name: | Fexinidazole |
ATC code: | P01CA03 | route: | oral |
n-compartments | 2 |
Fexinidazole is an oral nitroimidazole-based medication indicated for the treatment of human African trypanosomiasis (sleeping sickness), caused by Trypanosoma brucei gambiense. It is the first all-oral regimen for this disease and was approved by the European Medicines Agency and WHO for this indication. It is used in both first and second stage disease.
Pharmacokinetic parameters following oral administration of fexinidazole in adult patients with sleeping sickness. Parameters are based on PopPK modeling in infected individuals (adults) from a phase II/III clinical study.
Burrell-Saward, H, et al., & Croft, SL (2017). Dose-dependent effect and pharmacokinetics of fexinidazole and its metabolites in a mouse model of human African trypanosomiasis. International journal of antimicrobial agents 50(2) 203–209. DOI:10.1016/j.ijantimicag.2017.01.038 PUBMED:https://pubmed.ncbi.nlm.nih.gov/28552771
Tarral, A, et al., & Strub-Wourgaft, N (2014). Determination of an optimal dosing regimen for fexinidazole, a novel oral drug for the treatment of human African trypanosomiasis: first-in-human studies. Clinical pharmacokinetics 53(6) 565–580. DOI:10.1007/s40262-014-0136-3 PUBMED:https://pubmed.ncbi.nlm.nih.gov/24535888
Watson, JA, et al., & White, NJ (2019). Pharmacokinetic-Pharmacodynamic Assessment of the Hepatic and Bone Marrow Toxicities of the New Trypanoside Fexinidazole. Antimicrobial agents and chemotherapy 63(4) –. DOI:10.1128/AAC.02515-18 PUBMED:https://pubmed.ncbi.nlm.nih.gov/30670439