Biochem/physiol Actions
BTZ043 is the first in a new class of antibiotics that kills all clinically relevant strains of Mycobacterium Tuberculosis, including multi-drug resistant strains, with minimal inhibitory concentrations (MIC) in the ng/ml range (MIC = 2.3 nM against M. tuberculosis H37Rv and 9.2 nM against M. smegmatis). BTZ043 potently inhibits the enzyme decaprenylphosphoryl-β-D-ribose 2’-epimerase (DprE1), which is essential for the formation of decaprenylphosphoryl arabinose, a key component in cell wall synthesis. It appears that BTZ-043 diffuses and accumulates in centrally necrotizing granulomas (necrotic lesions) harboring Mycobacterium tuberculosis.