TBI-166 is a potential next-generation antituberculosis riminophenazine with activity against Mycobacterium tuberculosis (0.063 μg/ml).
TBI-166 shows MICs against 16 drug-sensitive clinical isolates range from <0.005 to 0.15 μg/ml, lower than those for clofazimine (CFZ) (0.026 to 0.633 μg/ml).
TBI-166 maintained activity against Mycobacterium fortuitum and Mycobacterium scrofulaceum despite having higher MICs.
TBI-166 exhibited activity against M. tuberculosis H37Rv infecting J774A.1 cells with CFU reductions of 0.54, 0.61, and 1.13 log10 at concentrations of 0.0625, 0.25, and 1 μg/ml, respectively.
TBI-166 demonstrated activity at least equivalent to that of CFZ against intracellular M. tuberculosis and in low-dose aerosol infection models of acute and chronic murine tuberculosis.
