by Gillon J, Simon F, Sidhu S, Louis M, Launay D, Wauthier V, Pelay-Gimeno M, Andel LV, Loyau S, Rembry S, Weinling E, Tarral A. Antimicrobial Agents and Chemotherapy 2025, e00580-25. doi: 110.1128/aac.00580-25
Summary: Acoziborole is an oxaborole 6-carboxamide active against Trypanosoma brucei gambiense and rhodesiense, the parasites responsible for human African trypanosomiasis. The authors of this manuscript conducted an open-label, phase I study in six healthy male participants to evaluate the mass balance, pharmacokinetics, metabolism pathways, and excretion of a single oral 960 mg dose of radiolabelled acoziborole. The excretion balance and systemic exposure of total circulating radioactivity were determined using accelerator mass spectrometry of blood, plasma, urine, and faeces samples. Metabolism profiling was performed in pools of plasma, urine, and faeces. Liquid chromatography coupled with tandem mass spectrometry quantified acoziborole and its metabolite SCYX-3109 in plasma and urine. Acoziborole showed good absorption, limited metabolism, minimal urinary elimination, and predominant but slow biliary-fecal elimination.
