Pharmacokinetics and Tolerability of Fexinidazole in Subjects with Hepatic Impairment.
Clin Drug InvestigAug 19, 2026 (epub)
Matthieu Gassiot, Jean Pierre Beaucire, Sophie Hays et al.
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In 30 seconds
This Phase I multicenter trial evaluated the pharmacokinetics of fexinidazole in 21 participants with mild and moderate hepatic impairment (HI) compared to healthy controls. Results indicated that in mild HI, fexinidazole exposure was similar or slightly higher, while in moderate HI, exposure was similar for fexinidazole and its metabolite M1, but lower for M2. The study supports the drug's safety and tolerability in this population.
Key findings
- In mild HI, fexinidazole exposure was similar or up to 1.40-fold higher than in healthy controls.
- In moderate HI, M2 exposure was lower, with C max at 0.44-fold compared to healthy controls.
- The terminal half-life of fexinidazole was longer in moderate HI, up to 1.77-fold.
- No serious adverse events occurred, indicating a good safety profile.
Why it matters
Understanding the pharmacokinetics of fexinidazole in patients with hepatic impairment is crucial for ensuring effective and safe treatment of human African trypanosomiasis, a neglected tropical disease.