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SCYX-7158 is an effective, safe and orally active treatment for human african trypanosomiasis (HAT). In the T. b. brucei S427 strain, the MIC value for SCYX-7158 is 0.6 μg/mL.

SCYX-7158 is active in vitro against relevant strains of Trypanosoma brucei, including T. b. rhodesiense and T. b. gambiense.In whole cell assays, SCYX-7158 exhibits potent activity against representative T. b. brucei, T. b. rhodesiense and T. b. gambiense strains. IC50 values for SCYX-7158 are approximately 0.07 μg/mL to 0.37 μg/mL following incubation of the parasite strains with SCYX-7158 for 72 h. In the T. b. brucei S427 strain, the MIC value for SCYX-7158 is 0.6 μg/mL, approximately two times the IC50 measured for this strain. In contrast to the potent activity of SCYX-7158 against trypanosomes, no significant inhibition of cell proliferation is observed in an in vitro mammalian cell (L929 mouse cell line) assay at drug concentrations up to 50 μg/mL. The potential for SCYX-7158 to inhibit cytochrome P450 (CYP) enzymes is evaluated using P450-Glo assays for the human isoforms CYP3A4, CYP1A2, CYP2C19, CYP2C9 and CYP2D6. The IC50 values for SCYX-7158 in these assays are all above 10 μM[1].

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