adult males of sub-Saharan African origin was determined. Acoziborole was well tolerated and no dose-related adverse events were observed. The drug appeared rapidly in plasma (at 1 h), reached t_max between 24 and 72 h, and remained stable for up to 96 h. The therapeutic single dose for administration under fasted conditions was fixed to 960 mg. The authors conclude that acoziborole can be safely assessed in patients as a potential single-dose oral cure for both stages of gambiense human African trypanosomiasis.