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BTZ043 is a inhibitor of decaprenyl-phosphoribose-epimerase (DprE1), It can display nanomolar bactericidal activity against Mycobacterium tuberculosis in vitro.
in vitro: The inhibition of BTZ-resistant DprE1 followed the trend observed in the MIC measurements, with the C387G mutant being more resistant to inhibition by PyrBTZ01, PyrBTZ02, and BTZ043 (7- to 9-fold increases in IC50) than the C387S mutant (2.5- to 4-fold increases in IC50).
in vivo: BTZ-043 were administered at 100 mg/kg twice daily by gavage, and sulfamethoxazole/trimethoprim (SXT), at 100 mg/kg sulfamethoxazole, was used as a positive control. |